THZ531|1702809-17-3--Shanghai xingMo Biotechnology

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Description

THZ531 is a covalent CDK12 and CDK13 covalent inhibitor. Cyclin-dependent kinases 12 and 13 (CDK12 and CDK13) play critical roles in the regulation of gene transcription. THZ531 irreversibly targets a cysteine located outside the kinase domain. THZ531 causes a loss of gene expression with concurrent loss of elongating and hyperphosphorylated RNA polymerase II. THZ531 substantially decreases the expression of DNA damage response genes and key super-enhancer-associated transcription factor genes. THZ531 dramatically induced apoptotic cell death. Small molecules capable of specifically targeting CDK12 and CDK13 may thus help identify cancer subtypes that are particularly dependent on their kinase activities.

Chemical Structure

Chemical Name

(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

SMILES Code

O=C(NC1=CC=C(C(N2C[C@H](NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)CCC2)=O)C=C1)/C=C/CN(C)C

Theoretical Analysis

XingMo Cat#:XM131
Product Name:THZ531
Synonyms:THZ531; THZ-531; THZ 531.
CAS#:1702809-17-3
Chemical Formula:C₃₀H₃₂ClN₇O₂
Exact Mass:557.2306
Molecular Weight:558.083

Technical Data

Appearance: solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years)

Solubility: Soluble in DMSO, not in water

Shelf Life:

>2 years if stored properly.

Drug Formulation:

This drug may be formulated in DMSO

Stock Solution Storage:

0 - 4℃ for short term (days to weeks), or -20℃ for long term (months).

WARNING: This product is for research use only, not for human or veterinary use

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