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382192 HMTase Inhibitor IV, UNC0638 - CAS 1255580-76-7 - Calbiochem

The HMTase Inhibitor IV, UNC0638 controls the biological activity of HMTase. This small molecule/inhibitor is primarily used for Cancer applications.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: 2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine, DNA Methyltransferase Inhibitor III, DNA MTase Inhibitor III, EHMT1/GLP Inhibitor II, EHMT2/G9a Inhibitor IV

382192
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Aperçu

Replacement Information

Products

RéférenceConditionnement Qté
382192-2MG Flacon en verre 2 mg
Description
OverviewA cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC50 = ≤ 15 and 19 nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC50 = 4.66 µM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC50 > 10 µM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC50 = 81 nM; EC50 = 11.2 µM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294, (Cat. No. 382190). Also, affects the activities of adrenergic α1A, adrenergic α1B and muscarinic M2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by ≤ 30% at 1 µM.




This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the UNC0638 probe summary on the SGC website.
Catalogue Number382192
Brand Family Calbiochem®
Synonyms2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine, DNA Methyltransferase Inhibitor III, DNA MTase Inhibitor III, EHMT1/GLP Inhibitor II, EHMT2/G9a Inhibitor IV
References
ReferencesVedadi, M., et al. 2011. Nat. Chem. Biol. 7, 566.
Liu, F., et al. 2011. J. Med. Chem. 54, 6139.
Product Information
CAS number1255580-76-7
FormOff-white powder
Hill FormulaC₃₀H₄₇N₅O₂
Chemical formulaC₃₀H₄₇N₅O₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% 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 at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Regulatory Review
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
Référence GTIN
382192-2MG 04055977190229

Documentation

HMTase Inhibitor IV, UNC0638 - CAS 1255580-76-7 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

HMTase Inhibitor IV, UNC0638 - CAS 1255580-76-7 - Calbiochem Certificats d'analyse

TitreNuméro de lot
382192

Références bibliographiques

Aperçu de la référence bibliographique
Vedadi, M., et al. 2011. Nat. Chem. Biol. 7, 566.
Liu, F., et al. 2011. J. Med. Chem. 54, 6139.

Informations techniques

Titre
White Paper - The Message in the Marks: Deciphering Cancer Epigenetics
Fiche technique

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.

Revision21-June-2023 JSW
Synonyms2-Cyclohexyl-N-(1-isopropylpiperidin-4-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-amine, DNA Methyltransferase Inhibitor III, DNA MTase Inhibitor III, EHMT1/GLP Inhibitor II, EHMT2/G9a Inhibitor IV
DescriptionA cell-permeable quinazolinamine compound that acts as a potent and reversible inhibitor of G9a and GLP HMTases (histone methyltransferases) (IC50 = ≤ 15 and 19 nM for G9a and GLP, respectively) and displays ~15-fold greater selectivity over DNMT1 and minimally blocks the activities of JMJD2E (IC50 = 4.66 µM) and SETD7, SETD8, PRMT3 and SUV39H2 (IC50 > 10 µM). Shown to lower H3K9Me2 levels in MDA-MB231 cells (IC50 = 81 nM; EC50 = 11.2 µM for cell toxicity) and 6-fold more potent than the HMTase Inhibitor, BIX-01294, (Cat. No. 382190). Also, affects the activities of adrenergic α1A, adrenergic α1B and muscarinic M2 by 90%, 69% and 64% and a panel of 26-receptors and ion-channels by ≤ 30% at 1 µM.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1255580-76-7
Chemical formulaC₃₀H₄₇N₅O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (10 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 Regulatory Review
ReferencesVedadi, M., et al. 2011. Nat. Chem. Biol. 7, 566.
Liu, F., et al. 2011. J. Med. Chem. 54, 6139.