SGC0946 (CAS 1561178-17-3) | Cayman Chemical
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SGC0946

Item № 13967
CAS № 1561178-17-3
Purity ≥98%
product image
                (CAS 1561178-17-3)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     5 mg $123.00 0.00
     10 mg $204.00 0.00
     50 mg $763.00 0.00

Pricing updated 2019-02-20. Prices are subject to change without notice.

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.1 Proper DOT1L function is necessary for transcriptional activation of many genes, DNA damage repair, and cell cycle regulation.2 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.3 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.3 The negative control, SGC0649, for SGC0956 is also available exclusively through the SGC. You can submit a request to receive the negative control here.

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Technical Information
Formal Name
5-bromo-7-[5-deoxy-5-[[3-[[[[4-(1,1-dimethylethyl)phenyl]amino]carbonyl]amino]propyl](1-methylethyl)amino]-β-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number
1561178-17-3
Molecular Formula
C28H40BrN7O4
Formula Weight
618.6
Purity
≥98%
Formulation
A crystalline solid
λmax
242, 280 nm
SMILES
CC(C)(C)C1=CC=C(NC(NCCCN(C(C)C)C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C(N=CN=C4N)=C4C(Br)=C3)O2)=O)C=C1
InChI Code
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
InChI Key
IQCKJUKAQJINMK-HUBRGWSESA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
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Additional Information

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References & Product Citations
Product Description References

1. Bernt, K.M., and Armstrong, S.A. A role for DOT1L in MLL-rearranged leukemias Epigenomics 3(6), 667-670 (2011).

2. Nguyen, A.T., He, J., Taranova, O., et al. Essential role of DOT1L in maintaining normal adult hematopoiesis Cell Research 21(9), 1370-1373 (2011).

3. Yu, W., Chory, E.J., Wernimont, A.K., et al. Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors Nat.Commun. 3, 1-12 (2012).

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