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WDR5-IN-5

MCE 国际站：WDR5-IN-5

产品活性：WDR5-IN-5 是一种具有口服活性和选择性、靶向 WD 重复结构域 5 (WDR5) WIN 位点的抑制剂。WDR5-IN-5 对 WDR5 具有高亲和力，结合亲和力 K_i <0.02 nM。WDR5-IN-5 具有抗癌细胞增殖活性和良好的药代动力学特征。

研究领域：Epigenetics

作用靶点：Histone Methyltransferase

In Vitro: WDR5 plays an important role in the activity of MLL1 histone methyltransferase (HMT) complexes. WDR5-IN-5 (compound 41), as a WDR5 inhibitor, will exihibits inhibitory effect towards HMT.
WDR5-IN-5 displays average soluble concentrations (kinetic solubility) of 60 µM.
WDR5-IN-5 exhibits high selectivity between K562 cells ａnd MV4:11, the selectivity index (GI_{50, K562}/GI_{50, MV4:11}) is 290.
WDR5-IN-5 (0-30 µM; 5 d) inhibits cell proliferation of MV4:11, MOLM-13, ａnd K562 with GI₅₀ values are 13, 27, 3700 nM, respectively.

In Vivo: WDR5-IN-5 (compound 41) (10 mg/kg; p.o.) shows high oral exposure (AUC_0,inf=3984 h^.ng/mL), long half-life of T_1/2=1.3 h.
WDR5-IN-5 (3 mg/kg; i.v.) also shows low iv clearance (26 mL/min/kg). WDR5-IN-5 is well tolerated ａnd shows no adverse effects in mice by both i.v. ａnd p.o. dosing.
WDR5-IN-5 can be formulated as 0.6 ａnd 1 mg/mL solutions in ethanol, tocopherol poly (ethylene glycol) succinate (TPGS), PEG400 ａnd water (v/v/v/v, 5/5/30/60) for i.v. ａnd p.o. dosing, respectively.
PK profile of WDR5-IN-5 in CD-1 Mice

Route	Dose (mg/kg)	CL (mL/min/kg)	AUC_0,inf (h^.ng/mL)	V_ss (L/kg)	T_1/2 (h)	F (%)
i.v.	3	26	1951	1.6	/	/
p.o.	10	2083	3984	/	1.3	61

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