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JAK3 Selective Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (14) Autophagy (8) BMX Kinase (1) Btk (1) c-Kit (1) EGFR (4) FLT3 (3) GSK-3 (2) HIV (2) IGF-1R (1) Isotope-Labeled Compounds (3) Itk (1) JAK (63) JNK (1) Mitophagy (4) PI3K (1) PKC (1) RET (1) STAT (4)
By Research Areas:	Cancer (39) Endocrinology (1) Inflammation/Immunology (29) Metabolic Disease (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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.

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-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-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-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.

HY-150688

JAK3-IN-13	JNK	Cancer
JAK3-IN-13 (compound 12n) 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-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-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 .

HY-122101

NSC114792	JAK Apoptosis	Cancer
NSC114792 is a selective *JAK3* inhibitor. NSC114792 induces apoptosis. NSC114792 decreases the protein expression of p-JAK3 and p-STAT5 .

HY-161354

JAK3 covalent inhibitor-2	JAK Apoptosis	Inflammation/Immunology
JAK3 covalent inhibitor-2 (compound J1b) is a selective, orally potent JAK3 inhibitor (IC₅₀=7.2 nM) with low toxicity, anti-inflammatory activity and good bioavailability .

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-100754

Ritlecitinib 5+ Cited Publications PF-06651600	JAK	Inflammation/Immunology
Ritlecitinib (PF-06651600) is an orally active and selective *JAK3* inhibitor with an IC₅₀ of 33.1 nM .

HY-11067

WHI-P97 2 Publications Verification	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-102046

FM-381 1 Publications Verification	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-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-100754C

Ritlecitinib tosylate 5+ Cited Publications PF-06651600 tosylate	JAK	Inflammation/Immunology
Ritlecitinib tosylate is an orally active and selective *JAK3* inhibitor with an IC₅₀ of 33.1 nM. Ritlecitinib tosylate is used for inflammatory and autoimmune diseases research .

HY-15270

BMS-911543 2 Publications Verification	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-100754A

Ritlecitinib (malonate) PF-06651600 (malonate)	JAK	Inflammation/Immunology
Ritlecitinib (PF-06651600) malonate is an orally active and selective *JAK3* inhibitor with an IC₅₀ of 33.1 nM. Ritlecitinib (malonate) can be used for the research of inflammatory and autoimmune diseases .

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-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-121874

EP009	JAK	Cancer
EP009 is a *JAK3* inhibitor that selectively inhibits IL-2-mediated *JAK3* tyrosine phosphorylation (IC50=10-20 μM in Kit225 cells) without affecting IL-3-induced JAK2 phosphorylation (up to 50 μM in BaF/3 cells). EP009 significantly reduced Kit225 cell viability (72 h, LD50=5.0 μM) while having no effect on BaF/3 cells. .

HY-107361

Golidocitinib 2 Publications Verification 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-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-50858

Ruxolitinib phosphate Maximum Cited Publications 154 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-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-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-16755

Solcitinib 1 Publications Verification 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-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-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-18300R

Filgotinib (Standard)	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-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-10410

TG101209 4 Publications Verification	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-19631B

Ilginatinib hydrochloride 1 Publications Verification 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-19631A

Ilginatinib 1 Publications Verification 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-19631

Ilginatinib maleate 1 Publications Verification 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-16997

Itacitinib 10+ Cited Publications 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-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-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-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 .

HY-W740378

1,2,3,4-Tetrahydro Staurosporin AFN-941	EGFR JAK	Others
1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC₅₀=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC₅₀=390 nM). It also binds to Janus kinase 3 (JAK3).

HY-50856

Ruxolitinib Maximum Cited Publications 154 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-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-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-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-10409

Fedratinib 40+ Cited Publications 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 40+ Cited Publications 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-50856R

Ruxolitinib (Standard)	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-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-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 .

Cat. No.	Product Name	Chemical Structure

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-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-10409S

Fedratinib-d9

Fedratinib-d₉ (TG-101348-d₉) is deuterium labeled Fedratinib. 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-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 .

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