ChemicalBook > CAS DataBase List > THZ-531

THZ-531

Product Name: THZ-531
CAS No.: 1702809-17-3
Chemical Name: THZ-531
Synonyms: THZ531;CPD1594;THZ-531;CS-2763;THZ531 ，S6595;THZ 531 (THZ531);THZ531, 10 mM in DMSO;THZ531; THZ-531; THZ 531;THZ 531,inhibit,CDK,THZ-531,Cyclin dependent kinase,Inhibitor,THZ531;(R,E)-N-(4-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide
CBNumber: CB83153031
Molecular Formula: C30H32ClN7O2
Formula Weight: 558.07
MOL File: 1702809-17-3.mol

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THZ-531 Property

Density: 1.342±0.06 g/cm3(Predicted)
storage temp.: -20°C
solubility: ≥55.8 mg/mL in DMSO; insoluble in H2O; ≥4.9 mg/mL in EtOH
form: solid
pka: 13.12±0.70(Predicted)
color: White to light yellow

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML2619
Product name: THZ531
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $97.8
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML2619
Product name: THZ531
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $394
Updated: 2025/07/31

Cayman Chemical

Product number: 26386
Product name: THZ531
Packaging: 10mg
Price: $477
Updated: 2024/03/01

Cayman Chemical

Product number: 26386
Product name: THZ531
Packaging: 25mg
Price: $692
Updated: 2024/03/01

Cayman Chemical

Product number: 26386
Product name: THZ531
Packaging: 1mg
Price: $44
Updated: 2024/03/01

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THZ-531 Chemical Properties,Usage,Production

Uses

THZ 531 is a first-in-class CDK 12 and CDK13 covalent inhibitor. THZ531 causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II.

Definition

ChEBI: THZ531 is a member of the class of indoles that is 5-chloro-4-(1H-indol-3-yl)-N-[(3R)-piperidin-3-yl]pyrimidin-2-amine in which the piperidine NH group is substituted by a 4-{[(2E)-4-(dimethylamino)but-2-enoyl]amino}benzoyl group. It is a first-in-class CDK12 and CDK13 covalent kinase inhibitor with IC50 of 158 nM and 69 nM, respectively. It has a role as an apoptosis inducer, an antineoplastic agent and an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor. It is a member of indoles, an organochlorine compound, a N-acylpiperidine, an aminopyrimidine, an enamide, a secondary carboxamide and a secondary amino compound.

Biological Activity

thz531 is a first-in-class cdk12 and cdk13 covalent inhibitor with ic50 values of 158 nm and 69 nm, respectively [1].complexes containing cdk12 and cdk13 regulate transcriptional elongation as well as processes, including mrna splicing and 3’-end rna processing. loss of cdk12 and cdk13, or of their cofactor cyclin k, impedes both pol ii processivity and rna processing [1].thz531 is an irreversible cdk12 and cdk13 covalent inhibitor. thz531 potently inhibited cdk12 and cdk13 with ic50 values of 158 nm and 69 nm, whereas inhibition of cdk7 and cdk9 was more than 50-fold weaker, with ic50s of 8.5 μm and 10.5 μm, respectively. in jurkat cells, thz531 irreversibly reduced cell proliferation with ic50 of 50 nm. thz531 induced apoptosis in a dose- and time-dependent way. thz531 also reduced pol ii c-terminal domain (ctd) ser2 phosphorylation, a mark of active transcriptional elongation, resulted in the loss of key super-enhancer-associated transcription factor genes and dna damage response (ddr) genes expression [1].1.zhang t, kwiatkowski n, olson cm, et al. covalent targeting of remote cysteine residues to develop cdk12 and cdk13 inhibitors. nat chem biol. 2016 oct;12(10):876-84.

IC 50

CDK12: 158 nM (IC₅₀); CDK13: 69 nM (IC₅₀); CDK7: 8.5 μM (IC₅₀); CDK9: 10.5 μM (IC₅₀)

THZ-531 Preparation Products And Raw materials

Raw materials

Preparation Products

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1702809-17-3, THZ-531Related Search:

THZ531

THZ-531

CPD1594

(S,E)-N-(4-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide

(R,E)-N-(4-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide

CS-2763

THZ531; THZ-531; THZ 531

2-Butenamide, N-[4-[[(3R)-3-[[5-chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-1-piperidinyl]carbonyl]phenyl]-4-(dimethylamino)-, (2E)-

THZ 531,inhibit,CDK,THZ-531,Cyclin dependent kinase,Inhibitor,THZ531

THZ531, 10 mM in DMSO

THZ531 ，S6595

THZ 531 (THZ531)

1702809-17-3