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OICR-9429

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OICR-9429

OICR-9429

Catalog No.: PC0071

Size: 5 mg,10 mg, 25 mg,50 mg, 100 mg, 200 mg, 500 mg

Description

OICR-9429 is a high-affinity WD repeat domain 5 inhibitor that competitively blocks the interaction of WDR5 with MLL proteins by binding to the central peptide-binding pocket of WDR5. OICR-9429 can inhibit histone H3K4 trimethylation and can be used to study a variety of cancers, including non-MLL rearranged leukemia, colon cancer, pancreatic cancer, prostate cancer and bladder cancer.

Molecular Weight 555.59
Formula C29H32F3N5O3
CAS No. 1801787-56-3
Appearance Solid
Color White to off-white
SMILES O=C(C1=CNC(C=C1C(F)(F)F)=O)NC2=CC(C3=CC(CN4CCOCC4)=CC=C3)=CC=C2N5CCN(C)CC5
Shipping Room temperature in continental US; may vary elsewhere.
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
In Vitro 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.
OICR-9429 (0-10 μM, 48 h) shows low sensitivity for TCCSUP with IC50 values of 121.42 μM.
OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 48 h) reduces BCa cell viability by decreasing WDR5-mediated H3K4me3.
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.
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.
OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 24 h, 48 h) suppresses the metastatic behaviour of bladder cancer cells.
OICR-9429 (70 μM, 120 μM, 140 μM and 240 μM; 48 h) suppresses PD-L1 expression induced by IFN-γ in BCa cells.
In Vivo OICR-9429 (30 mg/kg or 60 mg/kg, i.p) targeting WDR5 not only suppressed tumour proliferation and enhance the efficacy of cisplatin for BCa cells in vivo but also reduced the toxicity and side effects for normal tissues.
All of our services are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.

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