438190-29-5
SMI-4a
CAS: 438190-29-5
Molecular Formula: C11H6F3NO2S
438190-29-5 - Names and Identifiers
438190-29-5 - Physico-chemical Properties
| Molecular Formula | C11H6F3NO2S |
| Molar Mass | 273.23 |
| Solubility | Soluble in DMSO (55 mg/ml at 25 °C), ethanol (32 mg/ml at 25 °C), and water (slightl |
| Appearance | powder |
| Color | white to beige |
| Storage Condition | Desiccate at +4°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months. |
| MDL | MFCD01152003 |
| Use | A selective and ATP-competitive Pim kinase inhibitor |
| In vitro study | SMI-4a is an ATP competitive Pim1 inhibitor with an IC50 of 17 nM. SMI-4a highly selective for pim1. SMI-4a inhibition of substrate phosphorylation by Pim-1 in vitro. SMI-4a (5 M) inhibited the growth of pancreatic cancer and leukemia cells. SMI-4a acts on prostate and hematopoietic stem cells to reduce the phosphorylation of Pim target Bad. Results in cell cycle arrest, reversing Pim-1 of anti-apoptotic activity. SMI-4a increase the amount of p27Kip1 in the nucleus. SMI-4a treatment pre-T-LBL, inhibition of mTOR pathway. SMI-4a treatment pre-T-LBL, decreased MYC protein expression. SMI-4a treatment induced up-regulation of MAPK pathway. |
| In vivo study | Smi-4a (60 mg/Kg) treated twice daily significantly reduced tumor size and was well tolerated. One hour after SMI-4a oral feeding, tumors were harvested and p70 S6K phosphorylation was reduced compared to control mouse tumors while total p70 S6K expression was unchanged. |
438190-29-5 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | R36 - Irritating to the eyes R43 - May cause sensitization by skin contact |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
438190-29-5 - Introduction
SMI-4a is an effective Pim1 inhibitor with IC50 of 17 nM. It is moderately effective on Pim-2 and has no significant inhibition of other serine/threonine or tyrosine kinases.
Last Update：2022-10-16 17:41:40
438190-29-5 - Reference Information
| biological activity | SMI-4a (TCS PIM-1 4a) is an effective Pim1 inhibitor with IC50 of 17 nM, which is moderately effective on Pim-2 and does not significantly inhibit other serine/threonine or tyrosine kinases. |
| target | TargetValue Pim1 (Cell-free say) 17 nM |
| Target | Value |
| Pim1 (Cell-free assay) | 17 nM |
| in vitro study | SMI-4a is ATP competitive Pim1 inhibitor, IC50 is 17 nM. SMI-4a highly selective action on Pim1. SMI-4a inhibit substrate phosphorylation by Pim-1 in vitro. SMI-4a (5 μM) inhibits the growth of pancreatic cancer and leukemia cells. SMI-4a acts on prostate and hematopoietic stem cells to reduce phosphorylation of Pim target Bad. It leads to cell cycle arrest and reverses Pim-1 anti-apoptotic activity. SMI-4a increase the amount of p27Kip1 in the nucleus. SMI-4a treatment pre-T-LBL inhibited mTOR pathway. SMI-4a treatment pre-T-LBL reduced MYC protein expression. SMI-4a treatment induced up-regulation of MAPK pathway. |
| in vivo study | SMI-4a (60 mg/Kg) was treated twice a day, significantly reducing tumor size and having good tolerance. One hour after oral feeding of SMI-4a, tumors were collected. Compared with tumors in control mice, p70 S6K phosphorylation was reduced, while the total p70 S6K expression was unchanged. |
Last Update：2024-04-09 21:04:16
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Spot supply
Product Name: SMI-4a Visit Supplier Webpage Request for quotationCAS: 438190-29-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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