In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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 .
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 .
 Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288. doi: 10.1038/ncomms2304.
|Physical Appearance||A solid|
|Storage||Store at -20°C|
|Solubility||≥30.95 mg/mL in DMSO, ≥97.6 mg/mL in EtOH with ultrasonic,insoluble in H2O|
|Canonical SMILES||CC(C)(C)C1=CC=C(NC(NCCCN(C[[email protected]@H]2[[email protected]@H](O)[[email protected]@H](O)[[email protected]](N3C4=NC=NC(N)=C4C(Br)=C3)O2)C(C)C)=O)C=C1|
|Shipping Condition||Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.|
|General tips||For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.|
|Cell experiment :|
Molm13 MLL and A431 cell lines
The solubility of this compound in DMSO is >31 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
SGC0946 showed time- and dose-dependent reductions in the H3K79me2 mark in the Molm13 MLL cell line that has the MLL/AF9 translocation. Quantitative assessment of H3K79me2 levels as measured by automated epifluorescence microscopy in MCF10A cells showed a substantially improved DOT1L inhibitory potency of SGC0946 (IC50 8.8±1.6 nM) compared with EPZ004777 (IC50 84±20nM). A similar observation was made in A431 cells, with IC50s of 2.65 nM and 264nM for SGC0946 and EPZ004777, respectively.
 Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288.
|Description||SGC 0946 is a potent inhibitor of DOT1L methyltransferase with IC50 value of 0.3 nM.|
Quality Control & MSDS
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