1. JAK/STAT Signaling Stem Cell/Wnt Immunology/Inflammation Epigenetics Protein Tyrosine Kinase/RTK
  2. STAT Interleukin Related IFNAR JAK
  3. (R,R)-VVD-118313

(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer. (R,R)-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.

(R,R)-VVD-118313 Chemical Structure

(R,R)-VVD-118313 Chemical Structure

CAS No. : 2875046-31-2

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5 mg USD 800 In-stock
10 mg USD 1280 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

(R,R)-VVD-118313 is the isomer of VVD-118313 (HY-151385). VVD-118313 is a selective JAK1 inhibitor and blocks JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer[1]. (R,R)-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.

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.
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.

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.

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
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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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.

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Product Name:
(R,R)-VVD-118313
Cat. No.:
HY-151385A
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