|(E)-N'-(1-(5-氯-2-羟基苯基)亚乙基)-3-(吗啉磺酰基)苯甲酰肼|CsnPharm

CAS No.: 1423715-09-6

(E)-N'-(1-(5-Chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide Catalog No. CSN15764

Synonyms: HCI-2509;LSD1 Inhibitor VII

SP-2509 is a histone demethylase LSD1 (KDM1A) antagonist with IC50 of 13 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 KDM1A

IC50:13nM
描述SP2509 is a selective LSD1 antagonist with IC50 value of 13nM. Treatment with SP2509 induced more apoptosis and more cell growth inhibition of AML cells expressing mutant NPM1, OCI-AML3 cells, than mixed-lineage leukemia fusion oncoproteins (MV4-11 and MOLM13 cells) at concentration of 1μM for 48h and 96h, respectively. SP2509 at concentration increased the mRNA levels of p57KIP, KLF4 and p21 in OCI-AML3 cells post 16h. Differentiation of cultured and primary AML cells induced by 1μM SP2509 could also be observed after 96h. Intraperitoneal injection with SP2509 twice per week for 3 weeks significantly improved the survival of immunedepleted mice following tail-vein infusion and engraftment of cultured (OCI-AML3 xenografts, at dose of 25mg/kg) or primary human AML cells (at dose of 15mg/kg). Combined treatment of panobinostat could synergize with SP2509 and significantly improved the survival of the mice engrafted with the human AML cells, without exhibiting any toxicity. Inhibition of LSD1 by SP2509 partially reversed the reduction of H3K4 methylation in Utx-deficient HSPCs (hematopoietic stem and progenitor cells) post 12h and reversed the reduction of the expression of differentiation-related and tumor suppressor genes by Utx loss. Administration of SP2509 promoted the differentiation of Utx-null AML cells both in vitro and in vivo and, therefore, extended the survival of the leukemic mice.
作用机制SP2509 attenuated the binding of LSD1 with the corepressor CoREST, increased the permissive H3K4Me3 mark on the target gene promoters.^[1]
动物研究
剂量
Mice: 25 mg/kg^[1] (i.p.), 0.5 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 25 mg/kg^[1] (i.p.), 0.5 mg/kg^[3] (i.p.)
给药途径	i.p.

[1] Fiskus W, Sharma S, et al. Highly effective combination of LSD1 (KDM1A) antagonist and pan-histone deacetylase inhibitor against human AML cells. Leukemia. 2014 Nov;28(11):2155-64.
[2] Wu B, Pan X, et al. Epigenetic drug library screening identified an LSD1 inhibitor to target UTX-deficient cells for differentiation therapy. Signal Transduct Target Ther. 2019 Apr 26;4:11.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2836 mL
- 11.4182 mL
- 22.8364 mL
- 5 mM
- 0.4567 mL
- 2.2836 mL
- 4.5673 mL
- 10 mM
- 0.2284 mL
- 1.1418 mL
- 2.2836 mL

技术信息

CAS号

1423715-09-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H20ClN3O5S

运输

蓝冰

分子量

437.90

别名

HCI-2509;LSD1 Inhibitor VII

溶解度

DMSO	185.0 mg/mL (422.5 mM)
Water	insoluble

动物实验配方

10% DMSO+corn oil

5 mg/mL

大规格询价

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(E)-N'-(1-(5-Chloro-2-hydroxyphenyl)ethylidene)-3-(morpholinosulfonyl)benzohydrazide Catalog No. CSN15764

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