JSF-2414 (JSF2414) is a potent, small molecule GyrB/ParE dual binding inhibitor, simultaneously binds to ATP binding regions of DNA gyrase (GyrB) and topoisomerase (ParE) and displays potent in vitro activity against strains of MRSA, VRSA and VISA.

Cotransin CT8 (CT-08) is a substrate-selective co-translational translocation inhibitor, binds the Sec61 translocon to inhibit cotranslational translocation of a subset of secreted and type I transmembrane proteins.

ZINC20451377 is a small molecule that binds to hepatitis B surface antigen (HBsAg) with high affinity (Kd=65.3 nM), reduces HBsAg levels and HBV virion secretion in cell culture model for HBV.

ING-1466 is an orally active entry inhibitor of influenza A viruses (IAVs) with EC50 of 0.18 uM against IAV H1N1 (PR8-NS1-Gluc), binds to hemagglutinin (HA) and blocks HA-mediated viral infection.

CK-2-63 is a potent first-in-class M. tuberculosis cytochrome bd (cyt bd) inhibitor, demonstrates growth suppression of M. tuberculosis H37Rv with IC50 of 3.7 uM.

NACE2i is a cell permeable, specific and selective peptide inhibitor of nuclear ACE2, inhibits binding between IMP1α and ACE2 and SARS-CoV-2 viral replication. NACE2i specifically targets nuclear ACE2 and not other nuclear proteins targeted by the importin pathway. NACE2i has no impact on ACE2 enzymatic activity. NACE2i prevents inflammation and macrophage infiltration, and increases NK cell infiltration in bronchioles. NACE2i treatment increases the levels of the active histone mark, H3K27ac, restores host translation in infected hamster bronchiolar cells, and leads to an enrichment in methylated ACE2 in hamster bronchioles and lung macrophages. NACE2i has a dual mode of action: suppressing the lethal inflammation in severe COVID-19 and inhibiting viral replication by restoring host translation of anti-viral cytokines.

NBCoV2 is a highly potent small molecule viral fusion inhibitor with potential pan-Coronavirus activity (SARS-CoV IC50=13.8 nM, SARS-CoV-2 IC50=22.8 nM, MERS-CoV IC50=77 nM, cell-based single-cycle assays). NBCoV2 also has potent antiviral activity against all mutant pseudoviruses carrying single-, double-, or triple-mutations featured in the B.1.1.7 UK, B.1.351 RSA, and B.1.617.2 Delta variants (IC50=30-80 nM). NBCoV2 completely preventing the induction of any virus-induced CPE (IC100=1.25 uM, SARS-CoV-2 (US_WA-1/2020)). NBCoV2 bind to the S2 subdomain of the SARS-CoV-2 trimer, thus, inhibits the fusion of CoVs with the cell membran, and is specific for the SARS-CoV-2 S protein.

SB27012 (SB 27012) is a small molecule PPI inhibitor of the Spike RBD-ACE2 interaction (IC50=7.7 uM in ELISA assays), binds ACE2 (Kd=210 nM) without affecting ACE2 enzymatic activity.

BAY 1892005 is a small molecule that modulate mutant p53 condensation and nuclear accumulation, binds covalently to mutant p53R175H and p53Y220C and shows stabilization of p53WT and p53Y220C, exhibits anti-proliferative activity in a set of cell lines wit

GNE-684 is a potent, cross-species, specific RIP1 kinase (RIPK1) inhibitor with IC50 of 21, 189 and 691 nM for human, mouse and rat RIP1, respectively.

FX2149 (FX 2149) is a potent, BBB permeable inhibitor of LRRK2 GTP binding activity with IC90 of 10 nM, reduces PD-linked mutant LRRK2 variants (G2019S and R1441C) that bound with GTP.

MK-1468 is a potent, selective, brain-penetrant LRRK2 inhibitor with IC50 of 0.4 nM (G2019S LRRK2), potently inhibits the phosphorylation of LRRK2 serine 935 (pSer935) in hPBMCs with IC50 of 2.8 nM.

SW120619 is a specific small molecule inhibitor of WNK3 kinase with IC50 of 0.7 uM, weakly inhibits WNK1 and WNK2 with IC50 of 2.3 and 16.8 uM, respectively.

ML315 is a small molecule inhibitor of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases with IC50 of 68, 231, >10,000, 68, 282 and 1156 nM for CLK1/2/3/4 and DYRK1/2, respectively.

MW01 is a specific inhibitor for DNA damage-induced NF-κB activity, inhibits CLK2 and CLK4 with IC50 of 360 and 14.1 nM, does not inhibit CLK3.

GFH009 is a potent, selective CDK9 inhibitor, inhibits the activity of the CDK9/cyclin T1 regulatory complex of P-TEFb.

QBS10072S is a novel dual-function, BBB permeable chemotherapeutic agent with alkylating moiety and a selective large neutral amino acid transporter 1 (LAT1, SLC7A5) substrate, shows excellent BBB penetration and promising efficacy in vitro (U251 cell IC5

H3B-960 is a potent, selective and covalent inhibitor of Werner syndrome protein (WRN) helicase activity with IC50 of 60 nM.

HRO761 is a potent, selective, allosteric WRN inhibitor with IC50 of 100 nM (ATPase assay) and GI50 of 40 nM (SW48 cells), respectively. HRO761 binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation.

DI-87 ((R)-DI-87) is a highly potent, specific, orally bioavailable deoxycytidine kinase (dCK) inhibitor with IC50 of 3.15 nM.

Allopole is the first allosteric, specfic and cell-permeable inhibitor of the noncatalytic polo-box domain (PBD) of PLK1 (Polo-like kinase 1), Allopole is the prodrug of Allopole-A.

GSK3335103 is a highly potent and orally bioavailable nonpeptidic αvβ6 integrin inhibitor with pIC50 of 8.0. GSK3335103 shows high desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance, moderate volumes of distributio, high to complete oral bioavailabilities and high solubility in all physiological media.

AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells.

GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.

TYA-018 (TYA018) is a potent, isoform-selective inhibitor of HDAC6 with IC50 of 10 nM, inhibits tubulin acetylation (Ac-Tubulin) with EC50 of 120 nM in cell-based assay in induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs).

DP308 is a novel and effective 53BP1 tandem Tudor domain (TTD) inhibitor, disrupts the binding between 53BP1 and H4K20me2 peptide with IC50 of 1.69 uM.

IHMT-337 (IHMT337) is a potent, highly selective and irreversible EZH2 inhibitor, specifically inhibits the methylation at H3K27.

JYQ-42 is a potent, selective SIRT6 allosteric inhibitor, effectively inhibits SIRT6 deacetylation with IC50 of 2.33 uM, inhibits the deacetylation activity of SIRT6 in pancreatic cancer cell lines.

QAF-805 (QAF805) is a potent, dual adenosine-A2B receptor and adenosine-A3 receptor antagonist with Ki of 3.4 nM (A2B).

YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.

ASP4345 (ASP-4345) is a potent, selective positive allosteric modulator of the dopamine type 1 (D1) receptor that selectively binds to, and enhances the activity of, D1 receptors.

F17464 is a dopamine D3 receptor preferential antagonist exhibiting high affinity for human dopamine receptor subtype 3 (hD3) (Ki=0.17 nM) and 5-HT1a (Ki=0.16 nM) and a >50 fold lower affinity for the human dopamine receptor subtype 2 short and long form (hD2s/l) (Ki=8.9 and 12.1 nM, respectively). F17464 is a D3 receptor antagonist, 5-HT1a receptor partial agonist. F17464 blocks ketamine induced morphological changes, an effect D3 receptor mediated, in human dopaminergic neurons. F17464 increases dopamine release in the rat prefrontal cortex and mouse lateral forebrain-dorsal striatum and seems to reduce the effect of MK801 on % c-fos mRNA medium expressing neurons in cortical and subcortical regions. F17464 also rescues valproate induced impairment in a rat social interaction model of autism, with dose range 0.32-2.5 mg/kg i.p. in both rats and mice

ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3.

CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM.

ML353 (VU0478006) is a highly potent, selective, MPEP-site silent allosteric modulator of mGlu5 receptor with with sub-100 nM affinity.

CVN766 (CVN 766) is a potent, exquisitely selective orexin 1 receptor (OX1R) antagonist with IC50 of 8 nM, 1000-fold selective over OX2R.

JR1-157 is a potent selective sigma 2 receptor (σ2R) ligand with Ki value of 47 nM, >10-fold selectivity over σ1R.

WLB-89462 (WLB89462) is a potent, highly selective sigma-2 receptor (σ2R) ligand with Ki of 13 nM, >100-fold selective over σ1R (Ki=1777 nM).

S6821 (S 6821) is a potent and selective bitter taste receptor TAS2R8 with IC50 of 21 nM.

Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.

DFV890 (IFM-2427) is apotent, selective and orally active inhibitor of NLRP3 inflammasome, directly binds to NLRP3 and locks the protein in an inactive conformation,prevents NLRP3 inflammasome assembly in response to sterile danger signals.

OV350 (OV-350) is a potent, selective and direct K+-Cl- cotransporter KCC2 agonist with EC50 of 261.4 nM, with no effect on KCC2 plasma membrane accumulation and phosphorylation.

1PBC is a small molecule blocker of calcium-activated chloride channel TMEM16A, blocks TMEM16A completely with an IC50 of 4 uM at zero mV and saturating Ca2+ concentration (2 uM).

TMinh-23 is (Compound 10bm) is a potent, selective inhibitor of transmembrane protein 16A (TMEM16A or ANO1, DOG1, ORAOV2, TAOS-2) with IC50 of 30 nM in short-circuit current assays, weakly inhibits TMEM16B (IC50=400 nM, 13 -fold selectivity).

NV-6297 (NV6297) is a potent, selective mTORC1 pathway signaling inhibitor without inhibition on mTORC2, inhibits S6K1 phosphorylation (pS6K1 T389) in MCF7 cells with IC50 of 120 nM, directly and selectively targets GLUT-1.

Org 34167 HCl salt is a broad-spectrum inhibitor of HCN channels with IC50 of 23.4, 8.2 and 9.2 uM for HCN1, HCN2 and HCN4 channels, respectively, slowing activation and causing a hyperpolarising shift in voltage-dependence of activation.

Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV).

VU0546110 (VU 0546110) is a potent, selective inhibitor of the sperm-specific potassium channel SLO3 with IC50 of 1.29 uM, impairs sperm function.

LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.

AD-5591 (AD5591) is a potent, selective, new generation small molecule ALDH2 activator, has the improved biological activities and pharmacological properties compared to Alda-1. AD-5591 (100  μM) significantly increases the enzymatic activity of recombinant WT and mutant human ALDH2 proteins. AD-5591 is the active form of AD-9308.

AD-9308 is a water-soluble, orally bioavailable, potent, and highly selective ALDH2 activator, AD-9308 is a valine ester prodrug of a potent and selective small molecule ALDH2 activator AD-5591.

MZ-101 is a potent, selective inhibitor of glycogen synthase 1 (GYS1) with IC50 of 41 nM (human GYS1), with no inhibition against GYS2.

ADAM9i is a specific small molecule inhibitor of ADAM9 protein with binding KD of 5.9 uM and enzyme IC50 of 5.2 uM, promotes the selective degradation of KRAS and sensitizes pancreatic cancers to chemotherapy.

BAY-9835 is the first orally bioavailable ADAMTS7 inhibitor with IC50 of 6 nM, which is selective against a range of off-targets and metalloproteases except for ADAMTS12.

NAMPT activator (NAT) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 500 nM.

CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.

NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.

MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM.

ATF3W-aeg peptide is a selective, peptide inhibitor of activating transcription factor 3 (ATF3) with high affinity (Kd=151 nM), increases CCL4 expression levels in human macrophages.

SLU-PP-332 is a potent, selective pan ERRα/β/γ agonist with EC50 of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, in full-length ERR cell-based cotransfection/reporter assays.

BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells.

CS27109 is a potent, selective thyroid hormone receptor-β (THR-β) agonist with AC50 value of 1.98 uM, 12.6-fold selectivity over THR-α.

EN171 covalently targets both C38 and C96 on 14−3−3 to enhance 14−3−3 interactions with ERα, YAP, and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity.

(R)-SKBG-1 is a covalent small molecule ligand of RNA-binding protein NONO, engages NONO Cys145 and suppress an array of cancer-relevant genes and impair cancer cell proliferation.

(S)-CKi-1 is a selective, covalent inhibitor of creatine kinases (CKs), inhibits recombinant creatine kinase B (CKB) phosphotransfer activity with IC50 of 0.6 uM, depletes creatine phosphagen energetics in cells.

5M-8OH-Q is a specific small molecule inhibitor of UDP-glucose glycoprotein glucosyltransferase (UGGT), binds a CtUGGTGT24 “WY” conserved surface motif conserved across UGGTs (Kd=47 uM) but not present in other GT24 family glycosyltransferases.

AGI-25696 (AGI 25696) is a potent and selective inhibitor of methionine adenosyltransferase MAT2A, blocks the growth of MTAP-deleted tumors in vivo.

ARUK2001607 is a potent, selective and brain penetrant PI5P4Kγ inhibitor with binding KD of 7.1 nM, pIC50 of 7.1 (PI5P4Kγ+).

C902 is a small-molecule inhibitor targeting LIN28-let-7 interaction, shows dose-dependent inhibition in an EMSA validation assay with IC50 of 5 uM.

CMP05 (Endosomolytic compound CMP05) is a novel endosomolytic small-molecule compound that exhibits higher transfection efficiency/ability to induce endosomal escape of oligonucleotides (ONs) than current compounds such as chloroquine.

CPAG-1 (PGRMC2 activator CPAG-1) is a small-molecule activator of PGRMC2. CPAG-1 treatment had no effect on weight or food intake but treated mice had reduced fasting glycemia and insulin levels. CPAG-1 decreased Rev-Erbα protein in BAT of CPAG-1-treated mice. CPAG-1 also significantly increased labile heme in the nucleus of brown adipocytes from CPAG-1-treated mice within 4 days of treatment.

DB2313 is a small-molecule transcription factor PU.1 inhibitor abrogating DNA binding by PU.1 with Kd of 29 nM.

DS55980254 (DS 55980254) is potent, selective and orally active PTDSS1 (phosphatidylserine synthetase 1) inhibitor, suppresses phosphatidylserine (PS) production activity of PTDSS1 (IC50=100 nM) in cell-free assays, but not that of PTDSS2.

IDE-397 (GSK-4362676, GSK-676) is a potent, selective small molecule methionine adenosyltransferase 2a (MAT2A) inhibitor, displays broad anti-tumor activity across a panel of MTAP-deleted patient-derived xenografts.

Kakeimide is a potent GH3 inhibitor that selectively targets IAA-conjugating GH3 proteins at subnanomolar concentrations in vitro, shows auxin-like activity by inhibiting endogenous IAA catabolism.

Macrocyclic peptide D4-2 is a macrocyclic peptide consisting of 15 amino acids that binds to the ectodomain of mouse SIRPα (Kd=10 nM, IgV-B6 SIRPα) and efficiently blocks CD47-SIRPα interaction in an allosteric manner (IC50=0.18 uM).

NCP26 is a potent, ATP-competitive prolyl-tRNA synthetase (ProRS, PRS) inhibitor, inhibits recombinant human ProRS in the presence of 100 μM proline with KD of 0.35 nM in TR-FRET assays.

Ninerafaxstat 3HCl (CV-8972) is a small molecule compound that promotes glucose oxidation, decreases fatty acid oxidation and improve overall mitochondrial respiration, inhibits the growth and proliferation of cancer cells.

NOX-6-18 is a potent, selective GPR132 antagonist with IC50 of 17 nM.

PAT1inh-A0030 is a potent and selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor with IC50 of 1.0 uM, shows no activity on relevant ion transporters/channels (SLC26A3, SLC26A4, SLC26A9, CFTR, TMEM16A).

PAT1inh-B01 is a small-molecule, selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor, could fully inhibit PAT1-mediated anion exchange with IC50 of 350 nM.

PFKL activator NA-11 is a small-molecule, selective PFKL activator, inhibits the NOX2-dependent oxidative burst in neutrophils by activating the glycolytic enzyme phosphofructokinase-1 liver type (PFKL).

Varoglutamstat (PQ912) is a potent glutaminyl cyclase (QC) inhibitor with Ki values of 20-65 nM for human, rat, and mouse QC activity.

PSB-CB-27 is a potent, selective antagonist of GPR18 with IC50 of 650 nM, shows no inhibition on GPR55 and low affinity for CB1/CB2 receptors.

PXS-4748 (PXS4748) is a potent, selective and irreversible pan-lysyl oxidase (pan-LOX) inhibitor with IC50 of 2.0 uM and 3.2/0.6/1.4/0.2 uM for bovine (aorta) LOX and rh LOXL1/2/3/4, respectively.

S-181 (S 181) is a specific small-molecule activator (modulator) of β-glucocerebrosidase (GCase) with AC50 of 1.49 uM and a maximum activation of 780%.

S9-A13 is a highly potent and specific inhibitor of SLC26A9, potently inhibits SLC26A9-mediated Cl−/I− and Cl−/SCN− exchange activities with IC50 of 90.9 and 171.5 nM, respectively.S9-A13 does not inhibit other members of the SLC26 family and has no effects on Cl− channels such as CFTR, TMEM16A, or VRAC.S9-A13 (0-1 uM ) inhibits SLC26A9 currents in a dose-dependent manner in HEK293 cells, but shows little effects on CFTR currents in HEK293 cells at the highest concentration (5 uM).S9-A13 has a minor effect on ion transport in human airway epithelial cells and mouse trachea, despite clear expression of SLC26A9 in the apical membrane of ciliated cells.

SAR439883 (SAR 439883) is a novel potent, selective, orally active PKR inhibitor with IC50 of 0.68/0.69 uM against hPKR/mPKR, respectively.

SN34960 is a small molecule Perforin inhibitor, inhibits perforin-induced lysis of Jurkat T-lymphoma cells with IC50 of 6.65 uM, shows suboptimal physicochemical properties and toxicity toward the natural killer (NK) cells that secrete perforin in vivo.

SS-1-148 is a potent, selective inhibitor of human ornithine δ-aminotransferase (hOAT) with Ki of 60 uM, shows excellent selectivity over other related aminotransferases (e.g., GABA-AT).

TMX-4102 (TMX4102) is a highly potent, selective PIP4K2C binder with KD of 0.45 nM, shows no affinity for PIP4K2B and PIP4K2A (KD>10 uM).

TR-107 (TR107) is a highly potent, selective and orally bioavailable small-molecule activator of the mitochondrial protease ClpP with EC50 of 140 nM, binds to purified ClpP with Kd value of 180 nM in surface plasmon resonance (SPR) measurement.

Tryptolinamide (TLAM) is a small-molecule compound that activates mitochondrial respiration in cybrids generated from patient-derived mitochondria and fibroblasts from patient-derived iPSCs, inhibits phosphofructokinase-1 (PFK1) with an ATP-uncompetitive

UT-59 is a specific inhibitor of cholesterol-sensing membrane protein Scap, binds to Scap's cholesterol-binding site, blocks SREBP activation and inhibits lipid synthesis.

X-Neu5Ac (sodium) is a substrate for chromogenic assay of neuraminidase activity in bacterial expression systems; with a Km of 0.89 mM for neuraminidase.

YB-537 (YB537) is a potent, highly specific quinone reductase 2 (QR2) inhibitor with IC50 of 3 nM, shows no activity against QR1 (IC50>10 uM).

Rebecsinib (17S-FD-895) is a selective small-molecule inhibitor of splicing-mediated ADAR1 activation, prevents leukemia stem cell generation.

AG-946 (AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.

BI-9774 (BI 9774) is a potent pan-AMPK activator with EC50 of 64 nM in an ADP-Glo kinase assay with human AMPK (α1β1γ1) and EC50 of 8 nM in a cellular GLUT4 translocation assay.

cyclo-CRVLIR is a cyclic peptide that binds selectively to p110α RAS binding domain (p110α-RBD) with ITC Kd of 3 uM, blocks p110α/RAS interaction in vitro and KRAS cancer cell lines.

NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research.

OSSL_325096 is a novel potent small mlolecule p97/VCP inhibitor, suppresses cell proliferation and induces ER stress and apoptotic cell death in MM cell lines (IC50=0.1-0.5 uM).

HA-9104 is a specific small molecule inhibitor of E2 conjugating enzyme UBE2F with IC50 of 33.29 uM for inhibition of cullin-5 neddylation, abrogates UBE2F-NEDD8 thioester formation and inhibits cullin-5 neddylation.

BAY-405 is a potent and selective MAP4K1 inhibitor with IC50 of 6 nM. BAY-405 potentiates in vitro and in vivo antitumor T-cell reactivity which overcomes the suppression by TGFβ and PGE2.

Darizmetinib (HRX-0215, HRX0215) is a potent, selective inhibitor of MKK4 (MAP2K4/SEK1), shows potential for promoting liver regeneration or reducing or preventing hepatocyte death.

HRX-0233 (HRX0233) is a potent, selective MAP2K4 (MKK4) inhibitor, HRX-0233 is synergistic with RAS inhibitors in KRAS-mutant cancers.

NFX-179 (Nedometinib, NFX179) is a potent, specific, topical, metabolically labile MEK1/2 inhibitor with biochemical IC50 of 135 nM (MEK1).

Non-canonical p38α inhibitor NC-37 (NC-p38i NC-37) is a potent, highly selective, non-canonical inhibitor of p38α, inhibits TAB1-induced p38α autophosphorylation in vitro with IC50 of 0.27 uM.

BC-DXI-32982 is a potent inhibitor of the interaction between DX2 and KRAS4B with a half-maximal inhibitory concentration (IC50) of 0.18 μM, showing little effect on the PRKACA-PRKAR2A interaction.

RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM.

Tepotinib (EMD1214063, MSC2156119) is a potent, specific and ATP-competitive inhibitor of MET (HGFR) with IC50 of 23 nM for MET WT autophosphorylation and 2.2-42.6 nM for M1268T, Y1248H, H1112Y, L1213V, H1112L, V1110I, V1206L, and V1238I MET-mutated varia

WM-S1-030 is a highly potent, specific inhibitor of recepteur d'origine nantais (RON kinase, MST1R) with IC50 of 0.39 nM in in vitro enzyme activity.

DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of

OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.

NRPa-308 is a neuropilin-1 (NRP-1) antagonist, inhibits the VEGF-A165/NRP-1 binding with IC50 of 42 uM, exerts in vitro anti-angiogenic activity.

Z271-0326 is a first-in-class, potent and specifc inhibitor of NACK (Notch activation complex kinase) with SPR KD value of 0.89 uM, directly blocks NACK recruitment to the Notch ternary complex (NTC).

RXC004 (RXC-004) is a potent, selective Porcupine (PRCN) inhibitor, inhibits functional Wnt production from mouse L-Wnt3a cells with IC50 of 64 pM in luciferase reporters assays.

A drug-linker conjugate for antibody-drug conjugate by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide SuO-Val-Cit-PAB..

BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78.

KH-103 is a highly potent, catalytically-driven glucocorticoid receptor (GR) PTORAC degrader, demonstrate excellent performance in passively preventing ligand-induced gene expression activation in the absence of partial agonistic transcriptional triggerin

MS40 is a cereblon (CRBN)-based proteolysis targeting chimera (PROTAC) degrader of the onco-target WD repeat domain 5 (WDR5) [1]. WDR5 is an integral component of the MLL/KMT2A lysine methyltransferase protein complex. The WDR5-binding component of MS40 is the selective inhibitor OICR-9429, and the CRBN-targeting moiety is the immunomodulatory drug pomalidomide. MS40 promotes degradation of WDR5 and the pomalidomide transcription factor neo-substrates IKZF1 and IKZF3.

XY-07-35 is a potent, selective HDAC6 proteolysis targeting chimera (PROTAC) degrader with IC50 of 48.5 nM.

K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.

L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.

GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.

PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.

TEAD activator Q2 (Quinolinol Q2) is a small molecule activator of TEAD with EC50 of 2.6 uM in TEAD dual-luciferase reporter (DLR) assays, inhibits TEAD-palmitate interaction with IC50 of 1.7 uM.

VT-107, as an analogous to VT104, is an orally active and potent pan-TEAD auto-palmitoylation inhibitor. VT-107 can be used for the research of cancer.

Fluorofurimazine is a novel furimazine analogue, with increased aqueous solubility enabling higher signal emission than furimazine for bioluminescence imaging. Fluorofurimazine enables higher substrate loading and improved optical imaging sensitivity in in-vivo.

ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP). It exhibits an EC50 of 1.37 μM for α-casein hydrolysis by HsClpP. ZK53 treatment allosterically activates HsClpP to uncontrollably degrade the essential mitochondrial proteins and is inactive toward bacterial ClpP proteins.

N6F11 is a ferroptosis inducer, and can trigger the degradation of glutathione peroxidase 4 (GPX4) specifically in cancer cells. N6F11 can be used for ferroptosis study.

Lotiglipron (PF-07081532) is an orally active GLP-1R agonist. It reduces glucose and body weight, and has the potential to be used in Type 2 diabetes mellitus (T2DM) research.

HRX215 is a first-in-class MKK4 inhibitor with IC50 of 0.02 μM and shows above 100-fold selectivity against JNK1, BRAF, and MKK7. HRX215 increases liver regeneration after hepatectomy in murine and porcine models.

DB-lipidoid 11-10-8 is a degradable branched (DB) lipidoid. 11-10-8 LNP is more potent than MC3 LNP at delivering mRNA. 11-10-8 LNP enables roughly five-fold higher TTR genome editing efficiency and therapeutic FGF21 protein expression compared to MC3 LNP.

KSQ-4279 is a USP1 and PARP inhibitor. KSQ-4279 showed anti-proliferative effects in a subset of cell lines, often characterized by the presence of homologous recombination deficiencies (HRD), including mutations in BRCA1/2. The combination of KSQ-4279 with olaparib was able to induce strong and durable regressions across a number of ovarian and TNBC PDX models.

PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.

6-Diazo-5-oxo-L-nor-Leucine (DON) is a glutamine analog that inhibits glutaminases (Ki = 6 µM) and other glutamine-utilizing enzymes, including cytidine triphosphate synthase (CTPS), which uses glutamine in the synthesis of CTP.1,2,3 DON is commonly used in cells or tissues but its use in whole animals is limited by its teratogenicity.

Lipid GVS-18-B6 is a silicon ether ionizable lipid for mRNA delivery. GVS-18-B6 showes particularly good liver specificity, with a liver-to-spleen EGFP signal ratio of 92:1. GVS-18-B6 also showes rapid tissue clearance within 6 hours of dosing.

RMC-7977 is a reversible, tri-complex RAS inhibitor with broad spectrum activity for both mutant and wild-type (WT) KRAS, NRAS, and HRAS variants.RMC-7977 can lead to tumor regressions and was well tolerated in diverse RAS-addicted preclinical cancer models. RMC-7977 also can inhibit the growth of KRASG12C cancer models.

Lipid CAD9 (3-A2-7b is a cationic degradable (CAD) lipid. 3-A2-7b formulated LNP, LNP-CAD9, can deliver FLuc mRNA to the lungs in vivo. LNP-CAD9 co-delivering Cas9 mRNA/VEGFR2 single guide RNA (sgRNA) effectively induces VEGFR2 knock out in lung endothelial cells of female mice.

dCeMM1 is a RBM39 glue degrader. dCeMM1 shows functions by re-directing the activity of the CRL4DCAF15 ligase. dCeMM1 decreases the expression of RBM39 levels in WT KBM7 cells[1].

AAcid-PEG5-C2-Boc is a PEG derivative containing a t-butyl protected carboxyl group with a terminal carboxylic acid. The terminal carboxylic acid can be reacted with primary amine groups in the presence of activators (e.g. EDC, or DCC) to form a stable amide bond. The hydrophilic PEG spacer increases solubility in aqueous media. The t-butyl protected carboxyl group can be deprotected under acidic conditions.

Tri-GalNAc(OAc)3 is a triantenerrary N-acetylgalactosamine (tri-GalNAc) with an amino group, which is useful precursor for synthesis of GalNAc-LYTAC that engage the asialoglycoprotein receptor for targeted protein degradation. Tri-GalNAc(OAc)3 was first reported in Nat Chem Biol. 2021 Sep;17(9):937-946 (compound ). This product has no formal name at the moment.

DSPE-PEG2K-triGalNAc is a polar lipid composed of DSPE and tri-N-acetylgalactosamine that can be used to construct liposomes target to asialoglycoprotein receptor (ASGPR).

RMC-9805 is a first-in-class, mutant-selective, covalent and orally bioavailable KRAS-G12D(ON) inhibitor. RMC-9805 exhibits direct anti-tumor effects and indirectly transformed the TME through inhibition of cancer cell-intrinsic KRAS-G12D oncogenic signaling.

ABBV-303 is a novel c-Met targeted multispecific NK cell engager. ABBV-303 binding to NKG2D and CD16a results in redirection of both innate (NK cells) and adaptive (CD8+ T cells) immune cells to lyse c-Met expressing tumor cells.

ORIC-944 is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). ORIC-944 is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.

BBO-8520 is a first-in-class, direct covalent inhibitor of both KRAS-G12C (ON) and (OFF) states. BBO-8520 displays highly significant binding to KRAS-G12C in a global cysteine proteome analysis and is 100x more selective for KRAS-G12C than for WT-KRAS and other mutant isoforms, with no measurable activity against N- or H-RAS.

NST-628 is a potent pan-RAF-MEK molecular glue that prevents phosphorylation and activation of MEK by RAF. NST-628 demonstrates broad efficacy in cellular and patient-derived, in vivo tumor models harboring KRAS, NRAS, BRAF class II/III, and NF1 mutations.

VVD-214 (RO7589831) is a synthetic lethal allosteric inhibitor of WRN helicase. VD-214 covalently engages cysteine 727 of WRN in a nucleotide cooperative manner and inhibits ATP hydrolysis and helicase activity, resulting in widespread double-stranded DNA breaks, nuclear swelling, and cell death in MSI-high, but not microsatellite stable cells.

RMC-6236 is a first-in-class, potent, oral tri-complex RASMULTI(ON) small molecule inhibitor designed to treat cancers driven by a variety of RAS mutations.

U-101 is an ionizable lipid for mRNA delivery. U-101-LNP/IL-2F mRNA formulation demonstrats effective antitumor activity and safety.LNPs containing lipid U-101 and encapsulating mRNA encoding a fusion protein composed of IL-2, a linker, and CD25 inhibit tumor growth in an MC-38 mouse xenograft model.

AZD8421 is a highly selective CDK2 inhibitor with IC50 of 9 nM and shows selectivity over CDK1, CDK4 and CDK6. AZD8421 shows robust monotherapy activity in a CCNE1 amplified ovarian model OVCAR3 with regressions seen with monotherapy and in combination with palbociclib.

DBCO-PEG4-acid is a PEG Linker. PEG Linkers may be useful in the development of antibody drug conjugates.

HC-7366 is an orally bioavailable and efficacious GCN2 (general control nonderepressible 2) kinase activator with IC50 of 12 nM.

Bz-(Me)Tz-NHS is a click chemistry reagent containing an methyltetrazine group. Bz-(Me)Tz-NHS is 3rd generation Click-Linker for Cu-free click conjugation.

Lipid TE-EP8-S is a one-component ionizable cationic lipid for mRNA delivery to splenic T cells.

Lipid B3 is a biodegradable ionizable lipid for liver targeted delivery. Lipid B3-LNP shows high delivery efficacy and low toxicity in delivering RNA to liver cells.

SUN 75856, also known as N-trifluoroacetyl (TFA) protected aminolink C6 phosphoramidite for the synthesis of 5'-amino-modified oligonucleotides. TFA protection is smoothly removed during ammonia deprotection, and does not require any additional steps. If necessary, the resulting oligonucleotides can be purified by ion exchange chromatography, or gel electrophoresis. This product has no formal name at the moment.

Endosidine 5 (ES5), is one of the most potent small molecules interferes with recycling endosomes through Annexin A6, thereby promoting the release and expression of mRNA into the cytoplasm. The delivered mRNAs is greatly enhanced via inhibition of endocytic recycling in cells and in live mice. NAV2729 (NAV) and endosidin 5 (ES5), resulted in significant enhancement (1.5–2 folds) of LNP-mediated delivery of Fluc mRNAs. Incubation of NAV and ES5 together caused modest further increases in Fluc expression in comparison to the sole application of either compound.

NSC 102533 (Compound N3) is a potent inhibitor of mitochondrial electron transport. Antimalarial agent 14 can serve as an anti-malarial agent.

10-Methyl-9-(phenoxycarbonyl)acridinium fluorosulfonate, a phenyl ester of acridinium esters, is a fluorescent dye that produces chemiluminescent under neutral conditions. 10-Methyl-9-(phenoxycarbonyl)acridinium fluorosulfonate can be used for the measurement of hydrogen peroxide.

Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM. Butyl isobutyl phthalate shows a hypoglycemic effect and has the potential for diabetes treatment.

Pamicogrel (KBT3022) is a cyclooxygenase (COX) inhibitor.

Bis(trans-cinnamic acid)anhydride is a Parasite inhibitor tnat can be isolated from Cinnamomum zeylanicum and exhibits moderate activity against Plasmodium falciparum.

WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects.

(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of?dopamine receptor, a partial agonist of the?5-HT1A receptor, and an antagonist of the?α2B-adrenergic receptor, with?Kis of 0.71?nM, 4-15?nM, and 83?nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

N-[(1R)-4-[(Aminoiminomethyl)amino]-1-[[[(1R)-1-(4-hydroxyphenyl)ethyl]amino]carbonyl]butyl]-α-phenylbenzeneacetamide is an anticonvulsant agent with potential for the treatment of generalized tonic-clonic and partial seizures.

NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.