| Bioactivity | OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) [1]. | ||||||||||||
| Invitro | OICR-9429 (0-10 μM, 48 h) shows high sensitivity for T24, UM-UC-3 with IC50 values of 67.74 μM and 70.41 μM, respectively[1].OICR-9429 (0-10 μM, 48 h) shows low sensitivity for TCCSUP with IC50 values of 121.42 μM[1].OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 48 h) reduces BCa cell viability by decreasing WDR5-mediated H3K4me3[1].OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 48 h) inhibits the proliferation of BCa cells by regulating the G1/S phase transition[1].OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 24 h) enhances apoptosis of BCa cells in a time-dependent and dose-dependent manner and promotes cisplatin chemosensitivity in BCa cells[1].OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 24 h, 48 h) suppresses the metastatic behaviour of bladder cancer cells[1].OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 48 h) suppresses PD-L1 expression induced by IFN-γ in BCa cells[1]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| Name | OICR-9429 | ||||||||||||
| CAS | 1801787-56-3 | ||||||||||||
| Formula | C29H32F3N5O3 | ||||||||||||
| Molar Mass | 555.59 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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OICR-9429
CAS: 1801787-56-3 F: C29H32F3N5O3 W: 555.59
OICR-9429 is high affinity WD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein v
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