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526526 PIM3 Kinase Inhibitor VII, M-110 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

同义词: Nʹ-(1-(4-Chloro-2-hydroxyphenyl)propylidene)-2-((3-morpholinopropyl)amino)isonicotinohydrazide

526526
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概述

Replacement Information

重要规格表

Empirical Formula
C₂₂H₂₈ClN₅O₃

Products

产品目录编号包装 数量 / 包装
526526-10MGCN 玻璃瓶 10 mg
Description
OverviewA cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (Ki = 0.3 µM), and highly isoform-selective PIM inhibitor (IC50 = 2.5, 2.5, and 0.047 µM against PIM1, PIM2, and PIM3, respectively; [ATP] = 10 µM), while affecting CK2α2 only at much higher concentrations (IC50 = 5 µM, [ATP] = 10 µM) and exhibiting little or no activity against a panel of 258 other kinases (<40% inhibition at 5 µM). Shown to inhibit PIM3-dependent STAT3 Tyr705 phosphorylation in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells (by 73% and 83%, respectively; 10 µM for 18 h), while displaying little effect toward STAT3 Tyr694 phosphoylation in 22RV1 cultures.
Catalogue Number526526
Brand Family Calbiochem®
SynonymsNʹ-(1-(4-Chloro-2-hydroxyphenyl)propylidene)-2-((3-morpholinopropyl)amino)isonicotinohydrazide
References
ReferencesChang, M., et al. 2010. Mol. Cancer Ther. 9, 2478.
Product Information
FormPale yellow solid
Hill FormulaC₂₂H₂₈ClN₅O₃
Chemical formulaC₂₂H₂₈ClN₅O₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 6 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
526526-10MGCN 04055977270792

Documentation

PIM3 Kinase Inhibitor VII, M-110 - Calbiochem MSDS

职位

物料安全数据表 (MSDS) 

PIM3 Kinase Inhibitor VII, M-110 - Calbiochem 分析证书

标题批号
526526

参考

参考信息概述
Chang, M., et al. 2010. Mol. Cancer Ther. 9, 2478.
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.

Revision22-February-2013 JSW
SynonymsNʹ-(1-(4-Chloro-2-hydroxyphenyl)propylidene)-2-((3-morpholinopropyl)amino)isonicotinohydrazide
DescriptionA cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (Ki = 0.3 µM), and highly isoform-selective PIM inhibitor (IC50 = 2.5, 2.5, and 0.047 µM against PIM1, PIM2, and PIM3, respectively, with PIMtide as substrate, [ATP] = 10 µM), while affecting CK2α2 only at much higher concentrations (IC50 = 5 µM, [ATP] = 10 µM) and exhibiting little or no activity against a panel of 258 other kinases (<40% inhibition; [M-110] = 5 µM). M-100 treatment (10 µM for 18 hr) is shown to inhibit both basal (by 73% and 83% of DMSO control in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells, respectively) and IL-6-stimulated (by 69% of DMSO control in DU-145 cells) STAT3 phosphorylation on Tyr705, while displaying little effect toward Tyr694 phosphoylation (in 22RV1 cultures). Isoform-specific knockdowns in DU-145 cells likewise identify PIM-3, but not PIM-1 or -2, as the kinase responsible for cellular STAT3 Tyr705 phosphorylation.
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₂H₂₈ClN₅O₃
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesChang, M., et al. 2010. Mol. Cancer Ther. 9, 2478.