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THZ1 Hydrochloride (1604810-83-4 free base)

Catalog No. T23458 CAS T23458

Synonyms: THZ1 Hydrochloride

THZ1 is a covalent inhibitor of CDK7 (IC50: 3.2nM).

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THZ1 Hydrochloride (1604810-83-4 free base) Chemical Structure

THZ1 Hydrochloride (1604810-83-4 free base), CAS T23458

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5 mg	Inquiry	$ 78.00
10 mg	Inquiry	$ 143.00
25 mg	Inquiry	$ 282.00
1 mL * 10 mM (in DMSO)	Inquiry	$ 100.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	THZ1 is a covalent inhibitor of CDK7 (IC50: 3.2nM).
In vitro	THZ1 covalently modifies CDK7 by targeting C312 residue outside of the kinase domain, providing an unanticipated means of achieving covalent selectivity. THZ1 potently inhibits the proliferation of Jurkat and Loucy T-ALL cell lines (IC50: 50nM and 0.55nM, respectively). In the kinase binding assay, THZ1 shows a good binding affinity (IC50: 3.2nM [1].
In vivo	As an inhibitor of CDK7, THZ1 inhibits the phosphorylation of the C-terminal domain of RNAP polymerase II, effecting the regulation of transcription. THZ1 also inhibits the activation of the CDK proteins. It is reported to disrupt the CDK7 signaling pathways both in Jurkat cells and Loucy cells. THZ1 shows a broad-based activity with IC50 values less than 200nM in a variety of cancer cell lines. Among these cell lines, T-ALL is exceptional sensitivity to THZ1 due to the transcription effect of RUNX1 caused by THZ1 [1].

Synonyms	THZ1 Hydrochloride
Molecular Weight	602.51
Formula	C31H29Cl2N7O2
CAS No.	T23458

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: ≥30.1255mg/mL

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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