1. Epigenetics
    Apoptosis
  2. Histone Methyltransferase
    Apoptosis
  3. WDR5-IN-1

WDR5-IN-1 

Cat. No.: HY-133121
Handling Instructions

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.

For research use only. We do not sell to patients.

WDR5-IN-1 Chemical Structure

WDR5-IN-1 Chemical Structure

CAS No. : 2408842-51-1

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Description

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1].

In Vitro

WDR5-IN-1 (1 µM; 48 hours) shows an apparent decrease in G2M phase cells[1].
WDR5-IN-1 (0.01-3 µM; 24-48 hours) increases p53 and p21 protein levels[1]. WDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells), with GI50s ranging from 0.26-3.2 µM[1].

Cell Cycle Analysis[1]

Cell Line: MV4:11 cells
Concentration: 1 µM
Incubation Time: 48 hours
Result: Showed an approximate 4 fold increased SubG1 cells.

Western Blot Analysis[1]

Cell Line: MV4:11 cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 µM
Incubation Time: 24, 48 hours
Result: p53 and p21 protein levels started to increase from 8 h post treatment of compound 16 at 300 nM and continued to elevate up to 32 h.
Molecular Weight

514.59

Formula

C₃₀H₃₁FN₄O₃

CAS No.

2408842-51-1

SMILES

COC1=CC(OC)=CC(CN2C(C(C=C(CN3C(N(C)C=C3)=N)C=C4C5=C(C)C=C(F)C=C5)=C4CC2)=O)=C1

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

WDR5-IN-1Histone MethyltransferaseApoptosisMYCproliferativelymphomaneuroblastomaapoptosiscycleturmorigenesischromatin,Inhibitorinhibitorinhibit

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