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 (Compound 9) is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 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

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10 mM * 1 mL in DMSO USD 469 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
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10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
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100 mg USD 2520 In-stock
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Description

JAK3-IN-1 (Compound 9) is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM)[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)

In Vitro

JAK3-IN-1(Compound 9; 0-5 µM; 3 hours; BMDMs cells) treatment 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[1].
. JAK3-IN-1(Compound 9) most potently inhibits JAK3 and identified fms-related tyrosine kinase 3 (FLT3) and several tyrosine protein kinase (TEC)-family kinases as being potential off-targets. Enzymatic assays using the Z’-lyte or LanthaScreen formats confirmed enzymatic inhibition of FLT3 (IC50 = 13 nM), TTK protein kinase (TTK, IC50 = 49 nM), BLK proto-oncogene (BLK, IC50 = 157 nM) and tyrosine protein kinase TXK (TXK, IC50 = 36 nM). JAK3-IN-1 shows very low inhibition scores for other JAKs and wild-type (WT) EGFR, which is consistent with the over 180-fold higher IC50s against EGFRWT and TYK2 (IC50s =409 nM, > 10000 respectively). JAK3-IN-1 possesses over 165-fold higher IC50s for BTK or ITK (IC50s = 794 and 1070 nM respectively)[1].
JAK3-IN-1(Compound 9) selectively inhibits the proliferation of JAK3-dependent Ba/F3 cells (IC50 = 69 nM) relative to other JAK-dependent Ba/F3 cells, for which there was no antiproliferative effect at concentrations below 3.0 μM[1].

Western Blot Analysis[1]

Cell Line: BMDMs cells
Concentration: 0 µM, 0.1 µM, 0.5 µM, 1 µM, 5 µM
Incubation Time: 3 hours
Result: Completely inhibited IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibited IFNβ-induced p-STAT1 at a concentration of 5.0 μM.
In Vivo

JAK3-IN-1(Compound 9) shows reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng*hr/mL following a 10 mg/Kg oral dose and good oral bioavailability of 66%. After oral administration with JAK3-IN-1(Compound 9) (75 mpk, QD) for 8 days, the numbers of B or T lymphocytes in the tumor-bearing lungs and spleens of treated mice is not affected, however, the number of NK cells is reduced[1].

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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Keywords:

JAK3-IN-1JAKJanus kinaseFLT3BLKTTKantiproliferativeIL-4p-STAT6orallyCys909Inhibitorinhibitorinhibit

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