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Pathways Recommended:	JAK/STAT Signaling

Results for "

selective JAK inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	JAK (143) Ack1 (1) Akt (3) Apoptosis (31) Aurora Kinase (2) Autophagy (10) Bcl-2 Family (1) BMX Kinase (1) Btk (1) c-Kit (1) c-Myc (1) Cytochrome P450 (3) Deubiquitinase (1) Drug Derivative (1) EGFR (4) ERK (1) FGFR (1) FLT3 (8) Glucocorticoid Receptor (1) GSK-3 (3) HIV (3) IFNAR (4) IGF-1R (1) IKK (2) Interleukin Related (10) IRAK (1) Isotope-Labeled Compounds (6) Itk (1) JNK (1) LRRK2 (1) Mitophagy (4) Monoamine Oxidase (2) NF-κB (1) NO Synthase (2) p38 MAPK (2) Phosphatase (2) PI3K (4) PKC (1) PROTACs (3) Protease Activated Receptor (PAR) (1) Ras (1) Reactive Oxygen Species (ROS) (1) Reference Standards (9) RET (3) Src (1) STAT (28) Syk (4) TAM Receptor (1) Trk Receptor (1) Tyrosinase (1) VEGFR (2)
By Research Areas:	Cancer (86) Cardiovascular Disease (3) Endocrinology (1) Infection (3) Inflammation/Immunology (77) Metabolic Disease (1) Neurological Disease (3)
Click Chemistry:	Alkynes (1)

158

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: JAK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-148060

JAK-IN-21	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-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-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-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-144440

JAK1-IN-9	JAK	Cancer
JAK1-IN-9 (compound 23a) is a potent and selective *JAK1* inhibitor with an IC₅₀ of 72 nM. JAK1-IN-9 shows selective against other JAKs by 12 times or more .

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-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-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-161139

JAK1-IN-14	JAK	Inflammation/Immunology
JAK1-IN-14 (Compound 12a) is a potent and selective *JAK1* inhibitor. JAK1-IN-14 inhibits *JAK1* and *JAK2* with an IC₅₀ value of 12.6 nM and 135 nM. JAK1-IN-14 suppresses hepatic fibrosis levels and can be used for the research of liver fibrosis and inflammatory diseases .

HY-15315A

Baricitinib phosphate 60+ 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-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-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-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-13827

JAK-IN-1 2 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-153566

JAK1-IN-10	JAK	Cancer
JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, is a potent and selective *JAK1* inhibitor .

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-155746

JAK2-IN-9	JAK	Infection Inflammation/Immunology
JAK2-IN-9 (Compound A8) is a selective *JAK2* inhibitor (IC₅₀: 5 nM). JAK2-IN-9 inhibits the phosphorylation of JAK2, STAT3, and STAT5. JAK2-IN-9 has metabolic stabilities. JAK2-IN-9 induces apoptosis. JAK2-IN-9 can be used for research of myeloproliferative neoplasms (MPNs) .

HY-16997

Itacitinib 15+ 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-128450

JAK-STAT-IN-1	JAK STAT	Inflammation/Immunology Cancer
JAK-STAT-IN-1 (compound 1) is a selective *JAK-STAT* inhibitor. JAK-STAT-IN-1 can be used for the research of autoimmune disorder .

HY-137756

JAK2-IN-6 1 Publications Verification	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-161015

JAK1-IN-13	JAK	Inflammation/Immunology
JAK1-IN-13 (compound 36b) is an orally active, potent and highly selective inhibitor of *JAK1* with an IC₅₀ of 0.044 nM. JAK1-IN-13 significantly decreases STAT3 phosphorylation .

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-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-175684

JAK2-IN-14	JAK STAT Apoptosis	Cancer
JAK2-IN-14 is an orally active *JAK2* inhibitor with an IC₅₀ of 2 nM. JAK2-IN-14 demonstrates 89.5-, 80.5-, and 51-fold selectivity over *JAK1, JAK3, and TYK2, respectively. JAK2-IN-14 inhibits* STAT5 signaling pathway. JAK2-IN-14 causes tumor cell cycle arrest and apoptosis. JAK2-IN-14 can used for the study of myeloproliferative neoplasms (MPNs) .

HY-50856

Ruxolitinib Maximum Cited Publications 218 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-10410

TG101209 5 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-174999

JAK3-IN-18	JAK Tyrosinase	Neurological Disease Inflammation/Immunology
JAK3-IN-18 is an orally active *JAK3* and TEC inhibitor, with IC₅₀s of 0.5391 nM and 12.40 nM, respectively. JAK3-IN-18 demonstrates outstanding selectivity over AK1, AK2, and TYk2, with selectivity ratios exceeding 10,000-fold. JAK3-IN-18 demonstrates excellent therapeutic efficacy in the experimental autoimmune encephalomyelitis (EAE) mouse model. JAK3-IN-18 can be used for the study of multiple sclerosis .

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-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-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-N1405

Cucurbitacin I 10+ Cited Publications Elatericin B; JSI-124; NSC-521777	STAT JAK	Cancer
Cucurbitacin I is a natural selective inhibitor of *JAK2/STAT3*, with potent anti-cancer activity.

HY-13775

XL019 5+ Cited Publications	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-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-149296

JAK1-IN-12	JAK	Inflammation/Immunology
JAK1-IN-12 is a selective inhibitor of *JAK1, with IC₅₀* of 0.0246 μM. And IC₅₀s of 0.423 μM, 0.410 μM and 1.12 μM for JAK2, JAK3 and TYK2. JAK1-IN-12 promotes hair growth in mice. JAK1-IN-12 can be used for research of immune and inflammatory diseases .

HY-10409

Fedratinib 45+ 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 45+ 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-143884

JAK2/TYK2-IN-1	JAK	Inflammation/Immunology
JAK2/TYK2-IN-2 is a potent and selective TYK2 inhibitor with IC₅₀ values of 9 and 157 nM for TYK2 and *JAK2, respectively. JAK*2/TYK2-IN-2 has anti-inflammatory activity .

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-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-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-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-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-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-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-112724A

Ivarmacitinib sulfate SHR0302 sulfate	JAK Apoptosis	Inflammation/Immunology Cancer
Ivarmacitinib (SHR0302) sulfate 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-112724

Ivarmacitinib SHR0302	JAK Apoptosis	Inflammation/Immunology Cancer
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-161259

JAK-IN-36	JAK	Inflammation/Immunology
JAK-IN-36 (Compound 12e) is a potent and selective inhibitor of Janus Kinase 1 (JAK1) with a IC₅₀ value of 2.2 nM. JAK-IN-36 can be used in the study of autoimmune diseases .

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).

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1405

Cucurbitacin I Maximum Cited Publications 12 Publications Verification Elatericin B; JSI-124; NSC-521777	Triterpenes Classification of Application Fields Terpenoids Cucurbitaceae Plants Disease Research Fields Lagenaria siceraria (Molina) Standl. Cancer	STAT JAK
Cucurbitacin I is a natural selective inhibitor of *JAK2/STAT3*, with potent anti-cancer activity.

HY-N0918

Desmethoxyyangonin Demethoxyyangonin; 5,6-Dehydrokavain	other families Classification of Application Fields Source classification Other Diseases Other Phenylpropanoids Phenylpropanoids Plants Disease Research Fields	Monoamine Oxidase JAK IKK STAT NO Synthase Cytochrome P450
Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC₅₀: 0.123 µM). Desmethoxyyangonin exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin induces CYP3A23 expression and leads to skeletal muscle relaxation .

HY-125938

Cycloartenyl ferulate 1 Publications Verification Cycloartenol ferulate; Cycloartenol ferulic acid ester	Triterpenes Monophenols other families Classification of Application Fields Terpenoids Source classification Phenols Plants Inflammation/Immunology Disease Research Fields	Drug Derivative Apoptosis Reactive Oxygen Species (ROS) JAK STAT
Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity K_d = 0.5 μM) to activate the canonical *JAK1/2-STAT1* signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .

HY-N1405R

Cucurbitacin I (Standard) Elatericin B (Standard); JSI-124 (Standard); NSC-521777 (Standard)	Triterpenes Classification of Application Fields Terpenoids Source classification Cucurbitaceae Plants Disease Research Fields Lagenaria siceraria (Molina) Standl. Cancer	STAT JAK Reference Standards
Cucurbitacin I (Standard) is the analytical standard of Cucurbitacin I. This product is intended for research and analytical applications. Cucurbitacin I is a natural selective inhibitor of *JAK2/STAT3*, with potent anti-cancer activity.

HY-N0918R

Desmethoxyyangonin (Standard) Demethoxyyangonin (Standard); 5,6-Dehydrokavain (Standard)	other families Source classification Other Phenylpropanoids Phenylpropanoids Plants	Reference Standards Monoamine Oxidase JAK STAT NO Synthase IKK Cytochrome P450
Desmethoxyyangonin (Standard) is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin (Standard) is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC₅₀: 0.123 µM). Desmethoxyyangonin (Standard) exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin (Standard) induces CYP3A23 expression and leads to skeletal muscle relaxation .

Cat. No.	Product Name	Chemical Structure

HY-15315S

Baricitinib-d5
Baricitinib-d₅ is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.

HY-15315S1

Baricitinib-d3
Baricitinib-d₃ is the deuterium labeled Baricitinib. Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.

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-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-W727879

Upadacitinib-15N,d2

1 Publications Verification

Upadacitinib- ¹⁵N,d₂ (ABT-494- ¹⁵N,d₂) is the deuterium-labeled Upadacitinib (HY-19569). Upadacitinib- ¹⁵N,d₂ (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC₅₀=43 nM). Upadacitinib- ¹⁵N,d₂ (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib- ¹⁵N,d₂ (ABT-494) can be used for several autoimmune disorders research .

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 .

HY-145588S

Povorcitinib-d6
Povorcitinib-d₆ (INCB54707-d₆) is the deuterium labeled Povorcitinib (HY-145588). Povorcitinib (INCB54707) is a potent and selective JAK1 inhibitor that effectively reduces abscesses and inflammatory nodules. Povorcitinib is used to study cutaneous lupus erythematosus (CLE) and lichen planus (LP) .

HY-131968

BMS-986202

BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC₅₀ value of 0.19 nM and a K_i of 0.02 nM. BMS-986202 is remarkably selective over other kinases including Jak family members. BMS-986202 is also a weak inhibitor of CYP2C19 with an IC₅₀ value of 14 μM. BMS-986202 can be used for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus research. BMS-986202 is a de novo deuterium .

Cat. No.	Product Name		Classification

HY-U00318

JAK-IN-11		Alkynes
JAK-IN-11 is a potent and selective *JAK* inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment . JAK-IN-11 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
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