BIO-013077-01 is a pyrazole TGF-β inhibitor[1].A wide range of cellular functions such as cell proliferation, differentiation, adhesion, migration, and apoptosis are regulated by TGF-β superfamily members. The TGF-βs include the three major TGF-β isoforms, TGF-β1, TGF-β2, and TGF-β3 which are expressed in mammals. TGF-β transduces signals through a complex of two related but structurally and functionally distinct serine/threonine kinase receptors, termed type 1 and type II. Deregulation of TGF-β signaling has been also implicated in various human diseases including cancer, pancreatic diseases, and hematological malignancies[1].

A-395 potently inhibited the formation of H3K27me3 (via antagonizing EED in the trimeric PRC2 complex (EZH2:EED:SUZ12)) with IC50 = 34 ± 2 nM (Hill Slope = 0.7)

DGY-06-116 is an irreversible covalent, selective Src inhibitor.

SB290157 trifluoroacetate is a potent and selective C3a receptor antagonist with an IC50 of 200 nM.

NHC-triphosphate is an intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form. NHC-triphosphate is a weak alternative substrate for the viral polymerase and changes the mobility of the product in polyacrylamide electrophoresis gels[1].

ICCB-19 inhibits RIPK1-dependent apoptosis (RDA) with IC50 of 2.01 μM.

PfDHODH-IN-2, a dihydrothiophenone derivative (Compound 11), is a potent Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor with an IC50 of 1.11 µM. PfDHODH-IN-2 acts as an antimalarial agent and can be used for the research of malaria.

GNF-351 is a potent, pure aryl hydrocarbon receptor (AHR) antagonist (IC50=62 nM) devoid of partial agonist potential; antagonizes agonist and SAhRM-mediated suppression of SAA1, inhibit both DRE-dependent and -independent activity; decreases migration and invasion of HNSCC cells and prevents benzo[a]pyrene-mediated induction of the chemotherapy efflux protein ABCG2.

SP-146 is a potent, selective and non-ATP-competitive inhibitor of Aurora B with IC50 of 0.316 nM. SP-146 can be used for the research of triple negative breast cancer (TNBC).

GSK2814338, also known as Lp-PLA2 -IN-1, is a Lp-PLA2 inhibitor

Sanaid SI 60 is a biochemical.

EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.

beta-Estradiol 17-hemisuccinate

HM30181 is a potent and selective inhibitor of P-glycoprotein.

SR18662 is an optimized compund based on ML264 that inhibits Krüppel-like factor 5 (KLF5) with IC50 of 4.4 nM. SR18662 reduces the viability of multiple colorectal cancer cell lines. SR18662 induces apoptosis.

IPN-60090 dihydrochloride is an orally bioavailable and selective inhibitor of GLS1 (the kidney-type glutaminase), an important enzyme for metabolic energy production. IPN-60090 dihydrochloride can be used in the research of GLS1-mediated diseases[1][2].

A second-generation antihistamine that acts as a selective H1 receptor antagonist.

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.

P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.

p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.

Oliceridine hydrochloride (Olinvo, TRV130) is a potent, selective, and G protein biased μ opioid receptor (MOR) agonist with pEC50 of 8.1.

NUC-1031(SP) is S form of NUC-1031 at P site.Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.

Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.

Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.

NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressin

NAMPT inhibitor-linker 1 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressin

MtbHU-IN-1 is an inhibitor of Mycobacterium tuberculosis nucleoid-associated protein HU (MtbHU), with a Kd of 98 nM for binding to WT MtbHU.

MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC50 of 1 nM.

MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.