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HomeProduct name listSGC0946

SGC0946

Synonym(s):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-d]pyrimidin-4-amine

  • CAS NO.：1561178-17-3
  • Empirical Formula: C28H40BrN7O4
  • Molecular Weight: 618.57
  • MDL number: MFCD26523136
  • EINECS: 808-588-8
  • Update Date: 2026-01-13 11:18:12
SGC0946 Structural

What is SGC0946?

The Uses of SGC0946

SGC0946 is a potent DOT1L methyltransferase inhbiitor used in the treatment of leukemia seen effectively in vitro.

What are the applications of Application

SGC-0946 is an inhibitor of DOT1L1.

Biological Activity

sgc 0946 is a potent small-molecule inhibitor of protein methyltransferase (pmt) dot1l, a unique protein lysine methyltransferase (pkmt) catalyzing the methylation of histone h3 on lysine 79 (h3k79), with the half maximal inhibition concentration ic50 value of 0.3 nm [1].as a brominated analogue of epz004777, sgc 0946 exhibits substantially increased cellular inhibitory potency than its predecessor, where sgc 0946 reduces the methylation of h3k79 in both mcf10a (ic50: 8.8 nm) and a431 (ic50: 2.65 nm) cells compared with epz004777 (ic50: 84 nm and 264 nm respectively). this greatly increased cellular inhibitory potency of sgc 0946 can be attributed to lower off-rate and to improved cell permeability [1].

Biochem/physiol Actions

SGC0946 is a potent and selective inhibitor of Histone H3-lysine79 (H3K79) methyltransferase DOT1L with an IC50 of 0.3 nM in a radioactive enzyme assay, and over 100-fold selectivity for DOT1L over other histone methyltransferases. In cell studies, SGC0946 reduces H3K79 dimethylation with an IC50 of 2.6 nM in A431 cells and 8.8 nM in MCF10A cells. SGC0946 was found to selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia. For full characterization details, please visit the SGC0946 probe summary on the Structural Genomics Consortium (SGC) website.SGC0649 is the negative control for the active probe, SGC0946. To request a sample of the negative control from the SGC, click here.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

Storage

Store at -20°C

Properties of SGC0946

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 for SGC0946

Signal word Danger
Pictogram(s)
ghs
Skull and Crossbones
Acute Toxicity
GHS06
GHS Hazard Statements H301:Acute toxicity,oral
Precautionary Statement Codes P301+P310:IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

Computed Descriptors for SGC0946

New Products

2-(3-Methyl-1,2,4-oxadiazol-5-yl)acetic acid (as potassium salt) 2-fluoro-4-iodoaniline 4-Iodo-3,5-dimethylbenzonitrile Atorvastatin amide impurity/Atorvastatin EP Impurity F(Calcium Salt) Lantanoprost rc B Clidinium Bromide Impurity Noradrenaline EP Impurity D/Noradrenaline Methyl Ether Cetirizine EP Impurity A/Cetirizine CBHP Impurity N-Nitroso hydroxy Cetrizine EP Impurity-A (4-Fluoro-2-methoxy-5-nitro- phenyl)-[4- (1-methyl-1H- indol-3- yl)-pyrimidin-2-yl]- amine 6-bromo-4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole tert-butyl 4-(6-((7-cyclo pentyl -6-(dimethyl carbamoyl) -7H-pyrrolo [2,3-d]pyrimidin-2-yl) amino)pyridin-3-yl) piperazine-1-carboxylate 2-Fluoro-4-nitrotoluene 1-(2-amino-5-hydroxy phenyl)propan-1-one (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3- amine 3-(Dimethylamino)benzoic acid 2-Amino-5-chloropyridine 4-(Methylamino)-3-nitrobenzoic Acid 5-Chloro-2-Nitroaniline 3,5-dibenzyloxy Acetophenone 2,4-Diamino-6-hydroxypyrimidine 2-Chloro Benzylcyanide 3-chlorobenzyl cyanide 3,4 Diethoxy Benzylcyanide

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