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SMI-4a

SMI-4a

CAS: 438190-29-5

Molecular Formula: C11H6F3NO2S

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SMI-4a - Names and Identifiers

Name SMI-4a
Synonyms SMI-4a
(Z)-SMI-4a
TCS PIM-1 4a
(Z)-5-(3-(trifluoroMethyl)benzylidene)thiazolidine-2,4-dione
(5Z)-5-[[3-(TRIFLUOROMETHYL)PHENYL]METHYLENE]-2,4-THIAZOLIDINEDIONE
(5Z)-5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione
2,4-Thiazolidinedione, 5-[[3-(trifluoromethyl)phenyl]methylene]-, (5Z)-
(5E)-5-{[3-(trifluoromethyl)phenyl]methylidene}-1,3-thiazolidine-2,4-dione
CAS 438190-29-5
EINECS 200-256-5

SMI-4a - Physico-chemical Properties

Molecular FormulaC11H6F3NO2S
Molar Mass273.23
Solubility Soluble in DMSO (55 mg/ml at 25 °C), ethanol (32 mg/ml at 25 °C), and water (slightl
Appearancepowder
Colorwhite to beige
Storage ConditionDesiccate at +4°C
StabilityStable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
MDLMFCD01152003
UseA selective and ATP-competitive Pim kinase inhibitor
In vitro studySMI-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 studySmi-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.

SMI-4a - Risk and Safety

Hazard SymbolsXi - Irritant
Irritant
Risk CodesR36 - Irritating to the eyes
R43 - May cause sensitization by skin contact
Safety DescriptionS26 - 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 Germany3

SMI-4a - 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

SMI-4a - 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
TargetValue
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
SMI-4a
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Shanghai Macklin Biochemical Co., Ltd
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CAS: 438190-29-5
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Shanghai Yuanye Bio-Technology Co., Ltd.
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CAS: 438190-29-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: SMI-4a Visit Supplier Webpage Request for quotation
CAS: 438190-29-5
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Amole Biotechnology Co., Ltd.
Multiple SpecificationsSpot supply
Product Name: SMI-4a Request for quotation
CAS: 438190-29-5
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: SMI-4a Visit Supplier Webpage Request for quotation
CAS: 438190-29-5
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Spot supply
Product Name: TCS-PIM-1-4a Visit Supplier Webpage Request for quotation
CAS: 438190-29-5
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: SMI-4a Visit Supplier Webpage Request for quotation
CAS: 438190-29-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
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