GSK126

GSK126
Item number Size Datasheet Manual SDS Delivery time Quantity Price
Cay15415-1 1 mg -

6 - 10 business days*

84.00€
Cay15415-5 5 mg -

6 - 10 business days*

161.00€
Cay15415-10 10 mg -

6 - 10 business days*

241.00€
 
The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating... more
Product information "GSK126"
The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. GSK126 is a selective, S-adenosyl-methionine-competitive small molecule inhibitor of EZH2 methyltransferase activity (Ki = 0.57 nM, IC50 = 9.9 nM versus that of EZH1: Ki = 89 nM, IC50 = 680 nM). It is more than 1,000-fold selective for EZH2 over other histone methyltranferases, including both SET-domain-containing and non-SET-domain-containing methyltransferases. At concentrations of 7-252 nM, it has been shown to inhibit global H3K27 trimethylation levels and to reactivate silenced PRC2 target genes. Furthermore, GSK126 can inhibit the proliferation of EZH2 mutant DLBCL cell lines (IC50 = 28-61 nM) as well as the growth of EZH2 mutant DLBCL xenografts in mice receiving a daily dose of 50 mg/kg.Formal Name: N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide. CAS Number: 1346574-57-9. Molecular Formula: C31H38N6O2. Formula Weight: 526.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 15 mg/ml, Ethanol: 2 mg/ml. lambdamax: 235, 283 nm. SMILES: CC1=CN([C@@H](C)CC)C2=CC(C(C=C3)=CN=C3N4CCNCC4)=CC(C(NCC5=C(C)C=C(C)NC5=O)=O)=C21. InChi Code: InChI=1S/C31H38N6O2/c1-6-22(5)37-18-20(3)29-25(30(38)34-17-26-19(2)13-21(4)35-31(26)39)14-24(15-27(29)37)23-7-8-28(33-16-23)36-11-9-32-10-12-36/h7-8,13-16,18,22,32H,6,9-12,17H2,1-5H3,(H,34,38)(H,35,39)/t22-/m0/s1. InChi Key: FKSFKBQGSFSOSM-QFIPXVFZSA-N.
Keywords: N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide
Supplier: Cayman Chemical
Supplier-Nr: 15415

Properties

Application: Selective EZH2 methyltransferase inhibitor
MW: 526.7 D
Formula: C31H38N6O2
Purity: >98%
Format: Crystalline Solid

Database Information

CAS : 1346574-57-9| Matching products
KEGG ID : K11430 | Matching products

Handling & Safety

Storage: -20°C
Shipping: +20°C (International: -20°C)
Caution
Our products are for laboratory research use only: Not for administration to humans!
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