Eleven-Nineteen-Leukemia Protein IN-3

CAS: F: C28H27N5O2 W: 465.55

Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. E

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Bioactivity	Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro[1].
Invitro	Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) 对 MV4-11 和 MOLM-13 细胞系有显著的抑制作用，IC50 值分别为 4.8 µM 和 8.3 µM[1]。Eleven-Nineteen-Leukemia Protein IN-3 (5 µM；6 h) 显著提高内源性 ENL 蛋白的热稳定性，对 GAS41 蛋白的热稳定性无明显影响。Eleven-Nineteen-Leukemia Protein IN-3 能有效地抑制 MOLM-13 细胞生长[1]。Eleven-Nineteen-Leukemia Protein IN-3 (5 µM；72 h) 抑制了关键癌基因 MYC 的表达 (约 50 %)。Eleven-Nineteen-Leukemia Protein IN-3 与 JQ-1 (HY-13030) 协同作用时，能进一步下调 ENL 靶基因中 MYC 的表达[1]。 RT-PCR[1] Cell Line:
In Vivo	Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) (30 mg/kg；口服；单剂量) 具有口服暴露特性[1]。Eleven-Nineteen-Leukemia Protein IN-3 (5 mg/kg；静脉注射；单剂量) 在体内有较高的暴露量[1]。雄性 BALB/c 小鼠的药代动力学 (PK) 研究[1]Administration
Name	Eleven-Nineteen-Leukemia Protein IN-3
Formula	C28H27N5O2
Molar Mass	465.55
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Guo S, et al. Design, synthesis of novel benzimidazole derivatives as ENL inhibitors suppressing leukemia cells viability via downregulating the expression of MYC. Eur J Med Chem. 2023 Feb 15;248:115093.