573110

STAT5 Inhibitor III, Pimozide

The STAT5 Inhibitor III, Pimozide, also referenced under CAS 2062-78-4, controls the biological activity of STAT5. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 别名: STAT5 Inhibitor III, Pimozide, 1-(1-(4,4-Bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-2H-benzimidazol-2-one
• 经验公式（希尔记法）: C₂₈H₂₉F₂N₃O
• CAS号: 2062-78-4
• 分子量: 461.55
• MDL號碼: MFCD00055081
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: white
• 溶解度: DMSO: 50 mg/mL
• 運輸包裝: ambient
• 儲存溫度: −20°C
• SMILES 字串: O=C1NC2=CC=CC=C2N1C3CCN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3
• InChI: 1S/C28H29F2N3O/c29-22-11-7-20(8-12-22)25(21-9-13-23(30)14-10-21)4-3-17-32-18-15-24(16-19-32)33-27-6-2-1-5-26(27)31-28(33)34/h1-2,5-14,24-25H,3-4,15-19H2,(H,31,34)
• InChI 密鑰: YVUQSNJEYSNKRX-UHFFFAOYSA-N

说明

一般說明

A cell-permeable and orally available diphenylbutylpiperidine class of psychotropic drug with antagonistic activity against DAT (dopamine transporter) as well as several postsynaptic receptors, including D₁, D₂, D₃, D₄, α₁-/α₂-adrenergic, and 5-HT_2A receptors. In addition to its antipsychotic property, Pimozide is shown to inhibit the constitutive STAT5 Tyr694 phosphorylation (5 to 10 µM for 3h) and transcription activity (5 µM for 18 h) in Bcr-Abl+ K562 and KU812 cultures, while exhibiting little activity against IFNα-stimulated STAT1 phosphorylation or LIF-stimulated STAT3 phosphorylation in K562 cells (10 µM 1 h pretreatment). The mechanism of STAT5 inhibition is currently unknown and Primozide is reported to exhibit little inhibitory activity against cellular Bcr-Abl autophosphorylation or the kinase activities of Abl1 (Wt & T315I), Hck, Lyn A/B, and Src (≤7%) in cell-free kinase assays. Shown to exhibit selective antiproliferative activity against K562, KU812, and primary bone marrow mononuclear cells from CML patients (by >80%; 10 µM for 48 h), but not peripheral blood mononuclear cells from healthy individuals, due to G0/G1 cell cycle arrest and apoptosis induction.

A cell-permeable and orally available diphenylbutylpiperidine class of psychotropic drug with antagonistic activity against DAT (dopamine transporter) as well as several postsynaptic receptors, including D₁, D₂, D₃, D₄, α₁-/α₂-adrenergic, and 5-HT_2A receptors. In addition to its antipsychotic property, Pimozide is shown to inhibit the constitutive STAT5 Tyr694 phosphorylation (5 to 10 µM for 3h) and transcription activity (5 µM for 18 h) in Bcr-Abl+ K562 and KU812 cultures, while exhibiting little activity against IFNα-stimulated STAT1 phosphorylation or LIF-stimulated STAT3 phosphorylation in K562 cells (10 µM 1 h pretreatment). The mechanism of STAT5 inhibition is currently unknown and Primozide is reported to exhibit little inhibitory activity against cellular Bcr-Abl autophosphorylation or the kinase activities of Abl1 (Wt & T315I), Hck, Lyn A/B, and Src (≤7%) in cell-free kinase assays. Shown to exhibit selective antiproliferative activity against K562, KU812, and primary bone marrow mononuclear cells from CML patients (by >80%; 10 µM for 48 h), but not peripheral blood mononuclear cells from healthy individuals, due to G0/G1 cell cycle arrest and apoptosis induction. Acts as a selective and non-competitive inhibitor of human USP1/UAF1 and USP7 activities (IC₅₀ = 2 and 47 µM, respectively) with no effect on UCH-L1 and UCH-L3 (IC₅₀ >500 µM).

包裝

Packaged under inert gas

警告

Toxicity: Regulatory Review (Z)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions ar stable for up to 6 months at -20°C.

其他說明

Chen, J., et al. 2011. Chem. Biol18, 1390.
Nelson, E.A., et al. 2011. Blood117, 3421.

法律資訊

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

安全信息

• 象形圖: GHS07
• 訊號詞: Warning
• 危險聲明: H302
• 防範說明: P264 - P270 - P301 + P312 - P501
• 危險分類: Acute Tox. 4 Oral
• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable