3α-Aminocholestane

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

3α-Aminocholestane 是含有选择性 SH2 结构域的肌醇-5'-磷酸酶 1 (SHIP1) 的抑制剂，其 IC50值约为 2.5 μM。

3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.

OPM2 cell viability is effectively reduced by 3α-Aminocholestane (3AC) treatment. RPMI8226 and U266 cells show significantly less sensitivity to 3α-Aminocholestane treatment when compare with OPM2 cells, although viability is decreased significantly at concentrations of ≥12.5 μM. Treatment with 3α-Aminocholestane for 36 h severely reduces the percentage of cells in the S phase, which is accompanied by an increase of cells in the G2/M phase. In contrast, in the less proliferative RPMI8226 and U266 cells, cell cycle progression is blocked in the G0/G1 phase upon 3α-Aminocholestane treatment, in conjunction with a reduced percentage of cells undergoing the S phase.

It is found that 3α-Aminocholestane (3AC) results in reduced multiple myeloma (MM) growth in vivo, as determined by quantitation of free human Igλ light chain in the plasma after OPM2 challenge. In addition, reduced numbers of circulating OPM2 cells, as determined by human HLA-ABC staining, is observed in peripheral blood from 3α-Aminocholestane-treated mice compare with vehicle controls. Most importantly, 3α-Aminocholestane treatment results in significantly enhanced survival of mice after tumor challenge. In 3α-Aminocholestane-treated mice that resist treatment, it is found that MM tumors exhibit an upregulation of SHIP2, reminiscent of in vitro treatment of OPM2 cells and suggesting that SHIP1 inhibition may select for tumor cells with increased SHIP2 expression.

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Metabolic Enzyme/Protease

Phosphatase

Phosphatase

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2206-20-4

387.68

C27H49N

>98% (HPLC)

In Vitro:?Ethanol 中的溶解度 : 50 mg/mL (128.97 mM; 超声助溶)DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

[H][C@@]1(CC[C@@]2([H])[C@]3([H])CC[C@@]4([H])C[C@H](N)CC[C@]4(C)[C@@]3([H])CC[C@]12C)[C@H](C)CCCC(C)C

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(-20℃)

With Ice Pack

≥ 2 years