LSD1-IN-13 hydrochloride

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LSD1-IN-13 hydrochloride 

LSD1-IN-13 hydrochloride (compound 7e) 是一种口服有效的 LSD1 抑制剂,其 IC50 值为 24.43 nM。LSD1-IN-13 hydrochloride 可激活 CD86 表达,其 EC50 值为 470 nM。LSD1-IN-13 hydrochloride 诱导 AML (急性髓系白血病)细胞系分化。

LSD1-IN-13 hydrochloride

LSD1-IN-13 hydrochloride Chemical Structure

CAS No. : 2170347-90-5

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生物活性

LSD1-IN-13 hydrochloride (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 hydrochloride can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 hydrochloride induces differentiation of AML (acute myeloid leukemia) cell lines[1].

IC50 & Target

IC50: 24.43 ± 1.08 nM (LSD1), 5.00 ± 0.28 μM (LSD2), >100 μM (MAO-A), >100 μM (MAO-B)[1]

体外研究
(In Vitro)

LSD1-IN-13 hydrochloride (compound 7e) shows good selectivity over LSD2 (205-fold) and MAOs (>4000-fold)[1].
LSD1-IN-13 hydrochloride shows potent and selective antiproliferative activity in MV-4-11, with an IC50 of 1.36 μM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

LSD1-IN-13 hydrochloride (compound 7e) (MV-4-11 xenograft mice, 0-20 mg/kg, Orally, daily for 15 days) suppresses tumor growth significantly in a dose-dependent manner[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

448.02

Formula

C23H30ClN3O2S

CAS 号

2170347-90-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [1]. Li C, et al. Structure-Activity Relationship Study of Indolin-5-yl-cyclopropanamine Derivatives as Selective Lysine Specific Demethylase 1 (LSD1) Inhibitors. J Med Chem. 2022 Mar 10;65(5):4335-4349.

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