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TCS-PIM-1-4a

Pim inhibitor CAS# 327033-36-3

TCS-PIM-1-4a

Catalog No. BCC5461----Order now to get a substantial discount!

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TCS-PIM-1-4a: 5mg $69 In Stock
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Chemical structure

TCS-PIM-1-4a

3D structure

Chemical Properties of TCS-PIM-1-4a

Cas No. 327033-36-3 SDF Download SDF
PubChem ID 1361332 Appearance Powder
Formula C11H6F3NO2S M.Wt 273.23
Type of Compound N/A Storage Desiccate at -20°C
Synonyms SMI-4a
Solubility DMSO : ≥ 100 mg/mL (365.99 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (5E)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione
SMILES C1=CC(=CC(=C1)C(F)(F)F)C=C2C(=O)NC(=O)S2
Standard InChIKey NGJLOFCOEOHFKQ-VMPITWQZSA-N
Standard InChI InChI=1S/C11H6F3NO2S/c12-11(13,14)7-3-1-2-6(4-7)5-8-9(16)15-10(17)18-8/h1-5H,(H,15,16,17)/b8-5+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of TCS-PIM-1-4a

DescriptionTCS-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).

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

TCS-PIM-1-4a Dilution Calculator

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Preparing Stock Solutions of TCS-PIM-1-4a

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.6599 mL 18.2996 mL 36.5992 mL 73.1984 mL 91.498 mL
5 mM 0.732 mL 3.6599 mL 7.3198 mL 14.6397 mL 18.2996 mL
10 mM 0.366 mL 1.83 mL 3.6599 mL 7.3198 mL 9.1498 mL
50 mM 0.0732 mL 0.366 mL 0.732 mL 1.464 mL 1.83 mL
100 mM 0.0366 mL 0.183 mL 0.366 mL 0.732 mL 0.915 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on 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).

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Description

TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM).

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