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Cayman GSK3685032, 1 mg
Product Description
GSK3685032 is an inhibitor of DNA methyltransferase 1 (DMNT1; IC50 = 0.23 µM).1 It is selective for DMNT1 over DMNT3A/3L and DMNT3B/3L and a panel of 34 methyltransferases and 369 kinases (IC50s = >10 µM for all). GSK3685032 inhibits the proliferation of 51 hematological cancer cell lines (median IC50 = 0.64 µM). It decreases overall DNA methylation and gene expression in MV4-11, THP-1, and NOMO-1 acute myeloid leukemia (AML) cells in a time- and concentration-dependent manner. GSK3685032 increases the expression of the genes encoding chemokine (C-X-C) motif ligand 11 (CXCL11), IFN-α-inducible protein 27 (IFI27), and melanoma-associated antigen 4 (MAGEA4). In vivo, GSK3685032 (45, 30, or 15 mg/kg twice per day) reduces tumor volume and increases survival but does decrease blood numbers of neutrophils and red blood cells in SKM-1 and MV4-11 leukemia mouse xenograft models.
WARNING This product is not for human or veterinary use.
Technical Information
| Formal Name | α-[[6-(4-amino- |
| CAS Number | 2170137-61-6 |
| Molecular Formula | C22H24N6OS |
| Formula Weight | 420.5 |
| Purity | ≥98% |
| Formulation | A solid |
| Solubility(Learn about Variance in Solubility) | DMSO: Soluble: ≥10 mg/mL |
| SMILES | N#CC1=C(N2CCC(CC2)N)N=C(C(C#N)=C1CC)SC(C(N)=O)C3=CC=CC=C3 |
| InChi Code | InChI=1S/C22H24N6OS/c1-2-16-17(12-23)21(28-10-8-15(25)9-11-28)27-22(18(16)13-24)30-19(20(26)29)14-6-4-3-5-7-14/h3-7,15,19H,2,8-11,25H2,1H3,(H2,26,29) |
| InChi Key | KNKHRZYILDZLRE-UHFFFAOYSA-N |
Shipping & Storage Information
| Storage | -20°C |
| Shipping | Room temperature in continental US; may vary elsewhere |
| Stability | ≥ 4 years |
| SKU | CAYM-44360-1 |
|---|---|
| Supplier Part Number | 44360-1 |
| UM | EA |
| UNSPSC | 41116134 |
| Manufacturer | Cayman |
| Temperature | -20 |
| Refrigerated-Frozen | Y |
| CountryOfOrigin | China |
| ProductLine | CAYM |
| Qty | 1 |
| MinOrderQty | 1 |
| Weight | 7.000000 |
| Lead Time | 5 |
| Hazardous | N |
| CAS Number | 2170137-61-6 |
| Energy Star | No |
| Green | No |
| Controlled | N |