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Results for "

jak1-in-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (7) Autophagy (7) Cytochrome P450 (1) GSK-3 (2) HIV (3) IFNAR (1) Interleukin Related (6) Isotope-Labeled Compounds (3) JAK (73) PKC (2) Reference Standards (13) STAT (8) Syk (4) TNF Receptor (1)
By Research Areas:	Cancer (28) Cardiovascular Disease (1) Infection (1) Inflammation/Immunology (47) Metabolic Disease (2) Neurological Disease (1)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10961

Momelotinib 15+ 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-100754

Ritlecitinib 5+ Cited Publications PF-06651600	JAK Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .

HY-18300

Filgotinib 20+ Cited Publications GLPG0634	JAK HIV	Cancer
Filgotinib (GLPG0634) is a selective, orally available *JAK1* inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of *JAK1, JAK2*, JAK3 and TYK2 with IC₅₀ values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease .

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-15315A

Baricitinib phosphate Maximum Cited Publications 75 Publications Verification 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-19568

Peficitinib 10+ Cited Publications ASP015K; JNJ-54781532	JAK	Inflammation/Immunology
Peficitinib (ASP015K) is an orally active JAK inhibitor, with IC₅₀s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .

HY-103018

Gusacitinib 1 Publications Verification ASN-002	JAK Syk	Inflammation/Immunology Cancer
Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC₅₀ values of 5, 46, 4, 11 and 8 nM for SYK, *JAK1, JAK2*, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .

HY-100895

SAR-20347 1 Publications Verification	JAK	Cancer
SAR-20347 is an inhibitor of TYK2, *JAK1, JAK2* and JAK3 with IC₅₀s of 0.6, 23, 26 and 41 nM, respectively.

HY-12469

Decernotinib 4 Publications Verification VX-509; VRT-831509	JAK	Inflammation/Immunology
Decernotinib is a potent, orally active JAK3 inhibitor, with K_is of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.

HY-100754C

Ritlecitinib tosylate 5+ Cited Publications PF-06651600 tosylate	JAK Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .

HY-10962

Momelotinib sulfate 15+ 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-120469

2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide	JAK	Inflammation/Immunology
GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with K_is of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively .

HY-18300A

Filgotinib maleate 20+ Cited Publications GLPG0634 maleate	JAK HIV	Inflammation/Immunology
Filgotinib maleate (GLPG0634 maleate) is a selective, orally available *JAK1* inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of *JAK1, JAK2*, JAK3 and TYK2 with IC₅₀ values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease .

HY-174905

Quecitinib QY201	JAK Cytochrome P450	Inflammation/Immunology
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 .

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-102046

FM-381 2 Publications Verification	JAK	Inflammation/Immunology
FM-381, a chemical probe, 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 .

HY-108264

TCS 21311 NIBR3049	JAK PKC GSK-3	Cancer
TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC₅₀ of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC₅₀s of 13, 68, and 3 nM, respectively .

HY-101024

PF-06263276	JAK STAT	Inflammation/Immunology
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC₅₀s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. PF-06263276 inhibits pSTAT3 and TYK2 pathway. PF-06263276 has a protective effect against ear skin inflammation .

HY-152080

Blovacitinib TUL01101	JAK	Inflammation/Immunology
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 .

HY-19568R

Peficitinib (Standard) ASP015K (Standard); JNJ-54781532 (Standard)	Reference Standards JAK	Inflammation/Immunology
Peficitinib (Standard) is the analytical standard of Peficitinib. This product is intended for research and analytical applications. Peficitinib (ASP015K) is an orally active JAK inhibitor, with IC₅₀s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .

HY-116505

JAK1-IN-4	JAK	Cancer
JAK1-IN-4 is a potent and selective *JAK1* inhibitor, with IC₅₀s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC₅₀, 227 nM) .

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-159536

Frevecitinib KN-002; VR-588	JAK	Inflammation/Immunology
Frevecitinib (KN-002) is a potent pan-JAK inhibitor (i.e. JAK1, JAK2, JAK3, TYK2). Frevecitinib can be used for the study of asthma and other respiratory conditions such as chronic obstructive pulmonary disease (COPD).

HY-18300R

Filgotinib (Standard) GLPG0634 (Standard)	Reference Standards JAK	Cancer
Filgotinib (Standard) is the analytical standard of Filgotinib. This product is intended for research and analytical applications. Filgotinib (GLPG0634) is a selective and orally active *JAK1* inhibitor with IC₅₀ of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.

HY-143444

JAK-IN-20	JAK	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC₅₀s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo .

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-153440

Methyl 6-(1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-4-oxo-4,5-dihydropyrazolo[1,5-a]pyrazine-2-carboxylate	JAK	Cancer
JAK-IN-25 (compound 19) is a potent JAK inhibitor with IC₅₀s of 6 nM, 21 nM, 8 nM, 1051 nM for TYK2, JAK1, JAK2, JAK3, respectively. JAK-IN-25 inhibits human whole blood IL-12 (HEB IL-12) with an IC₅₀ of 28 nM. JAK-IN-25 has the potential for cancer 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-18300S

Filgotinib-d4 GLPG0634-d₄	JAK	Cancer
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.

HY-19568B

Peficitinib hydrochloride ASP015K hydrochloride; JNJ-54781532 hydrochloride	JAK	Inflammation/Immunology
Peficitinib (ASP015K) hydrochloride is an orally active JAK inhibitor, with IC₅₀s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .

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-108342

PF-00956980	JAK	Inflammation/Immunology
PF-00956980 is a reversible pan-JAK inhibitor with IC₅₀ values of 2.2, 23.1 and 59.9 μM for JAK1, JAK2 and JAK3, respectively. PF-00956980 can be used in the research of lung and skin inflammatory diseases .

HY-143885

JAK1/TYK2-IN-3	JAK	Inflammation/Immunology
JAK1/TYK2-IN-3 is a potent, selective and orally active dual *TYK2/JAK1* inhibitor with IC₅₀ values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC₅₀=140 nM) and JAK3 (IC₅₀=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related *TYK2/JAK1*-regulated genes, as well as the formation of Th1, Th2, and Th17 cells .

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-15315AR

Baricitinib phosphate (Standard) LY3009104 phosphate (Standard); inCB028050 phosphate (Standard)	JAK Reference Standards	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-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 .

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-19568A

Peficitinib hydrobromide ASP015K hydrobromide; JNJ-54781532 hydrobromide	JAK	Inflammation/Immunology
Peficitinib (ASP015K) hydrobromide is an orally active JAK inhibitor, with IC₅₀s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .

HY-157121

JAK-IN-34	JAK	Inflammation/Immunology
JAK-IN-34 (compound 11n) is a potent against of JAKs with IC₅₀ values of 0.40, 0.83, 2.10, 1.95 nM target JAK1, JAK2, JAK3, TYK2, respectively. JAK-IN-34 reduces joint swelling with good safety .

HY-103018A

Gusacitinib hydrochloride ASN-002 hydrochloride	JAK Syk	Inflammation/Immunology Cancer
Gusacitinib (ASN-002) hydrochloride is an orally active dual SYK/JAK kinase inhibitor with IC₅₀ values of 5, 46, 4, 11 and 8 nM for SYK, *JAK1, JAK2*, JAK3 and TYK2, respectively. Gusacitinib hydrochloride rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib hydrochloride can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .

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-178755

DEL1187-126-5-80	JAK	Inflammation/Immunology
DEL1187-126-5-80 is a JAK3 inhibitor with IC₅₀s of 52 and 7.9 nM against JAK3 WT in 0 and 60 min. DEL1187-126-5-80 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-5-80 can be used for the study of immune-mediated diseases .

HY-178763

DEL1187-126-28-16	JAK	Inflammation/Immunology
DEL1187-126-28-16 is a JAK3 inhibitor with IC₅₀s of 10 and 0.97 nM against JAK3 WT in 0 and 60 min. DEL1187-126-28-16 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-28-16 can be used for the study of immune-mediated diseases .

HY-178282

JAK1-IN-19	JAK	Inflammation/Immunology
JAK1-IN-19 (Compound 18) is a potent *JAK1* inhibitor with IC₅₀s of 0.02, 0.5, 91 and 0.2 nM against *JAK1, JAK2*, JAK3 and TYK2. JAK1-IN-19 exhibits improved rat and human intrinsic clearance. JAK1-IN-19 can be used for the studies of atopic dermatitis and other autoimmune diseases .

HY-18300AR

Filgotinib maleate (Standard) GLPG0634 maleate (Standard)	JAK HIV Reference Standards	Inflammation/Immunology
Filgotinib (maleate) (Standard) is the analytical standard of Filgotinib (maleate). This product is intended for research and analytical applications. Filgotinib maleate (GLPG0634 maleate) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib maleate can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib maleate also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib maleate can be used in the study of rheumatoid arthritis and inflammatory bowel disease .

HY-100754A

Ritlecitinib malonate PF-06651600 malonate	JAK Interleukin Related STAT	Inflammation/Immunology
Ritlecitinib (PF-06651600) malonate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib malonate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib malonate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE) .

HY-161019

JAK1/TYK2-IN-4	JAK	Inflammation/Immunology
JAK1/TYK2-IN-4 is a dual inhibitor of JAK and TYK2, with IC₅₀s of 39 nM and 21 nM, respectively. JAK1/TYK2-IN-4 has oral bioavailability .

HY-145336

JAK1/TYK2-IN-1	JAK	Cancer
JAK1/TYK2-IN-1 is a dual inhibitor of TYK2 and *JAK1* (IC₅₀ = 29 and 41 nM respectively).

HY-10961R

Momelotinib (Standard) CYT387 (Standard)	JAK Autophagy Apoptosis Reference Standards	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-10962R

Momelotinib sulfate (Standard) CYT387 sulfate salt (Standard)	JAK Autophagy Apoptosis Reference Standards	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).

Cat. No.	Product Name

HY-L008

JAK/STAT Compound Library

709 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 709 compounds that can be used in the study of the JAK/STAT signaling pathway and related diseases.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N14094

Tubulosine	Structural Classification Alkaloids Other Alkaloids Rubiaceae Plants Pogonopus tubulosus (A.Rich. ex DC.) K.Schum. Source Classification	JAK Apoptosis Autophagy
Tubulosine is an alkaloid. Tubulosine can be isolated from Pogonopus tubulosus (DC.) Schumann. Tubulosine is an ATP-competitive, selective JAK3 inhibitor with an IC₅₀ value of 9.9 nM. Tubulosine also inhibits the kinase activities of other JAK family members, the extent of inhibition is less than that of JAK3, with IC₅₀ values of 69.5, 84.9 and 76.3 nM for JAK1, JAK2 and TYK2, respectively. Tubulosine selectively inhibits JAK3 signalling by binding to the ATP-binding site of the kinase of JAK3. Tubulosine induces apoptotic and necrotic/autophagic cell death. Tubulosine inhibits the process of peptide chain elongation by eukaryotic polysomes by, specifically preventing the elongation-factor-2-dependent step of translocation. Tubulosine exhibits anticancer activity in breast cancer cells .

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 .

HY-18300S

Filgotinib-d4
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.

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 .

HY-103018S

Gusacitinib-d4

Gusacitinib-d₄ (ASN-002-d₄) is the deuterium labeled Gusacitinib (HY-103018). Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC₅₀ values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .

HY-19568S

Peficitinib-d3
Peficitinib-d₃ (ASP015K-d₃) is the deuterium labeled Peficitinib (HY-19568). Peficitinib (ASP015K) is an orally active JAK inhibitor, with IC₅₀s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively .

Cat. No.	Product Name		Classification

HY-178755

DEL1187-126-5-80		Alkynes
DEL1187-126-5-80 is a JAK3 inhibitor with IC₅₀s of 52 and 7.9 nM against JAK3 WT in 0 and 60 min. DEL1187-126-5-80 has no activity at all towards the C909S mutant, JAK1, JAK2, and TYK2. DEL1187-126-5-80 can be used for the study of immune-mediated diseases .

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