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.

• 別名: 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
• 実験式（ヒル表記法）: C₂₁H₂₆N₂S₂ · xHCl
• CAS番号: 130-61-0
• 分子量: 370.57 (free base basis)
• MDL番号: MFCD00012655
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic); protect from light
• 色: off-white
• 溶解性: water: 25 mg/mL
• 輸送温度: ambient
• 保管温度: 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
• InChI Key: NZFNXWQNBYZDAQ-UHFFFAOYSA-N

詳細

詳細

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)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Sachlos, E., et al. 2012. Cell149, 1284.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H302
• 注意書き: P264 - P270 - P301 + P312 - P501
• 危険有害性の分類: Acute Tox. 4 Oral
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3