JAK-2/3-IN-2

By Targets:	JAK (7) Apoptosis (2) FLT3 (1) Interleukin Related (1) nAChR (1) NO Synthase (1) RET (1) STAT (3) Syk (1)
By Research Areas:	Cancer (4) Inflammation/Immunology (5)

Targets Recommended: JAK AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-113573

Protosappanin A PTA	JAK STAT	Inflammation/Immunology
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 .

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 .

*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-146066

α7 nAchR-JAK2-STAT3 agonist 1	nAChR JAK STAT NO Synthase	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 .

HY-102084

LMT-28 5+ Cited Publications	Interleukin Related	Inflammation/Immunology
LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130 .

HY-157121

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

HY-107595

SD-1008	JAK STAT Apoptosis	Cancer
SD-1008 is a potent JAK inhibitor. SD-1008 inhibits tyrosyl phosphorylation of STAT3, JAK2 and Src. SD-1008 also reduces STAT3-dependent luciferase activity. SD-1008 enhances apoptosis induced by Paclitaxel in ovarian cancer cells via directly blocking the JAK-STAT3 signaling pathway .

HY-120214

TAS05567	Syk RET	Inflammation/Immunology
TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC₅₀ of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC₅₀s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases .

Cat. No.	Product Name

HY-L008

JAK/STAT Compound Library	423 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 423 compounds that can be used in the study of the JAK/STAT signaling pathway and related diseases.

JAK/STAT Compound Library

423 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 423 compounds that can be used in the study of the JAK/STAT signaling pathway and related diseases.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113573

Protosappanin A PTA	Structural Classification Classification of Application Fields Leguminosae Caesalpinia sappan L. Source classification Phenols Polyphenols Plants Inflammation/Immunology Disease Research Fields	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 .

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JAK-2/3-IN-2

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