TCS-PIM-1-4a

Modify Date: 2025-08-26 15:33:01

TCS-PIM-1-4a structure	Common Name	TCS-PIM-1-4a
	CAS Number	327033-36-3	Molecular Weight	273.231
	Density	1.5±0.1 g/cm3	Boiling Point	N/A
	Molecular Formula	C₁₁H₆F₃NO₂S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of TCS-PIM-1-4a

TCS-PIM-1-4a is a Pim inhibitor that blocks mTORC1 activity via activation of AMPK; kills a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 μM).IC50 value:Target: Pim SMI-4a a novel benzylidene-thiazolidine-2, 4-dione small molecule inhibitor of the Pim kinases, kills a wide range of both myeloid and lymphoid cell lines with precursor T-cell lymphoblastic leukemia/lymphoma (pre-T-LBL/T-ALL) being highly sensitive. Incubation of pre-T-LBL cells with SMI-4a induced G1 phase cell-cycle arrest secondary to a dose-dependent induction of p27(Kip1), apoptosis through the mitochondrial pathway, and inhibition of the mammalian target of rapamycin C1 (mTORC1) pathway based on decreases in phospho-p70 S6K and phospho-4E-BP1, 2 substrates of this enzyme. In addition, treatment of these cells with SMI-4a was found to induce phosphorylation of extracellular signal-related kinase1/2 (ERK1/2), and the combination of SMI-4a and a mitogen-activated protein kinase kinase 1/2 (MEK1/2) inhibitor was highly synergistic in killing pre-T-LBL cells. SMI-4a blocked the rapamycin-sensitive mTORC1 activity by stimulating the phosphorylation and thus activating the mTORC1 negative regulator AMP-dependent protein kinase (AMPK).

Name	SMI-4a
Synonym	More Synonyms

Description	TCS-PIM-1-4a is a Pim inhibitor that blocks mTORC1 activity via activation of AMPK; kills a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 μM).IC50 value:Target: Pim SMI-4a a novel benzylidene-thiazolidine-2, 4-dione small molecule inhibitor of the Pim kinases, kills a wide range of both myeloid and lymphoid cell lines with precursor T-cell lymphoblastic leukemia/lymphoma (pre-T-LBL/T-ALL) being highly sensitive. Incubation of pre-T-LBL cells with SMI-4a induced G1 phase cell-cycle arrest secondary to a dose-dependent induction of p27(Kip1), apoptosis through the mitochondrial pathway, and inhibition of the mammalian target of rapamycin C1 (mTORC1) pathway based on decreases in phospho-p70 S6K and phospho-4E-BP1, 2 substrates of this enzyme. In addition, treatment of these cells with SMI-4a was found to induce phosphorylation of extracellular signal-related kinase1/2 (ERK1/2), and the combination of SMI-4a and a mitogen-activated protein kinase kinase 1/2 (MEK1/2) inhibitor was highly synergistic in killing pre-T-LBL cells. SMI-4a blocked the rapamycin-sensitive mTORC1 activity by stimulating the phosphorylation and thus activating the mTORC1 negative regulator AMP-dependent protein kinase (AMPK).
Related Catalog	Signaling Pathways >> JAK/STAT Signaling >> Pim Research Areas >> Cancer
References	[1]. Lin YW, Beharry ZM, Hill EG, et al. A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. Blood. 2010 ;115(4):824-33. [2]. Beharry Z, Mahajan S, Zemskova M,et al. The Pim protein kinases regulate energy metabolism and cell growth. Proc Natl Acad Sci U S A. 2011;108(2):528-33. [3]. Benoit SR, Ji M, Fleming R,et al . Predictors of dropouts from a San Diego diabetes program: a case control study. Prev Chronic Dis. 2004:1(4):A10. [4]. Zuping Xia, Christian Knaak, Jian Ma et al. Synthesis and Evaluation of Novel Inhibitors of Pim-1 and Pim-2 Protein Kinases. J. Med. Chem., 2009, 52 (1), pp 74-86

Description

Related Catalog

Signaling Pathways >> JAK/STAT Signaling >> Pim

Research Areas >> Cancer

References

[1]. Lin YW, Beharry ZM, Hill EG, et al. A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. Blood. 2010 ;115(4):824-33.

[2]. Beharry Z, Mahajan S, Zemskova M,et al. The Pim protein kinases regulate energy metabolism and cell growth. Proc Natl Acad Sci U S A. 2011;108(2):528-33.

[3]. Benoit SR, Ji M, Fleming R,et al . Predictors of dropouts from a San Diego diabetes program: a case control study. Prev Chronic Dis. 2004:1(4):A10.

[4]. Zuping Xia, Christian Knaak, Jian Ma et al. Synthesis and Evaluation of Novel Inhibitors of Pim-1 and Pim-2 Protein Kinases. J. Med. Chem., 2009, 52 (1), pp 74-86

Density	1.5±0.1 g/cm3
Molecular Formula	C₁₁H₆F₃NO₂S
Molecular Weight	273.231
Exact Mass	273.007141
PSA	71.47000
LogP	2.30
Index of Refraction	1.602
InChIKey	NGJLOFCOEOHFKQ-VMPITWQZSA-N
SMILES	O=C1NC(=O)C(=Cc2cccc(C(F)(F)F)c2)S1
Storage condition	2-8℃

HS Code	2934999090

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

2,4-Thiazolidinedione, 5-[[3-(trifluoromethyl)phenyl]methylene]-, (5E)-

(5E)-5-[3-(Trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione

TCS-PIM-1-4a

(5Z)-5-[3-(Trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione

2,4-Thiazolidinedione, 5-[[3-(trifluoromethyl)phenyl]methylene]-, (5Z)-

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Shanghai Nianxing Industrial Co., Ltd
China
Product Name: TCS-PIM-1-4a
Price: Check
Purity: 99.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: TCS-PIM-1-4a
Price: ￥2586.0/50mg ￥586.0/5mg ￥686.0/10mg ￥1356.0/25mg
Purity: 98.0%
Delivery: 2 Day
Contact: Liu jia
Email: 2130147988@qq.com

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: SMI-4A
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Delivery: Inquiry
Contact: Ms Wang
Email: enquiry@dycnchem.com

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Price: $79/10mM*1mLinDMSO

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TCS-PIM-1-4a

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The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.