SGC 0946

DOT1L inhibitor,highly potent and selective CAS# 1561178-17-3

SGC 0946

Catalog No. BCC2216----Order now to get a substantial discount!

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SGC 0946: 5mg $46 In Stock
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Quality Control of SGC 0946

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Chemical structure

SGC 0946

3D structure

Chemical Properties of SGC 0946

Cas No. 1561178-17-3 SDF Download SDF
PubChem ID 56962337 Appearance Powder
Formula C28H40BrN7O4 M.Wt 618.57
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 33 mg/mL (53.35 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-[3-[[(2R,3S,4R,5R)-5-(4-amino-5-bromopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea
SMILES CC(C)N(CCCNC(=O)NC1=CC=C(C=C1)C(C)(C)C)CC2C(C(C(O2)N3C=C(C4=C3N=CN=C4N)Br)O)O
Standard InChIKey IQCKJUKAQJINMK-HUBRGWSESA-N
Standard InChI InChI=1S/C28H40BrN7O4/c1-16(2)35(12-6-11-31-27(39)34-18-9-7-17(8-10-18)28(3,4)5)14-20-22(37)23(38)26(40-20)36-13-19(29)21-24(30)32-15-33-25(21)36/h7-10,13,15-16,20,22-23,26,37-38H,6,11-12,14H2,1-5H3,(H2,30,32,33)(H2,31,34,39)/t20-,22-,23-,26-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SGC 0946

DescriptionSGC 0946 is a potent inhibitor of DOT1L methyltransferase with IC50 value of 0.3 nM.
TargetsDOT1L    
IC500.3 nM     

SGC 0946 Dilution Calculator

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SGC 0946 Molarity Calculator

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Preparing Stock Solutions of SGC 0946

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.6166 mL 8.0832 mL 16.1663 mL 32.3326 mL 40.4158 mL
5 mM 0.3233 mL 1.6166 mL 3.2333 mL 6.4665 mL 8.0832 mL
10 mM 0.1617 mL 0.8083 mL 1.6166 mL 3.2333 mL 4.0416 mL
50 mM 0.0323 mL 0.1617 mL 0.3233 mL 0.6467 mL 0.8083 mL
100 mM 0.0162 mL 0.0808 mL 0.1617 mL 0.3233 mL 0.4042 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

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Universidade da Beira Interior

The Institute of Cancer Research

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University of Auckland
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The University of Michigan
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DRURY University
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Jilin University
Jilin University
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Wuhan University
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Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
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Deemed University
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Auckland University
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The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on SGC 0946

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].

Reference

References:
[1] 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.

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Description

SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.

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