SMI-4a
Catalog #
27774-2
$370
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Description
SMI-4a is a potent inhibitor of Pim1 with IC50 = 17 -21 nM. It does not significantly inhibit other serine/threonine- or tyrosine-kinases. It induces G1 phase cell cycle arrest and induces apoptosis through the mitocondrial pathway. It downregulates c-myc and induces p27Kip1 expression. Inhibits PRAS40 phosphorylation and mTOR activity, as well as the mammalian target of rapamycin C1 (mTORC1) pathway. SMI-4a is a potential anti-cancer compound that blocks prostate cancer growth.
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Synonyms
5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione
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Product Data Gallery
Product Info
Storage and Usage
Citations
Format
white to beige powder
Target(s)
Pim1
Formula
C11H6F3NO2S
MW
273.2 Da
Solubility
Soluble in DMSO
Biological Activity
SMI-4a is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM for Pim-1 compared to an IC50 of 100 nM for Pim-2 and with little or no activity against a panel of 50 other kinases tested. SIM-4a kills a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 µM).
CAS Registry #
438190-29-5
Background
The serine/threonine Pim kinases have been suggested to promote the activity of the rapamycin-sensitive mammalian target of rapamycin (mTORC1), which regulates cell growth and survival. Pim kinases are overexpressed in solid cancers and hematologic malignancies, and as such have become targets of small molecule inhibitors to prevent the progression of various cancers. SIM-4a is a Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK.1 SMI-4a has been found to inhibit prostate cancer cell growth and induce G1 phase cell-cycle arrest in precursor T-cell lymphoblastic leukemia/lymphoma cell lines.
References
1. Y.W. Lin, et al.; Blood 115, 824 (2010).
2. F. Zhang, et al.; Cancer Biol. Ther. 8, 846 (2009).
3. Z. Xia, et al.; J.Med.Chem. 52, 74 (2009).
2. F. Zhang, et al.; Cancer Biol. Ther. 8, 846 (2009).
3. Z. Xia, et al.; J.Med.Chem. 52, 74 (2009).
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