OICR-9429

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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.

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