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JAK1/2-IN-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	JAK (24) Apoptosis (5) Aurora Kinase (1) Bcl-2 Family (1) Caspase (2) CDK (1) CXCR (1) FGFR (1) FLT3 (1) G Protein-coupled Receptor Kinase (GRK) (1) IFNAR (3) Interleukin Related (3) Isotope-Labeled Compounds (2) Reference Standards (1) STAT (6) TNF Receptor (1) VEGFR (1)
By Research Areas:	Cancer (12) Inflammation/Immunology (14) Metabolic Disease (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: JAK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-109053

Delgocitinib 2 Publications Verification JTE-052	JAK	Inflammation/Immunology
Delgocitinib (JTE-052) is a specific JAK inhibitor with IC₅₀s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .

HY-131906

JAK2-IN-7	JAK FLT3 Apoptosis	Cancer
JAK2-IN-7 is a selective JAK2 inhibitor with IC₅₀s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 ^V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .

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-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 .

HY-126242S

Tyk2-IN-7	JAK IFNAR Interleukin Related	Inflammation/Immunology
Tyk2-IN-7 is an orally active *TYK2* JH2 inhibitor, binds to TYK2 JH2 domain with IC₅₀ and K_i.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits *TYK2/JAK1/JAK2* kinase domain. Tyk2-IN-7 can inhibit the IL-23 and IFN-α signaling pathways. Tyk2-IN-7 is commonly used in the study of inflammatory conditions such as colitis .

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-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) .

HY-100849

JAK 3i	JAK	Inflammation/Immunology
JAK3i is a highly selective JAK3 inhibitor (IC₅₀: 0.43 nM). JAK3i forms a covalent bond with a cysteine in JAK3, but not the closely related kinase domains in JAK1, JAK2, or TYK2. JAK3i abolishes IL-2-driven T-cell proliferation in vivo and has the potential for autoimmune disease research .

HY-175983

JAK1/TYK2-IN-5	JAK	Cancer
JAK1/TYK2-IN-5 (compound A1) is a *JAK1/TYK2* inhibitor with K_i values of 0.0044 nM, 0.02 nM, 6.9 μM, 0.79 μM, 0.21 μM and 0.55 μM for TYK2 JH2, JAK1 JH2, JAK1 JH1, JAK2 JH1, JAK3 JH1 and TYK2 JH1, respectiverly. JAK1/TYK2-IN-5 inhibts IFNα induced TYK2/JAK1-mediated STAT activation .

HY-144031S

Tyk2-IN-8	Isotope-Labeled Compounds JAK	Inflammation/Immunology
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 .

HY-148060

JAK-IN-21 1 Publications Verification	JAK	Cancer
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 .

HY-162031

MMT3-72-M2	JAK	Metabolic Disease
MMT3-72-M2 is an MMT3-72 metabolite. MMT3-72-M2 is a selective *JAK1* inhibitor. MMT3-72-M2 inhibits JAK1, JAK2, TYK2, and JAK3 with IC₅₀ values of 10.8 nM, 26.3 nM, 91.6 nM, 328.7 nM, respectlly .

HY-120604

BVB808 NVP_BVB808	JAK STAT	Cancer
BVB808 (NVP_BVB808) is a selective JAK2 inhibitor with approximately 10-fold selectivity for JAK2 over other JAK family members (such as JAK1, JAK3 or TYK2) in vitro. BVB808 inhibits the activity of JAK2 and reduces the phosphorylation of STAT5, thereby blocking the *JAK2*-dependent cell proliferation and survival signaling pathways. BVB808 can be used in cancer research .

HY-168971

Paeoniflorin-6′-O-benzene sulfonate CP-25	IFNAR STAT TNF Receptor Interleukin Related CXCR JAK G Protein-coupled Receptor Kinase (GRK)	Inflammation/Immunology
Paeoniflorin-6′-O-benzene sulfonate (CP-25) is the inhibitor for G protein-coupled receptor kinase 2 (GRK2) that inhibits the translocation of GRK2 to the cell membrane, inhibits *JAK1/STAT3* signaling pathway. Paeoniflorin-6′-O-benzene sulfonate inhibits IL-17A/CXCL2-induced proliferation of HaCaT. Paeoniflorin-6′-O-benzene sulfonate reduces the levels of inflammatory factors and chemokines such as IL-17A, IL-17F, IFN-γ, TNF-α, IL-22, IL-23, CXCL2, CXCL3 and CXCL9, alleviates Imiquimod (HY-B0180)-induced psoriasis in mouse model ^[1].

HY-177006

*JAK1/2-IN-2*	JAK	Inflammation/Immunology Cancer
JAK1/2-IN-2 (Compound 37) is a potent and selective *JAK1/2* inhibitor with K_i values of 2 and 0.6 nM .

HY-109053A

Delgocitinib ethanolate JTE-052 ethanolate	JAK	Inflammation/Immunology
Delgocitinib ethanolate is a specific JAK inhibitor with IC₅₀s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .

HY-144032

Tyk2-IN-9	JAK	Inflammation/Immunology
Tyk2-IN-9 (Compound 26) is a selective Tyk-2 inhibitor with IC₅₀s of 0.076 and 1.8 nM for TYK2-JH2 and JAK1-JH2, respectively. Tyk2-IN-9 can be used for the research of inflammatory or autoimmune disease .

HY-144087

TYK2-IN-11	JAK	Inflammation/Immunology
TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC₅₀s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease .

HY-170927

JAK-IN-40	JAK STAT Apoptosis	Cancer
JAK-IN-40 (Compound 46) is the inhibitor for JAK that inhibits *JAK1, JAK2* and JAK3 with IC₅₀s of 0.022, 0.759 and 1.601 μM, respectively. JAK-IN-40 inhibits the phosphorylation of STAT3. JAK-IN-40 inhibits the proliferation of cancer cell Ba/F3 and JAK1-TEL Ba/F3 with GI₅₀ of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle of H1975 and H2087 at G2/M phase, induces apoptosis. JAK-IN-40 exhibits a synergistic antitumor effect with Osimertinib (HY-15772) .

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-168339

Tyk2-IN-22	JAK	Inflammation/Immunology
Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, *JAK1, and JAK3* with IC₅₀s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation ^[1].

HY-169984S

Tyk2-IN-22-d3	Isotope-Labeled Compounds STAT JAK	Inflammation/Immunology
Tyk2-IN-22-d3 (Compound 1) is the deuterated analog of Tyk2-IN-22 (HY-168339). Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, *JAK1, and JAK3* with IC₅₀s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation ^[1] .

HY-181528

JAK1/CDK7-IN-1	JAK CDK Apoptosis Caspase	Cancer
JAK1/CDK7-IN-1 is a *JAK1/CDK7* inhibitor. JAK1/CDK7-IN-1 forms a stable and tightly bound complex with *JAK1. JAK1/CDK7-IN-1* disrupts the cell cycle, induces G₂/M phase arrest, and increases the proportion of pre-G₁ phase cells. JAK1/CDK7-IN-1 induces cellular apoptosis (apoptosis) and necrosis. JAK1/CDK7-IN-1 is applicable to research related to breast cancer and prostate cancer .

HY-180274

JAK1/2-IN-3	JAK Apoptosis Caspase Bcl-2 Family	Cancer
JAK1/2-IN-3 is a *JAK1* and JAK2 inhibitor with IC₅₀ values of 14.73 nM and 10.03 nM, respectively. JAK1/2-IN-3 induces G2/M cell cycle arrest, and induces intrinsic apoptosis via increased Bax and caspase 3/7 levels and reduced Bcl2 expression. JAK1/2-IN-3 can be used for the study of leukemia cancer, breast cancer and colon cancer .

HY-109053R

Delgocitinib (Standard) JTE-052 (Standard)	Reference Standards JAK	Inflammation/Immunology
Delgocitinib (Standard) is the analytical standard of Delgocitinib (HY-109053). This product is intended for research and analytical applications. Delgocitinib (JTE-052) is a specific JAK inhibitor with IC₅₀s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .

HY-178913

Tyk2-IN-23	JAK STAT	Inflammation/Immunology
Tyk2-IN-23 is a potent, orally active, selective TYK2 inhibitor (IC₅₀ = 18 nM), exhibiting more than > 70-fold selectivity over JAK1/2/3 isoforms. Tyk2-IN-23 potently inhibits p-STAT3 in TYK2-dependent signaling activated by IFN-α and IL-10. Tyk2-IN-23 potently inhibits IFN-α-induced STAT1 phosphorylation in H9 cells. Tyk2-IN-23 can be used for the study of alopecia areata and allergic Rhinitis .

Cat. No.	Product Name	Chemical Structure

HY-126242S

Tyk2-IN-7
Tyk2-IN-7 is an orally active *TYK2* JH2 inhibitor, binds to TYK2 JH2 domain with IC₅₀ and K_i.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits *TYK2/JAK1/JAK2* kinase domain. Tyk2-IN-7 can inhibit the IL-23 and IFN-α signaling pathways. Tyk2-IN-7 is commonly used in the study of inflammatory conditions such as colitis .

Tyk2-IN-7

Tyk2-IN-7 is an orally active TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC₅₀ and K_i.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 can inhibit the IL-23 and IFN-α signaling pathways. Tyk2-IN-7 is commonly used in the study of inflammatory conditions such as colitis .

HY-144031S

Tyk2-IN-8
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 .

HY-169984S

Tyk2-IN-22-d3
Tyk2-IN-22-d3 (Compound 1) is the deuterated analog of Tyk2-IN-22 (HY-168339). Tyk2-IN-22 (Compound A8) is a selective inhibitor for tyrosine kinase 2 (Tyk2), that it inhibits Tyk2, *JAK1, and JAK3* with IC₅₀s of 9.7, 148.6, and 883.3 nM, respectively. Tyk2-IN-22 inhibits the downstream STAT5 phosphorylation ^[1] .

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