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Chemical Structure : RK-582
Catalog No.: PC-49498Not For Human Use, Lab Use Only.
RK-582 (RK582) is a highly selective, potent and orally efficacious tankyrase inhibitor with IC50 of 39.1 and 36.2 nM for TNKS/TNKS2, respectively.
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RK-582 (RK582) is a highly selective, potent and orally efficacious tankyrase inhibitor with IC50 of 39.1 and 36.2 nM for TNKS1/TNKS2, respectively.
RK-582 shows high potency comparable with that of RK-287107 and G007-LK, displays no significant effect (>200-fold selectivity) against human PARP family member enzymes PARP1, PARP2 (poly ADPribosylation), and PARP10 (mono ADP-ribosylation).
RK-582 exhibits a high potency for the inhibition of TCF reporter activities at IC50 values of HEK293 (0.3 nM) and DLD-1 cells (3.1 nM).
RK-582 exhibited potent GI50 (35 nM), high sensitivity and sigmoid dependency achieving complete growth inhibition at 10 uM on CRC cells via MTT assays.
RK-582 induced AXIN2 accumulation and downregulation of β-catenin.
RK-582 (10 or 20 mg/kg, twice daily, oral or i.p.) exhibited a markedly robust tumor growth inhibition in a COLO-320DM mouse xenograft model.
| M.Wt | 510.61 | |
| Formula | C27H35FN6O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Fumiyuki Shirai, et al. J Med Chem. 2020 Apr 23;63(8):4183-4204.
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