(R,R)-VVD-118313
Based on 1 Customer Validation
(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.
- Purity: 99.34%
- CAS No.: 2875046-31-2
- Formula: C19H22Cl2N2O3S
- Molecular Weight:429.36
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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JAK1 |
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.
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Cell Line:22Rv1 cells
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Concentration:0.01, 0.1, and 1 μM
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Incubation Time:2 hours
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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.
Chemical Information
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CAS No. 2875046-31-2
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Appearance Solid
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Molecular Weight 429.36
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Formula C19H22Cl2N2O3S
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Color White to off-white
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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]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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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)
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Handling Instructions (2659 KB)
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 |