Cat. No.: HY-18086

TCS PIM-1 1

(Synonyms: SC 204330)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC₅₀ of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC₅₀s >20000 nM).

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Pureté: 98.40%
CAS No.: 491871-58-0
Formule: C₁₈H₁₁BrN₂O₂
Masse moléculaire:367.20

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

TCS PIM-1 1 Chemical Structure

CAS No.: 491871-58-0

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (4)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
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Activité biologique

Description

TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC₅₀ of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC₅₀s >20000 nM)^[1].

IC₅₀ & Target^[1]

PIM1

50 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Pim :

In Vitro

TCS PIM-1 1 (compound 1), a substituted pyridone scaffold, binds convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggests that TCS PIM-1 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2. Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors. TCS PIM-1 1 serves both as a starting point for SAR chemical syntheses and was used for co-crystallization with Pim-1 protein^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 491871-58-0
Appearance Solid
Masse moléculaire 367.20
Formule C₁₈H₁₁BrN₂O₂
Color Light yellow to yellow
SMILES

OC1=C(C(N2)=CC(C3=CC=CC=C3)=C(C#N)C2=O)C=C(Br)C=C1
Synonyms

SC 204330
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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J Cent South Univ

2018, 43(5): 481-489.

TCS PIM-1 1 purchased from MedChemExpress. Usage Cited in: J Cent South Univ. 2018, 43(5): 481-489.

Effect of Pim-1 inhibitor on expression of T cell transcription factors in mice (n=5) A: Control group; B: TNBS group; C: TNBS+small doses of Pim-1 inhibitor group; D: TNBS+high doses of Pim-1 inhibitor group; E: TNBS+prednisone group.
iScience

Pim-1 kinase protects the liver from ischemia reperfusion injury by regulating dynamics-related protein 1. [Abstract]

2024 Jun 28;27(7):110280. PMID: 39055921
Neurosci Res

Pim1 kinase provides protection against high glucose-induced stress and apoptosis in cultured dorsal root ganglion neurons. [Abstract]

2021 Aug:169:9-16. PMID: 32593591
Clin Res Hepatol Gastroenterol

Pim-1 inhibitor attenuates trinitrobenzene sulphonic acid induced colitis in the mice. [Abstract]

2018 Sep;42(4):382-386. PMID: 29551611

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (272.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7233 mL

13.6166 mL

27.2331 mL

5 mM

0.5447 mL

2.7233 mL

5.4466 mL

10 mM

0.2723 mL

1.3617 mL

2.7233 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

TCS PIM-1 1 is dissolved in 0.5% DMSO^[2].

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Cheney IW, et al. Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7233 mL	13.6166 mL	27.2331 mL	68.0828 mL
	5 mM	0.5447 mL	2.7233 mL	5.4466 mL	13.6166 mL
	10 mM	0.2723 mL	1.3617 mL	2.7233 mL	6.8083 mL
	15 mM	0.1816 mL	0.9078 mL	1.8155 mL	4.5389 mL
	20 mM	0.1362 mL	0.6808 mL	1.3617 mL	3.4041 mL
	25 mM	0.1089 mL	0.5447 mL	1.0893 mL	2.7233 mL
	30 mM	0.0908 mL	0.4539 mL	0.9078 mL	2.2694 mL
	40 mM	0.0681 mL	0.3404 mL	0.6808 mL	1.7021 mL
	50 mM	0.0545 mL	0.2723 mL	0.5447 mL	1.3617 mL
	60 mM	0.0454 mL	0.2269 mL	0.4539 mL	1.1347 mL
	80 mM	0.0340 mL	0.1702 mL	0.3404 mL	0.8510 mL
	100 mM	0.0272 mL	0.1362 mL	0.2723 mL	0.6808 mL

Keywords

TCS PIM-1 1

4 Cited Publications

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TCS PIM-1 1

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

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Epigenetics Compound Library

Immunology/Inflammation Compound Library

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Kinase Inhibitor Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) TCS PIM-1 1

Voir tous les produits spécifiques à Isoform Pim

Activité biologique

Chemical Information

Publications (4)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

TCS PIM-1 1

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Publications Citing Use of MedChemExpress (MCE) TCS PIM-1 1

Voir tous les produits spécifiques à Isoform Pim

Activité biologique

Chemical Information

Publications (4)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

TCS PIM-1 1 Related Classifications

HY-18086 Related Classifications