MG SHIP1 Inhibitor; 3AC 1PC x 10MG

General description

A cell-permeable steroidal compound that selectively inhibits SHIP1-, but not SHIP2-, catalyzed PI(3,4,5)P3-to-PI(3,4)P2 dephosphorylation (IC₅₀ = 10 µM vs. >1 mM, respectively), while exhibiting little activity against the PTEN-catalyzed PI(3,4,5)P3-to-PI(4,5)P2 conversion (IC₅₀ >1 mM). 3AC in vivo treatment (2.292 umol/200 µl/mouse/daily i.p. for 7 d) is reported to boost both peripheral blood granulocyte production (by 4- to 5-fold) and the GVHD- (graft-versus-host disease) suppressing Mac1⁺Gr1⁺ MIR (myeloid immunoregulatory) cell population in lymphoid tissues (by 5.55- and 11.53-fold in spleen and lymph nodes, respectively), resulting in an impaired splenocyte allogeneic T cell response in MLR (mixed-leukocyte/lymphocyte reaction) assays (by ≥95%). Similarly, 3AC-treated (9.4 µM; 24 h) primary human PBMCs greatly lose their ability in priming allogeneic T cell response in MLR assays (by 74.5%). In addition, a faster blood cell recovery is also observed in mice receiving 3AC (2.292 umol/200 µl/mouse/daily i.p. for 7 d) after sub-lethal irradiation (550 Rads). Selectively inhibits the growth and survival of SHIP1-dependent human KG-1 and murine C1498 myelogenous leukemia lines (IC₅₀ = 11.5 µM), but not the SHIP1-negative human CML K562 and osteosarcoma MG63 lines. SHIP2 Inhibitor, AS1938909 is also available (Cat. No. 565840).

A cell-permeable steroidal compound that selectively inhibits SHIP1′ polyphosphatase activity toward PI(3,4,5)P3 (IC₅₀ = 10 µM), but not SHIP2 5′ or PTEN′ polyphosphatase activity toward PI(3,4,5)P3 (IC₅₀ >1 mM). Effectively inhibits SHIP1-mediated immune response both in vitro and in vivo, as well as SHIP1-dependent cancer cell survival. SHIP2 Inhibitor, AS1938909 is also available (Cat. No. 565840).

Legal Information

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

Other Notes

Brooks, R., et al. 2010. J. Immunol.184, 3582.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)