Search Result
Results for "
JAK-IN-3
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-40354
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- HY-40354A
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- HY-12000
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AG490
Maximum Cited Publications
165 Publications Verification
TyrphostIN AG490; TyrphostIN B42
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EGFR
STAT
JAK
Autophagy
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Cancer
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AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
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- HY-N0143
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Phlorizin
Maximum Cited Publications
15 Publications Verification
FloridzIN
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Caspase
JAK
GLUT
STAT
Apoptosis
Bacterial
SGLT
mTOR
Akt
NF-κB
PI3K
DNA/RNA Synthesis
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Infection
Neurological Disease
Metabolic Disease
Cancer
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Phlorizin (Floridzin) is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC50 of 0.04 μM and a Ki of 39 nM against hSGLT2, and an IC50 of 0.17 μM and a Ki of 0.31 μM against hSGLT1. Phlorizin promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin also exhibits antibacterial, anti-inflammatory and neuroprotective activities [3] .
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- HY-N1447
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-
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- HY-N2409
-
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Apoptosis
EGFR
JAK
STAT
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Cardiovascular Disease
Cancer
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Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC50: 1.3 μM), shutting down downstream signaling cascades [3] .
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- HY-50514
-
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JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
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Cancer
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AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo .
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- HY-N0732
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IAP
Akt
Caspase
NF-κB
TGF-beta/Smad
JAK
Bacterial
Apoptosis
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Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
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Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud with oral activity. Jolkinolide B downregulates XIAP, cIAP1, cIAP2, and phosphorylated Akt, upregulates Smac, activates caspase-3 and caspase-9, and inhibits NF-κB, TGFβ/smad3 and JAK/STAT3 pathways. Jolkinolide B exerts comprehensive biological effects including inducing cancer cell apoptosis, suppressing inflammatory responses, improving lung function, alleviating hepatic steatosis and eliminating intracellular Mycobacterium tuberculosis. Jolkinolide B can be used for the research of leukemia, histiocytic lymphoma, asthma, metabolic dysfunction-associated steatotic liver disease and tuberculosis [3] .
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- HY-153701S
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EnvudeucitINib; ESK-001
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JAK
Interleukin Related
IFNAR
Isotope-Labeled Compounds
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Inflammation/Immunology
|
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Envudeucitinibum (Envudeucitinib) is a highly selective, allosteric and orally active TYK2 inhibitor binding to the JH2 domain of TYK2. Envudeucitinibum has no off-target effects on other kinases (JAK1-3). Envudeucitinibum reduces signaling and production of proinflammatory cytokines including IL-12, IL-23, IL-17, and type I interferons (IFNs). Envudeucitinibum can be used for the research of plaque psoriasis, systemic lupus erythematosus (SLE), and other immune-mediated diseases .
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- HY-168894
-
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Ferroptosis
JAK
STAT
p38 MAPK
AMPK
GSK-3
Apoptosis
HSP
TNF Receptor
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
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CT-1 is a secreted protein belonging to the IL-6 cytokine family. Overexpression of CT-1 enhances cell proliferation, migration and angiogenesis via the ADMA/DDAH pathway. CT-1 inhibits the growth of triple-negative breast cancer cells by simultaneously inducing Ferroptosis in N2-type tumor-associated neutrophils and cancer cells. CT-1 activates the Jak/STAT-3, p42/p44 MAPK and AMPK pathways, and inhibits GSK-3β activity through phosphorylation to induce cardiomyocyte hypertrophy. CT-1 enhances the viability of cardiomyocytes and neurons, reduces cell Apoptosis, induces the expression of heat shock proteins (HSP) and BNP, and inhibits TNF levels. CT-1 exerts anti-tumor activity in mouse models of triple-negative breast cancer. CT-1 improves cognitive impairment in mice. CT-1 is applicable to the research of ischemic heart disease, triple-negative breast cancer, myocardial hypertrophy, Parkinson's disease, hypertensive heart disease, myocardial infarction, acute Chagas cardiomyopathy, high-fat diet-induced cognitive impairment and diabetes-related cognitive impairment [3] .
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- HY-145696
-
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PROTACs
JAK
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Inflammation/Immunology
Cancer
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SJ10542 is a potent and selective JAK2/3 PROTAC degrader. In PDX cells lSJBALL020589, SJ10542 has DC50 values of 14 and 11 nM for JAK2 and JAK3, respectively. SJ10542 exhibits antitumor activity and can be used for the research of hematological malignancies and autoimmune diseases . (Pink: Target protein ligand (HY-47073); Black: Linker (HY-W251248); Blue: E3 ligase ligand (HY-W890189); E3 ligase ligand+Linker (HY-176425))
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- HY-N0909
-
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20(S)-NotogINsenoside R2; GINsenoside Ng-R2
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Apoptosis
MEK
ERK
Reactive Oxygen Species (ROS)
Caspase
COX
β-catenin
Src
MDM-2/p53
JAK
STAT
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Notoginsenoside R2 (20(S)-Notoginsenoside R2; Ginsenoside Ng-R2) is an orally active notoginsenoside . Notoginsenoside R2 activates P90RSK and Nrf2 via the MEK1/2-ERK1/2 pathway to inhibit 6-OHDA-induced apoptotic damage in nerve cells. Notoginsenoside R2 upregulates SOX8/β-catenin by reducing miR-27a, thereby suppressing Aβ25-35-induced neuronal apoptosis and inflammatory responses . Notoginsenoside R2 alleviates lipid accumulation and mitochondrial dysfunction in diabetic nephropathy by inhibiting c-Src. Notoginsenoside R2 alleviates hepatic fibrosis by inducing hepatic stellate cell senescence and inhibiting the inflammatory microenvironment via JAK/STAT3 suppression . Notoginsenoside R2 can be used in research related to Parkinson's disease, Alzheimer's disease, diabetic nephropathy and hepatic fibrosis [3] .
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- HY-11067
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WHI-P97
1 Publications Verification
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JAK
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Inflammation/Immunology
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WHI-P97 is a potent and selective JAK-3 inhibitor. WHI-P97 is effective in preventing the development allergic asthma in vivo .
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- HY-40354S
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TasocitINib-13C3; CP-690550-13C3
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JAK
Apoptosis
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Inflammation/Immunology
Cancer
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Tofacitinib- 13C3 is the 13C-labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
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- HY-40354R
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TasocitINib (Standard); CP-690550 (Standard)
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Reference Standards
JAK
Apoptosis
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Inflammation/Immunology
Cancer
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Tofacitinib (Standard) is the analytical standard of Tofacitinib. This product is intended for research and analytical applications. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
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- HY-150538
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STAT
Apoptosis
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Cancer
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STAT3-IN-12 is a potent STAT3 signal inhibitor that can inhibit IL-6 induced JAK/STAT3 signalling pathway activation. STAT3-IN-12 inhibits cancer cell growth, migration, and induce cell apoptosis as well as cycle arrest. STAT3-IN-12 can be used in cancer-related research, such as hepatocellular carcinoma (HCC) and oesophageal carcinoma .
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- HY-120920
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Dopamine Receptor
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Inflammation/Immunology
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UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions .
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- HY-N0143A
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FloridzIN dihydrate
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SGLT
PI3K
Akt
GLUT
NF-κB
JAK
STAT
Caspase
Apoptosis
DNA/RNA Synthesis
mTOR
Bacterial
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Infection
Neurological Disease
Metabolic Disease
Cancer
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Phlorizin (Floridzin) dihydrate is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC50 of 0.04 μM and a Ki of 39 nM against hSGLT2, and an IC50 of 0.17 μM and a Ki of 0.31 μM against hSGLT1. Phlorizin dihydrate promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin dihydrate reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin dihydrate induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin dihydrate also exhibits antibacterial, anti-inflammatory and neuroprotective activities [3] .
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- HY-156621
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JAK
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Inflammation/Immunology
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Lepzacitinib is a Janus kinase inhibitor targeting to JAK 1/3. Lepzacitinib exhibits anti-inflammatory effect and inhibits atopic dermatitis and other skin diseases .
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- HY-153190
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W1131
1 Publications Verification
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Oxidative Phosphorylation
STAT
Ferroptosis
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Cancer
|
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W1131 is a potent STAT3 inhibitor, triggering ferroptosis. W1131 suppresses cancer progression in gastric cancer cell subcutaneous xenograft model, organoids model, and PDX model. W1131 effectively alleviates chemical resistance of cancer cells to 5-FU (HY-90006). W1131 regulates cell cycle, DNA damage response, and oxidative phosphorylation, including IL6-JAK-STAT3 pathway and ferroptosis pathway .
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- HY-178500
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Deubiquitinase
Apoptosis
STAT
JAK
Akt
PI3K
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Cancer
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WCY-8-67 is an orally active and selective USP5 inhibitor, with an IC50 value of 1.33 μM. WCY-8-67 induces apoptosis and suppresses JAK/STAT3 and PI3K/AKT signaling pathways in vitro. WCY-8-67 inhibits proliferation of AE-positive AML cells, induces G1 phase arrest and differentiation of AML cells. WCY-8-67 demonstrates potent anti-leukemic efficacy in mice. WCY-8-67 can be used for the study of acute myeloid leukemia .
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- HY-N7694
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TGF-β Receptor
JAK
STAT
Apoptosis
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Inflammation/Immunology
Cancer
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Isotoosendanin is an orally active TGFβR1 inhibitor and abrogating its kinase activity (IC50 = 6732 nM). Isotoosendanin inhibits the JAK/STAT3 signaling pathway by directly targeting SHP-2, enhancing its stability, and reducing its ubiquitination. Isotoosendanin inhibits TGF-β-induced reduces the migration, invasion, and metastasis in triple-negative breast cancer (TNBC) cells. Isotoosendanin exhibits anti-tumor efficacy in TNBC xenograft models and A549 xenograft tumors. Isotoosendanin exhibits significant anti-inflammatory effects in acetic acid-induced vascular permeability and λ-carrageenan-induced hind paw edema tests. Isotoosendanin can be used for the study of non-small cell lung cancer (NSCLC), TNBC and inflammation [3].
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- HY-111750
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JAK
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Inflammation/Immunology
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JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively .
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- HY-151285
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Apoptosis
JAK
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Inflammation/Immunology
Cancer
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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 .
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- HY-151259
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JAK
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Cancer
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TK4b is a dual JAK2/3 inhibitor with human JAK2 and JAK3 IC50s of 19.40 nM and 18.42 nM, respectively. TK4b can be used for the research of leukemia and myelofibrosis .
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- HY-40354S1
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- HY-178500A
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Deubiquitinase
Apoptosis
STAT
JAK
Akt
PI3K
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Cancer
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WCY-8-67 TFA is an orally active and selective USP5 inhibitor, with an IC50 value of 1.33 μM. WCY-8-67 TFA induces apoptosis and suppresses JAK/STAT3 and PI3K/AKT signaling pathways. WCY-8-67 TFA inhibits proliferation of AE-positive AML cells, induces G1 phase arrest and differentiation of AML cells. WCY-8-67 TFA demonstrates potent anti-leukemic efficacy in mice. WCY-8-67 TFA can be used for the study of acute myeloid leukemia .
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- HY-120457
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JAK
STAT
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Inflammation/Immunology
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WYE-151650 is a selective JAK-3 inhibitor. WYE-151650 suppresses IL-2-induced STAT-5 phosphorylation and cell proliferation mediated by JAK-3. WYE-151650 is promising for research of autoimmune diseases .
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- HY-N1447R
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Reference Standards
Apoptosis
Autophagy
Endogenous Metabolite
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Cancer
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Ganoderic acid A (Standard) is the analytical standard of Ganoderic acid A. This product is intended for research and analytical applications. Ganoderic acid A can inhibit of the JAK-STAT3 signaling pathway, also inhibit proliferation, viability, ROS.
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- HY-107459
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(E/Z)-TyrphostIN AG490; (E/Z)-TyrphostIN B42
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EGFR
STAT
JAK
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Cancer
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(E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
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- HY-10058
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JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
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Cancer
|
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AT9283 lactic acid is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 lactic acid inhibits growth and survival of multiple solid tumors in vitro and in vivo .
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- HY-107595
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SD-1008
1 Publications Verification
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JAK
STAT
Apoptosis
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Cancer
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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 .
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- HY-N2409R
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Apoptosis
EGFR
JAK
STAT
Reference Standards
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Cardiovascular Disease
Cancer
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Delphinidin (chloride) (Standard) is the analytical standard of Delphinidin (chloride). This product is intended for research and analytical applications. Delphinidin chloride is an anthocyanin isolated from berries and red wine. Delphinidin chloride exhibits endothelium-dependent vasodilation and anticancer activity. Delphinidin chloride also modulates JAK/STAT3 and MAPK signaling, thereby inducing apoptosis in HCT116 cells. Delphinidin chloride is also a potent inhibitor of EGFR (IC50: 1.3 μM), shutting down downstream signaling cascades [3] .
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- HY-175771
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STAT
c-Myc
Bcl-2 Family
Interleukin Related
JAK
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Cancer
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STAT3-IN-46 is a selective and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3) (KD = 323.3 nM). STAT3-IN-46 directly binds to the SH2 domain of the STAT3 and inhibits IL-6/JAK/STAT3 signaling pathway (IC50 = 0.87 μM) and downregulates c-Myc and Bcl-2 levels. STAT3-IN-46 can be used for the research of cancer, such as triple-negative breast cancer .
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- HY-176876
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Glucocorticoid Receptor
Interleukin Related
JAK
STAT
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Inflammation/Immunology
|
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Glucocorticoid receptor/IL-6-IN-1 (Compound 35) is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and IL-6 signaling pathway (IC50 values of 120 nM and 59 nM, respectively). Glucocorticoid receptor/IL-6-IN-1 inhibits IL-6-induced JAK/STAT3 phosphorylation, blocking inflammatory cytokine transcription. Glucocorticoid receptor/IL-6-IN-1 is promising for research of inflammatory diseases like rheumatoid arthritis and asthma .
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- HY-153858
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Raf
Discoidin Domain Receptor
MEK
TNF Receptor
Interleukin Related
JAK
STAT
Ras
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Cancer
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PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma .
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- HY-10652
-
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JAK
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Inflammation/Immunology
Cancer
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JAK-2/3-IN-1 is a potent JAK-2 and JAK-3 inhibitor extracted from patent US8163732B2, compound 46, has Kis of <250 nM for both isoforms .
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- HY-N12473
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JAK
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Inflammation/Immunology
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25-Deacetylcucurbitacin A is a Cucurbitane-Type triterpenoid and has the potential to be an anti-cancer agent and JAK/STAT3 signaling pathway inhibitor .
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- HY-151256
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JAK
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Cancer
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JAK-2/3-IN-2 (Compound 3h) is a JAK2 and JAK3 inhibitor with IC50s of 23.85 nM and 18.9 nM, respectively .
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- HY-40354S3
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- HY-40354S5
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- HY-103438A
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Apoptosis
Autophagy
Akt
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Cancer
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BIBU1361 dihydrochloride induces apoptosis and inhibits autophagy. BIBU1361 inhibits pro-survival pathways Akt/mTOR and gp130/JAK/STAT3, and decreased levels of pro-inflammatory cytokine IL-6 .
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- HY-103438
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Apoptosis
Akt
Autophagy
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Cancer
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BIBU1361 induces apoptosis and inhibits autophagy. BIBU1361 inhibits pro-survival pathways Akt/mTOR and gp130/JAK/STAT3, and decreased levels of pro-inflammatory cytokine IL-6 .
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- HY-40354S2
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- HY-E70789
-
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RET
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Others
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BCR-RET Recombinant Human Active Protein Kinase is a BCR-RET fusion protein in hematopoietic malignancies. BCR-RET overactivates the Ras-ERK pathway, in addition to JAK/STAT3 and PI3K/AKT pathways .
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- HY-50514R
-
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JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
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Cancer
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AT9283 (Standard) is the analytical standard of AT9283. This product is intended for research and analytical applications. AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo .
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- HY-153190A
-
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Ferroptosis
STAT
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Cancer
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W1131 TFA is a potent STAT3 inhibitor that induces ferroptosis. W1131 inhibits cancer progression in subcutaneous xenograft, organoid, and PDX models of gastric cancer. W1131 effectively alleviates cancer cell chemoresistance to 5-FU (HY-90006). W1131 regulates the cell cycle, DNA damage response, and oxidative phosphorylation, including the IL6-JAK-STAT3 pathway and the ferroptosis pathway .
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- HY-N0143R
-
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FloridzIN (Standard)
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Reference Standards
Caspase
JAK
GLUT
STAT
Apoptosis
Bacterial
SGLT
mTOR
Akt
NF-κB
PI3K
DNA/RNA Synthesis
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Infection
Neurological Disease
Metabolic Disease
Cancer
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Phlorizin (Floridzin) (Standard) is the analytical standard of Phlorizin. This product is intended for research and analytical applications. Phlorizin is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC50 of 0.04 μM and a Ki of 39 nM against hSGLT2, and an IC50 of 0.17 μM and a Ki of 0.31 μM against hSGLT1. Phlorizin promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin also exhibits antibacterial, anti-inflammatory and neuroprotective activities [3] .
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- HY-N0732R
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Reference Standards
IAP
Akt
Caspase
NF-κB
TGF-beta/Smad
JAK
Bacterial
Apoptosis
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Infection
Inflammation/Immunology
Cancer
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Jolkinolide B (Standard) is the analytical standard of Jolkinolide B (HY-N0732). This product is intended for research and analytical applications. Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud with oral activity. Jolkinolide B downregulates XIAP, cIAP1, cIAP2, and phosphorylated Akt, upregulates Smac, activates caspase-3 and caspase-9, and inhibits NF-κB, TGFβ/smad3 and JAK/STAT3 pathways. Jolkinolide B exerts comprehensive biological effects including inducing cancer cell apoptosis, suppressing inflammatory responses, improving lung function, alleviating hepatic steatosis and eliminating intracellular Mycobacterium tuberculosis. Jolkinolide B can be used for the research of leukemia, histiocytic lymphoma, asthma, metabolic dysfunction-associated steatotic liver disease and tuberculosis [3] .
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- HY-123939
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JAK
ROCK
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Cardiovascular Disease
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JAK1/3-IN-1 is a selective, orally active JAK1/3 inhibitor with IC50 values of 1.9 nM and 0.9 nM, respectively. JAK1/3-IN-1 significantly reduces the mean arterial blood pressure and significantly increases the heart rate in rabbits. JAK1/3-IN-1 decreases the mean arterial blood pressure in conscious telemetered rats and induces lethal cardiovascular effects .
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- HY-107459R
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(E/Z)-TyrphostIN AG490 (Standard); (E/Z)-TyrphostIN B42 (Standard)
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Reference Standards
EGFR
STAT
JAK
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Cancer
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(E/Z)-AG490 (Standard) is the analytical standard of (E/Z)-AG490 (HY-107459). This product is intended for research and analytical applications. (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine Kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
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- HY-181514
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STAT
CDK
c-Myc
Apoptosis
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Cancer
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STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a Kd value of 6.16 μM. STAT3-IN-53 binds directly to the SH2 domain of STAT3, inhibits phosphorylation at the Y705 site without affecting the total STAT3 protein level, and suppresses the IL-6/JAK/STAT3 pathway. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc. STAT3-IN-53 induces cell cycle arrest and promotes Apoptosis. STAT3-IN-53 exhibits anticancer activity against colorectal cancer .
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- HY-179715
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PROTACs
JAK
TNF Receptor
Interleukin Related
STAT
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Inflammation/Immunology
|
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PROTAC JAK1/2 degrader-1 (Compound A8) is a selective JAK1/2 PROTAC degrader, with DC50 values of 1.4 μM for JAK1 and 0.92 μM for JAK2. PROTAC JAK1/2 degrader-1 significantly inhibits the release of NO, IL-6 (IC50 = 12.89 μM) and TNF-α (IC50 = 17.17 μM). PROTAC JAK1/2 degrader-1 significantly alleviates inflammatory responses and colonic damage by inhibiting the JAK/STAT3 signaling pathway. PROTAC JAK1/2 degrader-1 can be used for research on colitis. (Pink: JAK1/2 ligand (HY-179716); Blue: CRBN ligand (HY-10984); Black: linker; CRBN ligand + linker (HY-131888A)) .
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| Cat. No. |
Product Name |
Type |
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- HY-N0143A
-
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FloridzIN dihydrate
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Biochemical Assay Reagents
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Phlorizin (Floridzin) dihydrate is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC50 of 0.04 μM and a Ki of 39 nM against hSGLT2, and an IC50 of 0.17 μM and a Ki of 0.31 μM against hSGLT1. Phlorizin dihydrate promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin dihydrate reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin dihydrate induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin dihydrate also exhibits antibacterial, anti-inflammatory and neuroprotective activities [3] .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N0143
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- HY-N1447
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- HY-N2409
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- HY-N0732
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Structural Classification
Euphorbia fischeriana Steud.
Classification of Application Fields
Terpenoids
Diterpenoids
Euphorbiaceae
Plants
Disease Research Fields
Cancer
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IAP
Akt
Caspase
NF-κB
TGF-beta/Smad
JAK
Bacterial
Apoptosis
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Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud with oral activity. Jolkinolide B downregulates XIAP, cIAP1, cIAP2, and phosphorylated Akt, upregulates Smac, activates caspase-3 and caspase-9, and inhibits NF-κB, TGFβ/smad3 and JAK/STAT3 pathways. Jolkinolide B exerts comprehensive biological effects including inducing cancer cell apoptosis, suppressing inflammatory responses, improving lung function, alleviating hepatic steatosis and eliminating intracellular Mycobacterium tuberculosis. Jolkinolide B can be used for the research of leukemia, histiocytic lymphoma, asthma, metabolic dysfunction-associated steatotic liver disease and tuberculosis [3] .
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- HY-N0909
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- HY-N7694
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- HY-N1447R
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-
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- HY-N2409R
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- HY-N12473
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-
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- HY-N0143R
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- HY-N0732R
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Structural Classification
Euphorbia fischeriana Steud.
Terpenoids
Diterpenoids
Euphorbiaceae
Plants
|
Reference Standards
IAP
Akt
Caspase
NF-κB
TGF-beta/Smad
JAK
Bacterial
Apoptosis
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Jolkinolide B (Standard) is the analytical standard of Jolkinolide B (HY-N0732). This product is intended for research and analytical applications. Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud with oral activity. Jolkinolide B downregulates XIAP, cIAP1, cIAP2, and phosphorylated Akt, upregulates Smac, activates caspase-3 and caspase-9, and inhibits NF-κB, TGFβ/smad3 and JAK/STAT3 pathways. Jolkinolide B exerts comprehensive biological effects including inducing cancer cell apoptosis, suppressing inflammatory responses, improving lung function, alleviating hepatic steatosis and eliminating intracellular Mycobacterium tuberculosis. Jolkinolide B can be used for the research of leukemia, histiocytic lymphoma, asthma, metabolic dysfunction-associated steatotic liver disease and tuberculosis [3] .
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-
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-153701S
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Envudeucitinibum (Envudeucitinib) is a highly selective, allosteric and orally active TYK2 inhibitor binding to the JH2 domain of TYK2. Envudeucitinibum has no off-target effects on other kinases (JAK1-3). Envudeucitinibum reduces signaling and production of proinflammatory cytokines including IL-12, IL-23, IL-17, and type I interferons (IFNs). Envudeucitinibum can be used for the research of plaque psoriasis, systemic lupus erythematosus (SLE), and other immune-mediated diseases .
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- HY-40354S
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Tofacitinib- 13C3 is the 13C-labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
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- HY-40354S1
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Tofacitinib- 13C3, 15N (Tasocitinib- 13C3, 15N) is 13C and 15N labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
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- HY-40354S3
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Tofacitinib- 13C (Tasocitinib- 13C) is 13C labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
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- HY-40354S5
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Tofacitinib-d3 (Tasocitinib-d3) is deuterium labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
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- HY-40354S2
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Tofacitinib- 13C,d3 (Tasocitinib- 13C,d3) is 13C labeled Tofacitinib. Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
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