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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Epigenetics >Histone Methyltransferase Inhibitors >SGC0946

SGC0946

SGC0946 Structure
  • ₹11009.03 - ₹44339.2
  • Product name: SGC0946
  • CAS: 1561178-17-3
  • MF: C28H40BrN7O4
  • MW: 618.57
  • EINECS:808-588-8
  • MDL Number:MFCD26523136
  • Synonyms:5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine;1-(3-((((2R,3S,4R,5R)-5-(4-Amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahy;SGC0946;1-(3-((((2R,3S,4R,5R)-5-(4-Amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)urea;5-Bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-beta-D-7H-Pyrrolo[2,3-;1-[3-[[[(2R,3S,4R,5R)-5-(4-Amino-5--bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydro-xytetrahydrofuran-2-yl]methyl](isopropyl)amino]pro-pyl]-3-[4-(2,2-dimethylethyl)phenyl]urea;7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 5-bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-;SGC0946 USP/EP/BP
Price2 Properties Safety Information Description
2 prices
Selected condition：

Brand

  • Sigma-Aldrich(India)

Package

  • 5MG
  • 25MG
  • ManufacturerSigma-Aldrich(India)
  • Product numberSML1107
  • Product descriptionSGC0946 ≥98% (HPLC)
  • Packaging25MG
  • Price₹44339.2
  • Updated2022-06-14
  • Buy
  • ManufacturerSigma-Aldrich(India)
  • Product numberSML1107
  • Product descriptionSGC0946 ≥98% (HPLC)
  • Packaging5MG
  • Price₹11009.03
  • Updated2022-06-14
  • Buy
Manufacturer Product number Product description Packaging Price Updated Buy
Sigma-Aldrich(India) SML1107 SGC0946 ≥98% (HPLC) 25MG ₹44339.2 2022-06-14 Buy
Sigma-Aldrich(India) SML1107 SGC0946 ≥98% (HPLC) 5MG ₹11009.03 2022-06-14 Buy

Properties

Melting point :125-126o C
Boiling point :771.5±60.0 °C(Predicted)
Density :1.48±0.1 g/cm3(Predicted)
storage temp. :-20°C
solubility :DMSO: soluble20mg/mL, clear
pka :12.39±0.70(Predicted)
form :powder
color :white to beige

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H301 Toxic if swalloed Acute toxicity,oral Category 3 Danger GHS hazard pictograms P264, P270, P301+P310, P321, P330,P405, P501
Precautionary statements:
P301+P310 IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

Description

DOT1L is a protein methyltransferase (PMT). It is the only enzyme known to methylate histone 3 at lysine 79 (H3K79), where it catalyzes mono-, di-, and trimethylation. Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation. SGC0946 is a potent inhibitor of DOT1L (IC50 = 0.3 nM) developed by the Structural Genomics Consortium (SGC). It is over 100-fold selective over other PMTs. It is active in cells, reducing H3K79 dimethylation in A431 and MCF10A cells (IC50s = 2.6 and 8.8 nM, respectively). SGC0946 is a brominated analog of EPZ004777, an S-adenosylmethionine-competitive inhibitor of DOT1L. Both SGC0946 and EPZ004777 selectively kill mixed lineage leukemia (MLL) cells, in which DOT1L is aberrantly localized via interaction with an oncogenic MLL fusion protein.

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