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532372 Sigma-AldrichCdk7 Inhibitor VIII, THZ1 - Calbiochem

Cdk7 Inhibitor; THZ1

Cdk7 Inhibitor VIII, THZ1 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
小册子
技术信息
Data Sheet

同义词: (E)-N-(3-(5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide, 4HCl, THZ1, HCl

Primary Target: Cdk7

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概述

Replacement Information

重要规格表

Empirical Formula
C₃₁H₂₈ClN₇O₂ •4HCl

价格及供货情况

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Description
Overview	A cell-permeable, non-toxic, phenylaminopyrimidinyl-acrylamide compound that acts as a highly potent, selective, ATP-site directed, and irreversible inhibitor of Cdk7 (IC₅₀ = 3.2 nM). Acts by allosterically and covalently modifying Cys312 located outside the canonical kinase domain. Shown to block the phosphorylation of Ser5 and Ser7 in RNAPII CTD, the intracellular substrate of Cdk7 (< 250 nM, 4 h in Jurkat cells). Does not affect the activity of C312S mutated Cdk7. Exhibits comparatively week activity towards Cdk12 (IC₅₀ = 250 nM), Cdk1, and Cdk2. Suppresses the proliferation and cell viability of T-ALL and CLL cell lines and induces apoptosis with significant reduction in the levels of MCL-1 and XIAP. Also induces a significant reduction in the transcript and protein levels of RUNX1, TAL, and GATA3 (~ 50 nM). Suppresses the growth of KOPTK1 cells xenografts in murine model (10 mg/kg, b.i.d). Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number	532372
Brand Family	Calbiochem®
Synonyms	(E)-N-(3-(5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide, 4HCl, THZ1, HCl

References
References	Kwiatkowski, N., et al. 2014. Nature 511, 616. Chipumuro, E., et al. Cell 159, 1126.

Product Information
Form	Yellow solid
Hill Formula	C₃₁H₂₈ClN₇O₂ •4HCl
Chemical formula	C₃₁H₂₈ClN₇O₂ •4HCl
Hygroscopic	Hygroscopic
Reversible	N
Quality Level	MQ100

Applications

Biological Information
Primary Target	Cdk7
Secondary target	Cdk12
Purity	≥96% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	-20°C
Protect from Light	Protect from light
Hygroscopic	Hygroscopic
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
5.32372.0001	04055977260083

Documentation

Cdk7 Inhibitor VIII, THZ1 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

Cdk7 Inhibitor VIII, THZ1 - Calbiochem 分析证书

标题	批号
532372	输入批号

参考

参考信息概述
Kwiatkowski, N., et al. 2014. Nature 511, 616. Chipumuro, E., et al. Cell 159, 1126.

小册子

标题
NPI Flyer- Epigenetics and Nuclear Function Feature
New Products - Antibodies, Small Molecule, Inhibitors

技术信息

标题
White Paper: Further considerations of antibody validation and usage.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	19-December-2014 JSW
Synonyms	(E)-N-(3-(5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-ylamino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide, 4HCl, THZ1, HCl
Description	A cell-permeable, acrylamide-bearing phenylaminopyrimidine that, despite its ATP-competitive affinities toward multiple kinases (IC₅₀ ≤1 µM against ATP probe binding to 22 kinases in a KiNativ panel screening), only effectively acts as an irreversible inhibitor against Cdk7 & Cdk12, and likely also Ckd13 & Cdk19, due to conformational positioning of a C-terminal Cys outside the kinase domain (C312 of human & murine Cdk7; C1539, C1517, C349 of human Cdk12, Cdk13, Cdk19, respectively) adjacent to the drug′s acrylamide moiety in the ATP cleft, allowing covalent bond formation. Due to the irreversible mode of action, 3 to 5 h incubation is shown to most effectively inhibit intracellular Ckd7 & Cdk12 (Effective conc. 100 to 500 nM in 293A, HeLa S3, Jurkat, and Loucy cultures). Likewise, drug washout following THZ1 incubation is demonstrated not to affect its potency against cellular Cdk7 substrates phosphorylatio(RNAPII S2/5/7, Cdk1 T161, Cdk2 T160, Cdk9 T186) or cell proliferation. A strong enrichment of factors involved in Cdk7 substrate RNAPII/RPB1-driven transcriptional regulation is found among THZ1-sensitive cell lines with T cell acute lymphoblastic leukemia (T-ALL; IC₅₀ in nM = 0.49/KOPTK1, 0.54/Loucy, 0.61/DND-41, 50 nM/Jurkat by cellular ATP measurement post 72 incubation) that depend on RUNX1 transcription for proliferation being particularly sensitive to THZ1-induced apoptotic death. Intravenous injection is efficacious in suppression KOPTK1 proliferation in mice (by 91%;10 mg/3.3 mL/Kg/12 h, BID, for 29 d one week following cancer cells injection) in vivo without affecting animal body weight.
Form	Yellow solid
Intert gas (Yes/No)	Packaged under inert gas
Chemical formula	C₃₁H₂₈ClN₇O₂ •4HCl
Purity	≥96% by HPLC
Solubility	DMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
Storage	Protect from light -20°C Hygroscopic
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	Kwiatkowski, N., et al. 2014. Nature 511, 616. Chipumuro, E., et al. Cell 159, 1126.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Cyclin-Dependent Kinase (Cdk) Inhibitors

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