Art. -Nr.: HY-16993

OICR-9429

15 Cited Publications

Kundenbewertung

Based on 15 publication(s) in Google Scholar

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) .

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Reinheit: 99.71%
CAS. Nr.: 1801787-56-3
Formel: C₂₉H₃₂F₃N₅O₃
Molecular Weight:555.59

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

OICR-9429 Chemical Structure

CAS. Nr.: 1801787-56-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 67.74 μM (T24 cell); 0.41 μM (UM-UC-3 cell); 121.42 μM (TCCSUP) ^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
K562	GI₅₀	>2500 nM Compound: OICR-9429	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 38085679]
MV4-11	GI₅₀	>2500 nM Compound: OICR-9429	Antiproliferative activity against human MV4-11 cells Antiproliferative activity against human MV4-11 cells	[PMID: 38085679]

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^[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

BCa cell lines (T24, UM-UC-3 and TCCSUP)
Concentration:

70 μM, 120 μM, 140 μM and 240 μM
Incubation Time:

5 days
Result:

Had a low proliferation rate and remarkably reduced the number of colonies formed by the three BCa cell lines in a dose-dependent manner.

Cell Cytotoxicity Assay^[1]

Cell Line:

BCa cell lines (T24, UM-UC-3 and TCCSUP)
Concentration:

0-10 μM
Incubation Time:

48 h
Result:

Inhibited cell viability in a dose-dependent manner in BCa cell lines.

Apoptosis Analysis^[1]

Cell Line:

BCa cell lines (T24, UM-UC-3 and TCCSUP)
Concentration:

70 μM, 120 μM, 140 μM and 240 μM
Incubation Time:

24 h
Result:

Showed no obvious apoptotic cells for 24 h but the apoptotic rate was significantly increased at 72 h and upregulated caspase 3/7 activity.

Cell Migration Assay ^[1]

Cell Line:

BCa cell lines (T24, UM-UC-3 and TCCSUP)
Concentration:

70 μM, 120 μM, 140 μM and 240 μM
Incubation Time:

24 h, 48 h
Result:

Reduced the migratory speed and decreased the migration of the three BCa cell lines.

Cell Invasion Assay^[1]

Cell Line:

BCa cell lines (T24, UM-UC-3 and TCCSUP)
Concentration:

70 μM, 120 μM, 140 μM and 240 μM
Incubation Time:

24 h, 48 h
Result:

Decreased the invasion of the three BCa cell lines.

Western Blot Analysis^[1]

Cell Line:

BCa cell lines (T24, UM-UC-3 and TCCSUP)
Concentration:

70 μM, 120 μM, 140 μM and 240 μM
Incubation Time:

48 h
Result:

Showed significant downregulation of H3K4me3 in treated cells but not WDR5 or total H3.
Reduced the expression of PD-L1 induced by IFN-γ in a dose-dependent manner at both the RNA and protein levels.

RT-PCR^[1]

Cell Line:

BCa cell lines (T24, UM-UC-3 and TCCSUP)
Concentration:

70 μM, 120 μM, 140 μM and 240 μM
Incubation Time:

48 h
Result:

Downregulated some genes related to the cell cycle, such as CDK1, PLK1, CCNE2, CCNB1, CCNA2, AURKA, and E2F1, genes related to apoptosis and DNA repair, such as BIRC5, XRCC2, AURKA, E2F1, and MCM2, and genes related to metastasis, such as AURKA and FOXM1.

Cell Cycle Analysis^[1]

Cell Line:

BCa cell lines (T24, UM-UC-3 and TCCSUP)
Concentration:

70 μM, 120 μM, 140 μM and 240 μM
Incubation Time:

48 h
Result:

Increased the cell population in the G0/G1 phase of three BCa cells and reduced cell population in the S and G2/M phases.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

xenograft mouse model^[1]
Dosage:

30 mg/kg, 60 mg/kg
Administration:

30 mg/kg, 60 mg/kg, i.p.
Result:

Suppressed tumour growth, small tumours and enhanced tumour sensitivity.

Chemical Information

CAS. Nr. 1801787-56-3
Appearance Solid
Molecular Weight 555.59
Formel C₂₉H₃₂F₃N₅O₃
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (15)

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Journal Impact Factor

Cancer Commun (Lond)

2025 Dec 26.

OICR-9429 purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Dec 26.

OICR-9429 (20 μM; 24 h). qPCR analysis of H3K4me3 enrichment at SPP1 promoter area in THP-1 cells under indicated treatment conditions.

OICR-9429 purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Dec 26.

OICR-9429 (20 μM; 24 h). Agarose gel electrophoresis analysis showed that the SPP1 promoter sequence in THP-1 cells was immunoprecipitated with anti-H3K4me3, anti-WDR5 and IgG antibodies under specified treatment conditions.

OICR-9429 purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Dec 26.

OICR-9429 (20 μM; 24 h). Western blotting shows the expression of OPN in THP-1 and U937 cells after specified treatment.
Nat Genet

Adenine DNA methylation associated with transcriptionally permissive chromatin is widespread across eukaryotes. [Abstract]

2025 Dec;57(12):3126-3136. PMID: 41254163
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

Catalytic Proximal Protein Oligomerization as an Anti-Tumor Strategy Targeting WDR5. [Abstract]

2026 Mar 13;17(1):3879. PMID: 41820364
Nat Commun

A histone-centric multi-omics study shows that increased H3K4 methylation sustains triple-negative breast cancer phenotypes. [Abstract]

2025 Sep 30;16(1):8716. PMID: 41028718
Nat Commun

Genotoxic stress-triggered β-catenin/JDP2/PRMT5 complex facilitates reestablishing glutathione homeostasis. [Abstract]

2019 Aug 21;10(1):3761. PMID: 31434880

OICR-9429 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761. [Abstract]

WDR5 inhibitor OICR-9429 (3 mg/kg) enhances the sensitivity of ovarian cancer to genotoxic chemotherapeutics in vivo. Representative images and the apoptotic rate the indicated chemotherapy-treated xenograft tumors.

OICR-9429 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761. [Abstract]

OICR-9429 (3 mg/kg). IB analysis of the level of cleaved-caspase 3 and cleaved-PARP1 in the indicated chemotherapy-treated xenograft tumors. GAPDH served as the loading control.
J Exp Clin Cancer Res

Kinesin family member 23, regulated by FOXM1, promotes triple negative breast cancer progression via activating Wnt/β-catenin pathway. [Abstract]

2022 May 7;41(1):168. PMID: 35524313
Adv Sci (Weinh)

H3K4me3-Mediated FOXJ2/SLAMF8 Axis Aggravates Thrombosis and Inflammation in β2GPI/Anti-β2GPI-Treated Monocytes. [Abstract]

2024 Jun;11(24):e2309140. PMID: 38639399
Cell Death Discov

Mitochondrial dysfunction-mediated metabolic remodeling of TCA cycle promotes Parkinson's disease through inhibition of H3K4me3 demethylation. [Abstract]

2025 Jul 29;11(1):351. PMID: 40730642
Acta Pharmacol Sin

P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. [Abstract]

2022 Feb;43(2):457-469. PMID: 33850273
Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
Clin Transl Med

ARID5B-mediated LINC01128 epigenetically activated pyroptosis and apoptosis by promoting the formation of the BTF3/STAT3 complex in β2GPI/anti-β2GPI-treated monocytes. [Abstract]

2024 Jan;14(1):e1539. PMID: 38224186
Cell Rep

UTP18-mediated p21 mRNA instability drives adenoma-carcinoma progression in colorectal cancer. [Abstract]

2023 Apr 21;42(5):112423. PMID: 37086406
Res Sq

2026 Feb 18.
Research Square Preprint

2022 Jan.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 32 mg/mL (57.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7999 mL

8.9994 mL

17.9989 mL

5 mM

0.3600 mL

1.7999 mL

3.5998 mL

10 mM

0.1800 mL

0.8999 mL

1.7999 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7999 mL	8.9994 mL	17.9989 mL	44.9972 mL
	5 mM	0.3600 mL	1.7999 mL	3.5998 mL	8.9994 mL
	10 mM	0.1800 mL	0.8999 mL	1.7999 mL	4.4997 mL
	15 mM	0.1200 mL	0.6000 mL	1.1999 mL	2.9998 mL
	20 mM	0.0900 mL	0.4500 mL	0.8999 mL	2.2499 mL
	25 mM	0.0720 mL	0.3600 mL	0.7200 mL	1.7999 mL
	30 mM	0.0600 mL	0.3000 mL	0.6000 mL	1.4999 mL
	40 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1249 mL
	50 mM	0.0360 mL	0.1800 mL	0.3600 mL	0.8999 mL

Keywords

OICR-9429

15 Cited Publications

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OICR-9429

Apoptosis Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Chemical Probe Library

Targeted Diversity Library

Anti-Prostate Cancer Compound Library

Cell Death Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) OICR-9429

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

OICR-9429

Apoptosis Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Chemical Probe Library

Targeted Diversity Library

Anti-Prostate Cancer Compound Library

Cell Death Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) OICR-9429

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

OICR-9429 Related Classifications

HY-16993 Related Classifications