CID 2745687 is a competitive, reversible antagonist of the orphan receptor GPR35.

Novel specific Rac1 inhibitor, interferring with the interaction of Rac1 with Dock180, a relevant Rac1 activator in glioma invasion, and to reduce Rac1-GTP levels

Novel vasorelaxing agent, stimulating soluble guanylyl cyclase, activating K+ channels, and blocking extracellular Ca2+ influx

Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.

MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer[1][2].

Novel inhibitor of chromosomal instability, potentiating MCAK in vivo and transiently suppressing chromosome mis-segregation in CIN cancer cells

Novel inhibitor of AMA1-RON2 interaction; Inhibitor of c-Src tyrosine kinase activity

Potent Allosteric Agonist-Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptors

Novel selective c-Myc inhibitorReference:1) Disruption of Myc-Max heterodimerization with improved cell-penetrating analogs of the small molecule 10074-G5; Oncotarget. 2013 Jun;4(6):936-47. GoTo Paper

Potent and ATP-binding site inhibitor of GSK-3

Novel DNMT1 Selective Antagonist

PCNA-I1 is an inhibitor of proliferating cell nuclear antigen (PCNA) that binds to PCNA trimers (Kd = 0.41 µM) and dose-dependently reduces the level of PCNA associated with chromatin in PC3 cells.

Potent, selective, and  competitive 15-hydroxyprostaglandin dehydrogenase (15-PGDH; HPGD) inhibitor

AA92593 has been used as a selective inhibitor of melanopsin.

α-Lapachone shows trypanocidal activity[1].

Canthin-6-one displays a wide range of biological activities, such as antimycobacterial activity.

Chrysoeriol, a natural flavonoid extracted from the tropical plant Coronopus didymus, exhibits potent antioxidant activity. Chrysoeriol shows significant inhibition of lipid peroxidation.

T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream).

(E)-Flupentixol is a non-neuroleptic isomer of (Z)-flupenthixol.

Tricin is a natural flavonoid present in large amounts in rice bran. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7[1][2][3].

Novel cyclin dependent kinase inhibitor

Moracin M is a phosphodiesterase-4 inhibitor isolated from Morus alba. Moracin M has anti-inflammatory activity. Moracin M inhibits lipopolysaccharide-induced inflammatory responses in nucleus pulposus cells via regulating PI3K/Akt/mTOR phosphorylation. Moracin M inhibits airway inflammation by interrupting the JNK/c-Jun and NF-κB pathways in vitro and in vivo.

Novel pathway-selective estrogen receptor (ER) inhibitor, inhibiting NF-kB transcriptional activity but being devoid of conventional estrogenic activity

Selective modulator of aryl hydrocarbon (Ah) receptor

Novel Kv2.1 and Kv2.2 inhibitor

Prodrug of INDY, a novel potent ATP-competitive Dyrk1A inhibitor

2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.

Potent activator of SHIP-1 inducing apoptosis of the cancer cell lines in vitro in both a time and dose dependant manner

10-Hydroxycanthin-6-one is an antileukemic canthin-6-one alkaloid from Brucea antidysenterica. Antitumor agent.

Novel inhibitor of TRPM6, promoting mesoderm and definitive endoderm differentiation of human embryonic stem cells through alteration of magnesium homeostasis

Inhibitor of of the metalloproteinase ADAM17; Inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage, blocking TACE as well as ADAM10

preQ1 is a precursor in the biosynthesis of queuosine, a bacterial nucleoside incorporated into tRNA by tRNA transglycosylase. preQ1 binds to an aptamer domain on tRNA that acts as a riboswitch to repress gene expression.

SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily.

Selective inhibitor of NADPH oxidase activity in low micromolar concentrations, interfering neither with ROS detection nor with XOD or eNOS activities

TSPC is an inhibitor for GA perception by in vitro and in planta evaluations.

ML-261 is a thienopyrrole-5-carboxamide that inhibits lipid droplet formation.

Potent, reversible, and ATP-competitive inhibitor of human Thymidylate kinase (TMPK)

Novel HCN4 CLP ligand, modulating channel function and completely abolishing the cAMP-induced shift in V1/2

Novel, more stable resveratrol analog, protecting cardiac against mitochondrial damage following H/R, thereby suppressing injury

HAT Inhibitor II is a novel p300/CBP-selective histone acetyltransferase inhibitor.Histone Acetyltransferase Inhibitor II is a potent and cell permeable p300 inhibitor, with an IC50 of 5µM; Histone Acetyltransferase Inhibitor II can be used in cancer research.

Cell permeable cAMP analog, acting as a cardiac stimulant and inhibiting phosphodiesterase

Inhibitor of ventricular tachyarrhythmias in intact mouse and rabbit ventricles by the suppression of SCaEs, independent of beta-blocking activity

Novel inhibitor of the VP40 matrix protein

Novel fluorescent tamoxifen derivative with unique SERM-like properties

Novel blood brain barrier (BBB) penetrable two-photon imaging probe, labelling plaques and cerebral amyloid angiopathies (CAAs)

ATP competitive tyrosine kinase inhibitor

SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD+ in mice.

Novel inhibitor of the binding of Ral to its effector RALBP1, inhibiting Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines

Potent TIR1 antagonist, blocking the formation of the TIR1-IAA-Aux/IAA complex and so inhibiting auxin-responsive gene expressionReferences:1) Smékalová V, Luptovčiak I, Komis G, Šamajová O, Ovečka M, Doskočilová A, Takáč T, Vadovič P, Novák O, Pechan T,

Novel inhibitor of SIRT6, sensitizing pancreatic cancer cells to gemcitabineREFERENCES1) Damonte P, Sociali G, Parenti MD, Soncini D, Bauer I, Boero S, Grozio A, Holtey MV, Piacente F, Becherini P, Sanguineti R, Salis A, Damonte G, Cea M, Murone M, Poggi

Potent and selective mGluR8-specific orthosteric agonist

Melittin (MLT, Forapin, Forapine) is an activator of phospholipase A2 (PLA2) that stimulates the activity of the low molecular weight PLA2, while it does not the increase the activity of the high molecular weight enzyme.

Gadobutrol (Gadovist, Gadavist) is a non-ionic macrocyclic gadolinium-based contrast agent (GBCA) that is usedfor tissue contrast enhancement in magnetic resonance imaging (MRI).

Neophytadiene is a diterpene found in Turbinaria ornate, with anti-inflammatory antioxidant and cardioprotective properties.

MC-Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

NITD-2, a dengue virus (DENV) polymerase inhibitor, inhibits the DENV RdRp-mediated RNA elongation. NITD-2 penetrates cell membrane poorly.

NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >500

DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [14C]

Enfumafungin, a triterpene glycoside, is isolated from extracts derived from an endophytic species of Hormonema. Enfumafungin is an antifungal compound that is acting on the fungal cell wall, as the (1,3)-beta-D-glucan synthase inhibitor. Enfumafungin is specific for yeasts and fungi (excluding Cryptococcus) and does not inhibit the growth of Bacillus subtilis[1][2].

MCHR1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHR1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.

SMS2-IN-1 is a potent and highly selective sphingomyelin synthase 2 (SMS2) inhibitor with an IC50 of 6.5 nM and a Kd of 37 nM. SMS2-IN-1 shows 150-fold selectivity for SMS2 over SMS1 (IC50 of 1000 nM).

Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII). Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibit

Sisunatovir (RV521), an orally available inhibitor of the RSV fusion (RSV-F) protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively.

Sisunatovir, also known as RV521, is a highly potent fusion inhibitor with efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clinical isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo.

BMS-986224 is a potent and selective apelin receptor (APJ) agonist with Ki of 0.074 nM, exhibiting similar receptor binding and signaling profile to (Pyr1) apelin-13.

BMS-986313 is a tricyclic-carbocyclic RORγt inverse agonist and shows potent GaL4-Luc reporter(GAL4) and human whole blood (hWB) activity (EC50s of 3.6 nM and 50 nM, respectively.

A Novel PROTACs building block.

Lenalidomide-5-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC

ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.

IXA6 is a novel small molecule compound of inducing IRE1 RNase activity.

IXA4 is the most selective for the IRE1–XBP1s signaling pathway.IXA4 selectively activate IRE1–XBP1s signaling and reduces secretion of APP through IRE1 activation.

(Rac)-X77 is a racemate of X77. X77 is a potent non-covalent inhibitor of the main protease of SARS-CoV-2 (SARS-CoV-2 Mpro). X77 binds to SARS-CoV-2 Mpro with a Kd value of 0.057 μM.

MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays.

Capromorelin Tartrate (CP 424391-18), a member of the growth hormone secretagogue (GHS) class of drugs, is a ghrelin receptor agonist and a novel therapy for stimulation of appetite in dogs with Ki of 7 nM for hGHS-R1a and EC50 of 3 nM for rat pituicyte.

Seralutinib (GB002) is an inhaled Pdgfr kinase inhibitor. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.

M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09  μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC50 values of  0.53  μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research.

β-Lactamase-IN-2 is a beta-lactamase inhibitor, extracted from patent WO 2019075084 A1, compound 1. β-Lactamase-IN-2 has anti-microbial and anti-bacterial effects.

2',3'-Dideoxy-5-iodocytidine is used for gene sequencing can be used as an antibiotic. 2',3'-Dideoxy-5-iodocytidine is particular effective against Mycobacterium.

Ibrexafungerp citrate is a triterpenoid antifungal. Similarly to echinocandins, it inhibits the synthesis of 1,3-β-d-glucan. However, it binds to a different site on the enzyme than echinocandins, resulting in limited cross-resistance. Ibrexafungerp exerts concentration-dependent fungicidal activity against Candida species and retains in vitro activity against most fluconazole-resistant strains.

Pyribencarb is a benzylcarbamate-type fungicide, which is active against a wide range of plant pathogenic fungi. Pyribencarb is a potent Qo inhibitor of cytochrome b. Pyribencarb is especially active against Botrytis cinerea and Sclerotinia sclerotirum.

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.

5-Propargylamino-ddUTP, a nucleoside molecule that can be used to synthesis of cyanine dye-nucleotide conjugate which is used in nucleic acid labeling or sequence analysis.

Complement factor D-IN-2 is an inhibitor of complement factor D extracted from patent WO2015130838A1, compound 190. Complement factor D-IN-2 targets factor D and inhibits the complement cascade at an early and essential point in the alternative complement pathway. Complement factor D-IN-2 can be used for the research of autoimmune diseases.

MCC7840 sodium, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. MCC7840 sodium can be used for the research of inflammatory diseases.

MCC7840, a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. MCC7840 can be used for the research of inflammatory diseases.

PD-1/PD-L1-IN 3, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC50s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 can be used for the research of various diseases, including cancer and infectious diseases.

PD-1/PD-L1-IN-NP19 is a PD-1/PD-L1 inhibitor, with an IC50 of 12.5 nM for human PD-1/PD-L1 interaction. PD-1/PD-L1-IN-NP19 could activate the immune microenvironment in tumor, which may contribute to its antitumor effects.

Enpatoran (M5049) is an orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran can block both innate and adaptive autoimmunity. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran (M5049) can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran (M5049) inhibits cytokine release, causing great potency in pharmacokinetic/pharmacodynamic properties.

EMAC10101d is a potent and selective toward hCA II inhibitor, with a Ki of 8.1 nM.

Ervogastat (PF-06865571) is a potent and well-tolerated diacylglycerol acyltransferase 2 inhibitor (DGAT2i). Ervogastat alone reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH). Ervogastat combination with Clesacostat (an acetyl CoA-carboxylase inhibitor (ACCi)) can be used for the research of NASH with liver fibrosis therapy.

RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.

RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM.

KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues.

Acoramidis (AG10) is an orally active and selective kinetic stabilizer of WT and V122I-TTR (transthyretin). Acoramidis (AG10) is used in the study for transthyretin amyloidosis.

7-Iodo-2',3'-dideoxy-7-deaza-guanosine is a dideoxynucleoside that can be used in DNA synthesis and sequencing reactions.

PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.

CC-90001 is a potent, selective and orally active inhibitor of c-Jun N-terminal kinase (JNK). CC-90001 shows 12.9-fold selectivity for JNK1 over JNK2 in a cell-based model. CC-90001 can be used for the research of idiopathic pulmonary fibrosis.

FLT3-IN-3 is a potent FLT3 inhibitor with IC50s of 13 and 8 nM for FLT3 WT and FLT3 D835Y, respectively.

DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.

NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.

Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo.

DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research.

MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain).

CDK7-IN-3 is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.

Dalfopristin (RP54476) is a semi-synthetic analogue of ostreogyrcin A. Quinupristin/dalfopristin (Q/D) is a parental streptogramin with a spectrum of activity that includes Gram-positive pathogens, including those resistant to other classes of antimicrobial compounds.

Ezeprogind (AZP-2006) is an orally active neurotrophic inducer. Ezeprogind targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.

Ezeprogind (AZP-2006) disulfate is an orally active neurotrophic inducer. Ezeprogind disulfate targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind disulfate is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.

PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. PF-05221304 is a substrate for organic anion transport polyp

AST5902 is the active metabolite of Alflutinib.

ALC-0159 is a PEG/lipid conjugate (i.e. PEGylated lipid). Formulations containing ALC-0159 have been used in the development of lipid nanoparticles (LNPs) for the delivery of mRNA-based vaccines.

SM-102 is an ionizable amino lipid that has been used in combination with other lipids in the formation of lipid nanoparticles.Administration of luciferase mRNA in SM-102-containing lipid nanoparticles induces hepatic luciferase expression in mice. Formulations containing SM-102 have been used in the development of lipid nanoparticles for delivery of mRNA-based vaccines.

MVL5 is a new Multivalent Cationic Lipid for siRNA Delivery.Improved total gene silencing and Lower non-specific gene silencing,Lower toxicity.

BAR501 impurity is an impurity found in the preparation of BAR501 that acts as an agonist of the G protein-coupled bile acid-activated receptor (GP-BAR1). BAR501 impurity (10 µM) induces a 150% increase in luciferase activity in a GP-BAR1 reporter gene assay.

Lats-IN-1 is a potent and ATP-competitive inhibitor of Lats1 and Lats2 kinases. Lats-IN-1 promotes Yap-dependent proliferation in postmitotic mammalian tissues.

CA77.1(CA) is a novel chaperone-mediated autophagy (CMA) activator for the treament of Alzheimer’s disease (AD).

GNE-0749 is a potent and selective pan-RAF inhibitor with Ki of 0.061 nM and <0.08 nM for CRAF and BRAF, respectively. Combinated with cobimetinib, GNE-0749 demonstrates synergistic pharmacodynamic effects in the KRAS mutant HCT116 tumor-bearing mice.

STM2457 is in stock, and we can ship it immeidately. STM2457 is a potent inhibitor of METTL3/METTL14 catalytic activity with IC50 of 16.9 nM, Kd of 1.4 nM, respectively. STM2457 is highly specific for METTL3 and shows significant anti-leukaemic effect.

HST5040 is a clinical candidate for the treatment of propionic acidemia (PA) and methylmalonic acidemia (MMA) with EC50 of 0.94 μM in P-CoA-lowering activity.

CVN424 is a potent and selective GPR6 inverse agonist (EC50 of 38 nM) for the treatment of parkinson's disease.

ATI-2173 is a novel liver-targeted molecule designed to deliver the 5′-monophosphate of clevudine for the treatment of chronic hepatitis B infection.

PF-07104091 is an orally bioavailable inhibitor of cyclin-dependent kinase 2 (CDK2), with potential antineoplastic activity. Upon administration, CDK2 inhibitor PF-07104091 selectively targets, binds to and inhibits the activity of CDK2. This may lead to cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. CDKs are serine/threonine kinases that are important regulators of cell cycle progression and cellular proliferation and are frequently overexpressed in tumor cells. CDK2/cyclin E complex plays an important role in retinoblastoma (Rb) protein phosphorylation and the G1-S phase cell cycle transition. CDK2/cyclin A complex plays an important role in DNA synthesis in S phase and the activation of CDK1/cyclin B for the G2-M phase cell cycle transition.

AT-273 is the nucleoside metabolite of AT-527.

LGD 3303 is an androgen receptor agonist.1 It selectively binds to the androgen receptor (Ki = 0.9 nM for the human receptor) over mineralocorticoid, glucocorticoid, and progesterone receptors (Kis = 1,261, 581, and 136 nM, respectively, for the human receptors). It also selectively induces reporter transcription in a reporter assay using CV-1 cells expressing the androgen receptor (EC50 = 3.6 nM) over CV-1 cells expressing the mineralocorticoid or progesterone receptors (EC50s = 3,695 and 2,233 nM, respectively). LGD 3303 (3 mg/kg per day) increases levator ani muscle mass, but not prostate muscle mass, in orchiectomized (ORDX) male rats. It increases body weight and gastrocnemius mass, bone mineral content and density in the lumbar spine and mid-femur, and bone formation rate in ovariectomized (OVX) female rats when administered at a dose of 3 mg/kg per day. LGD 3303 (30 mg/kg per day) increases the time spent in the male area in a sexual preference test by sexually experienced, but not sexually inexperienced, estradiol benzoate- and progesterone-primed OVX female rats.

AC-262536 is a selective androgen receptor modulator (SARM, Ki = 5.01 nM). It is also a partial agonist of the androgen receptor (EC50 = 1.58 nM in a luciferase assay).

Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.

BPH-1358 (NSC50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL).

Highly sensitive chromogenic peptide substrate for factor Xa. Determination of factor Xa activity for research, in-process and quality control of factor Xa preparations.

Chromogenic peptide substrate for the determination of thrombin and antithrombin III

LDN-209929 dihydrochloride is a potent and selective haspin kinase inhibitor (IC50=55 nM) with180-fold selectivity verses DYRK2 (IC50=9.9 μM). LDN-209929 is a optimized analogue of LDN-192960 .

Thioquinapiperifil dihydrochloride (KF31327), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study.

TCEP (Tris(2-carboxyethyl)phosphine) hydrochloride, a non-thiol reducing agent, promotes NF-κB-DNA binding in a dose-related manner.

Myelin Oligodendrocyte Glycoprotein 35-55, mouse, rat (MOG 35-55) is a minor component of CNS myelin that induces experimental autoimmune encephalomyelitis in C57BL/6 mice by an encephalitogenic T cell response.

QQN52061 is GPR34 receptor modulator, which can control function of GPR34 receptor (as antagonist or inverse agonist). QQN52061 was first reported in PCT Int. Appl. (2006), WO 2006088246. This product has not formal name. For the convenience of scientific communication, we named it by combining its Inchi key (3 letters from the first letter of each section) with the last 5 digit of its CAS#) according to MedKoo Chemical Nomenclature .

NSC-92828, also known as 3-Phenanthrenebutyric acid, is a Protein–protein interaction inhibitor (2P2 inhibitor or 2P2I). Protein–protein recognition is the cornerstone of multiple cellular and pathological functions. Therefore, protein–protein interaction inhibition (2P2I) is endowed with great therapeutic potential despite the initial belief that 2P2I was refractory to small-molecule intervention.

Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).

MLS-573151 (MLS000573151) is a selective GTPase Cdc42 inhibitor with an EC50 of 2 μM. MLS-573151 is inactive against other GTPases family members, such as Rab2, Rab7, H-Ras, Rac1, Rac 2 and RhoA wild-type. MLS-573151 acts by blocking the binding of GTP to

EN4, a covalent ligand that targets cysteine 171 (C171) of MYC, is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

XD2-149 is a napabucasin PROTAC as an effective degrader of the E3 ligase ZFP91 with IC50 of 1 μM and 0.8 μM in pancreatic cancer cell lines, MIA PaCa-2 and BxPC-3, respectively. XD2-149 also reduces the expression of STAT3, pSTAT3, and NQO1 proteins.

Dac51 is a potent FTO inhibitor with IC50 of 0.4 μM, which blocks FTO-mediated immune evasion and synergize with checkpoint blockade for better tumor control.

ABD957 is a potent and selective covalent inhibitor of the ABHD17 with IC50 of 0.2 μM (ABHD17B, recombinantly expressed) and impairs N-Ras depalmitoylation in human acute myeloid leukemia (AML) cells.

93-O17S is an imidazole-based synthetic lipidoid for in vivo mRNA delivery. Lipid nanoparticles (LNPs) with 93-O17S promotes both the cross-presentation of tumor antigens and the intracellular delivery of cGAMP (STING agonist).

Sulfopin is a covalent, highly selective inhibitor of Pin1 with Ki of 17 nM in the FP assay. Sulfopin also blocks Myc-driven tumors in vivo without any toxicity.

Jun8-76-3A is a potent and selective noncovalent SARS-CoV-2 Mpro inhibitor with Ki of 0.07 μM. Jun8-76-3A only selectively inhibits SARS-CoV-2 and SARS-CoV Mpro, but not other viral proteases and host proteases including calpain 1, cathepsins L and K, and trypsin.

iBAP (BAP1 inhibitor I) is a first-in-class inhibitor of the catalytic activity of BAP1 histone H2A deubiquitinase complex with IC50 of 0.5-1 uM in vitro,

Nifeviroc is a CCR5 antagonist potentially for treatment of inflammatory responses to HIV type-1 infection

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.,5-HT2B [1](Cell-free assay) 5-HT2A [1](Cell-free assay) Histamine H1 Receptor [1](Cell-free assay) Muscarinic M2 [1](Cell-free assay) Muscarinic M1 [1](Cell-free assay) View More 10.44(pKi) 10.22(pKi) 10.14(pKi) 9.38(pKi) 8.61(pKi)

ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 promotes ubiquitination and degradation of AR. ARV-110 can be used for the research of prostate cancer.

Vodobatinib (K0706) is a potent, third generation and orally active Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research.

MCU-i4 is a negative modulator of the mitochondrial calcium uniporter (MCU) complex that directly binds a specific cleft in MICU1 and decreases mitochondrial Ca2+ influx.,MCU-i4 decreases mitochondrial Ca2+ influx. Docking simulations reveal that MCU-i4 directly binds a specific cleft in MICU1, a key element of the MCU complex that controls channel gating. Accordingly, in MICU1-silenced or deleted cells, the inhibitory effect of MCU-i4 is lost. Moreover, MCU-i4 fails to inhibit mitochondrial Ca2+ uptake in cells expressing a MICU1 mutated in the critical amino acids that forge the predicted binding cleft.[1]

M4205 is a c-KIT inhibitor, with an IC50 of 10 nM for c-KIT V654A. M4205 has high activity on c-KIT mutations in exon 11, 13, 17.

CHAPS is a zwitterionic surfactant that decreases the sequence specificity of the nucleosome.,nucleosome [1]()

cis-Resveratrol exhibits signifcant antiviral activity. cis-Resveratrol inhibits enteroviruses with IC50s of 12.2 µM and 37.6 µM for coxsackievirus B3 (CVB3) and enterovirus 71 (EV71), respectively.

ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer.

SRS11-92, a Ferrostatin-1 (Fer-1) analogue, is a potent ferroptosis inhibitor. SRS11-92 inhibits ferroptotic cell death induced by Erastin in HT-1080 human fibrosarcoma cells (EC50=6 nM).

Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way.

Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus.

Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent and direct inhibitor of 5-LO (5-Lipoxygenase) that reduces 5-LO activity in cell-free assays. CDC also inhibits 12-LO and 15-LO.

JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.

JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.,hM4Di [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM4Di [1](Cell-free assay) 0.5 nM(EC50) 1.8 nM(Ki) 5 nM(EC50) 8.7 nM(Ki),JHU37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.[1],JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.[1]

RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM.

RMC-5552 is a potent and selective inhibitor of mTORC1. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 has anti-cancer activity.

YM-244769 dihydrochloride is a potent Na+/Ca2+ exchange (NCX) inhibitor that preferentially inhibits NCX3 (IC50=18 nM). Neuronal and renal protection.

5'-O-DMT-2'-O-TBDMS-N-Bz-Adenosine is an adenosine derivative and can be used as an intermediate for oligonucleotides synthesis.

LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.

2'-O-(2-Methoxyethyl)-uridine is a synthetic oligonucleotide conversed from uridine. 2'-O-(2-Methoxyethyl)-uridine has the potential for chemotherapeutic agents development.

11R-VIVIT is a potent NFAT inhibitor. 11R-VIVIT inhibits LPS or LPS plus IFN-γ-induced IL-12 p40, IL-12 p70, IL-23 and TNF secretion from bone marrow-derived macrophages (BMDMs). 11R-VIVIT also attenuates NO production and Nos2 mRNA expression in LPS-stimulated BMDMs. 11R-VIVIT improves symptoms in a mouse model of colitis. Exhibits immunosuppressive effects; enhances graft survival in mice.

2'-O-methyluridine is found in rRNA, snRNA, snoRNA and tRNA of Archaea, Bacteria, and Eukaryota.

Hydrofurimazine is a NanoLuc substrate whose enhanced aqueous solubility allows delivery of higher doses to mice. Hydrofurimazine enables sensitive bioluminescence imaging for either prolonged light production of high sensitivity.

DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo.

PROTAC BRD4 Degrader-13 (compound 9d) is a potent chimeric BRD4 degrader. PROTAC BRD4 Degrader-13 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.025 nM and 6.0 nM, respectively.

Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury

TRPC6-PAM-C20 is a selective TRPC6 positive allosteric modulator. TRPC6-PAM-C20 selectively activates TRPC6 over other TRP channels and also activates TRPA1. TRPC6-PAM-C20 induces transient increase in intracellular Ca2+ in HEK cells expressing TRPC6 (EC50=2.37 μM).

Inecalcitol (TX 522), a unique vitamin D3 analog, is an orally active vitamin D receptor (VDR) agonist. Inecalcitol can induce cell apoptosis and has potent anticancer activities[3.

XY028-140 (MS-140) is a potent and selective PROTAC-based CDK4/CDK6 kinase degrader. XY028-140 specifically inhibits RB-E2F signaling and reduces CDK4 and CDK6 protein levels in a dose- and time-dependent manner in vitro. In addition, XY028-140 can degrade its targets by linking them with ubiquitin-proteasome mechanism. Further, the degradation of CDK4/6 protein by XY028-140 is specifically mediated by CRBN. Therefore, XY028-140 effectively and selectively inhibits and degrades CDK4/6 kinase by targeting CDK4/6 kinase in CDK4/6i-S (CDK4/6 inhibitor-sensitive) tumor cells to the CRL4-CRBN-E3 ubiquitin complex. Compared with CDK6 wild-type cells, XY028-140 treatment of cells expressing wild-type or mutation-activated CDK6 resulted in a more effective degradation of CDK6 (S178P).

EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM.

Aurora kinase inhibitor-2 is a selective and ATP-competitive Aurora kinase inhibitor with IC50s of 310 nM and 240 nM for Aurora A and Aurora B, respectively.

Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes.

CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF.

NL1 is a select bacterial cystathionine γ-lyase (bCSE) inhibitor with IC50 of 5.8 μM (29.2 μM against hCSE). NL1 potentiates bactericidal antibiotics against pathogens.

NL2 is a select bacterial cystathionine γ-lyase (bCSE) inhibitor with IC50 of 1.8 μM (25.3 μM against hCSE). NL2 potentiates bactericidal antibiotics against pathogens.

NL3 is a select bacterial cystathionine γ-lyase (bCSE) inhibitor with IC50 of 0.7 μM (3.4 μM against hCSE). NL3 potentiates bactericidal antibiotics against pathogens.

AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.

BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC)[1]. BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM[2].

SJ6986 is a potent, selective, and orally bioavailable GSPT1/2 degrader with DC50 of 2.1 nM. SJ6986 demonstrates antiproliferative activity in MV4-11 and MHH-CALL-4 cell lines with IC50 of 1.5 nM and 0.4 nM, respectively.

Dodecylphosphocholine is a detergent widely utilized in NMR studies of membrane proteins.

2-(2,6-Dioxopiperidin-3-yl)phthalimidine (EM-12), a teratogenic Thalidomide analogue, is more active than Thalidomide and is much more stable for hydrolysis. 2-(2,6-Dioxopiperidin-3-yl)phthalimidine enhances 1,2-dimethylhydrazine-induction of rat colon adenocarcinomas.

Lipase Substrate is a substrate of lipase to detect activity.

FBPase-1 inhibitor-1 (compound 1) is a novel allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1).

Avexitide (Exendin (9-39)) is a specific and competitive antagonist of glucagon-like peptide-1 (GLP-1) receptor.

BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.

ICCB-19 hydrochloride is an inhibitor of TNFRSF1A Associated Via Death Domain (TRADD) with IC50 of 1.12 μM and 2.01 μM for protecting Velcade-induced apoptosis in Jurkat cells and protecting RDA in MEFs, respectively. ICCB-19 indirectly inhibits Receptor-interacting serine/threonine-protein kinase 1 (RIPK1). ICCB-19 effectively induces autophagy.

MK-8153 is a potent and selective ROMK (potassium channel, Kir1.1) blocker with IC50 of 2.5 nM in rat ROMK, rKir1.1/HEK293 cells. MK-8153 has a longer projected human half-life (~14 h) than MK-7145, which should provide a reduced peak-to-trough exposure ratio and potentially, a smoother, more extended diuretic response.

JNJ-61803534 is a potent RORγt inverse agonist with IC50 of 9.6 nM, selectively inhibiting RORγt-driven transcription versus closely-related family members, RORα and RORβ.

CDK4 inhibitor compound 12 is a novel inhibitor of CDK4 with the activity 97 μM.

LP-184 is a highly potent novel alkylating, next-generation analog of irofulven. LP-184 is an DNA damage repair (DDR) inhibitor and and shows broad anti-tumor cytotoxicity across a panel of NSCLC derived cell lines.

WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1 33. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.

FR179642 is a key intermediate in the synthesis of the echinocandin antifungal Micafungin. FR179642 is the cyclic peptide nucleus of the echinocandin-like antifungal lipopeptide FR901379.

Merafloxacin (CI-934), a fluoroquinolone antibacterial agent, is a selective programmed -1 ribosomal frameshifting (-1 PRF) inhibitor of beta coronaviruses. Merafloxacin exhibits in vitro activity against gram-positive and gram-negative bacteria.

Boc-Asp(OME)-Fluoromethyl Ketone is a broad range caspase inhibitor that inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8.

LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity.