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Key Documents

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Safety Information

SML1979

Sigma-Aldrich

FM-381

≥98% (HPLC)

Synonym(s):

(E)-2-Cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide, 2-Cyano-3-(5-(1-cyclohexyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2-yl)furan-2-yl)-N,N-dimethylacrylamide

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20 EA
CN¥3,228.10

CN¥3,228.10

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20 EA
CN¥3,228.10

About This Item

Empirical Formula (Hill Notation):
C24H24N6O2
CAS Number:
2226521-65-7
Molecular Weight:
428.49
UNSPSC Code:
12352202
NACRES:
NA.77

CN¥3,228.10

Please contact Customer Service for Availability
Request a Bulk Order

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

2-8°C

SMILES string

CN(C(/C(C#N)=C/C(O1)=CC=C1C2=NC3=CN=C(NC=C4)C4=C3N2C5CCCCC5)=O)C

InChI key

GJMZWYLOARVASY-NTCAYCPXSA-N

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This Item
SAB5200764SAB5200775SAB5200772
Anti-Stargazin Antibody Chemicon®, from rabbit

AB9876

Anti-Stargazin Antibody

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Atto 488 antibody produced in mouse clone S245-36, purified immunoglobulin

SAB5200764

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Atto 488 antibody produced in mouse

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Hrp antibody produced in mouse clone S245-36, purified immunoglobulin

SAB5200775

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Hrp antibody produced in mouse

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Apc antibody produced in mouse clone S245-36, purified immunoglobulin

SAB5200772

Monoclonal Anti-Tarp Gamma2/4/8 (Stargazin) - Apc antibody produced in mouse

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

antibody form

affinity isolated antibody

antibody form

purified immunoglobulin

antibody form

purified immunoglobulin

antibody form

purified immunoglobulin

species reactivity

rat, mouse

species reactivity

rat, mouse

species reactivity

rat, mouse

species reactivity

mouse, rat

clone

polyclonal

clone

S245-36, monoclonal

clone

S245-36, monoclonal

clone

S245-36, monoclonal

shipped in

dry ice

shipped in

wet ice

shipped in

wet ice

shipped in

wet ice

Biochem/physiol Actions

FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor (IC50 = 127 pM/JAK3, 52 nM/JAK1, 346 nM/JAK2, 459 nM/TYK2 by radiometric assay; [ATP] = 10 μM) that targets JAK3 gatekeeper (GK) Cys909 for a reversible covalent interaction, exhibiting much reduced or little potency against a panel of 409 other kinases. FM-381 is >3-fold more potent than the JAK1/3 inhibitor Tofacitinib (IC50 = 292 pM/JAK3, 496 pM/JAK1, 2.2 nM/JAK2, 8.9 nM/TYK2 by radiometric assay; [ATP] = 10 μM) in blocking JAK1/JAK3-mediated STAT5 phosphorylation in human CD4+ T-cells upon IL-2 stimulation (ECmax ∼100 nM with FM-381), while being ineffective (up to 1 μM) against JAK3-independent STAT1/3 phosphorylation following IL-6 or TNFα stimulation. For characterization details of FM-381, please visit the FM-381 probe summary on the Structural Genomics Consortium (SGC) website.

FM-479 is the negative control for the active probe, FM-381. FM-479 is available from Sigma. To learn more about and purchase FM-479, click here.

To learn about other SGC chemical probes, visit sigma.com/sgc
Highly potent and selective janus kinase JAK3 inhibitor that blocks JAK1/JAK3-mediated STAT5 phosphorylation in human CD4+ T-cells.

Features and Benefits

FM-381 is a chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

新产品

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Certificates of Analysis (COA)

Lot/Batch Number
0000033000
0000032999
0000028522

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Michael Forster et al.
Cell chemical biology, 23(11), 1335-1340 (2016-11-15)
Janus kinases (JAKs) are a family of cytoplasmatic tyrosine kinases that are attractive targets for the development of anti-inflammatory drugs given their roles in cytokine signaling. One question regarding JAKs and their inhibitors that remains under intensive debate is whether

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