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

JAK3-IN-1 

Cat. No.: HY-19544 Purity: 99.98%
Handling Instructions

JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM).

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

JAK3-IN-1 Chemical Structure

JAK3-IN-1 Chemical Structure

CAS No. : 1805787-93-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 469 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM). IC50 value: 4.8 nM [1] Target: JAK3 in vitro: JAK3-IN-1 provides a set of useful tools to pharmacologically interrogate JAK3-dependent biology. JAK3-IN-1 completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM. In a similar way, JAK3-IN-1 exhibits consistent potency and selectivity for JAK3 in leukemia cancer cell lines: TALL-1 and OCL-AML5. [1] in vivo: JAK3-IN-1 demonstrates reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng·h/mL following a 10 mg/kg oral dose and good oral bioavailability of 66%. [1]

IC50 & Target[1]

JAK3

4.8 nM (IC50)

JAK1

896 nM (IC50)

JAK2

1050 nM (IC50)

TTK

49 nM (IC50)

BTK

794 nM (IC50)

ITK

1070 nM (IC50)

Molecular Weight

508.02

Formula

C₂₆H₃₀ClN₇O₂

CAS No.

1805787-93-2

SMILES

O=C(C=C)NC1=CC(CNC2=NC(NC3=C(OC)C=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=CC=C1

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 : ≥ 47 mg/mL (92.52 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9684 mL 9.8421 mL 19.6843 mL
5 mM 0.3937 mL 1.9684 mL 3.9369 mL
10 mM 0.1968 mL 0.9842 mL 1.9684 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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JAK3-IN-1
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HY-19544
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