1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. FM381

FM381 

Cat. No.: HY-102046 Purity: 98.41%
Handling Instructions

FM381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper position +7 in JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.

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

FM381 Chemical Structure

FM381 Chemical Structure

CAS No. : 2226521-65-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
2 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 210 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
25 mg USD 700 In-stock
Estimated Time of Arrival: December 31
50 mg USD 990 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

FM381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909 at the gatekeeper position +7 in JAK3. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.

IC50 & Target[1]

JAK3

127 pM (IC50)

In Vitro

FM381 is screened against a panel of 410 kinases at concentrations of 100 nM and 500 nM. FM381 has no relevant effect on the activity of any tested kinases except JAK3 at a concentration of 100 nM. At 500 nM, FM381 moderately inhibits 11 other kinases besides JAK3 with residual activities below 50%. FM-381 is found to be inactive in a selectivity panel of frequently hit BRDs (BRD4, BRPF, CECR, FALZ, TAF1, BRD9). Strongest hits is 500 nM for [email protected] FM381 selectively Inhibit JAK3 Signaling in Human CD4+ T Cells. FM-381 shows an apparent EC50 of 100 nM in a dose dependent BRET assay and blocks IL2 stimulated (JAK3/JAK1 dependent) STAT5 phosphorylation at 100 nM, but not JAK3 independent IL6 (JAK1/2/TYK dependent) stimulated STAT3 signalling in Human CD4+ T cells up to 1 µM[1].

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 : 12.8 mg/mL (29.87 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3338 mL 11.6689 mL 23.3378 mL
5 mM 0.4668 mL 2.3338 mL 4.6676 mL
10 mM 0.2334 mL 1.1669 mL 2.3338 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

CD4+ T Cell cytokine stimulation assay is performed. T cells are purified from peripheral blood mononuclear cells from human donors. Equal numbers of cells are incubated for 1 hr with JAK inhibitors (FM381) (0, 10, 50, 100, 300 nM) or DMSO control and stimulated with cytokines for 30 min. The cells are lysed, and the proteins are separated via PAGE and transferred to a polyvinylidene fluoride membrane. The proteins of interest are blotted with specific antibodies and visualized with an infrared imaging system[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

428.49

Formula

C₂₄H₂₄N₆O₂

CAS No.

2226521-65-7

SMILES

CN(C(/C(C#N)=C/C1=CC=C(C2=NC3=CN=C(NC=C4)C4=C3N2C5CCCCC5)O1)=O)C

Shipping

Room temperature in continental US; may vary elsewhere

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FM381
Cat. No.:
HY-102046
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FM381

Cat. No.: HY-102046