2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Immunology/Inflammation
  3. JAK STAT IFNAR Interleukin Related
  4. VVD-118313

VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer. VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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

VVD-118313 Chemical Structure

VVD-118313 Chemical Structure

CAS No. : 2875046-27-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 756 In-stock
Solution
10 mM * 1 mL in DMSO USD 756 In-stock
Solid
5 mg USD 800 In-stock
10 mg USD 1280 In-stock
25 mg USD 2550 In-stock
50 mg USD 4050 In-stock
100 mg USD 6300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of VVD-118313:

VVD-118313 Related Antibodies

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

View All Isoforms
JAK1 JAK2 JAK3 Tyk2 JAK

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View All Isoforms
STAT3 STAT5 STAT6 STAT1

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer[1]. VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target[1]

JAK1

 

In Vitro

VVD-118313 (compound 5a; 0.01-10 μM; 3 h; primary human PBMCs) inhibits JAK1 by engagement of C817 and JAK2 by engagement of C838. VVD-118313 inhibits cysteine reactivity in a dose-dependent manner[1].
VVD-118313 (2 µM, 2h) blocks IFNα-simulated STAT1 and IL-6-stimulated STAT3 phosphorylation in WT- or C810A-JAK1-expressing 22Rv1 cells. VVD-118313 also blocks the constitutive phosphorylation of WT- and C810A-JAK1[1].
VVD-118313 (0.01-10 μM) selectively inhibits JAK1 signaling in primary human immune cells. VVD-118313 inhibits JAK1-dependent IFNα-pSTAT1, IL-6-pSTAT3, and IL-2-pSTAT5 pathways in human PBMCs in a dose-dependent manner[1].
VVD-118313 (0.1-0.4 μM; 24 h) inhibits T-cell activation induction. VVD-118313 inhibits the activation of human T cells co-stimulated with αCD3/αCD28 by a reduction in the proportion of CD25+ T cells. VVD-118313 blocks the secretion of the Th1-polarizing cytokine IFNγ and increases the production of IL-2[1].
VVD-118313 (0.1-0.5 μM; 2 h) inhibits on the production of pro-inflammatory cytokines and chemokines. VVD-118313 suppresses the induction of several pro-inflammatory chemokines, including CCL2/MCP-1, CXCL10/IP-10, and CCL4/MIP-1β[1].

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

VVD-118313 Related Antibodies

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 0.01, 0.1, and 1 μM
Incubation Time: 2 hours
Result: Showed labeling of recombinant WT-JAK1 and C810A-JAK1, but not C817A-JAK1.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 2 µM
Incubation Time: 2 hours
Result: Inhibited WT- and C810A-JAK1 phosphorylation with even greater potency than STAT1/STAT3 phosphorylation.
In Vivo

VVD-118313 (compound 5a; 25-50 mg/kg; i.h.; once) inhibits JAK1 signaling in TYK2 knockout mice[1].

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

Animal Model: TYK2 knockout mice[1]
Dosage: 25 and 50 mg/kg
Administration: Subcutaneous injection; once
Result: Revealed 75% engagement of JAK1_C816 at 25 and 50 mg/kg, while other JAK1 cysteines were unaffected in reactivity.
Molecular Weight

429.36

Formula

C19H22Cl2N2O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC[C@H](C1)C2=CC(Cl)=C(C=C2)Cl)C#C[C@]3(CCN(S(=O)(C)=O)C3)[H]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (232.90 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 2.3290 mL 11.6452 mL 23.2905 mL
5 mM 0.4658 mL 2.3290 mL 4.6581 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

V1

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C2

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Volume (final)

V2

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: ≥ 2.5 mg/mL (5.82 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.

    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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.82 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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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
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3290 mL 11.6452 mL 23.2905 mL 58.2262 mL
5 mM 0.4658 mL 2.3290 mL 4.6581 mL 11.6452 mL
10 mM 0.2329 mL 1.1645 mL 2.3290 mL 5.8226 mL
15 mM 0.1553 mL 0.7763 mL 1.5527 mL 3.8817 mL
20 mM 0.1165 mL 0.5823 mL 1.1645 mL 2.9113 mL
25 mM 0.0932 mL 0.4658 mL 0.9316 mL 2.3290 mL
30 mM 0.0776 mL 0.3882 mL 0.7763 mL 1.9409 mL
40 mM 0.0582 mL 0.2911 mL 0.5823 mL 1.4557 mL
50 mM 0.0466 mL 0.2329 mL 0.4658 mL 1.1645 mL
60 mM 0.0388 mL 0.1941 mL 0.3882 mL 0.9704 mL
80 mM 0.0291 mL 0.1456 mL 0.2911 mL 0.7278 mL
100 mM 0.0233 mL 0.1165 mL 0.2329 mL 0.5823 mL
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VVD-118313 Related Classifications

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:

VVD-1183132875046-27-6VVD118313VVD 118313JAKSTATIFNARInterleukin RelatedJanus kinaseInterferon-α/β receptorInterferon-alpha/beta receptor ILC817C838isoform-restricted allosteric cysteinetrans-phosphorylationcytokine signaling22Rv1 cellsInhibitorinhibitorinhibit

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