TCASK10

Research use only, not for human use.

TCASK10 is a potent, highly specific inhibitor of ASK1 with IC50 of 14 nM.

TCASK10 is a potent, highly specific inhibitor of ASK1 with IC50 of 14 nM, 30-fold selectivity over ASK2 (IC50=510 nM) and no activity against MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf; blocks downstream JNK1/p38 phosphorylation in cells, dose-dependently reduces mitogen (FBS, PDGF and EGF)-induced airway smooth muscle (ASM) growth, also prevents TGFb1-induced migration of ASM cells in vitro.

TC ASK 10 (Compound 10; 0-10 μM; 1 hour; INS-1 cells) treatment inhibits streptozotocin (STZ)-induced JNK in INS-1 pancreatic β cells from 0.3 μM. Phosphorylation of p38 is also inhibited in a dosedependent manner. Western Blot Analysis Cell Line:INS-1 cells Concentration:0 μM, 0.3 μM, 1 μM, 3 μM, 10 μM Incubation Time:1 hour Result:Was found to inhibit streptozotocin (STZ)-induced JNK in INS-1 pancreatic β cells from 0.3 μM. Phosphorylation of p38 was also inhibited in a dosedependent manner.

Pharmacokinetic profiles in rats are tested. TC ASK 10 (Compound 10?HCl; rat cassette doing at 0.1 mg/kg, iv and 1 mg/kg, po.) has a good oral bioavailability. The Cmax, Tmax and AUCpo,0-8h are 285.1 ng/mL, 1.67 h and 275.4 ng.h/mL, respectively for TC ASK 10.

TCASK 10

MAPK/ERK Signaling

MEK

MEK

——

——

1005775-56-3

432.349

C21H23Cl2N5O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (231.29 mM)

CC(C)(C)C1=CC=C(C=C1)C(=O)NC2=CN3C=C(C=CC3=N2)N4C=CN=C4.Cl.Cl

4-(1,1-Dimethylethyl)-N-[6-(1H-imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl]benzamide dihydrochloride

(-20℃)

With Ice Pack

≥ 2 years