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- CAS Registry #:912999-49-6
- Formula:C24H31N3O3
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| Description: |
AT13387, discovered by a high-throughput x-ray craystallography fragment-based platform, is a non-geldanamycin inhibitor of heat shock proterin 90 (HPS90), a molecule chaperone regulating signal transduction pathways for cell growth and survival. It has |
| Synonym(s): |
(2,4-dihydroxy-5-propan-2-ylphenyl)-[5-[(4-methylpiperazin-1-yl)methyl]-1,3-dihydroisoindol-2-yl]methanone |
| Biological Activity: |
AT13387 is a potent inhibitor of the proliferat ion and survival of many different cell lines (such as MES-SA cell line) from a variety of different tumor types. Across a panel of 30 tumor cell lines, AT13387 potently inhibits cell proliferation with GI50 values in the range 13-260 nM. AT13387 inhibits proliferation of the non-tumorigenic human prostate epithelial cell line PNT2 with a GI50 value of 480 nM. The inhibition of a number of isolated kinases by AT13387 is also investigated including CDK 1, CDK 2, CDK4, FGFR3, PKB-b, JAK2, VEGFR2, PDGFRβ and Aurora B. None of the tested kinases are significantly inhibited at concentrations below 30 µM. |
| Solubility: |
Soluble in DMSO |
| Storage / Stability: |
Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day. |
| Reference(s): |
Min H. et al. Pediatr Blood Cancer. 2012; 59(1): 185-188. |
| Scientific Category: |
Inhibitors / Activators |
| Product Type: |
Protease |
