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Results for "

JAK-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	JAK (41) Apoptosis (14) Aurora Kinase (1) Autophagy (11) Bacterial (2) Cathepsin (1) EGFR (1) FGFR (1) FLT3 (2) Fungal (2) HDAC (1) IFNAR (1) Influenza Virus (2) Interleukin Related (2) Isotope-Labeled Compounds (3) Itk (1) Mitophagy (4) NF-κB (1) p38 MAPK (1) Reference Standards (2) STAT (5) STING (1) Syk (1) VEGFR (1)
By Research Areas:	Cancer (27) Infection (2) Inflammation/Immunology (18)

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Targets Recommended: JAK Dan family AIM2 NEKs CD44

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13827

*JAK-IN-1* 1 Publications Verification	JAK	Inflammation/Immunology
JAK-IN-1 is a *JAK1/2/3* inhibitor with IC₅₀s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.

HY-50856

Ruxolitinib Maximum Cited Publications 187 Publications Verification INCB18424	JAK Autophagy Mitophagy Apoptosis	Cancer
Ruxolitinib (INCB18424) is an orally active and selective *JAK1/2* inhibitor with IC₅₀s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .

HY-148785

Nimucitinib	JAK	Others
Nimucitinib is a Janus kinase (JAK) inhibitor .

HY-50856R

Ruxolitinib (Standard) INCB18424 (Standard)	Reference Standards JAK Autophagy Mitophagy Apoptosis	Cancer
Ruxolitinib (Standard) is the analytical standard of Ruxolitinib. This product is intended for research and analytical applications. Ruxolitinib (INCB18424) is a potent and selective *JAK1/2* inhibitor with IC₅₀s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .

HY-145029

SYK/JAK-IN-1	Syk JAK	Inflammation/Immunology Cancer
SYK/JAK-IN-1 is dual SYK/JAK inhibitor with IC₅₀s of <5 nM for SYK and JAK2, respectively ^[1].

HY-170772

Dual Cathepsin L/JAK-IN-1	p38 MAPK STAT Interleukin Related Cathepsin JAK	Inflammation/Immunology
Dual Cathepsin L/JAK-IN-1 (Compound A8) is a dual inhibitor of Cathepsin L (CTSL) and JAK, with IC₅₀ values of 0.68 μM, 337.1 nM, 5.251 nM, 27.29 nM, and 172.6 nM for CTSL, *JAK1/2/3, and TYK2, respectively. Dual Cathepsin L/JAK-IN-1* effectively blocks the activation of the MAPK, NF-κB, and JAK/STAT signaling pathways, leading to significant anti-inflammatory therapeutic effects. Dual Cathepsin L/JAK-IN-1 can be used in research on acute lung injury (ALI) ^[1].

HY-156535

JAK kinase-IN-1	JAK	Inflammation/Immunology
JAK kinase-IN-1 (Example 1) is a JAK inhibitor. JAK kinase-IN-1 inhibits TYK2, JAK1, JAK2 and JAK3 with IC₅₀ values of 4.2 nM, 32 nM, 27 nM, 3473 nM respectively ^[1].

HY-157011

JAK-IN-33	JAK	Inflammation/Immunology
JAK-IN-33 (compound 3 (R)) is a *JAK* inhibitor .

HY-154969

JAK-IN-29	JAK	Others
JAK-IN-29 (compound 3) is a potent JAK inhibitor .

HY-50856S2

Ruxolitinib-d9 INCB18424-d₉	Isotope-Labeled Compounds Apoptosis JAK Autophagy Mitophagy	Cancer
Ruxolitinib-d₉ (INCB18424-d₉) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective *JAK1/2* inhibitor with IC₅₀s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .

HY-50859

Ruxolitinib sulfate INCB018424 sulfate	JAK Autophagy	Cancer
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective *JAK1/2* inhibitor to enter the clinic with IC₅₀s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.

HY-14986

JAK-IN-32	JAK	Others
JAK-IN-32 (XC) is a bi-aryl meta-pyrimidine inhibitor of JAK kinase .

HY-109175

Fosifidancitinib	JAK	Inflammation/Immunology
Fosifidancitinib is a potent and selective inhibitor of *JAK kinases 1/3*. Fociatinib is used in studies of allergies, asthma and autoimmune diseases ^[1].

HY-10961S8

Momelotinib-d4 dihydrochloride hydrate CYT387-d₄ hydrochloride hydrate	Isotope-Labeled Compounds JAK Autophagy Apoptosis	Cancer
Momelotinib-d₄ (CYT387-d₄) dihydrochloride hydrate is a deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀s of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3 .

HY-50856A

Ruxolitinib (S enantiomer) 4 Publications Verification S-RuxolitINib; S-INCB18424	JAK	Cancer
Ruxolitinib (S enantiomer) (S-Ruxolitinib) is the S-enantiomer of Ruxolitinib (HY-50856). Ruxolitinib (S enantiomer) is an orally active, potent *JAK* inhibitor .

HY-13961

GLPG0634 analog	JAK	Cancer
GLPG0634 analog (Compoun 176) is a broad spectrum JAK inhibitor with IC₅₀ values of <100 nM against JAK1, JAK2 and JAK3 .

HY-123289

CP-690550A	JAK	Inflammation/Immunology
CP-690550A is an analogue of Tofacitinib (HY-40354). CP-690550A is a dual inhibitor of JAK2 and *JAK3* .

HY-15315A

Baricitinib phosphate 55+ Cited Publications LY3009104 phosphate; INCB028050 phosphate	JAK	Inflammation/Immunology
Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable *JAK1/JAK2* inhibitor with IC₅₀ of 5.9 nM and 5.7 nM, respectively.

HY-13450

ZM 449829	JAK EGFR	Inflammation/Immunology
ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC₅₀ of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the *JAK3* .

HY-10963

Momelotinib mesylate CYT387 mesylate	JAK Autophagy	Cancer
Momelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of *JAK1/JAK2* with IC₅₀ of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.

HY-109178

Ifidancitinib ATI-50002; ATI-502	JAK	Others Inflammation/Immunology
Ifidancitinib (ATI-50002) is an orally available, potent and selective inhibitor of *JAK kinase 1/3* that disrupts γc cytokine signaling. Ifidancitinib is used in the research of allergy, asthma, and autoimmune diseases ^[1] .

HY-10961

Momelotinib 10+ Cited Publications CYT387	JAK Autophagy Apoptosis	Cancer
Momelotinib (CYT387) is an ATP-competitive inhibitor of *JAK1/JAK2* with IC₅₀a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.

HY-50858

Ruxolitinib phosphate Maximum Cited Publications 187 Publications Verification INCB018424 phosphate	JAK Autophagy Mitophagy	Cancer
Ruxolitinib phosphate (INCB018424 phosphate) is a potent *JAK1/2* inhibitor with IC₅₀s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.

HY-10962

Momelotinib sulfate 10+ Cited Publications CYT387 sulfate salt	JAK Autophagy Apoptosis	Cancer
Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of *JAK1/JAK2* with IC₅₀ of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC₅₀=155 nM).

HY-15315AR

Baricitinib phosphate (Standard)	JAK	Inflammation/Immunology
Baricitinib (phosphate) (Standard) is the analytical standard of Baricitinib (phosphate). This product is intended for research and analytical applications. Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.

HY-40354AS

Tofacitinib-d3 citrate TasocitINib-d₃ citrate; CP-690550-d₃ citrate	Isotope-Labeled Compounds JAK Apoptosis Bacterial Fungal Influenza Virus	Infection Inflammation/Immunology Cancer
Tofacitinib-d₃ (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

HY-40354AR

Tofacitinib citrate (Standard) TasocitINib citrate (Standard); CP-690550 citrate (Standard)	Reference Standards JAK Apoptosis Bacterial Fungal Influenza Virus	Infection Inflammation/Immunology Cancer
Tofacitinib (citrate) (Standard) is the analytical standard of Tofacitinib (citrate). This product is intended for research and analytical applications. Tofacitinib citrate is an orally available *JAK1/2/3* inhibitor with IC₅₀s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

HY-10961R

Momelotinib (Standard)	JAK Autophagy Apoptosis	Cancer
Momelotinib (Standard) is the analytical standard of Momelotinib. This product is intended for research and analytical applications. Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.

HY-W064657

Momelotinib dihydrochloride	JAK	Others
Momelotinib (dihydrochloride) is a *JAK1/JAK2* inhibitor that also antagonizes *ACVR1, leading to downregulation of Hepcidin* expression and increased availability of iron for erythropoiesis. Momelotinib (dihydrochloride) can reduce transfusion burden and spleen enlargement caused by myelofibrosis, showing potential value in research and application within the field of myelofibrosis ^[1].

HY-14722C

NVP-BSK805 trihydrochloride	JAK	Cancer
NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively ^[1].

HY-14722A

NVP-BSK805 dihydrochloride 3 Publications Verification	JAK	Cancer
NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively ^[1].

HY-138222

JANEX-1 hydrochloride WHI-P131 hydrochloride; JAK3 INhibitor I hydrochloride	JAK	Cancer
JANEX-1 (WHI-P131) hydrochloride is a potent and specific JAK3 inhibitor (K_i=2.3 μM). JANEX-1 hydrochloride shows potent JAK3 inhibitory activity (IC₅₀=78 μM), does not inhibit *JAK1* and *JAK2* .

HY-14722

NVP-BSK805 3 Publications Verification	JAK	Cancer
NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively ^[1].

HY-153568

JAK1-IN-11	JAK	Cancer
JAK1-IN-11 (compound 11) is a potent inhibitor of JAK，with IC₅₀s of 0.02 nM (JAK1)，and 0.44 nM (JAK2)，respectively. JAK1-IN-11 has high selectivity against JAK1 over JAK2 .

HY-10962R

Momelotinib sulfate (Standard)	JAK Autophagy Apoptosis	Cancer
Momelotinib (sulfate) (Standard) is the analytical standard of Momelotinib (sulfate). This product is intended for research and analytical applications. Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).

HY-174280

Modzatinib ITK kINase-IN-1	Itk JAK	Inflammation/Immunology
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* .

HY-125019

iJak-381	JAK STAT	Inflammation/Immunology
iJak-381 is a *JAK1/2* inhibitor with anti-inflammatory activity. iJak-381 blocks IL-13 signaling and also inhibits IL-4 and IL-6 signaling pathways. iJak-381 also reduced p-STAT6 levels and inhibited the influx of inflammatory cells into the lungs of mice. iJak-381 inhibits airway hyperresponsiveness (AHR) ^[1].

HY-149283

JAK/HDAC-IN-2	JAK HDAC Apoptosis	Cancer
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers ^[1].

HY-145015

Tuspetinib HM43239	FLT3 Apoptosis	Cancer
Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC₅₀s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells ^[1] .

HY-145015A

Tuspetinib hydrate HM43239 hydrate	FLT3 Apoptosis	Cancer
Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC₅₀s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells ^[1] .

HY-13775

XL019 5 Publications Verification	JAK Apoptosis	Cancer
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC₅₀s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .

HY-151262

JAK-IN-23	JAK STING NF-κB STAT	Inflammation/Immunology
JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC₅₀ values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC₅₀ values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD) ^[1].

HY-111077

INCB16562	JAK STAT	Inflammation/Immunology Cancer
INCB16562 is an orally active and selective inhibitor against *JAK1/2* markedly selective over JAK3. INCB16562 potently inhibits interleukin-6 (IL-6)-induced phosphorylation of STAT3. Additionally, INCB16562 inhibits the proliferation and survival of myeloma cells dependent on IL-6 for growth, as well as the IL-6–induced growth of primary bone marrow-derived plasma cells. INCB16562 antagonizes the growth of myeloma xenografts in mice with antitumor activity. INCB16562 is promising for research of multiple myeloma ^[1].

HY-145601

Tinengotinib TT 00420	Aurora Kinase FGFR VEGFR	Cancer
Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC₅₀=1.2-3.3 nM), *FGFR1/2/3* (IC₅₀=1.5-3.5 nM), VEGFRs, *JAK1/2* and *CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis*, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment ^[1] .

HY-156466

QL-1200186	STAT Interleukin Related IFNAR	Inflammation/Immunology
QL-1200186 is a selective, orally active, allosteric inhibitor targeting the tyrosine kinase TYK2 pseudokinase domain JH2 (IC₅₀=0.06 nM, TYK2 JH2), with 164-fold selectivity over TYK1 JH2 (IC₅₀=9.85 nM，TYK1 JH2). QL-1200186 first stabilizes the TYK2 JH2 conformation, inhibits the activity of the JH1 catalytic domain, and blocks the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. QL-1200186 can inhibit the production of Th1/Th17 cell-related cytokines (such as IFNγ, IL-23), reduce immune cell activation, and has no significant effect on JAK1/2/3 kinase activity. QL-1200186 can significantly improve skin inflammation in the Imiquimod (HY-B0180)-induced psoriasis mouse model and reduce the Psoriasis Area and Severity Index (PASI) score. QL-1200186 can be used in the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE) ^[1].

Cat. No.	Product Name

HY-L008

JAK/STAT Compound Library

584 compounds

The Janus kinase (JAK)/signal transducer and activator of transcription (STAT) pathway is central to signaling by cytokine receptors, a superfamily of more than 30 transmembrane proteins that recognize specific cytokines, and is critical in blood formation and immune response. Canonical JAK/STAT signaling begins with the association of cytokines and their corresponding transmembrane receptors. Activated JAKs then phosphorylate latent STAT monomers, leading to dimerization, nuclear translocation, and DNA binding. In mammals, there are four JAKs (JAK1, JAK2, JAK3, TYK2) and seven STATs (STAT1, STAT2, STAT3, STAT4, STAT5a, STAT5b, STAT6). Since the JAK/STAT pathway plays a major role in many fundamental processes, such as apoptosis and inflammation, dysfunctional proteins in the pathway may lead to a number of diseases. For example, alterations in JAK/STAT signalling can result in cancer and diseases affecting the immune system, such as severe combined immunodeficiency disorder (SCID).

MCE provides 584 compounds that can be used in the study of the JAK/STAT signaling pathway and related diseases.

Cat. No.	Product Name	Chemical Structure

HY-40354AS

Tofacitinib-d3 citrate
Tofacitinib-d₃ (citrate) is deuterium labeled Tofacitinib (citrate). Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.

HY-50856S2

Ruxolitinib-d9
Ruxolitinib-d₉ (INCB18424-d₉) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective *JAK1/2* inhibitor with IC₅₀s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3 . Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy .

HY-10961S8

Momelotinib-d4 dihydrochloride hydrate
Momelotinib-d₄ (CYT387-d₄) dihydrochloride hydrate is a deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀s of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3 .

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