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Isoforms Recommended:	JAK3

Results for "

JAK3

" in MCE Product Catalog:

By Targets:	Apoptosis (18) Autophagy (8) BMX Kinase (1) Btk (9) c-Kit (1) EGFR (4) FLT3 (5) GSK-3 (1) Itk (1) JAK (94) JNK (2) Mitophagy (2) p38 MAPK (1) PERK (2) PKC (1) Polo-like Kinase (PLK) (1) PROTACs (1) RET (1) Src (1) STAT (3) Syk (3) VEGFR (1)
By Research Areas:	Cancer (62) Inflammation/Immunology (51) Neurological Disease (2)

102

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas

HY-119935

JAK3 covalent inhibitor-1	JAK	Inflammation/Immunology
JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC₅₀ of 11 nM and shows 246-fold selectivity vs other JAKs.

HY-15508

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

HY-143716

JAK3/BTK-IN-1	JAK Btk	Inflammation/Immunology
JAK3/BTK-IN-1 is a potent inhibitor of *JAK3/BTK*. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-1 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 002).

HY-143718

JAK3/BTK-IN-3	JAK Btk	Inflammation/Immunology
JAK3/BTK-IN-3 is a potent inhibitor of *JAK3/BTK*. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-3 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 009)

HY-143717

JAK3/BTK-IN-2	JAK Btk	Inflammation/Immunology
JAK3/BTK-IN-2 is a potent inhibitor of *JAK3/BTK*. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-2 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 004)

HY-143720

JAK3/BTK-IN-5	JAK Btk	Inflammation/Immunology
JAK3/BTK-IN-5 is a potent inhibitor of *JAK3/BTK*. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-5 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, compound 35)

HY-143719

JAK3/BTK-IN-4	JAK Btk	Inflammation/Immunology
JAK3/BTK-IN-4 is a potent inhibitor of *JAK3/BTK*. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-4 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, compound 003)

HY-133747

JAK3-IN-9	JAK	Inflammation/Immunology
JAK3-IN-9 is an orally active *JAK3* inhibitor with IC₅₀ value of 1.7 nM. JAK3-IN-9 is highly selective to the *JAK3* signal path. JAK3-IN-9 is lowly toxic with high oral bioavailability, shows good anti-arthritis activity. JAK3-IN-9 can be used in autoimmune disease research.

HY-150688

JAK3-IN-13	JNK	Cancer
JAK3-IN-13 is a potent, selective and orally active *JAK3* inhibitor with IC₅₀ values of 4728, 2039, 8, 365 nM for NK1, JNK2, JNK3, Tyk2, respectively. JAK3-IN-13 shows antiproliferative activity. JAK3-IN-13 induces cell cycle arrest at G0/G1 phase. JAK3-IN-13 shows antitumor activity.

HY-147975

JAK3-IN-12	JAK	Inflammation/Immunology
JAK3-IN-12 (compound 5k) is a highly potent *JAK3* inhibitor with IC₅₀ values of 9.5 nM, 18 nM and 42 nM for JAK3, JAK1 and JAK2, respectively. JAK3-IN-12 can be used for researching rheumatoid arthritis.

HY-19544

JAK3-IN-1	JAK	Cancer
JAK3-IN-1 is a potent, selective and orally active *JAK3* inhibitor with an IC₅₀ of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for *JAK3* than JAK1 (IC₅₀ of 896 nM) and JAK2 (IC₅₀ of 1050 nM).

HY-146727

JAK3-IN-11	JAK	Inflammation/Immunology
JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active *JAK3* inhibitor with IC₅₀ value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases.

HY-101976

JAK3-IN-6
JAK Inflammation/Immunology

JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC₅₀ of 0.15 nM.

JAK3-IN-6	JAK	Inflammation/Immunology
JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC₅₀ of 0.15 nM.

HY-147754

JAK3/BTK-IN-6	Btk JAK	Inflammation/Immunology
JAK3/BTK-IN-6 (compound 14h) is a potent BTK and *JAK3* dual inhibitor, with IC₅₀ values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research.

HY-U00390

JAK3-IN-7
JAK Cancer

JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC₅₀ of <0.01 μM.

JAK3-IN-7	JAK	Cancer
JAK3-IN-7 is a potent and selective *JAK3* inhibitor extracted from patent WO2011013785A1, has an IC₅₀ of <0.01 μM.

HY-131014

FM-479	JAK	Inflammation/Immunology
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.

HY-12469

Decernotinib 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, JAK*2, and TYK2, respectively.

HY-100759

JAK2-IN-4
JAK Cancer

JAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC₅₀ values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.

JAK2-IN-4	JAK	Cancer
JAK2-IN-4 (compound 16h) is a selective *JAK2/JAK3* inhibitor, with IC₅₀ values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.

HY-123099

MS-1020	JAK	Cancer
MS-1020 is a potent and ATP-competitive *JAK3* inhibitor. MS-1020 inhibits JAK3/STAT signaling and induces apoptosis. MS-1020 promotes cell death. MS-1020 decreases the expression of tyrosine phosphorylated STAT3 levels. MS-1020 has the potential for the research of cancers harboring aberrant JAK3 signaling.

HY-152080

TUL01101	JAK	Inflammation/Immunology
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. TUL01101 can be used for the research of rheumatoid arthritis.

HY-19631A

Ilginatinib NS-018	JAK	Cancer
Ilginatinib (NS-018) is a highly active and orally bioavailable *JAK2* inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM).

HY-19631B

Ilginatinib hydrochloride NS-018 hydrochloride	JAK	Cancer
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable *JAK2* inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM).

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-19631

Ilginatinib maleate NS-018 maleate	JAK	Cancer
Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable *JAK2* inhibitor, with an IC₅₀ of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC₅₀, 33 nM), JAK3 (IC₅₀, 39 nM), and Tyk2 (IC₅₀, 22 nM).

HY-131140

BD750	JAK STAT	Cancer Inflammation/Immunology
BD750, an effective immunosuppressant and a *JAK3/STAT5* inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC₅₀ values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.

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-108419

WHI-P258	JNK	Cancer
WHI-P258, a quinazoline compound, binds to the active site of *JAK3* with an estimated K_i of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM.

HY-102046

FM-381	JAK	Inflammation/Immunology
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.

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-11067

WHI-P97
JAK Inflammation/Immunology

WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo.

WHI-P97	JAK	Inflammation/Immunology
WHI-P97 is a potent and selective *JAK-3* inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo.

HY-145696

SJ10542	PROTACs JAK	Cancer Inflammation/Immunology
SJ10542 is a potent and selective *JAK2/3* directing phenyl glutarimide (PG)-PROTAC with DC₅₀s of 14, 11, and 24 nM for JAK2, JAK3, and JAK2-fusion ALL, respectively. SJ10542 utilizes a PG ligand as the cereblon (CRBN) recruiter.

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.

HY-14722A

NVP-BSK805 dihydrochloride	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.

HY-14722

NVP-BSK805	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.

HY-100754

Ritlecitinib
PF-06651600
JAK Inflammation/Immunology

Ritlecitinib (PF-06651600) is an orally active and selective JAK3 inhibitor with an IC₅₀ of 33.1 nM.
HY-40354

Tofacitinib
Tasocitinib; CP-690550
JAK Apoptosis Inflammation/Immunology Cancer

Tofacitinib is an orally available JAK3/2/1 inhibitor with IC₅₀s of 1, 20, and 112 nM, respectively.
HY-40354D

(3R,4S)-Tofacitinib
JAK Inflammation/Immunology

(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC₅₀ of 1 nM.
HY-40354B

(3S,4R)-Tofacitinib
JAK Inflammation/Immunology

(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC₅₀ of 1 nM.
HY-40354C

(3S,4S)-Tofacitinib
JAK Inflammation/Immunology

(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC₅₀ of 1 nM.

Ritlecitinib PF-06651600	JAK	Inflammation/Immunology
Ritlecitinib (PF-06651600) is an orally active and selective *JAK3* inhibitor with an IC₅₀ of 33.1 nM.

Tofacitinib Tasocitinib; CP-690550	JAK Apoptosis	Inflammation/Immunology Cancer
Tofacitinib is an orally available *JAK3/2/1* inhibitor with IC₅₀s of 1, 20, and 112 nM, respectively.

(3R,4S)-Tofacitinib	JAK	Inflammation/Immunology
(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits *JAK3* with IC₅₀ of 1 nM.

(3S,4R)-Tofacitinib	JAK	Inflammation/Immunology
(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits *JAK3* with IC₅₀ of 1 nM.

(3S,4S)-Tofacitinib	JAK	Inflammation/Immunology
(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits *JAK3* with IC₅₀ of 1 nM.

HY-12589

ZM39923 hydrochloride	JAK	Cancer Neurological Disease
ZM39923 hydrochloride is a *JAK3* inhibitor, with a pIC₅₀ of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC₅₀ of 10 nM.

HY-12589A

ZM39923
JAK Cancer Neurological Disease

ZM39923 is a JAK3 inhibitor, with a pIC₅₀ of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC₅₀ of 10 nM.
HY-13895

WHI-P154
EGFR JAK Apoptosis Cancer

WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC₅₀s of 4 nM and 1.8 μM, respectively.

ZM39923	JAK	Cancer Neurological Disease
ZM39923 is a *JAK3* inhibitor, with a pIC₅₀ of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC₅₀ of 10 nM.

WHI-P154	EGFR JAK Apoptosis	Cancer
WHI-P154 is a potent EGFR inhibitor, and also modestly blocks *JAK3, with IC₅₀*s of 4 nM and 1.8 μM, respectively.

HY-10652

JAK-2/3-IN-1	JAK	Cancer Inflammation/Immunology
JAK-2/3-IN-1 is a potent *JAK-2* and *JAK-3* inhibitor extracted from patent US8163732B2, compound 46, has K_is of <250 nM for both isoforms.

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-100895

SAR-20347
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-15312

WP1066
STAT JAK Apoptosis Cancer

WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.

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.

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

WP1066	STAT JAK Apoptosis	Cancer
WP1066 is an inhibitor of *JAK2* and *STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3*.

HY-18300

Filgotinib GLPG0634	JAK	Cancer
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-151256

JAK-2/3-IN-2
JAK Cancer

JAK-2/3-IN-2 (Compound 3h) is a JAK2 and JAK3 inhibitor with IC₅₀s of 23.85 nM and 18.9 nM, respectively.
HY-111750

JAK-IN-3
JAK Inflammation/Immunology

JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC₅₀ values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
HY-15270

BMS-911543
JAK Cancer

BMS-911543 is a selective JAK2 inhibitor, with IC₅₀s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC₅₀, 75, 360, 66 nM, respectively).

HY-40354S

Tofacitinib-13C3 Tasocitinib-¹³C₃; CP-690550-¹³C₃	JAK Apoptosis	Inflammation/Immunology Cancer
Tofacitinib-¹³C₃ is the ¹³C-labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.

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-109053

Delgocitinib
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-10961

Momelotinib 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-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-50858

Ruxolitinib phosphate 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-13827

JAK-IN-1
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-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-19568

Peficitinib 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-10962

Momelotinib sulfate 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-151259

TK4b	JAK	Cancer
TK4b is a Janus kinase (JAK) inhibitor with the IC₅₀ values of 19.40 nM and 18.42 nM for JAK2 and JAK3, respectively. TK4b can be used in lymphoid-derived diseases and leukemia cancer research.

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-151258

TK4g	JAK	Cancer
TK4g is a Janus kinase (JAK) inhibitor with the IC₅₀ values of 12.61 nM and 15.80 nM for JAK2 and JAK3, respectively. TK4g can be used in lymphoid-derived diseases and leukemia cancer research.

HY-107361

Golidocitinib AZD4205	JAK	Cancer
Golidocitinib (AZD4205) is a selective *JAK1* inhibitor, with an IC₅₀ of 73 nM, weakly inhibits JAK2 (IC₅₀>14.7 μM), and shows little inhibition on JAK3 (IC₅₀>30 μM).

HY-101024

PF-06263276	JAK	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.

HY-139807

JAK-IN-14	JAK	Inflammation/Immunology
JAK-IN-14 is a potent and selective *JAK1* inhibitor, with an IC₅₀ of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16).

HY-18300A

Filgotinib maleate GLPG0634 maleate	JAK	Inflammation/Immunology
Filgotinib (maleate) 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. Filgotinib (maleate) can be used for rheumatoid arthritis (RA) and Crohn's disease research.

HY-16755

Solcitinib GSK-2586184; GLPG-0778	JAK	Inflammation/Immunology
Solcitinib is an orally active, competitive, potent, selective *JAK1* inhibitor, with an IC₅₀ of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.

HY-143444

JAK-IN-20	JAK	Inflammation/Immunology
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-147741

DPPY	JAK Btk EGFR	Cancer Inflammation/Immunology
DPPY (compound 6) is a potent PTK inhibitor with IC₅₀ values of <10, <10, <10 nM for EGFR, BTK, JAK3, respectively. DPPY shows anti-proliferative activity against B-cell lymphoma cells. DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).

HY-14435

Pyridone 6	JAK	Cancer
Pyridone 6 is a *pan-JAK* inhibitor, which potently inhibits the JAK kinase family, with IC₅₀s of 1 nM for *JAK2* and TYK2, 5 nM for *JAK3, and 15 nM for JAK1*, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.

HY-112708

Brepocitinib PF-06700841	JAK	Inflammation/Immunology
Brepocitinib (PF-06700841) is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC₅₀s of 17 nM and 23 nM, respectively. Brepocitinib also inhibits *JAK2* and *JAK3* with IC₅₀s of 77 nM and 6.49 μM, respectively.

HY-100754B

(2R,5S)-Ritlecitinib (2R,5S)-PF-06651600	JAK	Inflammation/Immunology
(2R,5S)-Ritlecitinib ((2R,5S)-PF-06651600) is a potent and selective *JAK3* inhibitor (IC₅₀=144.8 nM) extracted from patent US20150158864A1, example 68.

HY-10410

TG101209	FLT3 JAK RET Autophagy Apoptosis	Cancer
TG101209 is a selective *JAK2* inhibitor with IC₅₀ of 6 nM, less potent to *Flt3* and RET with IC₅₀ of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.

HY-112708A

Brepocitinib P-Tosylate PF-06700841 P-Tosylate	JAK	Inflammation/Immunology
Brepocitinib (PF-06700841) P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC₅₀s of 17 nM and 23 nM, respectively. Brepocitinib P-Tosylate also inhibits *JAK2* and *JAK3* with IC₅₀s of 77 nM and 6.49 μM, respectively.

HY-16997

Itacitinib INCB039110	JAK	Cancer
Itacitinib (INCB039110) is an orally active and selective inhibitor of *JAK1* with an IC₅₀ of 2 nM for human JAK1. Itacitinib shows >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.

HY-18009

(Z)-LFM-A13	Btk Polo-like Kinase (PLK) JAK	Cancer
LFM-A13 is a potent BTK, *JAK2, PLK* inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC₅₀s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.

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-146672

ITK inhibitor 6	Itk	Cancer
ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC₅₀s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities.

HY-137756

JAK2-IN-6	JAK	Cancer
JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective *JAK2* inhibitor with an IC₅₀ of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.

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-50856

Ruxolitinib INCB18424	JAK Autophagy Mitophagy Apoptosis	Cancer
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-147742

Thi-DPPY	JAK	Inflammation/Immunology
Thi-DPPY (compound 8e) is a potent and orally active *JAK3* inhibitor with IC₅₀ values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).

HY-80002

BMX-IN-1 BMX kinase inhibitor	Btk BMX Kinase	Cancer
BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys⁴⁹⁶ in the BMX ATP binding domain with an IC₅₀ of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC₅₀ value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

HY-130247

JAK2/FLT3-IN-1	JAK FLT3 Apoptosis	Cancer
JAK2/FLT3-IN-1 is a potent and orally active dual *JAK2/FLT3* inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.

HY-103018

Gusacitinib ASN-002	JAK Syk	Cancer Inflammation/Immunology
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-10409

Fedratinib TG-101348; SAR 302503	JAK Apoptosis	Cancer
Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active *JAK2* inhibitor with IC₅₀s of 3 nM for both *JAK2* and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

HY-10409A

Fedratinib hydrochloride hydrate TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate	JAK Apoptosis	Cancer
Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active *JAK2* inhibitor with IC₅₀s of 3 nM for both *JAK2* and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

HY-18303

AMG-47a	Src VEGFR p38 MAPK JAK	Inflammation/Immunology
AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC₅₀ of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, *Jak3* and MLR and IL-2 with IC₅₀s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.

HY-130247A

JAK2/FLT3-IN-1 TFA	JAK FLT3 Apoptosis	Cancer
JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual *JAK2/FLT3* inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.

HY-151285

JAK-2/3-IN-3	Apoptosis JAK	Cancer Inflammation/Immunology
JAK-2-/3-IN-3 (compound ST4j) is a potent *JAK2/3* inhibitor with IC₅₀s of 13.00 and 14.86 nM for *JAK2* and *JAK3, respectively. JAK-2-/3-IN-3 inhibits autophosphorylation of JAK2* and induces apoptosis in a dose- and time-dependent manner. JAK-2-/3-IN-3 can be used in studies of lymph derived diseases and leukemia.

HY-112724

Ivarmacitinib SHR0302	JAK Apoptosis	Cancer Inflammation/Immunology
Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly *JAK1. The selectivity of Ivarmacitinib for JAK1* is >10-fold for *JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3* phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.

HY-111553

TAS0728	EGFR	Cancer
TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC₅₀ of 13 nM. TAS0728 also shows IC₅₀s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for *BMX、HER4、BLK、EGFR、JAK3、SLK* and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2HER3, and downstream effectors.

HY-18949

JI6	FLT3 JAK c-Kit	Cancer
JI6 is a potent, selective and orally active *FLT3* inhibitor, with IC₅₀s of ∼40, 8, and 4 nM for *FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3* and c-Kit, with IC₅₀s of ∼250 and ∼500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia.

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	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-147826

EGFR-IN-60	EGFR Apoptosis	Cancer
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR^WT, EGFR^T790M, EGFR^L858R and *JAK3* with IC₅₀s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR^T790M mutation (IC₅₀=1.32 µM) over A431 cells overexpressing EGFR^WT (IC₅₀=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio.

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-N2959

Brevilin A	JAK STAT Apoptosis Autophagy	Cancer
Brevilin A is an orally active *STAT3/JAK* inhibitor (STAT3 IC₅₀= 10.6 µM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy.

HY-111745

Tyk2-IN-5	JAK	Inflammation/Immunology
Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a K_i value of 0.086 nM for Tyk2 JH2 and an IC₅₀ value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis.

HY-12736

GSK143	Syk PERK	Cancer Inflammation/Immunology
GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC₅₀=7.1). GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

HY-12736A

GSK143 dihydrochloride	Syk PERK	Cancer Inflammation/Immunology
GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC₅₀=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.

Cat. No.	Product Name

HY-L008

JAK/STAT Compound Library

349 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 349 compounds that can be used in the study of the JAK/STAT signaling pathway and related diseases.

Cat. No.	Product Name	Target	Category