IDO-IN-2 is an IDO inhibitor extracted from patent WO/2015031295 A1, compound example 1, has IC50 values of 0.068 μM in HeLa cell and 0.16 μM in HEK293 cell.

AZ7550 Mesylate is an active metabolite of AZD9291 (Osimertinib) and inhibits the activity of IGF1R with an IC50 of 1.6 μM.

IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.

Brevifolincarboxylic acid is extracted from Polygonum capitatum, has inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarboxylic acid has anticancer and anti-inflammatory activities

SC-43, a sorafenib derivative, is an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) and reduces liver fibrosis. SC-43 reduces p-STAT3 and induces apoptosis with anti-tumor activity.

Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is effective against caspases-1 (IC50 of 46.7 nM), caspases-4 (IC50 of 1.49 μM), caspases-5 (IC50 of 329 nM), and caspases-11 , but not the apoptotic caspases such as caspase-3.

BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.

Importazole is an inhibitor of importin-β transport receptors.

CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe.

Y-27632 is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

Ingenol is an extremely weak protein kinase C (PKC) activator.

INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.

inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.

RapaLink-1 is a third-generation mTOR inhibitor that overcomes resistance to existing first- and second-generation inhibitors; blocks mTOR signaling of the F2108L mTOR and M2327I mTOR drug resistant mutants; RapaLink-1 is more potent mTOR inhibitor than rapamycin.

FEN1-IN-4 (Compound 2) is a human flap endonuclease-1 (hFEN1) inhibitor.

Irinotecan hydrochloride is the hydrochloride salt of a semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata.

Rucaparib camsylate is a potent, orally available inhibitor of poly ADP-ribose polymerase (PARP) 1 and 2.

A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets.

WH-4-025 is a Salt-inducible kinase (SIK) inhibitor (WO2016023014 A2).

Valrubicin (AD-32) is a chemotherapy drug used to treat bladder cancer.

A-779 is a peptide antagonist of the Mas receptor, also known as the angiotensin (1-7) (Ang (1-7)) receptor (IC50 = 0.3 nM in a radioligand binding assay).

A new-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infections, the prodrug of the active compound VM-1500A..

CITCO is a potent constitutive androstane receptor (CAR) agonist (EC50 = 49 nM). CITCO altered expression of key drug-metabolizing enzymes and transporters in human hepatocytes, which positively affects the metabolic profile of CHOP. Coadministration of CITCO and CHOP in the coculture model led to significantly enhanced cytotoxicity in lymphoma cells but not in cardiomyocytes. Constitutive androstane receptor (Car)-driven regeneration protects liver from failure following tissue loss. The constitutive androstane receptor (CAR and NR1i3) is a key regulator of CYP2B6.

EHP-101 (VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. EHP-101 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. EHP-101 attenuates adipogenesis and prevents diet-induced obesity. EHP-101 (20 mg/kg/day; i.p.; for 3 weeks) induces a significant reduction in body weight gain, total fat mass, adipocyte volume and plasma triglycerides levels in HFD mice.

AH-7614 is a selective free fatty acid receptor 4 (FFA4/GPR120) antagonist.

E-3810 is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity.

Ceritinib, also known as LDK-378, is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). In Phase I trials, LDK378 showed a marked clinical response in 78 patients with anaplastic lymphoma kinase positive (ALK+) metastatic non-small cell lung cancer (NSCLC) who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib. LDK378 blocks the ALK protein and stops it sending growth signals to cancer cells, which may stop them growing. Ceritinib was approved in April 2014.

Crizotinib (PF-02341066;PF-2341066) is a potent, selective, orally bioavailable, ATP-competitive inhibitor of c-Met catalytic activity with Ki of 4 nM.

PFI-90 is a selective inhibitor of the histone demethylase KDM3B. PFI-90 induces apoptosis and cell differentiation resulting in delayed tumor progression in vivo.

A small molecule inhibitor of the NF-κB family member c-Rel with IC50 of 3 uM in EMSA assays.