PF-06260933 is a highly selective small-molecule inhibitor of MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4) with IC50 values of 3.7 and 160 nM for cell-freel assay (kinase) and cell assay, respectively. It also inhibits MINK and TNIK with IC50 values of 8 and 13 nM, respectively. PF-06260933 has been reported to improve fasting hyperglycemia […]

CB-1158 analog (CB-1158, INCB01158 or Numidargistat analog) is a potent and orally bioavailable small-molecule inhibitor of the arginase with potential immunomodulating activities. Myeloid cells are an abundant leukocyte in many types of tumors and contribute to immune evasion. Expression of the enzyme arginase 1 (Arg1) is a defining feature of immunosuppressive myeloid cells and leads […]

B-Raf IN 1 is a novel, potent and selective B-Raf inhibitor with IC50 of 24 nM; it is equally potent against c-Raf with IC50 of 25 nM. Moderate selectivity was observed for compound 10n versus p38a (IC50: 0.216 lM) and CAMKII (IC50: 0.822 lM), while high selectivity was observed versus CDK2, CDK4, PKCa, IKKb, JNK1, […]

MRK-016 (MRK016; MRK 016) is a novel, potent, orally bioactive and selective negative allosteric modulator (inverse agonist) of α5 subunit-containing GABAA with nootropic properties. It has been found to produce rapid, ketamine-like antidepressant effects in animal models of depression. Also MRK-016 (MRK) can protect against memory acquisition and consolidation errors in mice. Post-training treatment with […]

TAK-659 2HCl (TAK659 dihydrochloride) is a novel, potent, highly selective and orally bioavailable spleen tyrosine kinase (Syk) inhibitor with anticancer effects. It inhibits Syk with an IC50 of 3.2 nM. TAK-659 shows inhibition toward a SYK-dependent cell line (OCILY10) in a cell proliferation assay. TAK-659 is shown to be able to inhibit the growth of […]

Desmopressin (also known as DDAVP) is a synthetic octapeptide and an analogue of the human antidiuretic hormone arginine vasopressin. Compare with vasopressin, Desmopressin has improved pharmacokinetics such as prolonged half life and better pharmacodynamics such as higher selectivity for the V2 membrane receptor. Vasopressin is a hormone that reduces the production of urine and desmopressin […]

Mavorixafor triHCl (also known as AMD-1107, AMD070, X4P-001) is a potent, selective and orally bioavailable antagonist of CXCR4 with anti-HIV activity. It inhibits CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs. The CXC chemokine […]

Ritlecitinib (PF06651600; PF-06651600) malonate, the malonate salt of PF 06651600, is an irreversible JAK3 inhibitor with anti-inflammatory activity. It inhibits JAK3 with IC50 value of 33.1 nM, and exhibits no activity (IC50 > 10000 nM) against JAK1, JAK2, and TYK2. PF-06651600 has excellent pharmacokinetics/pharmacodynamics with low clearance, benign toxicity profile and high in vivo efficacy. […]

Norcantharidin (also known as NCTD; Endothall anhydride, Norcantharadine) is a dual inhibitor of c-Met and EGFR with anticancer activity. It can induce cell cycle arrest at G2/M phase in HCT116 and HT29 cells. NCTD inhibits not only the expression of the total EGFR and the p-EGFR (phosphorylated EGFR) but also the expression of the total […]

ML329 is a potent small molecule inhibitor of MITF (Micropthalmia-associated transcription factor) which inhibits TRPM-1 (melastatin, a MITF target gene) promoter activity with an IC50 of 1.2 μM. MITF is a lineage restricted basic helix-loop-helix leucine zipper transcription factor that is essential for melanocyte development, function and survival. 15% of human melanomas have MITF gene […]