1. Signaling Pathways
  2. Epigenetics
    JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Stem Cell/Wnt
  3. JAK

JAK

Janus kinase

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 Effect Purity Chemical Structure
  • HY-16379S
    Pacritinib-d4
    Inhibitor 98.42%
    Pacritinib-d8 (SB1518-d8) is the deuterium labeled Pacritinib (HY-16379). Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).
    Pacritinib-d<sub>4</sub>
  • HY-174905
    Quecitinib
    Inhibitor
    Quecitinib (QY201) is an orally active JAK1/TYK2 dual inhibitor. Quecitinib is also a substrate of cytochrome P450 3A and is mainly metabolized to mono-oxide and glucuronidation products. Quecitinib has favorable pharmacokinetic properties as well as safety. Quecitinib can be used in the research of atopic dermatitis and other autoimmune diseases.
    Quecitinib
  • HY-111471
    JAK-IN-5
    Inhibitor
    JAK-IN-5 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
    JAK-IN-5
  • HY-18301
    JAK-IN-35
    Inhibitor 99.30%
    JAK-IN-35 (compound TG46) is a JAK2 inhibitor that canb be used in cancer research.
    JAK-IN-35
  • HY-174280
    Modzatinib
    Inhibitor
    Modzatinib (ITK kinase-IN-1) (compound I) is an inhibitor targeting ITK kinase (IC50=8 nM, Jurkat cells) and can be used to study inflammatory diseases. Modzatinib has an IC50 of 23 nM for JAK3 in hPBMC cells (based on IL-2/pSTAT5 levels), wihout inhibitory effect against JAK2.
    Modzatinib
  • HY-18710
    BMS-066
    Inhibitor 99.09%
    BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.
    BMS-066
  • HY-153701
    JAK-IN-26
    Inhibitor 98.00%
    JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=17.2 nM).
    JAK-IN-26
  • HY-146066A
    (R)-α7 nAchR-JAK2-STAT3 agonist 1
    Agonist 99.59%
    (R)-α7 nAchR-JAK2-STAT3 agonist 1 is the R-enantiomer of α7 nAchR-JAK2-STAT3 agonist 1 (HY-146066). α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis.
    (R)-α7 nAchR-JAK2-STAT3 agonist 1
  • HY-161618
    MJ04
    Inhibitor 98.08%
    MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg).
    MJ04
  • HY-N6651
    Isocryptotanshinone
    Inhibitor ≥98.0%
    Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation[1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways[1][3][4]. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC[1][3][4].
    Isocryptotanshinone
  • HY-178500
    WCY-8-67
    Inhibitor
    WCY-8-67 is an orally active and selective USP5 inhibitor, with an IC50 value of 1.33 μM. WCY-8-67 induces apoptosis and suppresses JAK/STAT3 and PI3K/AKT signaling pathways in vitro. WCY-8-67 inhibits proliferation of AE-positive AML cells, induces G1 phase arrest and differentiation of AML cells. WCY-8-67 demonstrates potent anti-leukemic efficacy in mice. WCY-8-67 can be used for the study of acute myeloid leukemia.
    WCY-8-67
  • HY-161684
    JAK2-IN-10
    Inhibitor
    JAK2-IN-10 (compound 5) is a potent JAK2 V617F inhibitor with an IC50 value of ≤10 nM.
    JAK2-IN-10
  • HY-148060
    JAK-IN-21
    Inhibitor 99.72%
    JAK-IN-21 (Example 4) is a selective and potent JAK inhibitor with IC50s of 1.73, 2.04, 109 and 62.9 nM against JAK1, JAK2, J2V617F and TYK2, respectively.
    JAK-IN-21
  • HY-147330
    SJ1008030
    Inhibitor
    SJ1008030 (compound 8) is a JAK2 PROTAC which selectively degrades JAK2. SJ1008030 inhibits MHH–CALL-4 cell growth with an IC50 of 5.4 nM. SJ1008030 can be used for the research of leukemia.
    SJ1008030
  • HY-131014
    FM-479
    99.2%
    FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases. FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
    FM-479
  • HY-15315S
    Baricitinib-d5
    Inhibitor 98.98%
    Baricitinib-d5 is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
    Baricitinib-d<sub>5</sub>
  • HY-152080
    Blovacitinib
    Inhibitor 99.71%
    Blovacitinib (TUL01101) is a potent, selective and orally active JAK1 inhibitor, with an IC50s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Blovacitinib can be used for the research of rheumatoid arthritis.
    Blovacitinib
  • HY-144031S
    Tyk2-IN-8
    Inhibitor 98.04%
    Tyk2-IN-8 (compound 3) is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. Tyk2-IN-8 inhibits JAK1-JH1 with IC50 of 3.0 nM. Tyk2-IN-8 can be used for the research of autoimmune disease.
    Tyk2-IN-8
  • HY-170360
    UCB9386
    Inhibitor 99.89%
    UCB9386 is the selective and brain penetrant inhibitor for Nuak1 with a pIC50 of 10.1. UCB9386 inhibits Nuak2 and Kak2 with an inhibition rate of ca. 50% at 10 nM.
    UCB9386
  • HY-18300S
    Filgotinib-d4
    Inhibitor
    Filgotinib-d4 is the deuterium labeled Filgotinib. Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
    Filgotinib-d<sub>4</sub>
Cat. No. Product Name / Synonyms Species Source
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