1. Epigenetics
  2. WDR5
  3. WDR5-IN-4

WDR5-IN-4 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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WDR5-IN-4 Chemical Structure

WDR5-IN-4 Chemical Structure

CAS No. : 2407457-36-5

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Based on 3 publication(s) in Google Scholar

Other Forms of WDR5-IN-4:

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Description

WDR5-IN-4 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 [1][1].

IC50 & Target

Kd: 0.1 nM (WIN)[1]

Cellular Effect
Cell Line Type Value Description References
CHP-134 GI50
2.7 μM
Compound: 1
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
[PMID: 31858797]
Daudi GI50
6.8 μM
Compound: 1
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
[PMID: 31858797]
K562 GI50
17000 nM
Compound: 1
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
[PMID: 31858797]
MOLM-13 GI50
900 nM
Compound: 1
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
[PMID: 31858797]
MV4-11 GI50
600 nM
Compound: 1
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
[PMID: 31858797]
Raji GI50
16 μM
Compound: 1
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
[PMID: 31858797]
Ramos GI50
7.1 μM
Compound: 1
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
[PMID: 31858797]
SW480 GI50
> 29 μM
Compound: 1
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
[PMID: 31858797]
SW-620 GI50
6.5 μM
Compound: 1
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
[PMID: 31858797]
Molecular Weight

498.38

Formula

C25H22Cl2FN5O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Product Name:
WDR5-IN-4
Cat. No.:
HY-111753
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