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Technical Data
| Formula | C11H6F3NO2S |
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| Molecular Weight | 273.23 | CAS No. | 438190-29-5 | |
| Solubility (25°C)* | In vitro | DMSO | 55 mg/mL (201.29 mM) | |
| Ethanol | 32 mg/mL (117.11 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | SMI-4a (TCS PIM-1 4a) is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases. | ||
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| Targets |
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| In vitro | SMI-4a is an ATP competitive inhibitor of Pim1 with IC50 of 17 nM. SMI-4a shows high selectivity for Pim1 against a panel of kinases. SMI-4a inhibits the in vitro phosphorylation by Pim-1 of the known substrate, the translational repressor 4E-BP1. SMI-4a (5μM) inhibits pancreatic and leukemic cells growth. SMI-4a reduces phosphorylation of the Pim target Bad in prostate and hematopoietic cells. SMI-4a causes cell cycle arrest and reverses the antiapoptotic activity of Pim-1. SMI-4a increases the amount of p27Kip1 in the nucleus.[1] SMI-4a treatment of pre-T-LBL inhibits the mTOR pathway. SMI-4a reduces MYC protein expression in pre-T-LBL. SMI-4a treatment induces up-regulation of MAPK pathway. [2] | ||
| In vivo | SMI-4a (60 mg/Kg) treatment twice daily significantly reduce tumor size and is well tolerated. Tumors harvested 1 hour after the final oral gavage of SMI-4a demonstrates decreased phosphorylation of p70 S6K compared with tumors from mice treated with vehicle, whereas in comparison total p70 S6K expression isunchanged. [2] | ||
| Features | SMI-4a (5μM) synergizes with rapamycin (5 nM) to cause significant growth inhibition of leukemic cells. |
Protocol (from reference)
| Animal Study:[2] |
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References
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Customer Product Validation
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, , Blood, 2016, 127:2439-2450.
Selleck's SMI-4a has been cited by 11 publications
| Targeting macrophagic PIM-1 alleviates osteoarthritis by inhibiting NLRP3 inflammasome activation via suppressing mitochondrial ROS/Cl- efflux signaling pathway [ J Transl Med, 2023, 21(1):452] | PubMed: 37422640 |
| Multicellular immune dynamics implicate PIM1 as a potential therapeutic target for uveitis [ Nat Commun, 2022, 13-1:5866] | PubMed: 36195600 |
| Pim1 promotes IFN-β production by interacting with IRF3 [ Exp Mol Med, 2022, 54(11):2092-2103] | PubMed: 36446848 |
| Anti-platelet Properties of Pim Kinase Inhibition Is Mediated Through Disruption of Thromboxane A2 Receptor Signalling [ Haematologica, 2020, 28;haematol.2019.223529] | PubMed: 32467143 |
| PIM1 inhibition attenuated endotoxin-induced acute lung injury through modulating ELK3/ICAM1 axis on pulmonary microvascular endothelial cells [ Inflamm Res, 2020, 10.1007/s00011-020-01420-3] | PubMed: 33185705 |
| Pim-1 as a Therapeutic Target in Lupus Nephritis. [ Arthritis Rheumatol, 2019, 71(8):1308-1318] | PubMed: 30791224 |
| PIM1 inhibitor SMI-4a attenuated lipopolysaccharide-induced acute lung injury through suppressing macrophage inflammatory responses via modulating p65 phosphorylation. [ Int Immunopharmacol, 2019, 73:568-574] | PubMed: 31203114 |
| The role of dorsal root ganglia PIM1 in peripheral nerve injury-induced neuropathic pain. [ Neurosci Lett, 2019, 709:134375] | PubMed: 31349016 |
| Pim1 promotes cell proliferation and regulates glycolysis via interaction with MYC in ovarian cancer [ Onco Targets Ther, 2018, 11:6647-6656] | PubMed: 30349298 |
| Palbociclib treatment of FLT3-ITD+ AML cells uncovers a kinase-dependent transcriptional regulation of FLT3 and PIM1 by CDK6 [Uras IZ Blood, 2016, 127(23):2890-902] | PubMed: 27099147 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.