1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. JAK3-IN-6

JAK3-IN-6 

Cat. No.: HY-101976 Purity: 98.07%
Handling Instructions

JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.

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

JAK3-IN-6 Chemical Structure

JAK3-IN-6 Chemical Structure

CAS No. : 1443235-95-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 155 In-stock
Estimated Time of Arrival: December 31
50 mg USD 465 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.

IC50 & Target

JAK3

0.15 nM (IC50)

In Vitro

JAK3-IN-6 (compound 2), a potent inhibitor of JAK3 (0.15 nM) is 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold (IL-2 vs. IL-6) or 140-fold (IL-2 vs. EPO or GMCSF) selective in cellular reporter assays and >35-fold selective in human PBMC assays (IL-7 vs. IL-6 or GMCSF). Irreversible JAK3-IN-6 with a JAK1 selective inhibitor 3 (JAK1: 0.96 nM, JAK2: 14 nM, JAK3: >1500 nM, TYK2: 10 nM) are cross titrated to determine if there is an additive or synergistic effect of co-inhibiting JAK1 and JAK3 enzymes on IL-7 signaling in CD3+, CD4+ PBMCs. As shown, the predicted levels of pSTAT5 inhibition based on addition of JAK1 and JAK3 inhibition are very close to the measured effects of cross titrating each compound, demonstrating that there is an additive effect but no synergistic effect of inhibiting JAK1 and JAK3 on blocking STAT5 phosphorylation. Furthermore inhibition of either JAK1 or JAK3 alone is sufficient to fully inhibit pSTAT5[2].

Molecular Weight

350.37

Formula

C₁₉H₁₈N₄O₃

CAS No.

1443235-95-7

SMILES

O=C(C1=CNC2=NC=NC(C3=CC=CC(NC(C(C)=C)=O)=C3)=C21)OCC

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 : 260 mg/mL (742.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8541 mL 14.2706 mL 28.5413 mL
5 mM 0.5708 mL 2.8541 mL 5.7083 mL
10 mM 0.2854 mL 1.4271 mL 2.8541 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.17 mg/mL (6.19 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (6.19 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
JAK3-IN-6
Cat. No.:
HY-101976
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