3-a-Aminocholestane (3AC, SHIP1 Inhibitor)

Product Number: B-0341

3-a-aminocholestane (3AC, SHIP1 Inhibitor) - Echelon Biosciences
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SH2-Domain containing inositol 5-phosphatases (SHIP1 & SHIP2) dephosphorylate the 5-position of PI(3,4,5)P3 generating PI(3,4)P2. SHIP2 is ubiquitously expressed while SHIP1 is only found in hematopoietic lineage cells. 3AC is a selective inhibitor of SHIP1 (EC50 = 10 μM) and shows no inhibition of the other isoform, SHIP2, at concentrations up to 1 mM. 3AC promotes apoptosis of SHIP1-expressing leukemia cells (KG-1) and multiple myeloma cells (OPM) suggesting SHIP1 inhibition is a potential drug target for blood cancers. Mice treated with 3AC show increased numbers of MIR cells in the spleen and lymph nodes and increased numbers of granulocytes.

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Biochemical Reagents
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Inhibitor, SHIP
CAS Number

2206-20-4
Molecular Formula

C27H49N
Molecular Weight (g/mol)

387.68
Purity

95%
Storage

4 °C or below

Technical Data Sheet

1) R. Brooks, et al., “SHIP1 Inhibition Increases Immunoregulatory Capacity and Triggers Apoptosis of Hematopoietic Cancer Cells” J. Immun., 2010, 184, 3582-3589.
2) M. Fuhler, et al. “Therapeutic Potential of SH2 Domain-Containing Inositol-5-Phosphatase 1 (SHIP1) and SHIP2 Inhibition in Cancer” Mol. Med, 2012, 18, 65-75.
3) Drobek, A., J. Kralova, et al. (2015). “PSTPIP2, a Protein Associated with Autoinflammatory Disease, Interacts with Inhibitory Enzymes SHIP1 and Csk.” The Journal of Immunology. DOI:10.4049/jimmunol.1401494
4) Akyol, G. Y., et al. (2017). “IVIG activates FcgRIIB-SHIP1-PIP3 Pathway to stabilize mast cells and suppress inflammation after ICH in mice.” Scientific Reports 7(1): 15583.
5) Rasmussen, P., et al. (2019). “Inhibiting phosphatase SHIP-1 enhances suboptimal IgE-mediated activation of human blood basophils but inhibits IgE-mediated activation of cultured human mast cells.” Immunology Letters 210: 40-46.

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