Apexbio Technology LLC

LY2857785 is a type I reversible and competitive ATP kinase inhibitor against <b>CDK9</b> (<b>IC₅₀</b> 11 nM) and other transcription kinases <b>CDK8</b> (<b>IC₅₀</b> 16 nM), and <b>CDK7</b> (<b>IC₅₀</b> 246 nM).

IM-12 is an inhibitor of <b>GSK-3β</b>, with an <b>IC₅₀</b> of 53 nM, and also enhances Wnt signalling.

Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM; no inhibition on other HDAC forms. IC50 value: 5 nM [1] Target: HDAC6 inhibitor Nexturastat A displayed low micromolar activity compared to the low nanomolar activity against HDAC6.

kb-NB77-78 is an analog of CID797718, which is a by-product of the synthesis of the parental compound, CID755673(PKD1 inhibitor).

HG6-64-1 is a potent and selective <b>B-Raf</b> inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a <b>IC₅₀</b> of 0.09 μM on B-raf V600E transformed Ba/F3 cells.

Defactinib is a novel <b>FAK</b> inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

BAMB-4(ITPKA-IN-C14) is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 uM in ADP-Glo Assay. IC50 value: 37 uM Target: ITPKA inhibitor BAMB-4 exhibit the lowest inhibition frequency among the InsP3- Kinase inhibitors.

LDN-27219 is a potent inhibitor of hTGase(Tissue transglutaminase) with an IC50 of 0.6 uM. IC50 value: 0.6 uM [1] Target: hTGase inhibitor LDN-27219 is a potent inhibitor of the enzyme(hTGase), producing 100% inhibition at the screening concentration of 10 uM.

VU 0240551 is a small molecule inhibitor of the neuronal K-Cl cotransporter, KCC2 (IC50 = 560 nM for K+ uptake assay in KCC2-overexpressing cells). IC50 value: 560 nM [1] Target: K-Cl cotransporter(KCC2) VU 0240551 exhibits selectivity over the Na-K-2Cl cotransporter, NKCCl.

FR180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2 with Ki value of 0.31 uM and 0.14 uM respectively; has IC50 values of 0.51 and 0.33 μM in enzymatic assays against ERK1 and ERK2, respectively. IC50 value: 0.31 uM/0.14 uM(Ki for ERK1/ERK2); 0.51uM/0.33 μM(ERK1/ERK2) [1] [2] Target: ERK1/2 inhibitor in vi...

ML347(DN193719) is a highly selective ALK1/ALK2 inhibitor with IC50s of 46/32 nM; shows >300-fold selectivity for ALK2 vs.

CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively. IC50 value: 4.76 nM/6.87 nM(wild type/G2019S LRRK2) [1] Target: LRRK2 CZC-25146displayed a very clean profile, it inhibited only five kinases(PLK4, GAK, TNK1, CAMKK2 and PIP4K2C) ...

AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ. IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.) Target: RARα agonist Compound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical ...

AGN 205728 is a potent and selective RARγ antagonist with Ki/IC95 values of 3 nM/ 0.6 nM; no inhibiton on RARα and RARβ. IC50 value: 3 nM/ 0.6 nM(Ki/IC95) Target: RARγ antagonist More information can be found in the following patent, Compound 7a. Preparation of disubstituted chalcone oximes having RARγ retinoid receptor antagonist ...

AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM). IC50 value: 2 nM(Ki) Target: RARα antagonist AGN 196996 shows no activity in transactivation assays, but instead block the gene transcriptional activity induced by ATRA and other RAR agonists.

Helioxanthin 8-1 is an analogue of helioxanthin, exhibites significant in vitro anti-HBV/HCV/HSV-1/HIV activity with EC50 of >5/10/1.4/15 uM. IC50 value: >5/10/1.4/15 uM(HBV/HCV/HSV-1/HIV) [1] Target: Antiviral agent The cyclic hydrazide 28(Helioxanthin 8-1) showed the most potent antiHBV activity among those helioxanthin analogues...