WDR5-IN-1

CAS NO.：2408842-51-1
Empirical Formula: C30H31FN4O3
Molecular Weight: 514.59
MDL number: MFCD34469869
Update Date: 2025-04-17 18:22:24

What is WDR5-IN-1?

Biological Activity

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]. 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].

References

[1]. Tian J, et al.Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.J Med Chem. 2020 Jan 23;63(2):656-675.

Properties of WDR5-IN-1

Boiling point:	696.7±65.0 °C(Predicted)
Density	1.25±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
pka	2?+-.0.20(Predicted)
form	Solid
color	Light yellow to brown

Safety information for WDR5-IN-1

Computed Descriptors for WDR5-IN-1

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