OICR-9429 free base · Synonyms: OICR 9429 · OICR9429

OICR-9429, a chemical probe, is high affinity WD repeat domain 5 inhibitor.

For research use only. Not for human or veterinary use.

Target Apoptosis WDR5

Research area Cancer

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Data Sheet SDS COA

OICR-9429 structure

CAS No.: 1801787-56-3

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 650.00	BP-02219-250mg	In stock	Get quote
500 mg	USD 850.00	BP-02219-500mg	In stock	Get quote
1 g	USD 1,150.00	BP-02219-1g	In stock	Get quote
2 g	USD 1,900.00	BP-02219-2g	In stock	Get quote
5 g	USD 3,118.00	BP-02219-5g	In stock	Get quote

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Description

OICR-9429, a chemical probe, 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) . 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

Biological activity

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.

Identifiers

SMILES: CN1CCN(CC1)C1=CC=C(C=C1NC(=O)C1=CNC(=O)C=C1C(F)(F)F)C1=CC(CN2CCOCC2)=CC=C1
InChIKey: DJOVLOYCGXNVPI-UHFFFAOYSA-N

Specifications

MW (average): 555.5913
Formula: C₂₉H₃₂F₃N₅O₃
CAS No.: 1801787-56-3
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO : ≥ 32 mg/mL

Documents

References

[1].Jingtong Zhang, et al. Targeting WD repeat domain 5 enhances chemosensitivity and inhibits proliferation and programmed death-ligand 1 expression in bladder cancer. J Exp Clin Cancer Res. 2021 Jun 21;40(1):203.

Same target

Search Apoptosis

Same research area

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