382192 Sigma-AldrichHMTase 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.
More>> The HMTase Inhibitor IV, UNC0638 controls the biological activity of HMTase. This small molecule/inhibitor is primarily used for Cancer applications. Less<<Synonyms: 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
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Overview
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Pricing & Availability
Catalogue Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
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382192-2MG |
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Glass bottle | 2 mg |
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Description | |
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Overview | A 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 Number | 382192 |
Brand Family | Calbiochem® |
Synonyms | 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 |
References | |
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References | Vedadi, M., et al. 2011. Nat. Chem. Biol. 7, 566. Liu, F., et al. 2011. J. Med. Chem. 54, 6139. |
Product Information | |
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CAS number | 1255580-76-7 |
Form | Off-white powder |
Hill Formula | C₃₀H₄₇N₅O₂ |
Chemical formula | C₃₀H₄₇N₅O₂ |
Structure formula Image | |
Quality Level | MQ100 |
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Biological Information | |
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Purity | ≥98% by HPLC |
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Packaged under inert gas | Packaged under inert gas |
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Supplemental Information |
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Specifications |
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Global Trade Item Number | |
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Catalogue Number | GTIN |
382192-2MG | 04055977190229 |
Documentation
HMTase Inhibitor IV, UNC0638 - CAS 1255580-76-7 - Calbiochem SDS
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HMTase Inhibitor IV, UNC0638 - CAS 1255580-76-7 - Calbiochem Certificates of Analysis
Title | Lot Number |
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382192 |
References
Reference overview |
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Vedadi, M., et al. 2011. Nat. Chem. Biol. 7, 566. Liu, F., et al. 2011. J. Med. Chem. 54, 6139. |
Technical Info
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White Paper - The Message in the Marks: Deciphering Cancer Epigenetics |
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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.
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