1005775-56-3

1005775-56-3 structure

Name: TC ASK 10
Chemical Name: N-[6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl]-4-(2-methyl-2-propanyl)benzamide dihydrochloride
CAS Number: 1005775-56-3
Molecular Formula: C₂₁H₂₃Cl₂N₅O
Molecular Weight: 432.346
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2018-07-14 20:37:55
Modify Date: 2024-01-10 14:10:02
TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM)[1].

Name	N-[6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl]-4-(2-methyl-2-propanyl)benzamide dihydrochloride
Synonyms	N-[6-(1H-Imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl]-4-(2-methyl-2-propanyl)benzamide dihydrochloride Benzamide, 4-(1,1-dimethylethyl)-N-[6-(1H-imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl]-, hydrochloride (1:2) TCASK10

Description	TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM)[1].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> MAPK/ERK Pathway >> MAP3K
Target	ASK1:14 nM (IC50)
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[1]. Western Blot Analysis[1] 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.
In Vivo	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[1].
References	[1]. Terao Y, et al. Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7326-9.

Hazard Codes	Xi