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OICR-9429

Catalog No. T6916 CAS 1801787-56-3

Synonyms: OICR 9429

OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.

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OICR-9429, CAS 1801787-56-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 113.00
25 mg	In stock	$ 197.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 528.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 99.93%

Purity: 99.74%

Purity: 99.13%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.
Targets&IC50	WDR5:93 nM(Kd)
In vitro	OICR-9429 binds WDR5 with high affinity (Kd=93±28 nM) and competitively disrupts its interaction with a high-affinity Wdr5-interacting (WIN) peptide of MLL (Kdisp=64±4 nM)[1].
Kinase Assay	AR binding affinity: AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1?nM [3H]mibolerone are incubated with increasing concentrations of test compounds overnight. After the incubation, bound and free steroids are separated by treatment with 100?μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100?μL of supernatant fraction in 200?μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4?°C.
Cell Research	20,000 viable, actively proliferating primary human AML cells per well were seeded in 96-well plates in triplicates and treated with 0.05% DMSO or OICR-9429. Cell viability was measured using the Cell Titer-Glo luminescent cell viability assay on a VICTOR X4 luminometer after 72 h.(Only for Reference)

Synonyms	OICR 9429
Molecular Weight	555.59
Formula	C29H32F3N5O3
CAS No.	1801787-56-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 38 mg/mL (68.39 mM)

Ethanol: 12 mg/mL(21.6 mM)

References and Literature

1. Grebien F, et al. Nat Chem Biol. 2015, 11(8):571-8.

Citations

1. Yuan J, Peng H, Mo B, et al. Inhibition of Wdr5 Attenuates Ang-II-Induced Fibroblast-to-Myofibroblast Transition in Cardiac Fibrosis by Regulating Mdm2/P53/P21 Pathway. Biomolecules. 2022, 12(11): 1574.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Prostate Cancer Compound Library Anti-Liver Cancer Compound Library Anti-Lung Cancer Compound Library Reprogramming Compound Library Histone Modification Compound Library Anti-Pancreatic Cancer Compound Library Epigenetics Compound Library Methylation Compound Library Anti-COVID-19 Compound Library

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Piribedil Valemetostat SW2_110A WDR5-0102 OTS186935 FA BCI-121 WDR5-47 MS8511 HCl

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Keywords

OICR-9429 1801787-56-3 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Histone Methyltransferase JAK pancreatic MLL inhibit colon prostate cance OICR9429 bladder cancer (BCa) Inhibitor WD repeat domain 5 (WDR5) Apoptosis leukaemia H3K4 OICR 9429 inhibitor

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