1621523-07-6

1621523-07-6 structure

Name: THZ1-R
Chemical Name: THZ1-R
CAS Number: 1621523-07-6
Molecular Formula: C₃₁H₃₀ClN₇O₂
Molecular Weight: 568.069
Catalog: Research Areas Cancer
Create Date: 2018-01-04 10:31:29
Modify Date: 2024-01-20 11:55:10
THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.

Name	THZ1-R
Synonyms	Benzamide, N-[3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-4-[[4-(dimethylamino)-1-oxobutyl]amino]- N-(3-{[5-Chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino}phenyl)-4-{[4-(dimethylamino)butanoyl]amino}benzamide

Description	THZ1-R is a non-cysteine reactive analog of THZ1 which displays diminished activity for CDK7 inhibition. THZ1-R binds to CDK7 with a Kd of 142 nM.
Related Catalog	Research Areas >> Cancer
Target	CDK7:146 nM (IC50)
In Vitro	THZ1-R shows lower affinity at CDK7 than THZ1, with IC50 of 146 nM[1].
Cell Assay	Cells are seeded in 384-well microplates at 15% confluency in medium with 5% FBS and penicillin/streptavidin. Cells are treated with THZ1 or DMSO for 72 hrs and cell viability is determined using resazurin.
References	[1]. Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20.