CAS 327033-36-3|TCS-PIM-1-4a

Introduction：Basic information about CAS 327033-36-3|TCS-PIM-1-4a, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. TCS-PIM-1-4a BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Synonyms

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

Names

Name	SMI-4a
Synonym	More Synonyms

TCS-PIM-1-4a BiologicalActivity

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 >>PimResearch 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

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 >>PimResearch 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

Chemical & Physical Properties

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℃

Safety Information

HS Code	2934999090

Customs

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

Synonyms

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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