Cat. No.: HY-108264

TCS 21311

(Synonyms: NIBR3049)

Customer Review

Based on 1 Customer Validation

TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC₅₀ of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC₅₀s of 13, 68, and 3 nM, respectively.

For research use only. We do not sell to patients.

Purity: 99.49%
CAS No.: 1260181-14-3
Formula: C₂₇H₂₅F₃N₄O₄
Molecular Weight:526.51

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TCS 21311 Chemical Structure

CAS No.: 1260181-14-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

JAK3

8 nM (IC₅₀)

JAK2

2.55 μM (IC₅₀)

JAK1

1.017 μM (IC₅₀)

PKCα

13 nM (IC₅₀)

PKCθ

68 nM (IC₅₀)

GSK-3β

3 nM (IC₅₀)

All JAK Isoforms :

All PKC Isoforms :

All GSK-3 Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CTLL	IC₅₀	1294 nM Compound: 1	Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay	[PMID: 21155605]
Jurkat	IC₅₀	689 nM Compound: 1	Inhibition of antiTCR/antiCD28-stimulated IL2 production in human Jurkat cells by measuring bioluminescence Inhibition of antiTCR/antiCD28-stimulated IL2 production in human Jurkat cells by measuring bioluminescence	[PMID: 21155605]

In Vitro

TCS 21311 (NIBR3049) exhibits IC₅₀ values of 1.017, 2.550 and 8.055 μM for JAK1, JAK2 and TYK2, respectively in a enzymatic Jak assay^[1].
TCS 21311 (NIBR3049) shows moderate activity in this cellular assay (IC₅₀=689 nM, Jurkat cells), which is in good agreement with its enzymatic Pkc activity^[1].

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

Chemical Information

CAS No. 1260181-14-3
Appearance Solid
Molecular Weight 526.51
Formula C₂₇H₂₅F₃N₄O₄
Color White to yellow
SMILES

O=C(C(C1=CC(N2CCN(C(C(C)(O)C)=O)CC2)=CC=C1C(F)(F)F)=C3C4=CNC5=C4C=CC=C5)NC3=O
Synonyms

NIBR3049
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (189.93 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

1.8993 mL

9.4965 mL

18.9930 mL

5 mM

0.3799 mL

1.8993 mL

3.7986 mL

10 mM

0.1899 mL

0.9496 mL

1.8993 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

References

[1]. Thoma G, et al. Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.J Med Chem. 2011 Jan 13;54(1):284-8. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8993 mL	9.4965 mL	18.9930 mL	47.4825 mL
	5 mM	0.3799 mL	1.8993 mL	3.7986 mL	9.4965 mL
	10 mM	0.1899 mL	0.9496 mL	1.8993 mL	4.7482 mL
	15 mM	0.1266 mL	0.6331 mL	1.2662 mL	3.1655 mL
	20 mM	0.0950 mL	0.4748 mL	0.9496 mL	2.3741 mL
	25 mM	0.0760 mL	0.3799 mL	0.7597 mL	1.8993 mL
	30 mM	0.0633 mL	0.3165 mL	0.6331 mL	1.5827 mL
	40 mM	0.0475 mL	0.2374 mL	0.4748 mL	1.1871 mL
	50 mM	0.0380 mL	0.1899 mL	0.3799 mL	0.9496 mL
	60 mM	0.0317 mL	0.1583 mL	0.3165 mL	0.7914 mL
	80 mM	0.0237 mL	0.1187 mL	0.2374 mL	0.5935 mL
	100 mM	0.0190 mL	0.0950 mL	0.1899 mL	0.4748 mL

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TCS 21311

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

All JAK Isoforms

All PKC Isoforms

All GSK-3 Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

TCS 21311 Related Classifications

HY-108264 Related Classifications