WDR5-IN-4
Based on 5 publication(s) in Google Scholar
WDR5-IN-4 (Compound C6) is a WIN site inhibitor of chromatin-associated WD repeat domain 5 protein (WDR5), Kd The value is 0.1 nM. WDR5-IN-4 is able to displace WDR5 from chromatin and reduce the expression of related genes, causing translation inhibition and nucleolar stress. Has anti-cancer effects .
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- Pureté: 98.13%
- CAS No.: 2407457-36-5
- Formule: C25H22Cl2FN5O
- Masse moléculaire:498.38
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) WDR5-IN-4
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Activité biologique
Kd: 0.1 nM (WIN)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHP-134 | GI50 |
2.7 μM
Compound: 1
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Antiproliferative activity against human CHP134 cells expressing wild type p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human CHP134 cells expressing wild type p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
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[PMID: 31858797] |
| Daudi | GI50 |
6.8 μM
Compound: 1
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Antiproliferative activity against human Daudi cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human Daudi cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
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[PMID: 31858797] |
| K562 | GI50 |
17 μM
Compound: 1
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Antiproliferative activity against human K562 cells assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human K562 cells assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
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[PMID: 31858797] |
| MOLM-13 | GI50 |
900 nM
Compound: 1
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Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
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[PMID: 31858797] |
| MV4-11 | GI50 |
600 nM
Compound: 1
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Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as growth inhibition after 5 days by CellTiter-Glo luminescent assay
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[PMID: 31858797] |
| Raji | GI50 |
16 μM
Compound: 1
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Antiproliferative activity against human Raji cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human Raji cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
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[PMID: 31858797] |
| Ramos | GI50 |
7.1 μM
Compound: 1
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Antiproliferative activity against human Ramos cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human Ramos cells expressing mutant p53 assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
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[PMID: 31858797] |
| SW480 | GI50 |
>29 μM
Compound: 1
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Antiproliferative activity against human SW480 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human SW480 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
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[PMID: 31858797] |
| SW-620 | GI50 |
6.5 μM
Compound: 1
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Antiproliferative activity against human SW620 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
Antiproliferative activity against human SW620 cells assessed as growth inhibition after 5 days by Celltiter-Glo luminescent assay
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[PMID: 31858797] |
WDR5-IN-4 (0-50 μM, 3 days) inhibits the proliferation of MLL1-rearranged cancer cells MV4:11 and K562 cells with GI50s of 3.20 μM and 25.4 μM[1].
WDR5-IN-4 (2 μM, 6 days) arrests the cell cycle of MV4:11 at sub-G1 phase, induces apoptosis in MV4:11[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4:11 and K562
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Concentration:0-50 μM
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Incubation Time:6 days
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Result:Arrested the cell cycle at sub-G1 phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rnf220+/- mouse models[2]
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Dosage:100 μg
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Administration:intrauterine injection, single dose
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Result:Upregulated the expression of Hox genes.
Chemical Information
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CAS No. 2407457-36-5
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Appearance Solid
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Masse moléculaire 498.38
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Formule C25H22Cl2FN5O
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Color Light yellow to yellow
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SMILES
ClC1=CC=C(CNC(C2=CC(CN3C(N(C)C=C3)=N)=CC(C4=C(C)N=C(F)C=C4)=C2)=O)C=C1Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Rep
UTP18-mediated p21 mRNA instability drives adenoma-carcinoma progression in colorectal cancer. [Abstract]2023 Apr 21;42(5):112423. PMID: 37086406 -
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bioRxiv
SAGA/ATAC complexes sustain aberrant chromatin regulation and promote tumorigenesis in diffuse midline glioma. [Abstract]2026 Jan 23:2026.01.22.701194. PMID: 41648478 -
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Pureté et documentation
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Fiche technique (274 KB)
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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)
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Instruction de manipulation (2659 KB)
Références
[1]. Aho ER, et al. Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep. 2019 Mar 12;26(11):2916-2928.e13. [Content Brief]
[2]. Wang H, et al. The E3 ubiquitin ligase RNF220 maintains hindbrain Hox expression patterns through regulation of WDR5 stability[J]. Elife, 2024, 13: RP94657. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WDR5-IN-4 Related Classifications
HY-111753 Related Classifications
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