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JAK2/ACVR1 (ALK2)/ALK5 inhibitor

" in MedChemExpress (MCE) Product Catalog:

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By Research Areas:	Cancer (306) Cardiovascular Disease (27) Endocrinology (2) Infection (12) Inflammation/Immunology (160) Metabolic Disease (23) Neurological Disease (17)
Click Chemistry:	Alkynes (2)
Oligonucleotides:	Rat Pre-designed siRNA Sets (4) Mouse Pre-designed siRNA Sets (4) mRNA (3) Human Pre-designed siRNA Sets (4) siRNAs (12)

470

Inhibitors & Agonists

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Targets Recommended: Anaplastic lymphoma kinase (ALK) JAK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19928

Vactosertib 5+ Cited Publications EW-7197; TEW-7197	TGF-β Receptor	Cancer
Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC₅₀ of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC₅₀ of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect ^[1] ^[2].

HY-102055

JAK2 JH2 Tracer 5+ Cited Publications	JAK	Others
JAK2 JH2 Tracer (Tracer 5) is a fluorescent probe for **JAK2 JH2 domain, with a K_d** value of 0.2 μM ^[1] ^[2].

HY-130247

Flonoltinib 1 Publications Verification JAK2/FLT3-IN-1	JAK FLT3 Apoptosis	Cancer
Flonoltinib 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. Flonoltinib has anti-cancer activity ^[1].

HY-15480

NSC 42834 3 Publications Verification JAK2 inhibitor V; Z3	JAK	Cancer
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of *Jak2, inhibits Jak2-V617F* and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.

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 ^[1].

HY-N1356

Reticuline 1 Publications Verification	JAK STAT NF-κB Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology
Reticuline shows anti-inflammatory effects through *JAK2/STAT3* and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3 ^[1]. Reticuline exhibits cardiovascular effects ^[2].

HY-19928A

Vactosertib Hydrochloride 5+ Cited Publications EW-7197 Hydrochloride; TEW-7197 Hydrochloride	TGF-β Receptor	Cancer
Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC₅₀ of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC₅₀ of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect ^[1] ^[2].

HY-117887

Fidrisertib BLU-782; IPN-60130; ALK2-IN-1	TGF-β Receptor	Cancer
Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2 ^R206H, *ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2* and *ALK5* with IC₅₀s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively ^[1] ^[2].

HY-172240

Tosposertib TU2218 free base	Anaplastic lymphoma kinase (ALK) VEGFR	Inflammation/Immunology Cancer
Tosposertib (TU2218 free base) is an *ALK5/VEGFR2* dual inhibitor (IC₅₀ = 1.2 nM/4.9 nM). Tosposertib directly restores the activity of damaged cytotoxic T lymphocytes (CTLs) and natural killer cells inhibited by TGFβ and suppresses the activity and viability of regulatory T cells. Tosposertib can be used for the study of melanoma and colon cancer ^[1].

HY-146186

JAK2 JH2 binder-1	JAK	Cancer
JAK2 JH2 binder-1 (compound 11) is a potent and selective **JAK2 JH2 binder, with a K_d** of 37.1 nM. JAK2 JH2 binder-1 has the potential for various myeloproliferative neoplasms research ^[1].

HY-10327

GW-6604	TGF-β Receptor	Metabolic Disease
GW-6604 is an *ALK5* inhibitor with an IC₅₀ value of 140 nM for inhibiting its autophosphorylation, and can be used in the study of liver fibrosis ^[1].

HY-109179

Itacnosertib TP-0184	JAK Anaplastic lymphoma kinase (ALK) FLT3 STAT PI3K Akt mTOR TGF-beta/Smad TGF-β Receptor	Cancer
Itacnosertib (TP-0184) is the inhibitor for FLT3, *ACVR1* (ALK2, IC₅₀=8 nM) and *JAK2* (IC₅₀=8540 nM). Itacnosertib exhibits anti-leukemic activity ^[1] ^[2].

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-169326S

JAK2-IN-11	Isotope-Labeled Compounds JAK	Cancer
JAK2-IN-11 (Example 6) is a *JAK2* kinase inhibitor with IC₅₀ ≤10 nM against JH2 BIND WT/V617F. JAK2-IN-11 has antitumor activity ^[1].

HY-112815

ALK2-IN-2 1 Publications Verification	TGF-β Receptor	Cardiovascular Disease Inflammation/Immunology
ALK2-IN-2 is an orally active and selective inhibitor of *ALK2* (ACVR1), with an IC₅₀ value of 9 nM, and over 700-fold selectivity against ALK3. ALK2-IN-2 can inhibit oxidative stress and protect endothelial cells ^[1] ^[2].

HY-144043

ALK5-IN-8	TGF-β Receptor	Cancer
ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1) ^[1].

HY-151289

ALK5-IN-34	TGF-β Receptor TGF-beta/Smad	Cancer
ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC₅₀ value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer ^[1].

HY-146066

*α7 nAchR-JAK2-STAT3 agonist 1*	nAChR JAK STAT NO Synthase Interleukin Related	Inflammation/Immunology
α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC₅₀ value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis ^[1].

HY-112391

SD-1029 1 Publications Verification	JAK STAT	Cancer
SD-1029 is a *JAK2/STAT3* inhibitor ^[1]. SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation ^[2].

HY-174428

*PROTAC JAK2* degrader-1**	PROTACs JAK STAT Apoptosis	Cancer
PROTAC JAK2 degrader-1 is a *JAK2* PROTAC degrader, with a DC₅₀ of 27.35 nM. PROTAC JAK2 degrader-1 induces *JAK2* degradation via the ubiquitin-proteasome pathway. PROTAC JAK2 degrader-1 inhibits the *JAK2-STAT* signaling pathway. PROTAC JAK2 degrader-1 induces G₂/M phase arrest and apoptosis in cancer cells. PROTAC JAK2 degrader-1 exhibits antiproliferative activity against cancer cells. PROTAC JAK2 degrader-1 inhibits recombinant human erythropoietin (rhEPO)-mediated polycythemia and splenomegaly in mice. PROTAC JAK2 degrader-1 can be used for research on myeloproliferative neoplasms, including polycythemia vera ^[1].

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-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-161684

JAK2-IN-10	JAK STAT	Cancer
JAK2-IN-10 is a selective JAK2 V617F inhibitor with an IC₅₀ value of ≤10 nM ^[1]. JAK2-IN-10 can be used for the research of myeloproliferative neoplasms and other related diseases ^[1].

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 ^[1].

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) ^[1].

HY-109179A

Itacnosertib hydrochloride TP-0184 hydrochloride	JAK Anaplastic lymphoma kinase (ALK) FLT3 STAT PI3K Akt mTOR TGF-beta/Smad TGF-β Receptor	Cancer
Itacnosertib hydrochloride (TP-0184 hydrochloride) is the inhibitor for FLT3, *ACVR1* (ALK2, IC₅₀=8 nM) and *JAK2* (IC₅₀=8540 nM). Itacnosertib hydrochloride exhibits anti-leukemic activity ^[1] ^[2].

HY-10432R

A 83-01 (Standard)	Reference Standards TGF-β Receptor	Cancer
A 83-01 (Standard) is the analytical standard of A 83-01 (HY-10432). This product is intended for research and analytical applications. A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor *ALK4* and type I nodal receptor *ALK7, with IC₅₀s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4* and *ALK7*, respectively ^[1].

HY-151275

ALK5-IN-28	TGF-β Receptor TGF-beta/Smad	Cancer
ALK5-IN-28 (Compound Ex-05) is a selective *ALK-5* inhibitor (IC₅₀ ≤ 10 nM) that inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit tumor growth in vivo. ALK5-IN-28 can be used in the research of proliferative diseases such as cancer ^[1] ^[2].

HY-P990022

Prafnosbart DS-6016A	TGF-β Receptor	Metabolic Disease
Prafnosbart (DS-6016A) is an IgG1-kappa, anti-ACVR1 (activin A receptor type 1, ACVRLK2, ALK2, ACVR1A, SKR1) humanized monoclonal antibody. Prafnosbart can be used for bone metabolism disorders research ^[1].

HY-RS07018

JAK2 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA) JAK	Others
JAK2 Human Pre-designed siRNA Set A contains three designed siRNAs for JAK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

JAK2 Human Pre-designed siRNA Set A JAK2 Human Pre-designed siRNA Set A

HY-130247A

Flonoltinib TFA 1 Publications Verification JAK2/FLT3-IN-1 TFA	JAK FLT3 Apoptosis	Cancer
Flonoltinib 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. Flonoltinib TFA has anti-cancer activity ^[1].

HY-P1590

*Tyrosine Protein Kinase JAK 2* (Phospho-Tyr8, 9)**	JAK	Inflammation/Immunology Cancer
Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide corresponding to amino acids 475 to 491 of mouse JAK2.

HY-179428

JAK2-IN-17	JAK	Cancer
JAK2-IN-17 (compound 20) is a potent *JAK2* allosteric inhibitor. JAK2-IN-17 inhibits full-length JAK2 and JAK2 V617F with IC₅₀s of 160 and 130 nM, respectively. JAK2-IN-17 covalently modifies Lys677 in the pseudokinase domain ^[1].

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) ^[1].

HY-151283

ALK5-IN-33	TGF-β Receptor	Cancer
ALK5-IN-33 (Compound EX-10) is a selective, orally active *ALK-5* inhibitor with an IC₅₀ ≤10 nM ^[1].

HY-178231

ALK5-IN-85	TGF-β Receptor	Inflammation/Immunology Cancer
ALK5-IN-85 (Compound 19) is a TGFβRI (ALK5) inhibitor with an IC₅₀ < 100 ?nM. ALK5-IN-85 can be used for respiratory diseases including idiopathic pulmonary fibrosis, asthma, COPD and lumg cancer, and dermal and ocular fibrotic conditions research ^[1].

HY-174786

*Human ACVR1* mRNA**	mRNA	Cancer
Human ACVR1 mRNA encodes the human activin A receptor type 1 (ACVR1) protein, a member of type I receptor which signals a particular transcriptional response in concert with activin type II receptors.

HY-117810

JAK2-IN-1	JAK	Inflammation/Immunology
JAK2-IN-1 (eExample 2) is a *JAK2* inhibitor, and can be used for research of proliferative disease, inflammatory disease, or renal disease ^[1].

HY-156423

*Tubulin/JAK2-IN-1*	Microtubule/Tubulin JAK	Cancer
Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells ^[1].

HY-151285

JAK-2/3-IN-3	Apoptosis JAK	Inflammation/Immunology Cancer
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 ^[1].

HY-161662

ALK5-IN-80	TGF-β Receptor	Cancer
ALK5-IN-80 (Compound 29b) is a selective *ALK5* inhibitor with an IC₅₀ value of 3.7 nM. ALK5-IN-80 can be used for cancer research ^[1].

HY-RS00238

Acvr1 Rat Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Acvr1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Acvr1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Acvr1 Rat Pre-designed siRNA Set A Acvr1 Rat Pre-designed siRNA Set A

HY-RS00236

ACVR1 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
ACVR1 Human Pre-designed siRNA Set A contains three designed siRNAs for ACVR1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

ACVR1 Human Pre-designed siRNA Set A ACVR1 Human Pre-designed siRNA Set A

HY-RS00237

Acvr1 Mouse Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
Acvr1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Acvr1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Acvr1 Mouse Pre-designed siRNA Set A Acvr1 Mouse Pre-designed siRNA Set A

HY-144437

ALK5-IN-9	TGF-β Receptor	Cancer
ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC₅₀ values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease ^[1].

HY-146066A

*(R)-α7 nAchR-JAK2-STAT3 agonist 1*	nAChR JAK STAT NO Synthase	Others
(R)-α7 nAchR-JAK2-STAT3 agonist 1 is the R-enantiomer of α7 nAchR-JAK2-STAT3 agonist 1 (HY-146066). α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC₅₀ value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis ^[1].

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 ^[1].

HY-151273

ALK5-IN-27	TGF-β Receptor	Cancer
ALK5-IN-27 (Compound EX-04) is a potent *ALK-5* inhibitor with an IC₅₀ ≤10 nM. ALK5-IN-27 also inhibits *ALK-2* (selectivity ALK2/ALK5 ≤10) ^[1].

HY-176941

ALK2-IN-6	TGF-β Receptor	Cancer
ALK2-IN-6 (Compound 14a) is a selective *ALK2* inhibitor, with an IC₅₀ of 9 nM. ALK2-IN-6 can be used in the research of diffuse intrinsic pontine glioma ^[1].

HY-151270

ALK5-IN-25	TGF-β Receptor	Cancer
ALK5-IN-25 (compound EX-02) is a potent *ALK-5* inhibitor with an IC₅₀ ≤10 nM.ALK5-IN-25 also inhibits *ALK-2* (selectivity ALK2/ALK5≤10). ALK5-IN-25 can be used for the research of cancer ^[1].

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0484

Liensinine 15+ Cited Publications	Cardiovascular Disease Alkaloids Structural Classification other families Classification of Application Fields Phenols Polyphenols Plants Disease Research Fields Alkaloid Dimers Source Classification	Reactive Oxygen Species (ROS) Autophagy Apoptosis VEGFR JAK Amyloid-β p38 MAPK HIF/HIF Prolyl-Hydroxylase STAT PI3K JNK Akt
Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of *HIF-1α* and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the *JAK2/STAT3* signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke ^[1] ^[2] ^[5].

HY-N0678

Icaritin 5+ Cited Publications Anhydroicaritin	Flavonols Classification of Application Fields Plants Endogenous metabolite Human Gut Microbiota Metabolites Flavonoids Phenols Polyphenols Epimedium brevicornu Maxim. Berberidaceae Disease Research Fields Source Classification Cancer	JAK Autophagy Apoptosis
Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC₅₀ of 8 µM) and primary CML cells (IC₅₀ of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis ^[1] ^[2] ^[3.

HY-N0201

Atractylenolide I 5 Publications Verification	Classification of Application Fields Terpenoids Sesquiterpenes Astragalus caprinus L. Plants Compositae Disease Research Fields Source Classification Cancer	TNF Receptor Toll-like Receptor (TLR) JAK STAT
Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated *JAK2* and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.

HY-N7452

Coumermycin A1 Maximum Cited Publications 27 Publications Verification	Microorganisms Antibiotics Source Classification	JAK Bacterial Orthopoxvirus
Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria. Coumermycin A1 shows anti-orthopoxvirus activity.

HY-121471

Chrysoeriol 5+ Cited Publications	Flavonoids Classification of Application Fields Flavones Phenols Polyphenols Metabolic Disease Euphorbiaceae Plants Brassicaceae Phyllanthus Disease Research Fields Coronopus didymus	Endogenous Metabolite
Chrysoeriol is a kind of natural yellow ash, which can be used for heating plants Coronopus didymus. Chrysoeriol suppresses the JAK2/STAT3, IκB/p65, and NF-κB pathways, and has strong anti-inflammatory activity ^[1] ^[2] .

HY-N2515

Ginsenoside Rk1 5+ Cited Publications	Panax ginseng C. A. Meyer Triterpenes Classification of Application Fields Terpenoids Plants Inflammation/Immunology Disease Research Fields Araliaceae Source Classification	NF-κB PI3K JAK Apoptosis
Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures ^[1]. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of *Jak2/Stat3* signaling pathway and NF-κB ^[2]. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis ^[1]. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway .

HY-N1405

Cucurbitacin I 10+ Cited Publications 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-P2813

Hirudin 3 Publications Verification	Cardiovascular Disease Natural Products Animals Classification of Application Fields Disease Research Fields Source Classification Cancer	Thrombin Apoptosis
Hirudin is a thrombin inhibitor with blood anticoagulant property. Hirudin has potent anti-thrombotic, wound repair, anti-fibrosis, anti-tumor and anti-hyperuricemia effects. Hirudin also affects diabetic complications, cerebral hemorrhage, and others ^[1].

HY-N1356

Reticuline 1 Publications Verification	Cardiovascular Disease Alkaloids Classification of Application Fields Phenols Polyphenols Plants Lauraceae Isoquinoline Alkaloids Lindera aggregata (Sims) Kosterm. Disease Research Fields Source Classification	JAK STAT NF-κB Endogenous Metabolite
Reticuline shows anti-inflammatory effects through *JAK2/STAT3* and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3 ^[1]. Reticuline exhibits cardiovascular effects ^[2].

HY-N0635

Prim-O-glucosylcimifugin 4 Publications Verification	Natural Products Ophryosporus axilliflorus Hieron. Classification of Application Fields Umbelliferae Plants Inflammation/Immunology Disease Research Fields Source Classification	TNF Receptor NO Synthase COX
Prim-O-glucosylcimifugin exerts anti-inflammatory effects through the inhibition of iNOS and *COX-2* expression by through regulating JAK2/STAT3 signaling.

HY-N0807

Swertiamarin 1 Publications Verification	Monophenols other families Classification of Application Fields Phenols Zanthoxylum chiloperone var. angustifolium Metabolic Disease Plants Disease Research Fields Cancer	MMP NF-κB JAK Keap1-Nrf2
Swertiamarin is an orally active natural product with hypoglycemic, lipid-lowering, anti-rheumatic, and antioxidant activities. Swertiamarin can regulate the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promote osteoblast proliferation. Swertiamarin has antioxidant and hepatoprotective effects against carbon tetrachloride induced rat liver toxicity through the *Nrf2/HO-1* pathway. Swertiamarin can attenuate inflammatory mediators by regulating *JAK2/STAT3* transcription factors in adjuvant induced arthritis rats. Swertiamarin can be used in the research of diabetes and arthritis ^[1] ^[2] ^[5].

HY-N1535

Ponicidin 4 Publications Verification Rubescensine B	Structural Classification other families Classification of Application Fields Terpenoids Labiatae Diterpenoids Plants Inflammation/Immunology Disease Research Fields Butea monosperma Kuntze Source Classification	RIP kinase Apoptosis Reactive Oxygen Species (ROS) JAK STAT PI3K Akt Sirtuin Necroptosis Amyloid-β
Ponicidin (Rubescensine B) is an orally active *RIPK1* inhibitor with a K_d value of 135 nM. Ponicidin inhibits the *JAK2/STAT3* pathway to induce apoptosis, activates the PI3K/Akt pathway, upregulates *SIRT1* expression, alleviates oxidative stress, suppresses inflammatory responses and necroptosis, and blocks cell cycle progression. Ponicidin induces ROS production to exert antiproliferative and antiviral effects, while also improving cognitive function and reducing Aβ plaque deposition. Ponicidin can be used in studies related to hepatocellular carcinoma, Alzheimer's disease, and gastric cancer ^[1] ^[2] .

HY-113573

Protosappanin A PTA	Classification of Application Fields Leguminosae Caesalpinia sappan L. Phenols Polyphenols Plants Inflammation/Immunology Disease Research Fields Source Classification	Interleukin Related JAK STAT
Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses *JAK2/STAT3*-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3 ^[1].

HY-120692

Cyclanoline chloride	Alkaloids Structural Classification Cyclea insularis (Makino) Hatusima Plants Isoquinoline Alkaloids Menispermaceae Source Classification	JAK STAT Apoptosis
Cyclanoline chloride is an alkaloid. Cyclanoline chloride can be isolated from Fangji. Cyclanoline (chloride) inhibits the phosphorylation of *JAK2* and STAT3, and induces Apoptosis. Cyclanoline chloride suppresses tumor growth in subcutaneous bladder cancer xenograft models of nude mice. Cyclanoline chloride reverses cisplatin resistance in bladder cancer cells and enhances the efficacy of Cisplatin (HY-17394). Cyclanoline chloride can be used for research related to bladder cancer ^[1].

HY-N2963

Broussonin E 2 Publications Verification	Thymelaeaceae Daphne giraldii Nitsche Phenols Polyphenols Plants Source Classification	ERK p38 MAPK JAK STAT TNF Receptor Interleukin Related COX Arginase
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing *JAK2-STAT3* signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis ^[1].

HY-N4107

Phyllanthin 1 Publications Verification	Phyllanthus urinaria Linn. Classification of Application Fields Lignans Metabolic Disease Euphorbiaceae Phenylpropanoids Plants Disease Research Fields Source Classification	TGF-beta/Smad
Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties ^[1] ^[2] .

HY-N0918

Desmethoxyyangonin Demethoxyyangonin; 5,6-Dehydrokavain	other families Classification of Application Fields Other Diseases Other Phenylpropanoids Phenylpropanoids Plants Disease Research Fields Source Classification	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 ^[1] ^[2] .

HY-N1510

Kaempferol 3-O-gentiobioside	Flavonols Structural Classification Flavonoids Sauropus spatulifolius Beille Classification of Application Fields Phenols Polyphenols Metabolic Disease Euphorbiaceae Plants Disease Research Fields Source Classification	Glycosidase Notch Toll-like Receptor (TLR) NF-κB Mucin Reactive Oxygen Species (ROS) Bacterial TGF-beta/Smad Anaplastic lymphoma kinase (ALK)
Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a K_a value of 57 µM against human *NOTCH1* and an IC₅₀ value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of *MUC5AC, reduces nitrite and ROS* levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the *TGF-β/ALK5/Smad* signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma . It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer ^[1] ^[2] .

HY-N2282

Zingiberen newsaponin Zingiberensis newsaponin	Cardiovascular Disease Triterpenes Classification of Application Fields Terpenoids Dioscorea Zingiberensis C.H.Wright Plants Disease Research Fields Dioscoreaceae Source Classification	Aldose Reductase JAK STAT Autophagy Apoptosis NF-κB SOD Reactive Oxygen Species (ROS)
Zingiberen Newsaponin (Zingiberensis newsaponin) is an orally active type of steroid saponin compound. Zingiberen Newsaponin exerts anti-hepatocellular carcinoma (HCC) effects by inhibiting autophagy and the *AKR1C1/JAK2/STAT3* pathway. Zingiberen Newsaponin activates oxidative stress (upregulates ROS and MDA) and mitochondrial pathways, promoting cancer cell apoptosis. Zingiberen Newsaponin alleviates cerebral ischemia-reperfusion (I/R) injury by decreasing the concentration of pro-inflammatory cytokines and inhibits NF-κB. Zingiberen Newsaponin can enhance the activity of SOD, eliminate free radicals and protect nerve cells. Zingiberen Newsaponin induces platelet aggregation ^[1] ^[2] .

HY-N0885

Telocinobufagin 1 Publications Verification Telobufotoxin; Telocinobufogenin	Structural Classification Animals Classification of Application Fields Other Diseases Disease Research Fields Steroids Source Classification	JAK STAT mTOR PI3K Akt Polo-like Kinase (PLK) Na+/K+ ATPase Apoptosis Bacterial
Telocinobufagin (Telobufotoxin; Telocinobufogenin) is an orally active bufadienolide with potential anti-tumor effects. Telocinobufagin exerts its anti-cancer effects on non-small cell carcinoma, osteosarcoma, thyroid cancer, breast cancer and head and neck squamous cell carcinoma by inhibiting the STAT3, *JAK2/STAT3, LARP1-mTOR, PI3K/Akt/Snail* and *PLK1* pathways, and can also induce tumor cell apoptosis. Telocinobufagin enhances the Th1 immune response and protects against Salmonella typhimurium infection. Telocinobufagin has a strong cardiac-stimulating effect by inhibiting the activity of Na ⁺/K ⁺-ATPase, and it can promote renal fibrosis. Telocinobufagin demonstrates non-opioid analgesic effects in various acute pain models ^[1] ^[2] ^[5] .

HY-121471R

Chrysoeriol (Standard)	Structural Classification Flavonoids Flavones Phenols Polyphenols Euphorbiaceae Plants Brassicaceae Phyllanthus Coronopus didymus	Reference Standards Endogenous Metabolite
Chrysoeriol (Standard) is the analytical standard of Chrysoeriol. This product is intended for research and analytical applications. Chrysoeriol is a kind of natural yellow ash, which can be used for heating plants Coronopus didymus. Chrysoeriol suppresses the JAK2/STAT3, IκB/p65, and NF-κB pathways, and has strong anti-inflammatory activity ^[1] ^[2] .

HY-N12973

Peonidin 3-arabinoside	Structural Classification Phenols Polyphenols Ericaceae Plants Vaccinium uliginosum L. Source Classification	Anaplastic lymphoma kinase (ALK)
Peonidin 3-arabinoside is an anthocyanin found in vaccinium mytrillus. Peonidin 3-arabinoside binds to the *ALK5* and has anticancer activity. Peonidin 3-arabinoside also has antioxidant, anti-inflammatory, and anti-urinary tract infection properties ^[1] ^[2] .

HY-N5014

Liensinine perchlorate 15+ Cited Publications	Alkaloids Structural Classification other families Classification of Application Fields Phenols Polyphenols Plants Isoquinoline Alkaloids Inflammation/Immunology Disease Research Fields Source Classification	Reactive Oxygen Species (ROS) Autophagy Apoptosis VEGFR JAK Amyloid-β p38 MAPK HIF/HIF Prolyl-Hydroxylase STAT PI3K JNK Akt
Liensinine perchlorate is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine perchlorate suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine perchlorate activates AMPK and inhibits the expression of *HIF-1α* and VEGF, thereby suppressing angiogenesis. Liensinine perchlorate exerts anti-tumor effects through ROS-mediated inhibition of the *JAK2/STAT3* signaling pathway. Liensinine perchlorate can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke ^[1] ^[2] ^[5].

HY-N0678R

Icaritin (Standard) Anhydroicaritin (Standard)	Flavonols Structural Classification Human Gut Microbiota Metabolites Flavonoids Phenols Polyphenols Epimedium brevicornu Maxim. Plants Endogenous metabolite Berberidaceae Source Classification	JAK Reference Standards Autophagy Apoptosis
Icaritin (Standard) is the analytical standard of Icaritin. This product is intended for research and analytical applications. Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC₅₀ of 8 μM) and primary CML cells (IC₅₀ of 13.4 μM for CML-CP and 18 μM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis ^[1] ^[2][3.

HY-N1405R

Cucurbitacin I (Standard) Elatericin B (Standard); JSI-124 (Standard); NSC-521777 (Standard)	Triterpenes Structural Classification Classification of Application Fields Terpenoids Cucurbitaceae Plants Disease Research Fields Lagenaria siceraria (Molina) Standl. Source Classification 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-N13294

Cernuumolide J TMJ-105	Terpenoids Carpesium cernuum L. Sesquiterpenes Plants Compositae Source Classification	Apoptosis JAK STAT p38 MAPK JNK ERK
Cernuumolide J (TMJ-105) is an *JAK2/STAT3* inhibitor. Cernuumolide J induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of *JAK2, STAT3, and Erk, and activating the phosphorylation of JNK* and p38 MAPK. Cernuumolide J inhibits HEL leukemia cell growth in a time- and concentration-dependent manner, with an IC₅₀ value of 1.79 μM. Cernuumolide J can be used for research in the field of anti-cancer therapy ^[1].

HY-N0635R

Prim-O-glucosylcimifugin (Standard)	Structural Classification Natural Products Ophryosporus axilliflorus Hieron. Umbelliferae Plants Source Classification	TNF Receptor Reference Standards NO Synthase COX
Prim-O-glucosylcimifugin (Standard) is the analytical standard of Prim-O-glucosylcimifugin. This product is intended for research and analytical applications. Prim-O-glucosylcimifugin exerts anti-inflammatory effects through the inhibition of iNOS and COX-2 expression by through regulating JAK2/STAT3 signaling.

HY-N4107R

Phyllanthin (Standard)	Phyllanthus urinaria Linn. Structural Classification Lignans Euphorbiaceae Phenylpropanoids Plants Source Classification	Reference Standards TGF-beta/Smad
Phyllanthin (Standard) is the analytical standard of Phyllanthin. This product is intended for research and analytical applications. Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties ^[1] ^[2] .

HY-N8098

Pulchinenoside E2	Triterpenes Structural Classification Classification of Application Fields Terpenoids Ranunculaceae Plants Disease Research Fields Pulsatilla chinensis (Bunge) Regel Source Classification Cancer	STAT Autophagy JAK
Pulchinenoside E2 is a triterpenoid saponin. Pulchinenoside E2 inhibits the phosphorylation of STAT3 and *JAK2, blocks the nuclear translocation and transcriptional activity of STAT3, and suppresses STAT3*-dependent mitochondrial oxidative phosphorylation. Pulchinenoside E2 inhibits invasion, migration and autophagy of triple-negative breast cancer cells. Pulchinenoside E2 can be used in research related to triple-negative breast cancer ^[1].

HY-N0918R

Desmethoxyyangonin (Standard) Demethoxyyangonin (Standard); 5,6-Dehydrokavain (Standard)	Structural Classification other families Other Phenylpropanoids Phenylpropanoids Plants Source Classification	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 ^[1] ^[2] .

HY-N0201R

Atractylenolide I (Standard)	Structural Classification Terpenoids Sesquiterpenes Astragalus caprinus L. Plants Compositae Source Classification	TNF Receptor Reference Standards Toll-like Receptor (TLR) JAK STAT
Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.

HY-N2515R

Ginsenoside Rk1 (Standard)	Panax ginseng C. A. Meyer Triterpenes Structural Classification Terpenoids Plants Araliaceae Source Classification	Reference Standards NF-κB PI3K JAK Apoptosis
Ginsenoside Rk1 (Standard) is the analytical standard of Ginsenoside Rk1. This product is intended for research and analytical applications. Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures ^[1]. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB ^[2]. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis ^[1]. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway .

HY-N0484R

Liensinine (Standard)	Alkaloids Structural Classification other families Phenols Polyphenols Plants Alkaloid Dimers Source Classification	Reference Standards Reactive Oxygen Species (ROS) Autophagy Apoptosis VEGFR JAK Amyloid-β p38 MAPK HIF/HIF Prolyl-Hydroxylase STAT PI3K JNK Akt
Liensinine (Standard) is the analytical standard of Liensinine (HY-N0484). This product is intended for research and analytical applications. Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of *HIF-1α* and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the *JAK2/STAT3* signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke ^[1] ^[2] ^[5].

HY-N15564

Theleganbanin B	Microorganisms Phenols Polyphenols Source Classification	Drug Derivative
Theleganbanin B is a p-terphenyl derivative found in the Thelephora ganbajun. Theleganbanin B inhibits TNF-α, IL-6, and IL-1β production in LPS-induced BV-2 microglial cells. Theleganbanin B inhibits the phosphorylation of JAK2/STAT3. Theleganbanin B is promising for research of neurodegenerative diseases ^[1].

HY-N13352

Bufothionine	Structural Classification Alkaloids Animals Other Alkaloids Source Classification	Mitochondrial Metabolism STAT JAK Interleukin Related Atg7 Autophagy Pim
Bufothionine is an alkaloid. Bufothionine can be isolated from Cinobufacini. Bufothionine induces mitochondria-mediated Apoptosis. Bufothionine significantly reduces serum IL-6 concentration, suppresses p-Stat3 ^tyr705, p-Stat3 ^ser727 and *Jak2* expressions. Bufothionine upregulates *Atg5, Atg7* and LC3Ⅱ expressions. Bufothionine induces Autophagy. Bufothionine suppresses PIM3 expression. Bufothionine relieves symptoms of H22-tumor-bearing mice and exerts anti-inflammation activity. Bufothionine exerts anti-cancer activities against gastric cancer ^[1] ^[2].

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 ^[1] ^[2] .

Cat. No.	Product Name	Chemical Structure

HY-50856S

Deuruxolitinib
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), is an orally active *JAK1* and *JAK2* inhibitor. Deuruxolitinib demonstrates significant hair regrowth effects. Deuruxolitinib can be used for the research of alopecia areata ^[1].

HY-169326S

JAK2-IN-11
JAK2-IN-11 (Example 6) is a *JAK2* kinase inhibitor with IC₅₀ ≤10 nM against JH2 BIND WT/V617F. JAK2-IN-11 has antitumor activity ^[1].

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-161684

JAK2-IN-10
JAK2-IN-10 is a selective JAK2 V617F inhibitor with an IC₅₀ value of ≤10 nM ^[1]. JAK2-IN-10 can be used for the research of myeloproliferative neoplasms and other related diseases ^[1].

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 ^[1] ^[2].

HY-W062703S

(Rac)-Ruxolitinib-d9
(Rac)-Ruxolitinib D9 ((Rac)-INCB18424 D9) is the deuterium labeled (Rac)-Ruxolitinib. (Rac)-Ruxolitinib is a JAK2 inhibitor ^[1].

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 ^[1] ^[2].

HY-16379S

Pacritinib-d4
Pacritinib-d₈ (SB1518-d₈) is the deuterium labeled Pacritinib (HY-16379). Pacritinib (SB1518) is a potent inhibitor of both wild-type *JAK2* (IC₅₀=23 nM) and JAK2 ^V617F mutant (IC₅₀=19 nM). Pacritinib also inhibits FLT3 (IC₅₀=22 nM) and its mutant FLT3 ^D835Y (IC₅₀=6 nM).

HY-19569S1

Upadacitinib-d5

Upadacitinib-d₅ (ABT-494-d₅) is the deuterium labeled Upadacitinib (HY-19569). Upadacitinib (ABT-494) is a potent, orally active and selective JAK1 inhibitor (IC₅₀ = 43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) can be used for several autoimmune disorders research ^[1] ^[2].

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-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-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 ^[1].

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 ^[1] ^[2] .

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 ^[1] ^[2].

HY-13012S

RepSox-d5

RepSox-d₅ (E-616452-d₅) is the deuterium labeled RepSox (HY-13012). RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC₅₀ value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes ^[1] ^[2].

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 ^[1].

Targets Recommended: Anaplastic lymphoma kinase (ALK) JAK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13012G

RepSox E-616452; SJN 2511	TGF-β Receptor	Metabolic Disease
RepSox (E-616452) (GMP) is a RepSox (HY-13012) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RepSox is a potent and selective TGF-β-RI/ALK5 inhibitor ^[1].

HY-13227G

SD-208	TGF-β Receptor	Cancer
SD-208 (GMP) is SD-208 (HY-13227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC₅₀ of 48 nM, and > 100-fold selectivity over TGF-βRII.

HY-148748G

Butyzamide	JAK STAT p38 MAPK	Cardiovascular Disease
Butyzamide (GMP) is Butyzamide (HY-148748) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Butyzamide is an orally active activator of Mpl, a thrombopoietin (TPO) receptor. Butyzamide increases the phosphorylation level of JAK2, STAT3, STAT5 and MAPK. Butyzamide increases the level of platelets in mouse xenotransplantation assay ^[1].

HY-12278G

K02288	TGF-β Receptor	Cancer
K02288 (GMP) is K02288 (HY-12278) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC₅₀s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC₅₀s of of 5-34 nM.

HY-12071G

LDN193189 DM-3189	Organoid TGF-β Receptor	Cancer
LDN193189 GMP is LDN193189 (HY-12071) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. LDN193189 (DM-3189) is a potent selective BMP type I receptor (BMP I) inhibitor. LDN193189 efficiently inhibits transcriptional activity of the BMP type I receptors *ALK2* and *ALK3* with IC₅₀ values of 5 nM and 30 nM, respectively. LDN193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva ^[1] ^[2] ^[5].

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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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