JAK-IN-1

Name: JAK-IN-1
Brand: MedChemExpress
SKU: HY-13827
Rating: 4.5 (1 reviews)

Cat. No.: HY-13827 Purity: 99.44%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

JAK-IN-1 is a JAK1/2/3 inhibitor with IC₅₀s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.

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

JAK-IN-1 Chemical Structure

CAS No. : 1334673-53-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 795	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 795	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2400	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3850	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 6200	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE JAK-IN-1

•Patent. US20190248778A1.

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View All Isoforms

JAK1 JAK2 JAK3 Tyk2 JAK

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

JAK-IN-1 is a JAK1/2/3 inhibitor with IC₅₀s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.

IC₅₀ & Target

IC50: 0.26 nM (JAK1), 0.8 nM (JAK2), 3.2 nM (JAK3)^[1]

In Vitro

JAK-IN-1 inhibits the proliferation of human CD4 and CD8 T cells in a dose-dependent manner upon stimulation by anti-CD3/anti-CD28 antibody-coated beads partially mimicking the activation signals brought to a Tcell by an antigen-presenting cell. JAK-IN-1 is active in both mechanistic and functional cell-based assays using T-cells, one of the major cell types in which JAK3 is potentially relevant^[1].

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

In Vivo

JAK-IN-1 is JAK3 selective in vivo, as judged by higher potency inhibiting JAK1/JAK3- vs JAK2- or JAK1/JAK2/TYK2-driven signaling in whole blood assays. JAK-IN-1 potently inhibits IL-2 stimulated plasma concentrations of JAK-IN-1 for each dose. JAK-IN-1 prevents IL-2-driven STAT5 phosphorylation in a dose- and concentration-dependent manner, with approximately 50% inhibition observed at the 10 mg/kg dose (plasma concentration ∼480 nM)^[1].

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

Molecular Weight

380.44

Formula

C₂₀H₂₄N₆O₂

CAS No.

1334673-53-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CNC2=NC=C(C3CC3)N=C21)N[C@@H](C(N4CC(C#N)C4)=O)C(C)(C)C

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 : 66.67 mg/mL (175.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6285 mL	13.1427 mL	26.2854 mL
5 mM	0.5257 mL	2.6285 mL	5.2571 mL
10 mM	0.2629 mL	1.3143 mL	2.6285 mL

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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: ≥ 1.43 mg/mL (3.76 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.43 mg/mL (3.76 mM); Clear solution

This protocol yields a clear solution of ≥ 1.43 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 (14.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.44%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (250 KB) HNMR (541 KB) RP-HPLC (263 KB)

Handling Instructions (2659 KB)

References

[1]. Soth M, et al. 3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models. J Med Chem. 2013 Jan 10;56(1):345-56. [Content Brief]

Cell Assay ^[1]	Carboxyfluorescein succinimidyl ester (CFSE)-labeled human PBMCs were exposed to JAK-IN-1 prior to stimulation with anti-CD3/anti-CD28 antibodies. Cell proliferation was then measured by CFSE dilutions as detected by flow cytometry in CD4 positive and CD8 positive T cells after staining with fluorochrome-conjugated antibodies^[1] MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Adult (10−12 weeks old) C57BL/6 mice are treated with JAK-IN-1 (0.3, 1, 3, 10, 30, and 100 mg/kg). Mice received a single oral suspension dose of JAK-IN-1 or vehicle alone. Two hours after treatment by oral gavage, mice were euthanized for collecting whole blood in heparinized tubes^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Soth M, et al. 3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models. J Med Chem. 2013 Jan 10;56(1):345-56. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6285 mL	13.1427 mL	26.2854 mL	65.7134 mL
	5 mM	0.5257 mL	2.6285 mL	5.2571 mL	13.1427 mL
	10 mM	0.2629 mL	1.3143 mL	2.6285 mL	6.5713 mL
	15 mM	0.1752 mL	0.8762 mL	1.7524 mL	4.3809 mL
	20 mM	0.1314 mL	0.6571 mL	1.3143 mL	3.2857 mL
	25 mM	0.1051 mL	0.5257 mL	1.0514 mL	2.6285 mL
	30 mM	0.0876 mL	0.4381 mL	0.8762 mL	2.1904 mL
	40 mM	0.0657 mL	0.3286 mL	0.6571 mL	1.6428 mL
	50 mM	0.0526 mL	0.2629 mL	0.5257 mL	1.3143 mL
	60 mM	0.0438 mL	0.2190 mL	0.4381 mL	1.0952 mL
	80 mM	0.0329 mL	0.1643 mL	0.3286 mL	0.8214 mL
	100 mM	0.0263 mL	0.1314 mL	0.2629 mL	0.6571 mL

JAK-IN-1 Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JAK-IN-11334673-53-8JAKJanus kinaseInhibitorinhibitorinhibit

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JAK-IN-1

Customer Review

JAK-IN-1 Related Antibodies

1 Publications Citing Use of MCE JAK-IN-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

JAK-IN-1 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

JAK-IN-1 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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