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Merck
모든 사진(2)

Key Documents

573110

Sigma-Aldrich

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.

동의어(들):

STAT5 Inhibitor III, Pimozide, 1-(1-(4,4-Bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-2H-benzimidazol-2-one

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About This Item

실험식(Hill 표기법):
C28H29F2N3O
CAS Number:
Molecular Weight:
461.55
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

형태

solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

white

solubility

DMSO: 50 mg/mL

배송 상태

ambient

저장 온도

−20°C

SMILES string

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 key

YVUQSNJEYSNKRX-UHFFFAOYSA-N

일반 설명

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-HT2A 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-HT2A 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).

포장

Packaged under inert gas

경고

Toxicity: Regulatory Review (Z)

재구성

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

기타 정보

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

법적 정보

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

픽토그램

Exclamation mark

신호어

Warning

유해 및 위험 성명서

예방조치 성명서

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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