SKU : MC547005
CAS Number : 297730-17-7
Molecular Formula : C25H27N5O5 | Molecular Weight : 477.51
Synonyms : VX-944
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | AVN-944 |
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CAS Number | 297730-17-7 |
MDL Number | MFCD22200574 |
Molecular Formula | C25H27N5O5 |
Molecular Weight | 477.51 |
Synonyms | VX-944 |
AVN-944(VX-944) is a selective, noncompetitive inhibitor of the enzyme directed against human IMPDH with Ki of 6-10 nM for IMPDH1/IMPDH2. IC50 value: 6-10 nM (Ki) [1] Target: IMPDH in vitro: AVN-944 strikingly inhibit RNA synthesis within 2 h of exposure. Depletion of guanine nucleotides by MPA and AVN-944 also causes an early and near-complete reduction in levels of the 45S precursor rRNA synthesis and the concomitant translocation of nucleolar proteins including nucleolin, nucleophosmin, and nucleostemin from the nucleolus to the nucleoplasm [2]. AVN944 induced caspase-dependentand caspase-independent cell death in LNCaP, CWR22Rv1, and DU145 cells. AVN944 induced expression of p53-target proteins Bok, Bax and Noxa in androgen-responsive cell lines and suppressed expression of survivin in prostate cancer cells regardless of their androgen sensitivity. AVN944 also induced differentiation of androgen-independent prostate cancer cells as indicated by morphological changes and increased expression of genes coding for prostasomal proteins, keratins and other proteins, including tumor suppressor genes MIG-6 and NDRG1. AVN944-differentiated androgen-independent DU145 and PC-3 cells are sensitized to TRAIL-induced apoptosis as demonstrated by induction of caspases and PARP cleavage [3].
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