1. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  2. JAK
  3. JAK1-IN-17

JAK1-IN-17 (Compound 31) is a highly selective inhibitor of JAK1 with a Ki of 1.9 nM. JAK1-IN-17 exhibits a low whole blood shift, which allows maintaining good whole blood potency. JAK1-IN-17 is also a nitrile-containing analogue with consistent, yet weak reversible inhibition of CYP3A4 using a midazolam probe (IC50 = 7.9 μM). JAK1-IN-17 can be studied in cancer research.

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JAK1-IN-17

JAK1-IN-17 Chemical Structure

CAS No. : 1315490-71-1

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Description

JAK1-IN-17 (Compound 31) is a highly selective inhibitor of JAK1 with a Ki of 1.9 nM. JAK1-IN-17 exhibits a low whole blood shift, which allows maintaining good whole blood potency. JAK1-IN-17 is also a nitrile-containing analogue with consistent, yet weak reversible inhibition of CYP3A4 using a midazolam probe (IC50 = 7.9 μM). JAK1-IN-17 can be studied in cancer research[1].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 100 μM
Compound: 31
Inhibition of human ERG channel expressed in HEK293 cells by patch clamp assay
Inhibition of human ERG channel expressed in HEK293 cells by patch clamp assay
[PMID: 23659214]
TF-1 EC50
120 nM
Compound: 31
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins
[PMID: 23659214]
TF-1 EC50
130 nM
Compound: 31
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins in presence of whole blood
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins in presence of whole blood
[PMID: 23659214]
Molecular Weight

309.37

Formula

C17H19N5O

CAS No.
SMILES

N#C[C@H]1CC[C@H](N2C([C@H](O)C)=NC3=CN=C(NC=C4)C4=C32)CC1

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
JAK1-IN-17
Cat. No.:
HY-16641
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