324387
Dopamine Receptor Antagonist II, Thioridazine, HCl
The Dopamine Receptor Antagonist II, Thioridazine, HCl, also referenced under CAS 130-61-0, controls the biological activity of Dopamine Receptor. This small molecule/inhibitor is primarily used for Biochemicals applications.
别名:
Dopamine Receptor Antagonist II, Thioridazine, HCl, 10-(2-(1-Methyl-2-piperidyl)ethyl)-2-(methylthio)-10H-phenothiazine, HCl, 10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine, HCl
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About This Item
经验公式（希尔记法）:
C21H26N2S2 · xHCl
CAS Number:
分子量:
370.57 (free base basis)
MDL编号:
UNSPSC代码:
12352200
质量水平
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
off-white
溶解性
water: 25 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C21H26N2S2.ClH/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(24-2)15-19(21)23;/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3;1H
一般描述
A phenothiazine class antipsychotic and dopamine receptor (DR) antagonist that is reported to exhibit CSCs- (cancer stem cells) differentiating (EC50 ≤9.4 µM for v1H9) and anti-leukemic activity, without affecting non-neoplastic H9 hESC, adult fibroblast-derived iPSC, or HSPCs (hematopoietic stem-progenitor cells). However, Thioridazine′s high effective concentration (10 µM) against cancer cells suggests that other unidentified cellular targets/mechanisms in addition to DR antagonism may be also involved in its overall anti-CSC impact. Effectively augments AraC (Cat. No. 251010) in inhibiting primary AML in vitro colony formation (by 79%, 55%, and 100%, respectively, with 10 µM Thioridazine, 0.1 µM AraC, or a combination of both).
A phenothiazine class dopamine receptor (DR) antagonist that, in addition to its well known clinical use as an antipsychotic for schizophrenia treatment, is also reported to selectively induce the differentiation of neoplastic v1H9 (EC50 ≤9.4 µM in Oct4-GFP reporter assay) and v2H9, but not their parent non-neoplastic H9 hESC or adult fibroblast-derived iPSC. Both Thioridazine′s CSCs- (cancer stem cells) selective differentiation effect and anti-leukemic activity correlate well with the selective DR expression on CSCs and AML cells, but not H9, iPSC, normal HSCs (hematopoietic stem cells) or HSPCs (hematopoietic stem-progenitor cells). However, Thioridazine′s high effective concentration (10 µM) against cancer cells suggests that other unidentified cellular targets/mechanisms in addition to DR antagonism are involved in its overall anti-CSC impact. Effectively augments AraC (Cat. No. 251010) in inhibiting primary AML in vitro colony formation (by 79%, 55%, and 100%, respectively, with 10 µM Thioridazine, 0.1 µM AraC, or a combination of both) without exerting cytotoxic effect on normal HSPCs.
包装
Packaged under inert gas
警告
Toxicity: Regulatory Review (Z)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Sachlos, E., et al. 2012. Cell149, 1284.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral
储存分类代码
11 - Combustible Solids
WGK
WGK 3
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