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You are here:Home-Inhibitors & Agonists-JAK/STAT Signaling-JAK

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Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. Since members of the type I and type II cytokine receptor families possess no catalytic kinase activity, they rely on the JAK family of tyrosine kinases to phosphorylate and activate downstream proteins involved in their signal transduction pathways. The receptors exist as paired polypeptides, thus exhibiting two intracellular signal-transducing domains. JAKs associate with a proline-rich region in each intracellular domain, which is adjacent to the cell membrane and called a box1/box2 region. After the receptor associates with its respective cytokine/ligand, it goes through a conformational change, bringing the two JAKs close enough to phosphorylate each other. The JAK autophosphorylation induces a conformational change within itself, enabling it to transduce the intracellular signal by further phosphorylating and activating transcription factors called STATs. The activated STATs dissociate from the receptor and form dimers before translocating to the cell nucleus, where they regulate transcription of selected genes.

Cat. No. Product Name CAS No. Information
GY02911

CHZ-868

1895895-38-1

A potent type II JAK2 inhibitor; inhibits the proliferation of SET2 JAK2 V617F cells (GI50=59 nM); reverses type I JAK inhibitor persistence and demonstrates efficacy in myeloproliferative neoplasms; reduces mutant allele burden in vivo, shows significant efficacy in Jak2V617F-driven polycythemia vera; orally active.

GY02854

JAK3-IN-1

1805787-93-2

JAK3-IN-1 is a potent and selective JAK3 inhibitor with IC50 of 4.8 nM; displays >150 fold selectivity versus JAK1 and JAK2; exhibits decent pharmacokinetic properties and is suitable for use in vivo.

GY02601

SAR-20347

1450881-55-6

SAR-20347 (SAR20347) is a potent, selective inhibitor of JAK1 and Tyk2 with IC50 of 59 and 13 nM in TR-FRET assays, shows selectivity against JAK2 and JAK3 (IC50>800 nM); potently inhibits IL-12-mediated STAT4 phosphorylation with IC50 of 126 nM, inhibits JAK1-mediated IL-6 pSTAT3 signaling with IC50 of 345 nM in TF-1 and 407 nM in CD4+ cells, poorly inhibits JAK2 mediated STAT5 phosphorylation with IC50 of >1 uM; ameliorates imiquimod-induced psoriasis-like dermatitis in vivo.

GY02421

NS-018 maleate

1354799-87-3

NS-018 maleate (NS018, Ilginatinib) is a potent and highly selective JAK2 inhibitor (IC50=0.72 nM); displays 30-50-fold greater selectivity for JAK2 over JAK1, JAK3 and Tyk2; also inhibits Src family kinases(Src, Fyn); shows effective in mouse Ba/F3-JAK2V617F disease model.

GY06983

PF-956980

1262832-74-5

PF-956980 is a potent, highly specific JAK3 inhibitor with IC50 of 4 nM; shows only modest inhibition of PKA (6.7 uM) and LCK (10.9 uM) in vitro; selectively downregulates JAK2 and JAK3 mRNA, corresponding to changes observed at the protein level; shows in vivo activity consistent with in vitro enzyme and whole blood assays (39 ng/ml); dose-dependently inhibits the DTH response in mice with EC50 of 5 mg/kg.

GY10246

iJak-381

1831144-46-7

iJak-381 (iJak381) is a potent, selective inhalable and lung-restricted inhibitor of JAK1 with IC50 of 8.52 nM, displays 6.3/704/28 fold selectivity over JAK2/JAK3/TYK2; suppresses STAT 6 activation by IL-1, suppresses ovalbumin-induced lung inflammation in both murine and guinea pig asthma models and improved allergen-induced airway hyperresponsiveness in mice; In a model driven by human allergens, iJak-381 had a more potent suppressive effect on neutrophil-driven inflammation compared to systemic corticosteroid administration, reduces lung pathology without affecting systemic Jak1 activity in rodents.

GY10258

SAR-20347

1450881-55-6

SAR-20347 (SAR20347) is a potent, selective inhibitor of JAK1 and Tyk2 with IC50 of 59 and 13 nM in TR-FRET assays, shows selectivity against JAK2 and JAK3 (IC50>800 nM); potently inhibits IL-12-mediated STAT4 phosphorylation with IC50 of 126 nM, inhibits JAK1-mediated IL-6 pSTAT3 signaling with IC50 of 345 nM in TF-1 and 407 nM in CD4+ cells, poorly inhibits JAK2 mediated STAT5 phosphorylation with IC50 of >1 uM; ameliorates imiquimod-induced psoriasis-like dermatitis in vivo.

GY10485

ZT55

2138488-38-5

ZT55 (JAK inhibitor ZT55) is a novel potent, highly-selective tyrosine kinase JAK2 inhibitor with IC50 of 31 nM; displays no significant activity against JAK1/3 (IC50>10 uM); exhibits potent effects on the cellular JAK-STAT pathway, inhibiting tyrosine phosphorylation in JAK2V617F and downstream STAT3/5 transcription factors; inhibits the proliferation of the JAK2V617F-expressing HEL cell line, leading to cell cycle arrest at the G2/M phase and induction of caspase-dependent apoptosis; significantly suppressed the growth of HEL xenograft tumors in vivo, blocks erythroid colony formation of peripheral blood hematopoietic progenitors from patients carrying the JAK2V617F mutation.

GY06863

JAK2 inhibitor G5-7

939681-36-4

JAK2 inhibitor G5-7 is a small molecule, allosteric JAK2 inhibitor that selectively inhibits JAK2-mediated phosphorylation and activation of EGFR and STAT3 by binding to JAK2; demonstrates inhibitor of U87MG/EGFR and U87MG/EGFRvIII with IC50 of 0.75 and 1.0 uM, arrests cell cycle at G2 phase in both U87MG/EGFRvIII and U87MG/EGFRvIII/PTEN cells; significantly inhibits EGFR Tyr1068 phosphorylation but has no effect on EGFR Tyr1045 phosphorylation; decreases GBM tumor volume and extends the life span of tumor-bearing nude mice after oral administration.

GY02113

CYT387 Mesylate

1056636-07-7

A potent and selective JAK1/JAK2 inhibitor with IC50 of 11/18 nM; shows significantly less activity against other kinases, including JAK3 (IC50=155 nM); inhibits JAK2V617F (JH1-JH2) withIC50 of 11 nM; inhibits growth of Ba/F3-JAK2V617F and HEL cells (IC50=1500 nM) or Ba/F3-MPLW515L cells (IC50=200 nM).

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