Search Result
Results for "
activator
" in MCE Product Catalog:
2752
Inhibitors & Agonists
31
Biochemical Assay Reagents
201
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-148313
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-
- HY-144287
-
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- HY-125996
-
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NR1H4 activator 1
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FXR
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Inflammation/Immunology
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NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.
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- HY-148480
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- HY-139791
-
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KCNQ2/3 activator-1
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Potassium Channel
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Cancer
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KCNQ2/3 activator-1 is an activator of Kv7.2/Kv7.3 (KCNQ2/3) potassium channel. KCNQ2/3 activator-1 has the potential in relieving pain (the main problem from medical treatment) (extracted from patent WO2021113757A1, compound A).
|
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- HY-147037
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AMPK activator 7
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AMPK
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Metabolic Disease
Cardiovascular Disease
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AMPK activator 7 (compound I-3-24) is a an AMPK activator with the EC50 of 8.8 nM. AMPK activator 7 can be used for the research of diseases involving AMPK, particularly diseases such as type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia and/or hypertension.
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- HY-145390
-
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Nrf2 activator-1
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Keap1-Nrf2
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Inflammation/Immunology
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Nrf2 activator-1 is a potent activator of NF-E2 related factor 2 (Nrf2). Nrf2 activator-1 has the potential for the research of COPD and other respiratory diseases, including asthma, Acute Lung Injury (ALI), Acute Respiratory Distress Syndrome (ARDS) and pulmonary fibrosis (extracted from patent WO2018109647A1).
|
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- HY-P0078
-
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TRAP-6
PAR-1 agonist peptide; Thrombin Receptor activator Peptide 6
|
Protease Activated Receptor (PAR)
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Inflammation/Immunology
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TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4.
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- HY-152943
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- HY-148684
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AMPK activator 10
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AMPK
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Metabolic Disease
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AMPK activator 10 is an orally active, potent AMPK activator with EC150 of 44.3 nM by cell-ELISA. AMPK activator 10 increases the phosphorylation levels of ACC. AMPK activator 10 exhibits a glucose lowering effect.
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- HY-101788
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- HY-152264
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- HY-146109
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RyRs activator 1
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Parasite
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Infection
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RyRs activator 1 (compound 7f) is a potent activator of ryanodine receptors (RyRs). RyRs activator 1 at 0.5 mg/L displays 100% larvicidal activity. The larvicidal activity of RyRs activator 1 is 90% at 0.01 mg/L.
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- HY-153354
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- HY-131334
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AMPK activator 4
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AMPK
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Metabolic Disease
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AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.
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- HY-135825
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TFEB activator 1
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Autophagy
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Neurological Disease
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TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
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- HY-146110
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RyRs activator 2
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Parasite
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Infection
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RyRs activator 2 (compound 7o) is a potent activator of ryanodine receptors (RyRs). RyRs activator 2 is 30% larvicidal activity, comparable to chlorantraniliprole (30%) and better than cyantraniliprole (10%).
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- HY-139674
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- HY-134477
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NF-κΒ activator 2
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NF-κB
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Neurological Disease
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NF-κΒ activator 2 is a potent and orally active NF-ҡB activator, with an EC50 of 1.58 μM. NF-κΒ activator 2 induces SOD2 through increasing NF-ҡB expression and activation. NF-κΒ activator 2 can be used for the research of amyotrophic lateral sclerosis (ALS).
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- HY-104038
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- HY-148210
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AMPK activator 9
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AMPK
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Metabolic Disease
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AMPK activator 9 (ZM-6) is a potent AMPK (α2β1γ1) activator with an EC50 value of 1.1 µM. AMPK activator 9 has the potential for the research of type 2 diabetes.
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- HY-147397
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PKM2 activator 3
|
Pyruvate Kinase
|
Cancer
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PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer.
(AC50: the concentration which gives 50% activation of enzyme.)
|
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- HY-13971
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- HY-135884
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- HY-134476
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- HY-148404
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p53 Activator 5
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MDM-2/p53
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Cancer
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p53 Activator 5 (compound 134A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 5 can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA. p53 Activator 5 shows anti-tumor activity.
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- HY-148402
-
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p53 Activator 3
|
MDM-2/p53
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Cancer
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p53 Activator 3 (compound 87A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 3 can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA. p53 Activator 3 shows anti-tumor activity.
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- HY-111317
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SIRT1 activator 3
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Sirtuin
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Metabolic Disease
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SIRT1 activator 3 is a potent activator of Sirt1 and suppresses TNF-α in a dose-dependent manner. SIRT1 activator 3 has the potential for anti-obesity or anti-diabetic researches.
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- HY-19702
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- HY-148324
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PKM2 activator 5
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Pyruvate Kinase
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Cancer
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PKM2 activator 5 (compound 8) is a PKM2 activator with an AC50 value of 0.316 µM. PKM2 activator 5 has the potential to alter the aberrant metabolism of cancer cells.
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- HY-135883
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- HY-U00292
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- HY-146398
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AMPK activator 6
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AMPK
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Metabolic Disease
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AMPK activator 6 (Compound GC) reduces lipid content and activates the AMPK pathway in HepG2 and 3T3-L1 cells. AMPK activator 6 significantly suppresses the increase in triglyceride (TG) , total cholesterol (TC), low-density lipoprotein-C (LDL-C), and other biochemical indices in blood serum. AMPK activator 6 can be used for the research of non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome.
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- HY-124873
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SERCA2a activator 1
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Calcium Channel
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Cardiovascular Disease
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SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.
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- HY-139692
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EAAT2 activator 1
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EAAT2
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Neurological Disease
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EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently.
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- HY-12647
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- HY-143316
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NPR-C activator 1
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Others
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Neurological Disease
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NPR-C activator 1 (Compound 1) is a potent activator of natriuretic peptide receptor C (NPR-C). C-type natriuretic peptide (CNP) is involved in the regulation of vascular homeostasis. NPR-C activator 1 is identified as a potent agonist (EC50 ∼ 1 μM) with promising in vivo pharmacokinetic properties.
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- HY-152756
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Caspase-3/7 activator 2
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Apoptosis
Caspase
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Cancer
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Caspase-3/7 activator 2 is an effective activator of Caspase-3/7. Caspase-3/7 activator 2 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability.
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- HY-152748
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Caspase-3/7 activator 1
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Apoptosis
Caspase
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Cancer
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Caspase-3/7 activator 1 is an effective activator of Caspase-3/7. Caspase-3/7 activator 1 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability.
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- HY-152758
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Caspase-3/7 activator 3
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Apoptosis
Caspase
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Cancer
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Caspase-3/7 activator 3 is an effective activator of Caspase-3/7. Caspase-3/7 activator 3 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability.
|
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- HY-128574
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- HY-147368
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PKM2 activator 2
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Pyruvate Kinase
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Cancer
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PKM2 activator 2 is a pyruvate kinase M2 (PKM2) activitor with an AC50 value of 66 nM. PKM2 activator 2 may show anti-tumor proliferation effect and relieve the Warburg effect, while PKM2 activation can restore normal glycolytic metabolism in cells.
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- HY-147038
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AMPK activator 8
|
AMPK
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Metabolic Disease
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AMPK activator 8 (compound 2) is an AMP-activated protein kinase (AMPK) activator with EC50s of 11, 27, 4, 2, and 4 nM for rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ1, rAMPK α2β2γ3, respectively. AMPK activator 8 can be used for the research of type 2 diabetes.
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- HY-136073
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- HY-148416
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p53 Activator 7
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MDM-2/p53
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Cancer
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p53 Activator 7 is a p53 mutation Y220C (MDM-2/p53) activator with an EC50 of 104 nM. p53 Activator 7 can bind to p53 mutant and restore its ability to bind DNA (WO2022213975A1; Example B-1).
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- HY-135516
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Wnt pathway activator 1
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Wnt
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Cancer
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Wnt pathway activator 1 is a potent Wnt activator extracted from patent WO2012024404A1, compound 1, has an EC50s of 28-29 nM.
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- HY-151203
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PKG1α activator 3
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Others
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Cardiovascular Disease
|
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PKG1α activator 3 is a PKG1α activator (EC50 basal/partial=13/0.52 μM). PKG1α activator 3 shows anti-proliferative effects to smooth muscle cell, and can be used in cardiovascular disease research.
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- HY-148948
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Nampt activator-3
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NAMPT
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Neurological Disease
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NAMPT activator-3, a NAT derivative, is a NAMPT activator with an EC50 of 2.6 μM and a KD of 132 nM. NAMPT activator-3 effectively protects cultured cells from FK866 (HY-50876)-mediated toxicity. NAMPT activator-3 exhibits strong neuroprotective efficacy in a chemotherapy-induced peripheral neuropathy (CIPN) mouse model without any overt toxicity.
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- HY-147831
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EIF2α activator 1
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Eukaryotic Initiation Factor (eIF)
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Cancer
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EIF2α activator 1 (Compound 40) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 1 increases the expression level of eIF2α downstream proteins, ATF and CHOP. EIF2α activator 1 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.00 and 19.3 μM, respectively.
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- HY-147832
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EIF2α activator 2
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Eukaryotic Initiation Factor (eIF)
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Cancer
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EIF2α activator 2 (Compound 1) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 2 exhibits high potency in SRB cell proliferation assays (IC50=0.46 μM). EIF2α activator 2 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.79 and 10.52 μM, respectively.
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- HY-111671
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SOS1 activator 1
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Ras
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Cancer
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SOS1 activator 1 (Compound 64) is a potent activator of SOS1-mediated nucleotide exchange with a Kd of 44 nM. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP for GTP on RAS.
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- HY-122760
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- HY-150602
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20S Proteasome activator 1
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Proteasome
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Neurological Disease
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20S Proteasome activator 1 is a potent 20S proteasome activator with EC200 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases.
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- HY-146095
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p53 Activator 2
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MDM-2/p53
DNA/RNA Synthesis
Apoptosis
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Cancer
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p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models.
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- HY-148815
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- HY-151430
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- HY-148822
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Nampt activator-2
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NAMPT
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Neurological Disease
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Nampt activator-2 (compound 34) is a potent NAMPT activator, with EC50 of 0.023 μM. Nampt activator-2 shows moderate activity against CYP2C9 (0.060 μM), 2D6 (0.41 μM) and 2C19 (0.59 μM).
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- HY-145992
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- HY-146086
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- HY-149244
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Nrf2 activator-7
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Keap1-Nrf2
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Others
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Nrf2 activator-7 (Compound 12b) is a potent Nrf2 activator and significantly activates the Nrf2 signaling pathway in NCM460D cells.
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- HY-130723
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AMPK activator 2
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AMPK
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Cancer
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AMPK activator 2 (compound 7a), a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549).
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- HY-148751
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TRPV1 activator-1
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TRP Channel
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Cancer
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TRPV1 activator-1 (compound 8), a capsaicin analog, has an altered neck structure. TRPV1 activator-1 interacts specifically with T551 residue.
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- HY-145879
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Nrf2 activator-2
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Keap1-Nrf2
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Cancer
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Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells.
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- HY-151431
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Nrf2/HO-1 activator 2
|
Keap1-Nrf2
Reactive Oxygen Species
ERK
Akt
JNK
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Neurological Disease
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Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD).
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- HY-146168
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Nrf2 activator-5
|
Keap1-Nrf2
|
Inflammation/Immunology
|
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Nrf2 activator-5 (compound 1) is a potent Nrf2 activator that can attenuate H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglial cells. Nrf2 activator-5 exhibits antioxidant and anti-inflammatory activities.
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- HY-144231
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SIK1 activator 1
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Others
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Metabolic Disease
|
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SIK1 activator 1 exhibited remarkable inhibitory activity on hepatic gluconeogenesis by enhancing the SIK1 phosphorylation and ameliorated the hyperglyceamia of type 2 diabetic mice.
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- HY-126429
-
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Nav1.1 activator 1
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Sodium Channel
|
Neurological Disease
|
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Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant τ of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.
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- HY-144828
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- HY-U00280
-
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Potassium Channel Activator 1
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Others
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Neurological Disease
|
|
Potassium Channel Activator 1 is an agent for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, such as one or more disorders or conditions independently selected from the group consisting of: schizophrenia and other psychotic states; mood disorders ADHD; aggression; movement disorders.
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- HY-148752
-
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- HY-146173
-
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- HY-148712
-
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SIRT6 activator 12q
|
Apoptosis
Sirtuin
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Cancer
|
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SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC50 values of 171.20, >200, >200, >200, 0.58 μM for SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, respectively. SIRT6 activator 12q inhibits cell growth and migration. SIRT6 activator 12q induces Apoptosis and cell cycle arrest at G2 phase. SIRT6 activator 12q shows anticancer activity.
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- HY-151527
-
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PI3K/Akt/CREB activator 1
|
Akt
PI3K
Epigenetic Reader Domain
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Neurological Disease
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PI3K/Akt/CREB activator 1 (compound AE-18) is a potent, orally active PI3K/Akt/CREB activator. PI3K/Akt/CREB activator 1 promotes neuronal proliferation, induced differentiation of Neuro-2a cells into a neuron-like morphology, and accelerated the establishment of axon-dendrite polarization of primary hippocampal neurons through upregulating brain-derived neurotrophic factor via the PI3K/Akt/CREB pathway. PI3K/Akt/CREB activator 1 can be used in research of vascular dementia (VaD).
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- HY-146174
-
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- HY-18377
-
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Bioymifi
DR5 activator
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TNF Receptor
Apoptosis
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Cancer
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Bioymifi (DR5 Activator), a potent TRAIL receptor DR5 activator, binds to the extracellular domain (ECD) of DR5 with a Kd of 1.2 μM. Bioymifi can act as a single agent to induce DR5 clustering and aggregation, leading to apoptosis.
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- HY-123962
-
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G6PD activator AG1
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Others
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Metabolic Disease
|
|
G6PD activator AG1 is a potent and selective glucose-6-phosphate dehydrogenase (G6PD) activator with an EC50 of 3 µΜ. G6PD activator AG1 reduces hemolysis of human erythrocytes.
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- HY-15098
-
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Apoptozole
Apoptosis activator VII
|
HSP
Apoptosis
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Cancer
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Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14 μM, respectively, and can induce apoptosis.
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- HY-106199
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- HY-P1328
-
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TAT-14
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Keap1-Nrf2
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Others
|
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TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
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- HY-P1536
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- HY-115627
-
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PKUMDL-LC-101-D04
GPX4-activator-1d4
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Glutathione Peroxidase
|
Inflammation/Immunology
|
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PKUMDL-LC-101-D04 (GPX4-Activator-1d4) is a potent ferroptosis regulator glutathione peroxidase 4 (GPX4) allosteric activator (pEC50=4.7). PKUMDL-LC-101-D04 increases GPX4 activity to 150% at 20 μM in the cell-free assay and 61 μM in cell extracts.
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- HY-P1328A
-
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TAT-14 TFA
|
Keap1-Nrf2
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Others
|
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TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
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- HY-108904
-
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Urokinase (peptidolytic)
Urokinase-type plasminogen activator; Uronase; Win 22005; Win-Kinase
|
Ser/Thr Protease
|
Cancer
Cardiovascular Disease
|
|
Urokinase peptidolytic (Urokinase-type plasminogen activator) is a serine protease, an inactive form (zymogen) of the serine protease plasminogen. Activation of plasmin triggers a proteolytic cascade reaction, which in turn participates in thrombolysis or extracellular matrix degradation, implicated in vascular disease and cancer-related research.
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- HY-133987
-
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AP-1/NF-κB activation inhibitor 1
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NF-κB
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Inflammation/Immunology
|
|
AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
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- HY-145983
-
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Suc-Gly-Pro-AMC
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FAP
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Cancer
|
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Suc-Gly-Pro-AMC is a fibroblast activation protein (FAP)-specific substrate. Suc-Gly-Pro-AMC can be used to study the activity of FAP.
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- HY-10072
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- HY-112472
-
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S3969
|
Sodium Channel
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Metabolic Disease
|
|
S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). The apparent EC50 for S3969 activation of hENaC is 1.2 μm.
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- HY-121320
-
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Raptinal
|
Caspase
Apoptosis
|
Cancer
|
|
Raptinal, a agent that directly activates caspase-3, initiates intrinsic pathway caspase-dependent apoptosis. Raptinal is able to rapidly induce cancer cell death by directly activating the effector caspase-3, bypassing the activation of initiator caspase-8 and caspase-9.
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- HY-106029
-
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4α-TPA
α-TPA
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Others
|
Cancer
|
|
4α-TPA is an inactive form of TPA, and is used as a negative control for TPA-activated events.
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- HY-W187305
-
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MASM7
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Others
|
Others
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|
MASM7 is a mitofusin activator, and can achieve mitochondrial fusion via mitofusins. MASM7 can increase Mito AR with an EC50 value of 75 nM in MEFs in concentration-responsively, and can promote mitochondrial fusion by directly activating MFN2 or MFN. MASM7 also demonstrates direct binding to the HR2 domain of MFN2 with Kd value of 1.1 μM.
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- HY-N1033
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-
- HY-122098
-
-
- HY-A0144
-
-
- HY-141432
-
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Cbl-b-IN-3
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Cbl-b-IN-3 (Compound 23) is a casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 of < 1 nM. Cbl-b is an E3 ubiquitin ligase that negatively regulates T-cell activation.
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- HY-139553
-
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Zunsemetinib
ATI-450; CDD-450
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MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases.
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- HY-10255AS
-
|
Sunitinib-d10
SU 11248-d10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
|
-
- HY-19345
-
|
Vacquinol-1
NSC13316
|
Others
|
Cancer
|
|
Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates MAPK pathways. Vacquinol-1 specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model. Vacquinol-1 also induces apoptosis in hepatocellular carcinoma (HCC)cell.
|
-
- HY-19345A
-
|
Vacquinol-1 dihydrochloride
NSC13316 dihydrochloride
|
Others
|
Cancer
|
|
Vacquinol-1 (NSC13316) dihydrochloride is a MKK4-specific activator that activates MAPK pathways. Vacquinol-1 dihydrochloride specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model. Vacquinol-1 dihydrochloride also induces apoptosis in hepatocellular carcinoma (HCC)cell.
|
-
- HY-147057A
-
|
FAP-2286 acetate
|
FAP
|
Cancer
|
|
FAP-2286 acetate is the conjugate of a fibroblast activation protein (FAP)-binding peptide. FAP-2286 acetate can be labeled with radionuclides for diagnostic applications. FAP-2286 acetate has antitumor activity.
|
-
- HY-107753
-
|
XRP44X
|
Ras
|
Cancer
Inflammation/Immunology
|
|
XRP44X inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2. XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules.
|
-
- HY-117958
-
|
HJC0197
|
Ras
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
|
-
- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-N8218
-
-
- HY-147311
-
-
- HY-W019721
-
|
Cyclosporin D
|
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
|
Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A. Cyclosporin A is a potent immunosuppressant agent, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc).
|
-
- HY-147204
-
|
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE
|
Others
|
Cancer
|
|
Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE (compound S6) is a potent anticancer agent, which can be specific activated by tumor microenvironment. Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE can suppress tumor growth in mice (extracted from patent CN104147612A).
|
-
- HY-102011
-
|
BMS-1166
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
|
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-113313
-
|
Aldosterone
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
|
-
- HY-139303
-
|
LUF5771
|
Others
|
Endocrinology
|
|
LUF5771 is a potent allosteric recombinant luteinizing hormone (recLH) and Org 43553 inhibitor. LUF5771 is able to partially activate the LH receptor with low efficacy.
|
-
- HY-111516
-
-
- HY-114981
-
|
SRTCX1002
|
Sirtuin
|
Inflammation/Immunology
|
|
SRTCX1002 is a potent activator of SIRT1 (STAC), suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB Activity. SRTCX1002 suppresses stimuli-induced NF-κB transcriptional activation and LPS-induced TNFα secretion with IC50s of 0.71 and 7.58 µM, respectively.
|
-
- HY-103349
-
|
PETCM
|
Caspase
Apoptosis
|
Cancer
|
|
PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.
|
-
- HY-15870
-
|
SR 11302
|
AP-1
|
Cancer
Inflammation/Immunology
|
|
SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).
|
-
- HY-N9615
-
-
- HY-117917
-
-
- HY-13856
-
|
(R)-PS210
|
PDK-1
|
Cancer
|
|
(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC50 value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.
|
-
- HY-124702
-
|
ICA-105574
|
Potassium Channel
|
Cardiovascular Disease
|
|
ICA-105574 is a potent and efficacious hERG channel activator. The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation. ICA-105574 steeply potentiates current amplitudes more than 10-fold with an EC50 value of 0.5 +/- 0.1 μM and a Hill slope (n(H)) of 3.3 +/- 0.2.
|
-
- HY-16785
-
|
Veledimex
INXN-1001; RG-115932
|
Interleukin Related
|
Cancer
Inflammation/Immunology
|
|
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys.
|
-
- HY-P99482
-
|
Blisibimod
A 623; AMG 623
|
TNF Receptor
|
Inflammation/Immunology
|
|
Blisibimod (A 623) is a potent and selective tetravalent inhibitor of B-cell activating factor (BAFF). Blisibimod can be used for the research of systemic lupus erythematosus (SLE).
|
-
- HY-N10227
-
-
- HY-144329
-
-
- HY-144328
-
-
- HY-P1430
-
-
- HY-P1430A
-
-
- HY-19121A
-
|
TCV-309 chloride
|
Platelet-activating Factor Receptor (PAFR)
|
Cancer
|
|
TCV-309 chloride is a potent and specific platelet activating factor (PAF) antagonist. TCV-309 chloride specifically inhibits PAF-induced aggregation of rabbit and human platelets, and [3H]PAF binding to rabbit platelet microsomes with IC50 values of 33 nM, 58 nM and 27 nM, respectively. TCV-309 chloride has beneficial effects in anaphylactic shock.
|
-
- HY-109897
-
-
- HY-151196
-
-
- HY-122052
-
|
UK‑396082
|
Others
|
Metabolic Disease
|
|
UK‑396082 is a potent thrombin activated fibrinolytic inhibitor (TAFI) inhibitor. UK‑396082 increases plasmin activity and induces a parallel decrease in ECM levels. UK‑396082 can be used in research of chronic kidney disease (CKD).
|
-
- HY-115537
-
|
NAE-IN-M22
|
Apoptosis
|
Cancer
|
|
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
|
-
- HY-101923B
-
-
- HY-101923A
-
-
- HY-101923
-
-
- HY-142972
-
|
19(S)-HETE
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
19(S)-HETE is an arachidonic acid metabolite produced by cytochrome P450 enzymes. 19(S)-HETE is a full orthosteric agonist of the prostacyclin (IP) receptor with an EC50 value of 567 nM. 19(S)-HETE inhibits platelet activation and relaxation of vessels.
|
-
- HY-113492
-
-
- HY-115768
-
|
Compound 48/80
Poly-p-methoxyphenethylmethylamine
|
Others
|
Cancer
Neurological Disease
|
|
Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways.
|
-
- HY-111447
-
-
- HY-P99484
-
|
Botensilimab
AGEN 1181
|
CTLA-4
|
Cancer
|
|
Botensilimab (AGEN 1181), a humanized anti-cytotoxic T-lymphocyte antigen 4 (CTLA-4) monoclonal antibody, is an innate and adaptive immune activator. Botensilimab can be used for the research of cancer.
|
-
- HY-12545
-
|
Brevetoxin-3
PbTx-3
|
Sodium Channel
|
Inflammation/Immunology
|
|
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
|
-
- HY-137331
-
|
FAPI-46
|
FAP
|
Cancer
|
|
FAPI-46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI-46 can be used for tumor imaging of a multitude of different cancers.
|
-
- HY-10595
-
-
- HY-101042
-
|
AG-494
Tyrphostin AG 494
|
EGFR
CDK
|
Cancer
|
|
AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
|
-
- HY-P9952
-
|
Belimumab
LymphoStat B
|
TNF Receptor
|
Inflammation/Immunology
|
|
Belimumab (LymphoStat B) is a human IgG1λ monoclonal antibody that inhibits B-cell activating factor (BAFF). Belimumab can be used for systemic lupus erythematosus (SLE) research.
|
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis.
|
-
- HY-136501
-
|
MRS2395
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6.
|
-
- HY-114842
-
|
TDRL-551
|
Others
|
Cancer
|
|
TDRL-551 is a potent replication protein A (RPA) inhibitor (IC50=18 µM). TDRL-551 inhibits RPA-DNA interaction and increases the efficacy of Platinum (Pt)-based chemotherapy in lung and ovarian cancer. RPA plays essential roles in both nucleotide excision repair (NER) and homologous recombination (HR), along with its role in DNA replication and DNA damage checkpoint activation.
|
-
- HY-B1121
-
-
- HY-B1121A
-
-
- HY-N10322
-
|
2-Hydroxyemodin
|
Drug Metabolite
|
Others
|
|
2-Hydroxyemodin is an active metabolite of emodin in the hepatic microsomes. Emodin is an anthraquinone present in fungal metabolites and constituent of rhubarb. 2-Hydroxyemodin proves to be mutagenic to Salmonella typhimurium TA1537 in the absence of activation system.
|
-
- HY-P1934A
-
|
Cyclo(L-Phe-L-Pro)
|
Fungal
IFNAR
Reactive Oxygen Species
|
Cancer
Inflammation/Immunology
Infection
|
|
Cyclo(L-Phe-L-Pro), isolated from Pseudomonas fluorescens and Pseudomonas alcaligenes cell-free culture supernatants is an antifungal cyclic dipeptide. Cyclo(L-Phe-L-Pro) inhibits IFN-β production by interfering with retinoic-acid-inducible gene-I (RIG-I) activation. Cyclo(L-Phe-L-Pro) exhibits free-radical scavenging activity with the IC50 of 24 µM in the DPPH assay.
|
-
- HY-P2230
-
|
Angstrom6
A6 Peptide
|
PAI-1
|
Cancer
|
|
Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.
|
-
- HY-W271064
-
|
1-Methylpyrene
|
Fluorescent Dye
|
Others
|
|
1-Methylpyrene is a ubiquitous environmental pollutant and rodent carcinogen. Its mutagenic activity depends on sequential activation by various CYP and sulfotransferase (SULT) enzymes. 1-Methylpyrene induces chromosome loss and mitotic disturbance, proba
|
-
- HY-15394
-
-
- HY-14530
-
|
Pelitrexol
AG 2037
|
Antifolate
|
Cancer
|
|
Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice.
|
-
- HY-14165
-
-
- HY-P99902
-
|
Simlukafusp alfa
FAP-IL2v
|
Interleukin Related
|
Cancer
|
|
Simlukafusp alfa (FAP-IL2v) is an immunocytokine comprising an antibody against fibroblast activation protein α (FAPα) and an IL-2 variant that only binds IL-2Rβγ. Isotype: human IgG1.
|
-
- HY-100164
-
|
SDZ-MKS 492
MKS 492
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats.
|
-
- HY-146180
-
|
FSDD0I
|
FAP
|
Cancer
|
|
FSDD0I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD0I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging.
|
-
- HY-146181
-
|
FSDD1I
|
FAP
|
Cancer
|
|
FSDD1I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD1I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging.
|
-
- HY-146182
-
|
FSDD3I
|
FAP
|
Cancer
|
|
FSDD3I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD3I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging.
|
-
- HY-B1456A
-
|
Fenoprofen
LILLY-53858
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation.
|
-
- HY-112257
-
|
S-23
|
Androgen Receptor
|
Metabolic Disease
|
|
S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.
|
-
- HY-128643
-
|
FAPI-4
|
FAP
|
Cancer
|
|
FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios.
|
-
- HY-108391
-
|
C8-Ceramide
N-Octanoyl-D-erythro-sphingosine
|
Apoptosis
PKC
Autophagy
|
Cancer
Inflammation/Immunology
|
|
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
|
-
- HY-151343
-
-
- HY-117724
-
|
AZ3976
|
PAI-1
|
Cardiovascular Disease
|
|
AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay.
|
-
- HY-150978
-
|
DDAO-C6
|
Fluorescent Dye
|
Others
|
|
DDAO-C6 is a cridone ester derivative, highly specific fluorescence for detecting human serum albumin (HSA). DDAO-C6 acts as an enzymatic activatable near-infrared fluorescent probe in visually sensing endogenous lipase from gut microbes (Ex/Em=600/658 nm). Storage: protect from light.
|
-
- HY-145239
-
|
PD-1/PD-L1-IN-13
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8 + T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model.
|
-
- HY-120035
-
|
DD1
|
Proteasome
Ribosomal S6 Kinase (RSK)
Apoptosis
|
Cancer
|
|
DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation.
|
-
- HY-P9947
-
|
Efalizumab
|
Integrin
|
Others
|
|
Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research.
|
-
- HY-P9945
-
|
Mepolizumab
SB 240563
|
Interleukin Related
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Mepolizumab (SB 240563) is a humanized monoclonal antibody that binds to and neutralizes interleukin-5 (IL-5), the major cytokine involved in eosinophil proliferation, activation, and survival. Mepolizumab can be used for the research of eosinophilic granulomatosis with polyangiitis (EGPA) and severe eosinophilic asthma.
|
-
- HY-P1375A
-
-
- HY-P1396
-
-
- HY-117656
-
|
ESI-05
NSC 116966
|
Acyltransferase
|
Metabolic Disease
Neurological Disease
|
|
ESI-05 is a specific exchange proteins directly activated by cAMP 2 (EPAC2) inhibitor. ESI-05 inhibits cAMP-mediated EPAC2 GEF activity with an IC50 of 0.43 μM. ESI-05 can be used for the research of diabetes, insulin secretion and neurological disorders.
|
-
- HY-124858
-
|
SC99
|
STAT
JAK
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities.
|
-
- HY-121035
-
|
7BIO
7-Bromoindirubin-3-Oxime
|
CDK
GSK-3
|
Neurological Disease
|
|
7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice[1].
|
-
- HY-137446
-
-
- HY-12884
-
|
OAC2
|
Oct3/4
|
Others
|
|
OAC2 is an Oct4-activating compound which activates expression through the Oct4 gene promoter.
|
-
- HY-19734
-
|
NK-252
|
Keap1-Nrf2
|
Cancer
|
|
NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
|
-
- HY-147292
-
-
- HY-107301
-
-
- HY-12831
-
-
- HY-108848
-
|
Reteplase
BM 06.022
|
Others
|
Metabolic Disease
|
|
Reteplase (BM 06.022) is a recombinant plasminogen activator, consists of the kringle 2 and protease domains of human tissue-type plasminogen activator.
|
-
- HY-19339
-
-
- HY-121131
-
-
- HY-N2164
-
-
- HY-100508
-
|
ITSA-1
|
HDAC
|
Cancer
|
|
ITSA-1 is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation.
|
-
- HY-13103
-
|
NS 11021
|
Potassium Channel
|
Others
|
|
NS 11021 is a potent and specific Ca 2+-activated big-conductance K + Channels (KCa1.1 channels) activator. NS 11021 at concentrations above 0.3 μM activates KCa1.1 in a concentration-dependent manner by parallelshifting the channel activation curves to more negative potentials.
|
-
- HY-15122
-
-
- HY-15416
-
-
- HY-P1308
-
-
- HY-P0283
-
-
- HY-131012
-
-
- HY-15122A
-
-
- HY-18723
-
|
Yoda 1
|
Piezo Channel
Akt
ERK
Potassium Channel
|
Cardiovascular Disease
|
|
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca 2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
|
-
- HY-112956
-
|
Drotrecogin alfa (activated)
|
Others
|
Inflammation/Immunology
|
|
Drotrecogin alfa activated (DrotAA) is recombinant human activated protein C (APC). Drotrecogin alfa activated prevents smoke-induced increases in pulmonary microvascular permeability and proinflammatory cytokine IL-1β in rats. Drotrecogin alfa activated inhibits coagulation and inflammation and promotes fibrinolysis. Drotrecogin alfa activated can be used for severe sepsis reaearch.
|
-
- HY-P1308A
-
-
- HY-114304
-
|
COH000
|
E1/E2/E3 Enzyme
|
Cancer
|
|
COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
|
-
- HY-P0297
-
-
- HY-132247A
-
|
(±)-ErSO
|
Others
|
Cancer
|
|
(±)-ErSO is the racemate of ErSO. ErSO is a selective anticipatory unfolded protein response (a-UPR) activator.
|
-
- HY-107988
-
-
- HY-N6631
-
-
- HY-122974
-
-
- HY-N0336
-
|
3-Butylidenephthalide
Butylidenephthalide
|
Parasite
|
Infection
|
|
3-Butylidenephthalide (Butylidenephthalide) is a phthalic anhydride derivative identified in Ligusticum chuanxiong Hort, and has larvicidal activity (LC50 of 1.56 mg/g for Spodoptera litura larvae).
|
-
- HY-78263
-
|
MNS
NSC 170724; 5-(2-Nitrovinyl)benzodioxole
|
Src
Syk
|
Cancer
|
|
MNS (NSC 170724), the beta-nitrostyrene derivative, is a potent tyrosine kinase inhibitor and a broad-spectrum antiplatelet agent. MNS completely inhibits U46619, ADP-, arachidonic acid-, collagen-, and thrombin-induced platelet aggregation with IC50 values of 2.1, 4.1, 5.8, 7.0, and 12.7 μM, respectively. MNS inhibits Src, Syk, and FAK with IC50 of 27.3, 2.8, and 97.6 μM, respectively.
|
-
- HY-P3414A
-
|
Proteasome-activating peptide 1 TFA
|
Proteasome
|
Neurological Disease
|
|
Proteasome-activating peptide 1 TFA is a peptide and a potent proteasome activator. Proteasome-activating peptide 1 TFA increases the chymotrypsin-like proteasomal catalytic activity and, consequently, proteolytic rates both in vitro and in culture. Proteasome-activating peptide 1 TFA prevents protein aggregation in a cellular model of amyotrophic lateral sclerosis.
|
-
- HY-N0277
-
-
- HY-N3425
-
|
Kazinol U
|
AMPK
|
Others
|
|
Kazinol U inhibits melanogenesis through the inhibition of tyrosinase-related proteins via AMPK activation.
|
-
- HY-142163
-
|
S62798
|
Others
|
Cardiovascular Disease
|
|
S62798 is a selective and potent inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) with an IC50 value of 6 mM.
|
-
- HY-N1446B
-
-
- HY-108356
-
|
NS3694
|
Apoptosis
|
Cancer
|
|
NS3694, a diarylurea compound, is an apoptosome inhibitor. NS3694 inhibits apoptosome formation and caspase activation.
|
-
- HY-100548
-
|
GSK621
|
AMPK
Autophagy
Apoptosis
|
Cancer
|
|
GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
|
-
- HY-100221
-
-
- HY-N0509
-
-
- HY-139214
-
|
IXA4
|
IRE1
|
Neurological Disease
|
|
IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 activates IRE1/XBP1s signaling without globally activating the unfolded protein response (UPR) or other stress-responsive signaling pathways (e.g., the heat shock response or oxidative stress response). IXA4 reduces secretion of APP through IRE1 activation.
|
-
- HY-110273
-
-
- HY-N0625A
-
-
- HY-12070
-
|
DPH
|
Bcr-Abl
|
Cancer
|
|
DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.
|
-
- HY-19635A
-
-
- HY-100381
-
-
- HY-B0493
-
-
- HY-110153
-
|
NS19504
|
Potassium Channel
|
Neurological Disease
|
|
NS19504 is a Ca 2+-activated K + channel (BK channel, KCa1.1 channel) activator (EC50=11.0 µM) with relaxing effect on bladder smooth muscle spontaneous phasic contractions.
|
-
- HY-102052
-
|
DCEBIO
|
Potassium Channel
|
Inflammation/Immunology
|
|
DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl - secretion in T84 colonic cells. DCEBIO stimulates Cl - secretion via the activation of hIK1 K + channels and the activation of an apical membrane Cl - conductance.
|
-
- HY-101047
-
|
D-erythro-Sphingosine
Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine
|
PKC
Phosphatase
Endogenous Metabolite
|
Cancer
|
|
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
|
-
- HY-N1446
-
-
- HY-148553
-
-
- HY-70002
-
-
- HY-P3410
-
|
Trichomide A
|
SHP2
Phosphatase
|
Inflammation/Immunology
|
|
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases.
|
-
- HY-N4231
-
-
- HY-15336
-
|
AG 555
Tyrphostin AG 555
|
EGFR
Reverse Transcriptase
|
Cancer
|
|
AG 555 (Tyrphostin AG 555), a potent antiretroviral agent, is a potent and selective inhibitor of EGFR and blocks Cdk2 activation.
|
-
- HY-N2312
-
|
Mogrol
|
ERK
STAT
|
Cancer
|
|
Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
|
-
- HY-113261
-
-
- HY-10484
-
-
- HY-P0282
-
|
TAT peptide
|
HIV
|
Infection
|
|
TAT peptide is a cell penetrating peptide (GRKKRRQRRRPQ) derived from the trans-activating transcriptional activator (Tat) from HIV-1.
|
-
- HY-103239
-
-
- HY-N10782
-
-
- HY-70062
-
-
- HY-100489
-
|
TBHQ
tert-Butylhydroquinone
|
Keap1-Nrf2
ERK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma.
|
-
- HY-143315
-
-
- HY-131018
-
-
- HY-P2271
-
|
MM 54
|
Apelin Receptor (APJ)
|
Cancer
|
|
MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation.
|
-
- HY-N1446S5
-
-
- HY-134975
-
|
NY2267
|
c-Myc
|
Cancer
|
|
NY2267 is a disruptor of Myc-Max interaction, with an IC50 of 36.5 μM. NY2267 inhibits Myc- and Jun-induced transcriptional activation.
|
-
- HY-P0282A
-
|
TAT peptide TFA
|
HIV
|
Infection
|
|
TAT peptide (TFA) is a cell penetrating peptide (GRKKRRQRRRPQ) derived from the trans-activating transcriptional activator (Tat) from HIV-1.
|
-
- HY-14714
-
-
- HY-N1380
-
-
- HY-N2632
-
|
Uvarigrin
|
Apoptosis
|
Cancer
|
|
Uvarigrin, isolated from the roots of Uvaria calamistrata, induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation.
|
-
- HY-P2615
-
|
Ac-VDVAD-AFC
|
Fluorescent Dye
|
Cancer
|
|
Ac-VDVAD-AFC is a caspase-specific fluorescent substrate. Ac-VDVAD-AFC can measure caspase-3-like activity and caspase-2 activity and can be used for the research of tumor and cancer.
|
-
- HY-122203
-
|
PCS1055 dihydrochloride
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively.
|
-
- HY-134964
-
-
- HY-14754
-
|
Salirasib
S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
|
Ras
Autophagy
|
Cancer
|
|
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
|
-
- HY-P2519
-
-
- HY-P99638
-
-
- HY-B0167
-
-
- HY-103368
-
|
Eact
|
Chloride Channel
|
Neurological Disease
|
|
Eact is a selective and potent activator of TMEM16A, directly activates the TRPV1 channels in sensory nociceptors and produces itch, acute nociception and thermal hypersensitivity.
|
-
- HY-15542A
-
|
FRAX597
|
PAK
|
Cancer
|
|
FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
|
-
- HY-17538
-
-
- HY-104047
-
-
- HY-136172
-
|
ESI-08
|
Ras
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation.
|
-
- HY-N8617
-
|
Trijuganone C
|
Caspase
|
Cancer
|
|
Trijuganone C, a natural product extracted from Salvia miltiorrhiza, inhibits the proliferation of cancer cells through induction of apoptosis mediated by mitochondrial dysfunction and caspase activation.
|
-
- HY-75342
-
-
- HY-107586
-
|
Demethylasterriquinone B1
DAQ B1; L-783281; Dimethylasterriquinone
|
Insulin Receptor
Akt
|
Endocrinology
|
|
Demethylasterriquinone B1 is a selective insulin receptor activator. Demethylasterriquinone B1 stimulates tyrosine phosphorylation of the IR β subunit, and the activation of PIK3 and AKT.
|
-
- HY-P2519A
-
-
- HY-15027
-
-
- HY-143313
-
-
- HY-P0240A
-
-
- HY-108594
-
-
- HY-15542B
-
|
FRAX486
|
PAK
|
Cancer
|
|
FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
|
-
- HY-N4182
-
-
- HY-19635
-
|
G-5555
|
PAK
|
Cancer
|
|
G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
|
-
- HY-101069
-
-
- HY-N2432
-
|
Paederoside
|
HBV
|
Cancer
Infection
|
|
Paederoside is a monoterpene S-methyl thiocarbonate isolated from Paederia pertomentosa. Paederoside shows a high anti-tumor promoting activity against the Epstein-Barr virus activation.
|
-
- HY-N6892
-
|
3'-O-Acetylhamaudol
|
Others
|
Cancer
|
|
3'-O-Acetylhamaudol, isolated from Angelica polymorpha, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation.
|
-
- HY-P99371
-
|
Lirentelimab
AK002; Anti-Siglec-8 Reference Antibody (lirentelimab)
|
Apoptosis
|
Inflammation/Immunology
|
|
Lirentelimab (AK002) is a humanized IgG1 monoclonal antibody that targets sialic acid-binding Ig-like lectin 8 (SIGLEC8). Lirentelimab induces cell apoptosis of IL-5-activated eosinophils and inhibits IgE-mediated mast cell activation. Lirentelimab can be used for the research of eosinophilic gastritis and duodenitis.
|
-
- HY-144289
-
|
BMS-820132
|
Glucokinase
|
Metabolic Disease
|
|
BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation.
|
-
- HY-18739
-
|
Phorbol 12-myristate 13-acetate
PMA; TPA; Phorbol myristate acetate
|
PKC
SphK
NF-κB
|
Inflammation/Immunology
|
|
Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells.
|
-
- HY-143314
-
-
- HY-122550
-
|
Artemisitene
|
Keap1-Nrf2
Topoisomerase
Apoptosis
|
Cancer
|
|
Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability.
|
-
- HY-118208
-
|
ML-097
CID-2160985
|
Ras
|
Cancer
|
|
ML-097 (CID-2160985) is a pan Ras-related GTPases activator that can activate Rac1, cell division cycle 42, Ras, and Rab7.
|
-
- HY-133614
-
|
Dihydroisopimaric acid
|
Potassium Channel
|
Others
|
|
Dihydroisopimaric acid activates large conductance Ca 2+ activated K + (BK) channels alphabeta1 in the direct measurement of BKalphabeta1 opening under whole-cell voltage clamp.
|
-
- HY-B0289
-
-
- HY-143212
-
|
18:0-22:6 DG
1-Stearoyl-2-docosahexaenoyl-sn-glycerol
|
Liposome
p38 MAPK
|
Others
|
|
18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol that can bind to RasGRP and modulate MAP kinases activation.
|
-
- HY-N10445
-
-
- HY-13764
-
-
- HY-147179
-
-
- HY-15723A
-
-
- HY-P0240
-
-
- HY-101594
-
-
- HY-101675
-
-
- HY-N6065
-
|
Praeruptorin A
|
NF-κB
|
Inflammation/Immunology
|
|
Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation.
|
-
- HY-108593
-
-
- HY-N1446S
-
-
- HY-123879
-
|
BAA473
|
Interleukin Related
|
Inflammation/Immunology
|
|
BAA473 is a bile acid analog and is a potent activator of the pyrin inflammasome that induces the secretion of interleukin 18 (IL-18) through activation of the inflammasome in both myeloid and intestinal epithelial cells.
|
-
- HY-N0878
-
|
Bufotalin
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation.
|
-
- HY-N5101
-
-
- HY-101047S
-
|
D-erythro-Sphingosine-d7
Erythrosphingosine-d7; erythro-C18-Sphingosine-d7; trans-4-Sphingenine-d7
|
PKC
Phosphatase
Endogenous Metabolite
|
Cancer
|
|
D-erythro-Sphingosine-d7 is the deuterium labeled D-erythro-Sphingosine. D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator[1][2][3][4].
|
-
- HY-N0831
-
|
Jaceosidin
|
Bcl-2 Family
COX
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Jaceosidin is a flavonoid isolated from Artemisia vestita, induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression. Jaceosidin exhibits anti-cancer, anti-inflammatory activities, decreases leves of inflammatory markers, and suppresses COX-2 expression and NF-κB activation.
|
-
- HY-109545
-
|
Isopropyl unoprostone
Unoprostone isopropyl ester; UF-021
|
Potassium Channel
|
Others
|
|
Isopropyl unoprostone (Unoprostone isopropyl ester), an analogue of a prostaglandin metabolite, is a potent large conductance Ca 2+-activated K + (BK) channels activator. Isopropyl unoprostone has antiglaucoma effects, lowering intraocular pressure (IOP) by increasing aqueous humour outflow. Isopropyl unoprostone can improve retinal sensitivity and the protection of central retinal sensitivity.
|
-
- HY-P2518
-
-
- HY-100783A
-
|
(-)-Bicuculline methochloride
l-Bicuculline methochloride
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methochloride (l-Bicuculline methochloride) is a potent GABAA receptor antagonist. (-)-Bicuculline methochloride blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-117755
-
|
PF-739
|
AMPK
|
Metabolic Disease
|
|
PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes.
|
-
- HY-103427
-
-
- HY-18749
-
-
- HY-N10446
-
-
- HY-100783
-
|
(-)-Bicuculline methobromide
l-Bicuculline methobromide
|
GABA Receptor
|
Neurological Disease
|
|
(-)-Bicuculline methobromide (l-Bicuculline methobromide) is a potent GABAA receptor antagonist. (-)-Bicuculline methobromide blocks afterhyperpolarizations (AHPs) mediated by Ca 2+-activated K + channels in various types of neurons.
|
-
- HY-N1446S1
-
-
- HY-18633
-
|
MDK83190
|
Apoptosis
|
Cancer
|
|
MDK83190 is a potent apoptosis activator, induces Apaf-1 oligomerization, increases procaspase-9 processing and subsequent caspase-3 activation in a cyto c-dependent Manner.
|
-
- HY-B0167S
-
-
- HY-N1446S3
-
-
- HY-B0493S1
-
-
- HY-N1446S2
-
-
- HY-139040
-
|
2-(Tetradecylthio)acetic acid
|
PPAR
|
Metabolic Disease
|
|
2-Tetradecylthio acetic acid is a pan-peroxisome proliferator activated receptor (pan-PPAR) activator. 2-Tetradecylthio acetic acid induces hypolipidemia. 2-Tetradecylthio acetic acid reduces plasma lipids and enhances hepatic fatty acid oxidation in rodents. 2-Tetradecylthio acetic acid increases the expression of genes involved in fatty acid uptake, activation, accumulation, and oxidation.
|
-
- HY-P2518A
-
-
- HY-17397
-
|
Strontium Ranelate
Distrontium renelate; S12911
|
CaSR
|
Metabolic Disease
|
|
Strontium Ranelate (S12911) is an antiosteoporotic agent that acts by reducing bone resorption and promoting bone formation, thereby inducing a positive bone balance. Strontium Ranelate can also activate the calcium-sensing receptor (CaSR) in non skeletal cells, resulting in the activation of inositol 1, 4, 5-triphosphate production and mitogen-activated protein kinase signaling.
|
-
- HY-14452
-
|
Fatostatin
125B11
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
|
-
- HY-111363
-
-
- HY-112878
-
-
- HY-N0019
-
-
- HY-15964
-
-
- HY-N0865
-
|
Ingenol
(-)-Ingenol
|
PKC
|
Cancer
|
|
Ingenol is a PKC activator, with a Ki of 30 μM, with antitumor activity.
|
-
- HY-13626
-
|
Spisulosine
ES-285
|
PKC
|
Cancer
|
|
Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation.
|
-
- HY-124306
-
|
ML-099
CID-888706
|
Ras
|
Cancer
|
|
ML-099 (CID-888706) is a pan Ras-related GTPases activator that can activate Rac1, cell division cycle 42, Ras, Rab7, and Rab-2A.
|
-
- HY-N0052A
-
|
Sanguinarine chloride
Sanguinarin chloride; Sanguinarium chloride; Pseudochelerythrine chloride
|
Apoptosis
Autophagy
Bacterial
Parasite
|
Cancer
|
|
Sanguinarine (Sanguinarin) chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
|
-
- HY-N0052
-
|
Sanguinarine
Sanguinarin; Sanguinarium; Pseudochelerythrine
|
Apoptosis
Autophagy
|
Cancer
|
|
Sanguinarine (Sanguinarin), a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
|
-
- HY-136251
-
|
BRD0539
|
CRISPR/Cas9
|
Infection
|
|
BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay.
|
-
- HY-117103
-
|
AMG131
INT131
|
PPAR
|
Metabolic Disease
|
|
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM).
|
-
- HY-105173
-
|
Teverelix
EP 24332
|
GnRH Receptor
Histamine Receptor
|
Cancer
Endocrinology
|
|
Teverelix (EP 24332) is a GnRH antagonist. Teverelix binds competitively and reversibly to GnRH receptors, thereby suppressing the release of LH and FSH. Teverelix can be used in the research of prostatic hyperplasia, endometriosis, and prostate cancer.
|
-
- HY-119874
-
-
- HY-N4323
-
-
- HY-12364
-
|
C75
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM. C75 is a potent CPT1A activator.
|
-
- HY-W067427
-
|
BAY32-5915
|
IKK
|
Cancer
|
|
BAY32-5915 is a potent IKKα inhibitor with an IC50 value of 60 nM. BAY32-5915 has not affect Doxorubicin (HY-15142A)-induced NF-κB activation.
|
-
- HY-B0493S
-
-
- HY-100472
-
|
ZYZ-488
|
Caspase
|
Cancer
|
|
ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3.
|
-
- HY-101796
-
|
NSC-70220
|
Others
|
Cancer
|
|
NSC-70220 is a selective and allosteric SOS1 inhibitor. NSC-70220 inhibits allosteric site activation, and partially inhibited catalytic site activation. NSC-70220 has an anticancer effect.
|
-
- HY-N1446S4
-
-
- HY-132247
-
|
ErSO
|
Others
|
Cancer
|
|
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer.
|
-
- HY-N8498
-
|
GKK1032B
|
Apoptosis
|
Cancer
|
|
GKK1032B is an alkaloid compound that can be found in endophytic fungus Penicillium sp. GKK1032B can induce the apoptosis of human osteosarcoma MG63 cells through caspase pathway activation.
|
-
- HY-152472
-
|
ENT-C225
|
Trk Receptor
|
Neurological Disease
|
|
ENT-C225 is an effective activator of TrkB neurotrophin receptor. ENT-C225 has high effect on activating TrkB receptor (TrkBR), and has good physicochemical properties and neuroprotective properties.
|
-
- HY-14255
-
-
- HY-112060
-
-
- HY-13529
-
-
- HY-14290A
-
-
- HY-P0256
-
-
- HY-117962
-
|
(Rac)-BI 703704
|
Guanylate Cyclase
|
Metabolic Disease
|
|
(Rac)-BI 703704 is a potent soluble guanylyl cyclase (sGC) activator. (Rac)-BI 703704 reduces progression of renal damage in the ZSF1 rat, and highlight the potential of sGC activation as an effective therapy for diabetic nephropathy.
|
-
- HY-P99384
-
|
Vofatamab
B-701; MFGR-1877S; RG-7444
|
FGFR
|
Cancer
|
|
Vofatamab (B-701) is an anti-FGFR3 monoclonal antibody (mAb). Vofatamab blocks activation of both the wildtype and genetically activated receptor. Vofatamab can be used in the research of metastatic urothelial carcinoma (mUC).
|
-
- HY-N1380S
-
-
- HY-N6258
-
|
Kahweol
|
AMPK
Apoptosis
|
Metabolic Disease
|
|
Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
|
-
- HY-N0608
-
|
Myrislignan
|
NF-κB
|
Inflammation/Immunology
|
|
Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
|
-
- HY-12754
-
|
ML228
CID-46742353
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
|
-
- HY-10162
-
|
Olaparib
AZD2281; KU0059436
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
|
-
- HY-N1380S3
-
-
- HY-10249
-
|
GSK-690693
|
Akt
AMPK
Autophagy
|
Cancer
|
|
GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation.
|
-
- HY-14452A
-
|
Fatostatin hydrobromide
125B11 hydrobromide
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
|
-
- HY-110105
-
|
NS8593 hydrochloride
|
Potassium Channel
|
Neurological Disease
|
|
NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
|
-
- HY-N1380S4
-
-
- HY-N1380S2
-
-
- HY-N0699
-
|
Daphnoretin
Dephnoretin; Thymelol
|
PKC
Influenza Virus
|
Infection
|
|
Daphnoretin (Dephnoretin), isolated from Wikstroemia indica, possesses antiviral activity. Daphnoretin likes PMA, may direct activation of protein kinase C which in turn activated NADPH oxidase and elicited respiratory burst.
|
-
- HY-128591
-
|
DIPQUO
|
Phosphatase
|
Metabolic Disease
|
|
DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.
|
-
- HY-148189
-
|
Aldometanib
LXY-05-029
|
AMPK
|
Metabolic Disease
|
|
Aldometanib (LXY-05-029) is an orally active aldolase inhibitor. Aldometanib can activate lysosomal adenosine monophosphate-activated protein kinase (AMPK) and decreases blood glucose. Aldometanib can be used for the research of metabolic homeostasis.
|
-
- HY-14233
-
-
- HY-B1197
-
-
- HY-14909
-
-
- HY-59047
-
-
- HY-P0136
-
-
- HY-10164
-
-
- HY-100295
-
-
- HY-U00040
-
-
- HY-B0099S
-
|
Edaravone-d5
MCI-186-d5
|
MMP
Apoptosis
|
Neurological Disease
|
|
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
|
-
- HY-N6688
-
|
Verruculogen
|
Potassium Channel
Bacterial
Antibiotic
|
Infection
|
|
Verruculogen is a toxin produced mainly by Penicillium and Aspergillus spp. and causes severe tremors in affected animals. Verruculogen inhibits Ca 2+-activated K + channels. Verruculogen is an M phase inhibitor of the mammalian cell cycle.
|
-
- HY-15553B
-
|
Mibefradil dihydrochloride hydrate
Ro 40-5967 dihydrochloride hydrate
|
Calcium Channel
|
Cardiovascular Disease
|
|
Mibefradil dihydrochloride hydrate (Ro 40-5967 dihydrochloride hydrate) is a effectively long-acting calcium channel antagonist, used as an antihypertensive agent. Mibefradil dihydrochloride hydrate acts via a higher affinity block for low-voltage-activated (T) than for high-voltage-activated (L) calcium channels.
|
-
- HY-P0256A
-
-
- HY-128920
-
|
Phortress free base
|
Cytochrome P450
|
Cancer
|
|
Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
|
-
- HY-P3452
-
|
Tetrapeptide-30
|
Tyrosinase
|
Inflammation/Immunology
|
|
Tetrapeptide-30 is a skin-brightening peptide consisting of four amino acids. Tetrapeptide-30 can act as a tyrosinase inhibitor, lightening hyperpigmentation and evening out skin tone by reducing the amount of tyrosinase and inhibiting melanocyte activation.
|
-
- HY-P1120
-
-
- HY-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-N8041
-
|
Mogroside III A2
|
HSV
|
Infection
|
|
Mogroside III A2 is a cucurbitane glycoside. Mogroside III A2 can inhibit Epstein-Barr virus early antigen (EBV-EA) activation. Mogroside III A2 shows weak inhibitory effects on activation of NOR 1.
|
-
- HY-N0608A
-
|
(Rac)-Myrislignan
|
NF-κB
|
Inflammation/Immunology
|
|
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
|
-
- HY-P1120A
-
-
- HY-N0896
-
|
Inulicin
1-O-Acetylbritannilactone
|
NF-κB
COX
|
Cancer
Inflammation/Immunology
|
|
Inulicin (1-O-Acetylbritannilactone) is an active compound that inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone) inhibits LPS-induced PGE2 production and COX-2 expression, and NF-κB activation and translocation.
|
-
- HY-N2433
-
|
Paederosidic acid methyl ester
|
Potassium Channel
|
Neurological Disease
|
|
Paederosidic acid methyl ester is a ATP‐sensitive K + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level.
|
-
- HY-17538S
-
-
- HY-12372
-
|
Sanggenon G
|
IAP
Caspase
|
Cancer
|
|
Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). Sanggenon G binds specifically to the BIR3 domain of XIAP with a binding affinity of 34.26 μM. Sanggenon G enhances caspase activation.
|
-
- HY-100602
-
-
- HY-U00434
-
-
- HY-N3989
-
-
- HY-14181
-
-
- HY-N3463
-
-
- HY-N0553
-
-
- HY-N0441
-
-
- HY-101214
-
-
- HY-101738A
-
-
- HY-100934
-
-
- HY-100153
-
-
- HY-14181A
-
-
- HY-123054
-
|
BTSA1
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
BTSA1 is a potent, high affinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis.
|
-
- HY-P2705
-
|
Mastoparan X
|
Endogenous Metabolite
|
Others
|
|
Mastoparan X is a GTP-binding regulatory protein (G protein)-activating peptide, and a tetradecapeptide from wasp venom. Mastoparan X acts function by the direct activation of G protein that couple to phospholipase C to cause secretion from various kinds of cells.
|
-
- HY-138936
-
|
SSK1
|
p38 MAPK
Apoptosis
|
Inflammation/Immunology
|
|
SSK1, a senescence-specific killing compound, is a β-galactosidase-targeted proagent attenuates inflammation. SSK1 is activated by lysosomal β-galactosidase and selectively killed senescent cells through the activation of p38 MAPK and induction of apoptosis.
|
-
- HY-135388
-
|
ent-Ezetimibe
ent-SCH 58235
|
Drug Metabolite
|
Cardiovascular Disease
|
|
ent-Ezetimibe (ent-SCH 58235) is the RRS-enantiomer of Ezetimibe. Ezetimibe is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
|
-
- HY-B0289S
-
-
- HY-B0887S
-
|
Permethrin-d5
|
Parasite
|
Infection
|
|
Permethrin-d5 (NRDC-143-d5) is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation[1][2].
|
-
- HY-152096
-
|
(R)-ZG197
|
Bacterial
|
Infection
|
|
(R)-ZG197 is a highly selective Staphylococcus aureus Caseinolytic protease P (SaClpP) activator with an EC50 of 1.5 μM. (R)-ZG197 also activates Homo sapiens ClpP (HsClpP) with an EC50 of 31.4 μM.
|
-
- HY-136268
-
-
- HY-19706
-
|
ARS-853
|
Ras
Apoptosis
|
Cancer
|
|
ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
|
-
- HY-136059
-
-
- HY-12303
-
|
OAC1
|
Oct3/4
TET Protein
|
Cancer
|
|
OAC1 is a potent Oct4 activator. OAC1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. OAC1 activates OCT4 through upregulation of HOXB4 expression. OAC1 increases transcription of the Oct4-Nanog-Sox2 triad and TET1. OAC1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time.
|
-
- HY-P99666
-
|
Interferon alfa
|
IFNAR
|
Infection
|
|
Interferon alfa is a type I interferon that activates novel genes and exerts potent antiviral and antiproliferative activity on target cells. Signaling by Interferon alfa requires receptor-dependent activation of Stat1 and Stat2 to form a heterodimeric STAT that binds to the DNA-binding protein IRF-9 (p48) and forms ISGF-3 (IFN-stimulated gene factor 3). The driver genes are then further activated by ISGF-3 to achieve antiviral function.
|
-
- HY-108573
-
|
P-1075
|
Potassium Channel
|
Cardiovascular Disease
|
|
P-1075 is a potent activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6), with an EC50 value of 45 nM for SUR2B-KIR6 channel activation. P-1075 also P1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts.
|
-
- HY-101180
-
|
C2 Ceramide
Ceramide 2
|
Phosphatase
Mitochondrial Metabolism
Apoptosis
Autophagy
|
Endocrinology
Metabolic Disease
|
|
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation, autophagy and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
|
-
- HY-108599
-
|
DCP-LA
FR236924
|
PKC
CaMK
Phosphatase
Apoptosis
|
Neurological Disease
|
|
DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca( 2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis.
|
-
- HY-117727A
-
|
Leriglitazone hydrochloride
Hydroxypioglitazone hydrochloride
|
PPAR
|
Metabolic Disease
|
|
Leriglitazone (Hydroxypioglitazone) hydrochloride, a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) hydrochloride PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) hydrochloride binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50 of 680 nM.
|
-
- HY-117727
-
|
Leriglitazone
Hydroxypioglitazone
|
PPAR
|
Metabolic Disease
|
|
Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.
Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.
Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with a Ki of 1.2 μM，Leriglitazone induces transcriptional efficacy of the PPARγ (LBD) with an EC50
of 680 nM.
|
-
- HY-109121
-
|
Reldesemtiv
CK-2127107
|
Others
|
Cardiovascular Disease
|
|
Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model.
|
-
- HY-108638
-
|
NSC 146109 hydrochloride
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and can be used for breast cancer research. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes.
|
-
- HY-17500
-
|
Ataciguat
HMR-1766
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Ataciguat (HMR-1766) is a nitric oxide-independent soluble guanylate cyclase (sGC) activator. Ataciguat is able to activate the ferric heme-iron redox form of sGC that stimulate the production of cyclic GMP (cGMP). Ataciguat exhibits vasodilator effects.
|
-
- HY-N0219
-
|
Bicuculline
(+)-Bicuculline; d-Bicuculline
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline ((+)-Bicuculline; d-Bicuculline), as a convulsant alkaloid, is a competitive neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+-activated potassium (SK) channels and subsequently blocks the slow afterhyperpolarization (slow AHP) .
|
-
- HY-P99166
-
-
- HY-103666
-
|
CY-09
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation.
|
-
- HY-131265
-
-
- HY-10162S1
-
|
Olaparib-d8
AZD2281-d8; KU0059436-d8
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib-d8 is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
- HY-N10458
-
|
Asperbisabolane L
|
NF-κB
|
Inflammation/Immunology
|
|
Asperbisabolane L, a sesquiterpenoid, exerts the anti-inflammatory activity by inhibiting the NF-κB-activated pathway. Asperbisabolane L inhibits the translocation of NF-κB from cytoplasm to the nucleus. Asperbisabolane L also inhibits NO production in LPS-activated BV-2 microglia cells.
|
-
- HY-12316
-
|
20(S)-Hydroxycholesterol
20α-Hydroxycholesterol
|
Smo
Endogenous Metabolite
|
Cancer
|
|
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
|
-
- HY-15027S
-
-
- HY-N6577
-
-
- HY-N10125
-
-
- HY-76847
-
-
- HY-100242
-
-
- HY-50662
-
-
- HY-U00411
-
-
- HY-76847A
-
-
- HY-15341
-
-
- HY-15300
-
-
- HY-N8418
-
-
- HY-136094
-
-
- HY-104005
-
-
- HY-16397A
-
-
- HY-101804
-
-
- HY-19739
-
|
JW74
|
Wnt
|
Cancer
|
|
JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling with an IC50 of 420 nM.
|
-
- HY-100581
-
|
CORM-3
|
NF-κB
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
CORM-3, a carbon monoxide-releasing molecule, attenuates NF-κB p65 nuclear translocation, reduces ROS generation and enhances intracellular glutathione and superoxide dismutase levels. CORM-3 reduces NLRP3 inflammasome activation.
|
-
- HY-P0190
-
|
Iberiotoxin
|
Potassium Channel
|
Cardiovascular Disease
|
|
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels.
|
-
- HY-W006230
-
|
Anthraflavic acid
|
Others
|
Cancer
|
|
Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.
|
-
- HY-139667
-
|
PKM2-IN-3
|
Pyruvate Kinase
|
Neurological Disease
|
|
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
|
-
- HY-148174
-
|
JNJ-3790339
|
DGK
|
Cancer
|
|
JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation.
|
-
- HY-N3796
-
|
Echinulin
Echinuline
|
NF-κB
|
Inflammation/Immunology
|
|
Echinulin (Echinuline) is a cyclic dipeptide carrying a triprenylated indole moiety. Echinulin contributes to the activation of T cell subsets, which leads to NF-κB activation.Echinulin exerts its immune roles by the NF-κB pathway.Echinulin has the potential to serve as a immunotherapeutic agent.
|
-
- HY-N2025
-
|
Oroxin A
|
PPAR
Glucosidase
|
Metabolic Disease
|
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
|
-
- HY-108635
-
-
- HY-N3807
-
|
Enniatin B1
|
Acyltransferase
ERK
NF-κB
|
Cancer
Infection
Cardiovascular Disease
|
|
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
|
-
- HY-148683
-
|
EG-011
|
Arp2/3 Complex
|
Cancer
|
|
EG-011 is the first-in-class and potent Wiskott-Aldrich syndrome protein (WASP) activator. EG-011 activates the auto-inhibited form of WASP with strong actin polymerization. EG-011 has selective anti-tumor activity in lymphomas.
|
-
- HY-P1121A
-
-
- HY-113673
-
|
A-935142
|
Potassium Channel
|
Cardiovascular Disease
|
|
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.
|
-
- HY-118131
-
|
PKR-IN-C51
|
Ser/Thr Protease
|
Infection
|
|
PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages.
|
-
- HY-B0069
-
|
Fludarabine
F-ara-A; NSC 118218
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
STAT
Apoptosis
|
Cancer
|
|
Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes.
|
-
- HY-101329
-
|
Anthracene-9-carboxylic acid
9-Anthracenecarboxylic acid
|
Chloride Channel
|
Others
|
|
Anthracene-9-carboxylic acid (9-Anthracenecarboxylic acid) is an anthracene derivative traditionally used to block and identify Ca 2+-activated Cl - currents (CaCCs) in various cell types, like diverse smooth muscle cells, epithelial cells and salivary gland cells.
|
-
- HY-N3552
-
|
Catalposide
|
NF-κB
|
Inflammation/Immunology
|
|
Catalposide, an iridoid glycoside that could be isolated from Catalpa ovate G. Don (Bignoniaceae), inhibits TNF-α, IL-1β, and IL-6 productions and NF-κB (p65) activation in lipopolysaccharide-activated RAW 264.7 macrophages.
|
-
- HY-153339
-
|
E235
|
Others
|
Cancer
|
|
E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research.
|
-
- HY-103697
-
|
Gardiquimod
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
|
Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-100447
-
-
- HY-B1140
-
-
- HY-139858
-
-
- HY-N9404
-
-
- HY-P5125
-
-
- HY-15332
-
-
- HY-128642
-
|
FAPI-2
|
FAP
|
Cancer
|
|
FAPI-2 is a fibroblast activation protein (FAP) inhibitor for cancer research.
|
-
- HY-12359
-
-
- HY-151647
-
|
3-Azidopropanoic acid-PFP ester
|
Biochemical Assay Reagents
|
Others
|
|
3-Azidopropanoic acid-PFP ester is an azidopropanoic acid linker that contains an activated PFP ester. The azide group can undergo copper-catalyzed Click Chemistry reactions with alkynes, DBCO and BCN to form triazole linkages. The activated PFP ester can react with amine groups to form stable amide bonds.
|
-
- HY-10162S3
-
|
Olaparib-d4-1
AZD2281-d4-1; KU0059436-d4-1
|
PARP
Autophagy
Mitophagy
|
Cancer
|
|
Olaparib-d4-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].
|
-
- HY-P99274
-
|
Xentuzumab
BI 836845; Anti-Human IGF1 and IGF2 Recombinant Antibody
|
IGF-1R
|
Cancer
|
|
Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a humanized monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKT activation.
|
-
- HY-14266
-
|
Dapivirine
TMC120; R147681
|
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
|
Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
|
-
- HY-N1990
-
|
Gypenoside XLIX
|
PPAR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
|
-
- HY-110302
-
|
6'-GNTI dihydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.
|
-
- HY-136427
-
-
- HY-12343
-
|
ML277
CID-53347902
|
Potassium Channel
|
Cardiovascular Disease
|
|
ML277 (CID-53347902) is a potent and selective activator of K(v)7.1 (KCNQ1) potassium channel activator (EC50=270 nM), rescues function of pathophysiologically important mutant channel complexes in human induced pluripotent stem cell-derived cardiomyocytes.
|
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-N2485
-
|
4'-Methoxyresveratrol
4'-O-Methylresveratrol
|
NF-κB
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities. 4'-Methoxyresveratrol alleviates AGE-induced inflammation through suppressing RAGE-mediated MAPK/NF-κB signaling pathway and NLRP3 inflammasome activation.
|
-
- HY-P4101
-
|
Cys(Npys)-TAT (47-57)
|
HIV
|
Infection
|
|
Cys(Npys)-TAT (47-57) is a peptide fragment of TAT peptide and it is able to interact with plasmid DNA electrostatically. Cys(Npys)-TAT (47-57) is corresponding to the transduction domain of TAT with an activated cysteine residue C. TAT is a small nuclear transcriptional activator protein encoded by HIV-1.
|
-
- HY-12512
-
|
cGAMP
Cyclic GMP-AMP; 3',3'-cGAMP
|
STING
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMPP) functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
|
-
- HY-18085G
-
-
- HY-117727S
-
|
Leriglitazone-d4
Hydroxypioglitazone-d4
|
PPAR
|
Metabolic Disease
|
|
Leriglitazone-d4 is deuterium labeled Leriglitazone. Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM，induces transcriptional efficacy of the PPARγ (LBD) with EC50 of 680 nM[1].
|
-
- HY-15477A
-
|
YS-49 monohydrate
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-15477
-
|
YS-49
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-112558
-
-
- HY-P1260
-
-
- HY-124960
-
-
- HY-17517
-
|
Tiadinil
|
Bacterial
|
Infection
|
|
Tiadinil is a plant activator of systemic acquired resistance, boosts the production of herbivore-induced plant volatiles; fungicide.
|
-
- HY-112473
-
-
- HY-12639
-
|
Bephenium
|
Parasite
|
Infection
|
|
Bephenium is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator.
|
-
- HY-B1058A
-
-
- HY-B1058
-
-
- HY-101371
-
|
Hesperin
|
Keap1-Nrf2
|
Cancer
|
|
Hesperin is a bioactive ingredient present in Japanese horseradish (wasabi) and has been shown to be an Nrf2 activator.
|
-
- HY-P5125A
-
-
- HY-32348
-
-
- HY-Y1683
-
|
DL-Menthol
Racementhol
|
GABA Receptor
|
Others
|
|
DL-Menthol is a relative configuration of (-)-Menthol. DL-Menthol relates to the activation of GABAA receptor.
|
-
- HY-111441
-
-
- HY-105198
-
-
- HY-12885A
-
-
- HY-P0195
-
-
- HY-P0249A
-
-
- HY-107854
-
-
- HY-15840
-
|
YLF-466D
C24
|
AMPK
|
Cancer
|
|
YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
|
-
- HY-114398
-
|
BAY-293
|
Ras
|
Cancer
|
|
BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
|
-
- HY-103697A
-
|
Gardiquimod diTFA
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
|
Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-12519
-
|
Oltipraz
RP 35972; NSC 347901
|
HIF/HIF Prolyl-Hydroxylase
HIV
Keap1-Nrf2
Parasite
|
Cancer
|
|
Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
|
-
- HY-B0167A
-
-
- HY-120514
-
|
JNc-440
|
TRP Channel
Potassium Channel
|
Cardiovascular Disease
|
|
JNc-440 is a potent antihypertensive agent. JNc-440 can enhance the interaction of TRPV4 and Ca 2+-activated potassium channel 3 (KCa2.3) in endothelial cells. JNc-440 can also enhance vasodilation, and exerted antihypertensive effects in mice.
|
-
- HY-10119
-
|
Vorapaxar
SCH 530348
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-115685
-
|
3-Methyl-GABA
|
GABA Receptor
|
Neurological Disease
|
|
3-Methyl-GABA is a potent GABA aminotransferase activator. 3-Methyl-GABA can fit the binding pocket of GABAA receptor (GABAaR). 3-Methyl-GABA can activate L-glutamic acid decarboxylase (GAD). 3-Methyl-GABA has anticonvulsant activity.
|
-
- HY-P0316
-
|
TP508
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
|
TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-15027S1
-
-
- HY-116626
-
|
SM-7368
|
NF-κB
p38 MAPK
MMP
|
Cancer
|
|
SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation. SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
|
-
- HY-110385
-
|
cGAMP disodium
Cyclic GMP-AMP disodium; 3',3'-cGAMP disodium
|
STING
Endogenous Metabolite
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMPP) disodium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
|
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-110385A
-
|
cGAMP diammonium
Cyclic GMP-AMP diammonium; 3',3'-cGAMP diammonium
|
STING
Endogenous Metabolite
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
|
-
- HY-17363
-
-
- HY-W015445
-
|
SD-169
|
p38 MAPK
|
Metabolic Disease
|
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
|
-
- HY-136477
-
|
Pentagamavunon-1
PGV-1
|
Apoptosis
COX
VEGFR
NF-κB
|
Cancer
|
|
Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.
|
-
- HY-10119A
-
|
Vorapaxar sulfate
SCH 530348 sulfate
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner.
|
-
- HY-136173
-
|
Batoprotafib
TNO155
|
SHP2
Phosphatase
|
Cancer
|
|
Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.
|
-
- HY-100234A
-
-
- HY-18772
-
|
O4I2
|
Oct3/4
|
Others
|
|
O4I2 is a potent Oct3/4 inducer. O4I2 induces the expression of pluripotent-associated genes Lin28, Sox2 and Nanog, and suppresses Rex1.
|
-
- HY-135303
-
|
GLPG1205
|
GPR84
|
Inflammation/Immunology
|
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
|
-
- HY-100234
-
-
- HY-12639A
-
-
- HY-153098
-
-
- HY-N1260
-
|
Scutebarbatine A
(-)-Scutebarbatine A
|
Apoptosis
|
Cancer
|
|
Scutebarbatine A inhibits the proliferation of HCC cells and triggers their apoptosis via the activation of MAPK and ER stress.
|
-
- HY-U00458
-
|
K-80003
TX-803
|
Akt
|
Cancer
|
|
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
|
-
- HY-W040055
-
-
- HY-P1576A
-
|
AMARA peptide TFA
|
AMPK
|
Others
|
|
AMARA peptide (TFA) is a substrate for salt-inducible kinase (SIK) and adenosine monophosphate activated protein kinase (AMPK).
|
-
- HY-P1260A
-
-
- HY-B1897A
-
|
Menadione bisulfite sodium
Menadione sodium bisulfite; Vitamin K3 sodium bisulfite
|
Others
|
Others
|
|
Menadione bisulfite (sodium) is used as an agent to induce acute oxidative stress, and to function as a plant-defense activator against several pathogens.
|
-
- HY-143510
-
|
RMC-4627
|
mTOR
|
Cancer
|
|
RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.
|
-
- HY-P0021
-
-
- HY-107421
-
|
Prostratin
|
PKC
HIV
|
Cancer
Infection
|
|
Prostratin, a natural terpenoid compound, is a PKC activator, with a Ki of 12.5 nM and shows inhibitory effect on HIV-1.
|
-
- HY-138652
-
-
- HY-18965
-
-
- HY-N0486
-
-
- HY-145938
-
|
OncoFAP
|
FAP
|
Cancer
|
|
OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
|
-
- HY-137477
-
-
- HY-15252
-
-
- HY-124240
-
-
- HY-117793
-
-
- HY-N0019S
-
-
- HY-107543
-
|
8-CPT-2Me-cAMP sodium
|
Ras
|
Others
|
|
8-CPT-2Me-cAMP sodium is a selective activator of exchange proteins activated by cAMP (Epac), the cAMP sensitive guanine nucleotide exchange factors (GEFs) for the small GTPases Rap1 and Rap2. 8-CPT-2Me-cAMP sodium activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50> 10 μM). 8-CPT-2Me-cAMP sodium stimulates Epac-mediated Ca 2+ release in pancreatic β-cells in vitro.
|
-
- HY-111673
-
|
8-CPT-Cyclic AMP sodium
8-CPT-cAMP sodium; 8-(p-Chlorophenylthio)-cAMP sodium
|
PKA
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Epac and is a potent Epac activator.
|
-
- HY-153128
-
|
DOCK2-IN-1
|
DOCK
|
Inflammation/Immunology
|
|
DOCK2-IN-1 (compound 3), a CPYPP (HY-110100) analogue, is an inhibitor of DOCK2 as well (IC50=19.1 μM). DOCK2-IN-1 binds to DOCK2 DHR-2 domain in a reversible manner to inhibits its catalytic activity. DOCK2-IN-1 blocks the activation of both chemokine receptor- and antigen receptor-mediated Rac in lymphocytes. DOCK2-IN-1 significantly suppresses chemotactic response and T cell activation.
|
-
- HY-139308
-
|
T0467
|
Mitochondrial Metabolism
|
Neurological Disease
|
|
T0467 activates parkin mitochondrial translocation in a PINK1-dependent manner in vitro. T0467 do not induce mitochondrial accumulation of PINK1in dopaminergic neurons. T0467 is a potential compound for PINK1-Parkin signaling activation, and can be used for parkinson's disease and related disorders research.
|
-
- HY-15027S2
-
|
5-Aminosalicylic acid-13C6
Mesalamine-13C6; 5-ASA-13C6; Mesalazine-13C6
|
PPAR
PAK
NF-κB
Endogenous Metabolite
|
|
|
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid[1]. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB[2][3][4].
|
-
- HY-129390
-
|
Orelabrutinib
ICP-022
|
Btk
|
Cancer
|
|
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
|
-
- HY-B1816
-
-
- HY-124037
-
|
SRT 1460
|
Sirtuin
|
Cancer
|
|
SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues.
|
-
- HY-P0316A
-
|
TP508 TFA
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
|
TP508 TFA is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 TFA activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-108586
-
|
NS3623
|
Potassium Channel
|
Neurological Disease
|
|
NS3623 is an activator of human ether-a-go-go-related gene (hERG1/KV11.1) potassium channels. NS3623 activates the IKr and Ito currents and has antiarrhythmic effect. NS3623 has a dual mode of action, being an inhibitor of hERG1 channels.
|
-
- HY-148905
-
|
p-Aminophenylmercuric acetate
|
Cathepsin
|
Infection
|
|
p-Aminophenylmercuric acetate is an organomercurial activator of matrix metalloproteinases (MMP). P-Aminophenylmercuric acetate participates in the activation and inhibition of MMP-8 by attacking protein sulfhydryl or inducing cysteine switching reaction. p-Aminophenylmercuric acetate promotes the shedding of betacellulin precursor (pro-BTC). p-Aminophenylmercuric acetate influences the binding of agonists and antagonists to the opiate receptor.
|
-
- HY-50694
-
|
Senicapoc
ICA-17043
|
Potassium Channel
|
Others
|
|
Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca 2+-activated K + channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca 2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM.
|
-
- HY-117433
-
-
- HY-113313S1
-
|
Aldosterone-d7
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Aldosterone-d7 is the deuterium labeled Aldosterone. Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level[1][2].
|
-
- HY-128468
-
-
- HY-N10884
-
|
Withasomniferolide A
|
Others
|
Others
|
|
Withasomniferolide A is a withanolide, isolated from a GABAA receptor positive activator methanol extract of the roots of Withania somnifera.
|
-
- HY-19800
-
|
ML-098
CID-7345532
|
Ras
|
Cancer
|
|
ML-098 (CID-7345532) is an activator of the GTP-binding protein Rab7 with an EC50 of 77.6 nM.
|
-
- HY-101790
-
-
- HY-N0897
-
|
Corylifol A
Corylifol-A; Corylinin
|
STAT
|
Others
|
|
Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
|
-
- HY-152860
-
-
- HY-13523
-
-
- HY-100181
-
-
- HY-118172
-
-
- HY-108599A
-
|
DCPLA-ME
DCPLA methyl ester
|
PKC
|
Neurological Disease
|
|
DCPLA-ME, the methyl ester form of DCPLA, is a potent PKCε activator for use in the treatment of neurodegenerative diseases.
|
-
- HY-N1913
-
-
- HY-111498
-
-
- HY-101625
-
|
Recilisib
ON 01210
|
Akt
PI3K
|
Cancer
|
|
Recilisib (ON 01210) is a radioprotectant, which can activate AKT, PI3K activities in cells.
|
-
- HY-N6971
-
-
- HY-15530
-
-
- HY-103074
-
-
- HY-B1399
-
-
- HY-N2318
-
-
- HY-50703
-
|
MK-2461
|
c-Met/HGFR
|
Cancer
|
|
MK-2461 is a novel ATP-competitive multitargeted inhibitor of activated c-Met with a mean IC50 of 2.5 nM.
|
-
- HY-117102
-
|
ANI-7
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
|
-
- HY-14993
-
|
SCH79797
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- HY-14994
-
|
SCH79797 dihydrochloride
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- HY-119672
-
|
Oct4 inducer-1
|
Oct3/4
|
Others
|
|
Oct4 inducer-1 (compound OAC-3) is a potent Oct4 activator. Oct4 inducer-1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. Oct4 inducer-1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time.
|
-
- HY-133596
-
|
12,14-Dichlorodehydroabietic acid
|
Potassium Channel
GABA Receptor
|
Neurological Disease
|
|
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release.
|
-
- HY-139504
-
|
CC-99677
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). CC-99677 is extracted from patent WO2020236636, compound 1.
|
-
- HY-10255AS1
-
|
Sunitinib-d4
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
|
-
- HY-119039
-
|
RU-301
|
TAM Receptor
|
Cancer
Inflammation/Immunology
|
|
RU-301 is a pan TAM inhibitor that blocks Gas6-induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis.
|
-
- HY-77251
-
|
TAK1/MAP4K2 inhibitor 1
|
MAP4K
MAP3K
|
Cancer
|
|
TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
|
-
- HY-132173
-
|
GL0388
|
Bcl-2 Family
|
Cancer
|
|
GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
|
-
- HY-114372
-
|
Lycopodine
|
Lipoxygenase
Caspase
Apoptosis
|
Cancer
|
|
Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
|
-
- HY-124822
-
|
COH-SR4
|
AMPK
|
Cancer
Metabolic Disease
|
|
COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders.
|
-
- HY-14266S
-
|
Dapivirine-d11
TMC120-d11; R147681-d11
|
HIV
Reverse Transcriptase
Apoptosis
Autophagy
|
Infection
|
|
Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2].
|
-
- HY-N0516
-
|
Casticin
Vitexicarpin
|
STAT
|
Inflammation/Immunology
|
|
Casticin is a methyoxylated flavonol isolated from Vitex rotundifolia, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
|
-
- HY-12695
-
-
- HY-101346
-
-
- HY-N0628
-
-
- HY-N10196
-
-
- HY-15577
-
|
GSK3787
|
PPAR
|
Cancer
|
|
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.
|
-
- HY-10590
-
-
- HY-P99911
-
-
- HY-19793
-
-
- HY-B0887
-
|
Permethrin
NRDC-143
|
Parasite
|
Infection
|
|
Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
|
-
- HY-145882
-
-
- HY-18985
-
-
- HY-14645A
-
|
(+)-DHMEQ
(1R,2R,6R)-Dehydroxymethylepoxyquinomicin; (1R,2R,6R)-DHMEQ
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
(+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ is the enantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kB than its enantiomer (+)-DHMEQ.
|
-
- HY-114745
-
|
MoTP
|
Others
|
Cancer
|
|
MoTP is a specific platelet activating factor receptor antagonist and can induce melanocyte ablation. MoTP can be used for the research of cancer.
|
-
- HY-103638
-
-
- HY-112125A
-
-
- HY-19097
-
-
- HY-101580
-
|
Paliroden
SR 57667
|
Others
|
Neurological Disease
|
|
Paliroden is an orally bioactive neurotrophic, non-peptidic compound that activates synthesis of endogenous neurotrophines, used for treatment of Alzheimer's Disease and Parkinson's.
|
-
- HY-139401
-
|
FAPI-34
|
FAP
|
Cancer
|
|
FAPI-34 is a fibroblast-activating protein (FAP) inhibitor with favorable pharmacokinetic and biochemical properties. (patent WO2019154886A1).
|
-
- HY-111202
-
-
- HY-12519S
-
|
Oltipraz-d3
RP 35972-d3; NSC 347901-d3
|
HIF/HIF Prolyl-Hydroxylase
HIV
Keap1-Nrf2
|
Cancer
|
|
Oltipraz-d3 is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
|
-
- HY-108591
-
|
L-364,373
R-L3
|
Potassium Channel
|
Cardiovascular Disease
|
|
L-364,373 (R-L3) is a voltage-gated Kv7.1 (KCNQ1)/mink channels activator. L-364,373 activates Iks (slow delayed rectifier potassium current) and shortens action potential duration in guinea pig cardiac myocytes, and suppresses early afterdepolarizations in rabbit ventricular myocytes.
|
-
- HY-148853
-
|
SRI-42127
|
Interleukin Related
|
Others
|
|
SRI-42127 is a HuR translocation inhibitor. HuR is an RNA regulator that binds to AREs, and HuR translocations promote the production of inflammatory cytokines in glial cells. However, SRI-42127 can destroy mRNA stability and inhibit gene promoter activation. SRI-42127 also inhibits microglial cell activation and attenuates recruitment/chemotaxis of neutrophils and monocytes.
|
-
- HY-142125
-
|
Broussochalcone A
|
Xanthine Oxidase
Reactive Oxygen Species
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Broussochalcone A is an antioxidant and an inhibitor of Xanthine Oxidase (IC50=2.21 μM), with free radical scavenging activity. Broussochalcone A inhibits iron-induced lipid peroxidation and nitric oxide synthesis in lipopolysaccharide (LPS) -activated macrophages. Broussochalcone A also induces Apoptosis of human renal carcinoma cells by increasing ROS levels and activating FOXO3 signaling pathways.
|
-
- HY-12496
-
|
NS-1619
|
Potassium Channel
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
NS-1619 is an opener of large conductance Ca 2+-activated K + (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells.
|
-
- HY-130354
-
|
Dibutyryl-cGMP sodium
Bt2cGMP sodium
|
Potassium Channel
|
Cardiovascular Disease
|
|
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels.
|
-
- HY-103308
-
|
TRAM-39
|
Potassium Channel
|
Neurological Disease
|
|
TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease.
|
-
- HY-112769
-
|
EX229
|
AMPK
|
Metabolic Disease
|
|
EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
|
-
- HY-B1546
-
|
Benzamil
Benzylamiloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
|
Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
|
-
- HY-116084
-
-
- HY-18307
-
|
SYN1143
|
c-Met/HGFR
|
Cancer
|
|
SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated.
|
-
- HY-B1546A
-
|
Benzamil hydrochloride
Benzylamiloride hydrochloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
|
Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM.
|
-
- HY-152468
-
|
Antitumor agent-83
|
Apoptosis
|
Cancer
|
|
Antitumor agent-83 is an activator of pro-apoptotic protein BAX and has significant anti-proliferation effect on tumor cells. Antiumor agent-83 mediates cell Apoptosis by inducing the conformational activation of BAX and has inhibitory effect on A549 cell cycle. Antiumor agent-83 has good metabolic stability and CYPs spectrum in vitro.
|
-
- HY-N8264
-
|
Moringin
|
TRP Channel
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities.
|
-
- HY-107460
-
|
LDN-211904 oxalate
|
Ephrin Receptor
|
Cancer
|
|
LDN-211904 oxalate (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 µM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC.
|
-
- HY-16561
-
|
Resveratrol
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
|
-
- HY-125665
-
|
Pheophorbide A
|
Others
|
Cancer
|
|
Pheophorbide A is an intermediate product in the chlorophyll degradation pathway and can be used as a photosensitizer. Pheophorbide A acts as a lymphovascular activator with antitumor activity.
|
-
- HY-137455
-
-
- HY-66021
-
|
6-FAM
6-Carboxyfluorescein
|
Fluorescent Dye
|
Others
|
|
6-FAM (6-Carboxyfluorescein) contains a carboxylic acid that can be used to react with primary amines via carbodiimide activation of the carboxylic acid.
|
-
- HY-128586A
-
-
- HY-16785A
-
-
- HY-14351
-
-
- HY-147010
-
-
- HY-107004A
-
-
- HY-N10114
-
-
- HY-N2283
-
-
- HY-B0686
-
-
- HY-N0593
-
-
- HY-N1533
-
-
- HY-145944
-
|
ASR-488
|
Apoptosis
|
Cancer
|
|
ASR-488 activates the mRNA-binding protein CPEB1, induces apoptosis and inhibits bladder cancer growth.
|
-
- HY-100941
-
-
- HY-143477
-
-
- HY-P1534
-
-
- HY-145542
-
-
- HY-N2506
-
-
- HY-113221
-
-
- HY-N0593A
-
-
- HY-N1838
-
-
- HY-P0249
-
-
- HY-N6617
-
-
- HY-150213
-
-
- HY-15869
-
-
- HY-128586
-
-
- HY-14831
-
|
Arhalofenate
MBX 102; JNJ 39659100
|
PPAR
|
Metabolic Disease
|
|
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
|
-
- HY-13519
-
-
- HY-100354
-
-
- HY-P4103
-
-
- HY-151520
-
-
- HY-78131B
-
-
- HY-100407
-
|
JNJ16259685
|
mGluR
|
Neurological Disease
|
|
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
|
-
- HY-N0411
-
|
β-Carotene
Provitamin A; beta-Carotene
|
Endogenous Metabolite
Apoptosis
Reactive Oxygen Species
|
Cancer
Metabolic Disease
|
|
β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities.
|
-
- HY-W017212
-
|
Methyl cinnamate
Methyl 3-phenylpropenoate
|
Tyrosinase
Bacterial
AMPK
|
Infection
Metabolic Disease
|
|
Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway.
|
-
- HY-109001A
-
|
(1S,2R)-Alicapistat
(1S,2R)-ABT-957
|
Proteasome
|
Neurological Disease
|
|
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
|
-
- HY-109001
-
|
Alicapistat
ABT-957
|
Proteasome
|
Neurological Disease
|
|
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
|
-
- HY-N7018
-
|
20-Hydroxyganoderic Acid G
|
Others
|
Inflammation/Immunology
|
|
20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the agent discovery of nerve inflammation diseases associated with microglia activated by LPS.
|
-
- HY-B1221
-
|
Flufenamic acid
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
|
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
-
- HY-16592
-
|
Brefeldin A
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
Bacterial
|
Cancer
Infection
|
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
|
-
- HY-16124
-
|
Canfosfamide
TLK-286; TER286
|
DNA-PK
Apoptosis
|
Cancer
|
|
Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies.
|
-
- HY-14600
-
-
- HY-103370
-
|
Talniflumate
BA 7602-06
|
Chloride Channel
|
Inflammation/Immunology
|
|
Talniflumate (BA 7602-06) is the proagent of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase. Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome.
|
-
- HY-107818
-
|
4-Hydroxychalcone
|
NF-κB
|
Inflammation/Immunology
Cardiovascular Disease
|
|
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice.
|
-
- HY-103238
-
|
RSVA405
|
AMPK
STAT
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity.
|
-
- HY-B1456AS
-
-
- HY-116003
-
|
12,13-DiHOME
|
Endogenous Metabolite
|
Metabolic Disease
|
|
12,13-DiHOME is a stimulator of Brown adipose tissue (BAT), as well as a thermogenic lipokine that activates BAT in response to cold. (±)12,13-DiHOME activates BAT fuel uptake and enhances cold tolerance, via promoting the translocation of the FA transporters FATP1 and CD36 to the cell membrane. (±)12,13-DiHOME can be used for research of metabolic disorders.
|
-
- HY-Y1832
-
|
o-Vanillin
2-Vanillin
|
Fungal
|
Cancer
Infection
|
|
o-Vanillin (2-Vanillin) is a nature product, could be extracted from Vanilla planifolia, Pinus koraiensis fruit. o-Vanillin is a potent antifungal agent. o-Vanillin inhibits the growth of mycelia by disrupting the integrity of cell walls and cell membranes. o-Vanillin inhibits Doxorubicin (HY-15142A)- and 4-hydroperoxycyclophosphamide-induced NF-κB activation.
|
-
- HY-131035
-
|
Lys-CoA TFA
|
Histone Acetyltransferase
|
Cancer
|
|
Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation.
|
-
- HY-12323
-
|
ISX-9
Isoxazole 9
|
Calcium Channel
|
Neurological Disease
|
|
ISX-9 (Isoxazole 9) is a potent inducer of adult neural stem cell differentiation. ISX-9 activates Ca 2+ influx through both voltage-gated Ca 2+ channels and NMDA receptors and increases neuroD expression. ISX-9 also induces cardiomyogenic differentiation of Notch-activated epicardium-derived cells (NECs).
|
-
- HY-100410
-
|
FCCP
Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone
|
Mitochondrial Metabolism
|
Cancer
|
|
FCCP is an uncoupler of oxidative phosphorylation (OXPHOS) in mitochondria. FCCP induces activation of PINK1 leading to Parkin Ser65 phosphorylation.
|
-
- HY-W011641
-
-
- HY-19354
-
|
Aglafoline
Aglafolin; Rocaglamide U; (-)-Methyl rocaglate
|
Others
|
Cardiovascular Disease
|
|
Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor).
|
-
- HY-100181B
-
-
- HY-B0513
-
-
- HY-15251
-
-
- HY-N6630
-
-
- HY-148031
-
-
- HY-P9969
-
|
Matuzumab
EMD 72000
|
EGFR
|
Cancer
|
|
Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth.
|
-
- HY-103683
-
-
- HY-15285
-
-
- HY-P3965
-
-
- HY-139742
-
|
ADTL-SA1215
|
Sirtuin
|
Cancer
|
|
ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer.
|
-
- HY-12213
-
|
CDDO-EA
CDDO ethyl amide; TP319; RTA 405
|
Keap1-Nrf2
|
Cancer
|
|
CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.
|
-
- HY-127018
-
|
Maltoheptaose
|
Others
|
Metabolic Disease
|
|
Maltoheptaose is an activator of phosphorylase B to prepare heptulose-2-phosphate. Maltoheptaose is a maltooligosaccharide contanins seven glucose units.
|
-
- HY-110274
-
-
- HY-N2084
-
-
- HY-136352
-
|
Adenosine 5'-succinate
|
Others
|
Others
|
|
Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin.
|
-
- HY-N9481
-
-
- HY-B0686A
-
-
- HY-131281
-
-
- HY-50910
-
-
- HY-P1562
-
|
PUMA BH3
|
Bcl-2 Family
|
Cancer
|
|
PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
|
-
- HY-101239
-
-
- HY-101833
-
-
- HY-101746
-
|
GSK376501A
|
PPAR
|
Metabolic Disease
|
|
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
|
-
- HY-126421
-
-
- HY-W007355
-
-
- HY-127018A
-
-
- HY-12524
-
|
Bikinin
Abrasin
|
GSK-3
|
Others
|
|
Bikinin is a non-steroidal, ATP-competitive inhibitor of plant GSK-3/Shaggy-like kinases and activates BR (brassinosteroids) signaling.
|
-
- HY-131282
-
-
- HY-N0593B
-
-
- HY-14233S
-
-
- HY-N6946
-
|
Mitraphylline
|
Others
|
Inflammation/Immunology
|
|
Mitraphylline is the major pentacyclic oxindolic alkaloid presented in Uncaria tomentosa. Mitraphylline inhibits lipopolysaccharide-mediated activation of primary human neutrophils.
|
-
- HY-101790A
-
-
- HY-112920
-
|
TM-25659
|
Others
|
Metabolic Disease
|
|
TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
|
-
- HY-13757A
-
|
Tamoxifen
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen activates autophagy and induces apoptosis. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse.
|
-
- HY-N11020
-
|
Cabenoside D
|
EBV
|
Infection
Inflammation/Immunology
|
|
Cabenoside D (compound 8) is a triterpenoid glycoside, which can be isolated from the methanol extract of lichen root. Cabenoside D shows anti-inflammatory activity and inhibits inflammation induced by 12-O-tetracylacyl hormone-13-acetate (TPA) in mice. Cabenoside D also inhibits TPA-induced Epstein-Barr virus (EBV) early antigen (EBV-EA) activation.
|
-
- HY-147187
-
|
MNK8
|
STAT
Apoptosis
Bcl-2 Family
Survivin
|
Cancer
|
|
MNK8 is a potent STAT3 (signal transducer and activator of transcription 3) inhibitor. MNK8 inhibits STAT3 activation and reduced its DNA binding ability. MNK8 shows good growth inhibition against hepatocellular carcinoma (HCC) cells. MNK8 induces apoptosis in HCC cells. MNK8 reduces prosurvival proteins expression and migration/invasion of HCC cells.
|
-
- HY-12005
-
|
Fingolimod hydrochloride
FTY720
|
LPL Receptor
PAK
|
Inflammation/Immunology
Cancer
|
|
Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator.
|
-
- HY-P1061
-
|
Colivelin
|
STAT
Amyloid-β
|
Neurological Disease
|
|
Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
|
-
- HY-P3412
-
|
MMI-0100
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia ex vivo and in vivo. MMI-0100 suppresses IL-6 expression without effect on IL-8 expression. MMI-0100 suppresses fibrotic processes such as vein graft disease.
|
-
- HY-108915
-
-
- HY-101446
-
|
HIOC
|
Trk Receptor
ERK
Apoptosis
|
Neurological Disease
|
|
HIOC is a potent and selective activator of TrkB (tropomyosin related kinase B) receptor. HIOC can pass the blood-brain and blood-retinal barriers.HIOC activates TrkB/ERK pathway and decreases neuronal cell apoptosis. HIOC attenuates early brain injury after SAH (subarachnoid hemorrhage). HIOC shows protective activity in an animal model for light-induced retinal degeneration.
|
-
- HY-125021
-
|
2BAct
|
Eukaryotic Initiation Factor (eIF)
|
Neurological Disease
|
|
2BAct is a highly selective, and orally active eIF2B (eukaryotic initiation factor 2B) activator with an EC50 of 33 nM. 2BAct prevents neurological defects caused by a chronic integrated stress response. 2BAct is able to penetrate the central nervous system (CNS). 2BAct displays improved solubility and pharmacokinetics relative to eIF2B activator ISRIB (HY-12495).
|
-
- HY-103474
-
|
Bicuculline methiodide
(+)-Bicuculline methiodide; d-Bicuculline methiodide
|
GABA Receptor
|
Neurological Disease
|
|
Bicuculline methiodide is a potent GABA(A) receptors blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca 2+ -activated K + channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca 2+ -activated K + current.
|
-
- HY-150971
-
|
ICy-Q
|
Pyroptosis
|
Cancer
|
|
ICy-Q is a quinone oxidoreductase 1 (NQO-1)-activated near-infrared (NIR) reagent which can react with NQO-1 to release the reduction product ICy-OH. ICy-OH selectively induces pancreatic cancer cell death through the pyroptosis pathway. ICy-Q can be used as an effective tool for rapid and accurate diagnosis of intraoperative pathological sections.
|
-
- HY-150587
-
|
Anti-inflammatory agent 31
|
ERK
NF-κB
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver.
|
-
- HY-100487
-
|
TAK-243
MLN7243
|
E1/E2/E3 Enzyme
NF-κB
Apoptosis
|
Cancer
|
|
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
|
-
- HY-16312
-
|
MDL-29951
|
iGluR
|
Neurological Disease
|
|
MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [ 3H]glycine binding in vitro and in vivo.
|
-
- HY-111098
-
-
- HY-111634
-
|
Epsilon-momfluorothrin
|
Others
|
Cancer
|
|
Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats.
|
-
- HY-151631
-
|
MRV03-070
|
Bacterial
|
Infection
|
|
MRV03-070 is an inhibitor of colibactin-activating peptidase ClbP with an IC50 value of 69 nM, acts like biosynthetic precursor precolibactin.
|
-
- HY-N10887
-
-
- HY-133127
-
|
AR453588
|
Glucokinase
|
Metabolic Disease
|
|
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity.
|
-
- HY-76847S
-
-
- HY-152097
-
|
(S)-ZG197
|
Bacterial
|
Infection
|
|
(S)-ZG197 is a highly selective Staphylococcus aureus Caseinolytic protease P (SaClpP) activator with an EC50 of 1.4 μM.
|
-
- HY-108439
-
|
Neurodazine
|
Wnt
Hedgehog
|
Neurological Disease
|
|
Neurodazine is a neurogenic inducer, serve as a promoter of neurogenesisin pluripotent cells. Neurodazine promotes neurogenesis by activating Wnt and Shh signaling pathways..
|
-
- HY-111973
-
|
Phaseic acid
|
Others
|
Metabolic Disease
|
|
Phaseic acid is a Abscisic acid terpenoid catabolite that can able to activate a subset of Abscisic acid repectors. Phaseic acid is a plant hormone associated with photosynthesis arrest and abscission.
|
-
- HY-111928
-
-
- HY-N2209
-
|
Angeloylgomisin H
|
PPAR
|
Metabolic Disease
|
|
Angeloylgomisin H, as a major lignin extract of Schisandra rubriflora, has the potential to improve insulin-stimulated glucose uptake by activating PPAR-γ.
|
-
- HY-102066
-
|
Utatrectinib
AZD-7451
|
Trk Receptor
|
Cancer
|
|
Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors.
|
-
- HY-W089922
-
|
D-erythro-Sphingosine hydrochloride
Erythrosphingosine hydrochloride; erythro-C18-Sphingosine hydrochloride; trans-4-Sphingenine hydrochloride
|
TRP Channel
|
Neurological Disease
|
|
D-erythro-Sphingosine (Erythrosphingosine) hydrochloride is a specific TRPM3 activator. D-erythro-Sphingosine also induces retinoblastoma protein dephosphorylation.
|
-
- HY-111789
-
-
- HY-133127A
-
-
- HY-N10359
-
-
- HY-12885
-
|
ADU-S100
MIW815; ML RR-S2 CDA
|
STING
|
Inflammation/Immunology
|
|
ADU-S100 (MIW815), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.
|
-
- HY-12357
-
-
- HY-117962A
-
-
- HY-76847S3
-
-
- HY-15253
-
-
- HY-13694
-
-
- HY-131283
-
-
- HY-B0923
-
|
Danthron
Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone
|
AMPK
Autophagy
Bacterial
Virus Protease
|
Cancer
|
|
Danthron is a natural product extracted from the traditional Chinese medicine Salvia miltiorrhiza Bunge. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.
|
-
- HY-Y0152
-
|
Cinchonine
(8R,9S)-Cinchonine; LA40221
|
Apoptosis
Parasite
|
Cancer
|
|
Cinchonine is a natural compound present in Cinchona bark. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
|
-
- HY-B0809S
-
-
- HY-P0249B
-
-
- HY-B1140S
-
-
- HY-76847S2
-
-
- HY-P3965A
-
-
- HY-N0606
-
-
- HY-N0892
-
-
- HY-N6913
-
|
3α-Hydroxymogrol
|
AMPK
|
Metabolic Disease
|
|
3α-Hydroxymogrol is a triterpenoid isolated from Siraitia grosvenorii Swingle, acts as a potent AMPK activator, and enhances AMPK phosphorylation.
|
-
- HY-76847S1
-
-
- HY-B0099
-
-
- HY-16561S1
-
|
Resveratrol-13C6
trans-Resveratrol-13C6; SRT501-13C6
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
|
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
|
-
- HY-108596
-
|
BL-1249
|
Potassium Channel
|
Inflammation/Immunology
|
|
BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
|
-
- HY-16561S
-
|
Resveratrol-d4
trans-Resveratrol-d4; SRT501-d4
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
|
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
|
-
- HY-17363S1
-
|
Dimethyl fumarate-d2
|
Autophagy
HIV
Keap1-Nrf2
Endogenous Metabolite
Reactive Oxygen Species
|
|
|
Dimethyl fumarate-d2 is the deuterium labeled Dimethyl fumarate[1]. Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research[2][3].
|
-
- HY-16915
-
|
RPR-260243
|
Potassium Channel
|
Cardiovascular Disease
|
|
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel.
|
-
- HY-P1740
-
|
RGD peptide (GRGDNP)
|
Integrin
Apoptosis
|
Inflammation/Immunology
|
|
RGD peptide (GRGDNP) is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) plays an important role in cell adhesion, migration, growth, and differentiation.
|
-
- HY-124151
-
|
Adenosine-2'-monophosphate
2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate
|
Adenosine Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Adenosine-2'-monophosphate (2'-AMP) is converted by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway). Adenosine-2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A2A receptor activation.
|
-
- HY-P1061A
-
|
Colivelin TFA
|
STAT
Amyloid-β
Apoptosis
|
Neurological Disease
|
|
Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
|
-
- HY-P3624
-
|
Cenderitide
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Cenderitide is a potent agonist of particulate guanylyl cyclase receptor (pGC). Cenderitide is a natriuretic peptide (NP) composed of C-type natriuretic peptide (CNP) fused to the C-terminus of Dendroaspis natriuretic peptide (DNP). Cenderitide activates both pGC-A and pGC-B, activates the second messenger cGMP, suppresses aldosterone, and preserves GFR without reducing blood pressure. Cenderitide can be used for heart failure research.
|
-
- HY-131296
-
|
5-A-RU-PABC-Val-Cit-Fmoc
|
Others
|
Inflammation/Immunology
|
|
5-A-RU-PABC-Val-Cit-Fmoc is the proagent of 5-A-RU. 5-A-RU, a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways.
|
-
- HY-110247
-
|
TRAF-STOP inhibitor 6877002
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
Cardiovascular Disease
|
|
TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques.
|
-
- HY-Z0816
-
|
Dehydronitrosonisoldipine
|
Calcium Channel
|
Others
|
|
Dehydronitrosonisoldipine, a derivative of Nisoldipine (HY-17402), is an irreversible and cell-permeant sterile alpha and TIR motif-containing 1 (SARM1) inhibitor. Dehydronitrosonisoldipine acts mainly by blocking SARM1 activation but not its enzymatic activities. Dehydronitrosonisoldipine inhibits SARM1 and axon degenration (AxD) by covalently modifying cysteines, also inhibits the Vincristine-activated cADPR production in neurons. Dehydronitrosonisoldipine can be used for researching neurodegenerative disorders.
|
-
- HY-142694
-
-
- HY-N0492S
-
-
- HY-134205A
-
|
CBR-470-1
|
Keap1-Nrf2
|
Metabolic Disease
Neurological Disease
|
|
CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP +-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.
|
-
- HY-114363A
-
|
SRI 31215 TFA
|
c-Met/HGFR
|
Cancer
|
|
SRI 31215 (TFA) is a Matriptase/Hepsin/hepatocyte growth factor activator (HGFA) triplex inhibitor and mimics the activity of HAI-1/2 (endogenous inhibitors of HGF activation). SRI 31215 has potent inhibitory activity against matriptase, hepsin and HGFA with IC50 values of 0.69 μM, 0.65 μM and 0.30 μM, respectively. SRI 31215 can be used for the research of cancer.
|
-
- HY-137862
-
|
1-Oleoyl lysophosphatidic acid
1-Oleoyl-sn-glycero-3-phosphate; 1-Oleoyl-LPA
|
LPL Receptor
|
Neurological Disease
|
|
1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant lysophosphatidic acid (LPA) species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation. 1-Oleoyl lysophosphatidic acid increases SRE-driven β-galactosidase activity.
|
-
- HY-19356
-
|
Rocaglamide
Roc-A
|
NF-κB
HSP
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
|
-
- HY-12695B
-
-
- HY-P3523
-
|
KGDS
|
Integrin
|
Others
|
|
KGDS is synthetic peptides, targeting integrin GPIIb-IIIa located on the membrane of human activated platelets. Amino acid sequence: Lys-Gly-Asp-Ser.
|
-
- HY-15002
-
|
AST 487
NVP-AST 487
|
RET
FLT3
VEGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
|
-
- HY-132878
-
|
FgGpmk1-IN-1
|
Others
|
Infection
|
|
FgGpmk1-IN-1 is a novel fusarium graminearum mitogen-activated protein kinase (FgGpmk1) inhibitor with an EC50 value of 3.46 μg/mL.
|
-
- HY-N8816
-
-
- HY-119240
-
-
- HY-N3196
-
-
- HY-120272
-
|
SMAP-2
DT-1154
|
Phosphatase
|
Cancer
|
|
SMAP-2 (DT-1154) is an orally active protein phosphatase 2A (PP2A) activator, with anti-cancer activity.
|
-
- HY-10535
-
|
Evofosfamide
TH-302
|
Apoptosis
|
Cancer
|
|
Evofosfamide (TH-302) is a hypoxia-activated proagent with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.
|
-
- HY-15718A
-
-
- HY-B1378
-
-
- HY-W015061
-
-
- HY-147295
-
|
Odetiglucan
BTH 1677; Imprime PGG
|
Others
|
Cancer
Inflammation/Immunology
|
|
Odetiglucan, a novel beta glucan, is a potent immunostimulant. Odetiglucan activates innate immune effector cells and triggers a coordinated anti-cancer immune response.
|
-
- HY-137207
-
|
MK-28
|
PERK
|
Neurological Disease
|
|
MK-28 is a potent and selective PERK activator. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
|
-
- HY-115453
-
|
UBCS039
|
Sirtuin
Autophagy
|
Cancer
|
|
UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.
|
-
- HY-19205A
-
-
- HY-101929
-
-
- HY-P3710
-
-
- HY-131763
-
-
- HY-108634
-
-
- HY-N0486S13
-
-
- HY-148507
-
|
GSK1790627
|
MEK
|
Cancer
|
|
GSK1790627 is the N-deacetylated metabolite of Trametinib (HY-10999). Trametinib is an orally active MEK inhibitor, and activates autophagy and induces apoptosis.
|
-
- HY-76814
-
|
Calcitriol-d6
|
VD/VDR
|
Metabolic Disease
|
|
Calcitriol-d6 is the deuterium labeled Calcitriol. Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR)[1].
|
-
- HY-U00123
-
-
- HY-125465
-
|
SLLN-15
|
Autophagy
|
Cancer
|
|
SLLN-15 is an oral active, selective and potent enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC).
|
-
- HY-13108
-
|
Bz 423
BZ48
|
Bcl-2 Family
|
Inflammation/Immunology
|
|
Bz 423 is a pro-apoptotic 1,4-benzodiazepine with therapeutic properties in murine models of lupus demonstrating selectivity for autoreactive lymphocytes, and activates Bax and Bak.
|
-
- HY-N2530
-
-
- HY-12306
-
|
8-Bromo-cAMP sodium salt
8-Br-Camp sodium salt
|
PKA
|
Cancer
|
|
8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA).
|
-
- HY-13294
-
-
- HY-100611
-
-
- HY-139573
-
-
- HY-129088
-
-
- HY-75992
-
|
trans-Doxercalciferol
|
VD/VDR
|
Others
|
|
trans-Doxercalciferol is an isomer of Doxercalciferol. Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.
|
-
- HY-N10926
-
|
(+)-Glaucarubinone
|
AP-1
|
Cancer
|
|
(+)-Glaucarubinone is a potent AP-1 (activator protein-1) inhibitor with an EC50 value of 0.13 µM. (+)-Glaucarubinone shows noncytotoxic.
|
-
- HY-113505
-
|
Delta-12-Prostaglandin J2
Δ12-PGJ2
|
Endogenous Metabolite
Apoptosis
|
Cancer
|
|
Delta-12-Prostaglandin J2 (Δ12-PGJ2) is a cyclopentenone prostaglandin (PG) with anti-proliferative effect on various tumor cell growth. Delta-12-Prostaglandin J2, a naturally occurring dehydration product of prostaglandin D2, is able to induce apoptosis in HeLa cells via caspase activation.
|
-
- HY-15671
-
|
GKA50
|
Glucokinase
|
Metabolic Disease
|
|
GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats.
|
-
- HY-102011A
-
|
BMS-1166 hydrochloride
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
|
BMS-1166 hydrochloride is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 hydrochloride induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 hydrochloride antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-148368
-
|
CYD-4-61
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis.
|
-
- HY-124697
-
|
BMP signaling agonist sb4
|
TGF-β Receptor
|
Cancer
|
|
BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
|
-
- HY-137638
-
|
Sp-5,6-DCl-cBIMPS
|
PKA
|
Metabolic Disease
|
|
Sp-5,6-DCl-cBIMPS is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS stimulates insulin release. Sp-5,6-DCl-cBIMPS inhibits U46619-induced activation of Rho, Gq and G12/G13 in platelets.
|
-
- HY-N1970
-
|
5,7-Dihydroxychromone
|
Keap1-Nrf2
Arenavirus
Caspase
PARP
|
Neurological Disease
|
|
5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells.
|
-
- HY-124748A
-
|
ENMD-1068 hydrochloride
|
Protease Activated Receptor (PAR)
Apoptosis
|
Inflammation/Immunology
|
|
ENMD-1068 hydrochloride is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 hydrochloride reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 hydrochloride also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 hydrochloride can be used in the study of endometriosis and liver fibrosis.
|
-
- HY-13757
-
|
Tamoxifen Citrate
ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 µM and 1.8 µM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse.
|
-
- HY-13757AS1
-
|
Tamoxifen-d3
ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3
|
Estrogen Receptor/ERR
Apoptosis
Autophagy
HSP
|
Cancer
|
|
Tamoxifen-d3 is the deuterium labeled Tamoxifen[1]. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[2][3][4]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[6]. Tamoxifen activates autophagy and induces apoptosis[5]. Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse[7].
|
-
- HY-141645
-
|
IMM-H007
WS070117
|
AMPK
TGF-β Receptor
NF-κB
JNK
AP-1
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
|
IMM-H007 (WS070117) is an orally active and potent AMPK (AMP-activated protein kinase) activator and TGFβ1 (transforming growth factor β1) antagonist. IMM-H007 has protective effects in cardiovascular diseases via activation of AMPK. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 degradation. IMM-H007 resolves hepatic steatosis in HFD-fed hamsters by the regulation of lipid metabolism. IMM-H007 can be used for the research of nonalcoholic fatty liver disease (NAFLD) and inflammatory atherosclerosis.
|
-
- HY-N0486S11
-
-
- HY-P1314
-
-
- HY-16397AS
-
-
- HY-N0377
-
-
- HY-16511
-
|
Upamostat
WX-671
|
Ser/Thr Protease
PAI-1
|
Cancer
|
|
Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
|
-
- HY-W011303
-
-
- HY-112675
-
-
- HY-U00123A
-
-
- HY-75041
-
|
Calcitriol Impurities A
|
VD/VDR
|
Metabolic Disease
|
|
Calcitriol Impurities A is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- HY-138558
-
-
- HY-115938
-
|
BEC2
|
Others
|
Metabolic Disease
|
|
BEC2 is an ester derivative of Baicalin, with good lipid-lowering activity. BEC2 can direct activate the carnitine palmitoyltransferase 1A (CPT1A).
|
-
- HY-115890
-
|
Thiocysteine
|
Reactive Oxygen Species
|
Others
|
|
Thiocystine is the trisulfide analog of cysteine, it can modify cysteine in proteins. Thiocystine is an activator for aminolevulinate synthetase. Thiocystine can be used for cysteine metabolism research.
|
-
- HY-N0605
-
-
- HY-N3055
-
|
Pinusolide
|
Apoptosis
|
Cancer
|
|
Pinusolide is a known platelet-activating factor (PAF) receptor binding antagonist. Pinusolide not only decreases the proliferation activity of tumor cells but specifically induces apoptosis.
|
-
- HY-P3107
-
-
- HY-N0197
-
-
- HY-50714
-
|
Quiflapon sodium
MK-591 sodium
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
|
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
|
-
- HY-W048510
-
|
Epiquinidine
|
Others
|
Others
|
|
Epiquinidine, a quinine analogue, can be used as the ggTas2r1 agonist. Epiquinidine activates ggTas2r1 at or beyond 10 µM.
|
-
- HY-133739
-
|
NBD-125
|
RAR/RXR
|
Cancer
|
|
NBD-125 (B-12), a berberine analogue, is an RXRα activator, with an IC50 of 31.10 μM in KM12C cell.
|
-
- HY-143401
-
|
Hit 1
|
Others
|
Metabolic Disease
|
|
Hit 1 is an activator of ansulin degrading enzyme (IDE), with an EC50 of 5.5 μM. Hit 1 can decrease glucose-stimulating insulin secretion.
|
-
- HY-N0510A
-
|
Aristolochic acid sodium salt
Aristolochic acid I sodium; TR 1736 sodium; Sodium aristolochate
|
Biochemical Assay Reagents
|
Others
|
|
Aristolochic acid sodium salt (Sodium aristolate 1) is a component of some Chinese herbal medicines and is responsible for nephrotoxicity. It is a proagent that is activated by reduction of nitro groups to amines, resulting in the formation of cytotoxic DNA adducts.
|
-
- HY-139787A
-
|
Donidalorsen sodium
|
Others
|
Others
|
|
Donidalorsen (sodium) is an antisense oligonucleotide designed to reduce the production of prekallikrein (PKK). PKK plays an important role in the activation of inflammatory mediators associated with acute attacks of Hereditary angioedema (HAE).
|
-
- HY-15725
-
-
- HY-145788
-
-
- HY-110192
-
-
- HY-109030
-
-
- HY-16642A
-
-
- HY-100965
-
-
- HY-N10483
-
|
Telekin
|
Apoptosis
|
Cancer
|
|
Telekin is an eucalyptus-type sesquiterpene lactone compound found in Carpesium divaricatum. Telekin can activate mitochondria-mediated cell apoptosis and has anticancer activity.
|
-
- HY-112929
-
|
DT-061
|
Phosphatase
|
Cancer
|
|
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
|
-
- HY-N2370
-
-
- HY-19700
-
-
- HY-N10062
-
|
Amakusamine
|
RANKL/RANK
|
Others
|
|
Amakusamine inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced formation of multinuclear osteoclasts with an IC50 value of 10.5 μM in RAW264 cells.
|
-
- HY-139787
-
|
Donidalorsen
|
Others
|
Others
|
|
Donidalorsen is an antisense oligonucleotide designed to reduce the production of prekallikrein (PKK). PKK plays an important role in the activation of inflammatory mediators associated with acute attacks of Hereditary angioedema (HAE).
|
-
- HY-13296
-
|
PYR-41
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
|
-
- HY-109128
-
|
Danicamtiv
MYK-491
|
Myosin
|
Cancer
|
|
Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.
|
-
- HY-145127
-
|
ETZ
C3-CA-DTZ
|
Fluorescent Dye
|
Neurological Disease
|
|
ETZ (C3-CA-DTZ) is a promising luciferase substrate (prosubstrate) activatable in vivo by nonspecific esterase to enhance the brain delivery of the luciferin.
|
-
- HY-131958
-
|
D942
|
AMPK
|
Cancer
|
|
D942 is a cell penetrant AMPK activator and partially inhibits the mitochondrial complex I. In multiple myeloma cells, D942 inhibits cell growth.
|
-
- HY-104026B
-
-
- HY-19084
-
-
- HY-P3641
-
-
- HY-139212
-
|
IXA6
|
IRE1
|
Others
|
|
IXA6 is a novel IRE1/XBP1s activator, and can induce IRE1 RNase activity.
|
-
- HY-111498A
-
|
RGX-104
Abequolixron
|
LXR
|
Cancer
Inflammation/Immunology
|
|
RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
|
-
- HY-N0629
-
-
- HY-12885B
-
-
- HY-153344
-
|
FX-909
|
PPAR
|
Cancer
|
|
FX-909 is a covalent peroxisome proliferator-activated receptor gamma (PPARG) inverse agonist. FX-909 can be used for the research of cancer.
|
-
- HY-116084S
-
-
- HY-100671
-
|
L002
|
Histone Acetyltransferase
STAT
|
Cancer
Inflammation/Immunology
|
|
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
|
-
- HY-P3316
-
|
OSK-1
|
Potassium Channel
|
Inflammation/Immunology
Neurological Disease
|
|
OSK-1 is a potent Kv channel blocker with IC50s of of 0.6 nM, 5.4 nM, 0.014 nM for Kv1.1, Kv1.2 and Kv1.3, respectively. OSK1 is a moderate blocker of Ca 2+-activated KCa3.1 channel with an IC50 of 225 nM. OSK-1 belongs to α-KTx3 toxins and is used as a immunosuppressive agent.
|
-
- HY-B1221S1
-
-
- HY-P3444
-
|
CD31
PECAM-1
|
SHP2
Bacterial
|
Metabolic Disease
Inflammation/Immunology
|
|
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation -.
|
-
- HY-15186
-
|
Ipatasertib
GDC-0068; RG7440
|
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models.
|
-
- HY-117433S
-
-
- HY-112671
-
|
CDDO-dhTFEA
RTA dh404
|
Keap1-Nrf2
NF-κB
|
Inflammation/Immunology
|
|
CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB. CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats.
|
-
- HY-10201
-
|
Sorafenib
Bay 43-9006
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Sorafenib (Bay 43-9006) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is a ferroptosis activator.
|
-
- HY-15671A
-
|
GKA50 quarterhydrate
|
Glucokinase
|
Metabolic Disease
|
|
GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats.
|
-
- HY-16708A
-
|
ZLN024 hydrochloride
|
AMPK
|
Metabolic Disease
|
|
ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
|
-
- HY-121629
-
|
PS210
|
PDK-1
|
Cancer
|
|
PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.
|
-
- HY-P1740A
-
|
RGD peptide (GRGDNP) (TFA)
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
RGD peptide (GRGDNP) TFA is an inhibitor of integrin-ligand interactions. RGD peptide (GRGDNP) TFA competitively inhibits α5β1 binding with extracellular matrice (ECM). RGD peptide (GRGDNP) TFA promotes apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing. RGD peptide (GRGDNP) TFA plays an important role in cell adhesion, migration, growth, and differentiation.
|
-
- HY-101329S
-
|
Anthracene-9-carboxylic acid-d9
9-Anthracenecarboxylic acid-d9
|
Chloride Channel
|
Others
|
|
Anthracene-9-carboxylic acid-d9 is the deuterium labeled Anthracene-9-carboxylic acid[1]. Anthracene-9-carboxylic acid (9-Anthracenecarboxylic acid) is an anthracene derivative traditionally used to block and identify Ca2+-activated Cl- currents (CaCCs) in various cell types, like diverse smooth muscle cells, epithelial cells and salivary gland cells[2].
|
-
- HY-N0674A
-
|
Dehydrocorydaline chloride
13-Methylpalmatine chloride
|
Bcl-2 Family
Caspase
PARP
p38 MAPK
Parasite
Autophagy
|
Cancer
Infection
|
|
Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline chloride shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
|
-
- HY-N0822
-
|
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
AIM2
|
Cancer
|
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
|
-
- HY-15371
-
|
Forskolin
Coleonol; Colforsin; HL 362
|
Adenylate Cyclase
FXR
Autophagy
|
Cancer
Endocrinology
Metabolic Disease
Inflammation/Immunology
|
|
Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
|
-
- HY-107544
-
|
8-pCPT-2'-O-Me-cAMP-AM
|
PKA
|
Metabolic Disease
|
|
8-pCPT-2'-O-Me-cAMP-AM is a cyclic AMP analogue, selectively activates Epac-Rap signaling pathway. 8-pCPT-2'-O-Me-cAMP-AM protects renal function by activating Epac from ischemia injury. 8-pCPT-2'-O-Me-cAMP-AM also stimulates insulin secretion by interaction with PKA pathway.
|
-
- HY-B1221S
-
-
- HY-128358
-
|
MR-L2
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM.
|
-
- HY-127019
-
|
Nigericin
|
Sodium Channel
NOD-like Receptor (NLR)
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K +/H + ionophore, promoting K +/H + exchange across mitochondrial membranes.Nigericin can be a NLRP3 activator that induces the release of IL-1β as a NALP3-dependent manner. Nigericin triggers eryptosis, an effect paralleled by ROS formation, and in part due to induction of oxidative stress. Nigericin triggers apoptosis.
|
-
- HY-10201A
-
|
Sorafenib Tosylate
Bay 43-9006 Tosylate
|
Raf
VEGFR
FLT3
Autophagy
Ferroptosis
Apoptosis
|
Cancer
|
|
Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator.
|
-
- HY-16708
-
|
ZLN024
|
AMPK
|
Metabolic Disease
|
|
ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
|
-
- HY-N1490
-
-
- HY-17394
-
-
- HY-122908
-
|
Atuliflapon
AZD5718
|
FLAP
|
Cardiovascular Disease
|
|
Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.
|
-
- HY-N6781
-
|
Ophiobolin A
|
Phosphodiesterase (PDE)
|
Cancer
Infection
|
|
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
|
-
- HY-N0177
-
|
Diosgenin
|
STAT
|
Metabolic Disease
|
|
Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57.
|
-
- HY-13772
-
-
- HY-112650
-
-
- HY-139621
-
-
- HY-115769
-
|
1,2-Didecanoylglycerol
|
PKC
|
Endocrinology
|
|
1,2-Didecanoylglycerol, a synthetic diacylglycerol, is metabolized by platelets to 1,2-didecanoylphosphatidic acid (PA10) and activates protein kinase C (PKC).
|
-
- HY-101360
-
-
- HY-120872
-
|
AJS1669 free acid
|
Others
|
Metabolic Disease
|
|
AJS1669 free acid is a potent and orally available glycogen synthase (GS) activator. AJS1669 improves glucose metabolism and reduces body fat mass in mice[1].
|
-
- HY-N0754
-
|
Eupalinolide A
|
HSP
|
Inflammation/Immunology
|
|
Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
|
-
- HY-B0649S1
-
-
- HY-19330
-
-
- HY-N4322
-
-
- HY-77274
-
|
Calcitriol Impurities D
|
VD/VDR
|
Metabolic Disease
|
|
Calcitriol Impurities D is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- HY-P1026
-
-
- HY-N0474
-
-
- HY-112331
-
|
SJ000291942
|
TGF-β Receptor
|
Cancer
|
|
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
|
-
- HY-A0084
-
|
Procainamide hydrochloride
|
Autophagy
|
Cancer
|
|
Procainamide hydrochloride is an anti-arrhythmic agent and is used to treat cardiac arrhythmia; induces rapid block of the batrachotoxin(BTX)-activated sodium channels of the heart muscle and acts as antagonist to long gating closures.
|
-
- HY-136232
-
-
- HY-103087
-
|
FIN56
|
Ferroptosis
|
Others
|
|
FIN56 is a specific inducer of ferroptosis. FIN56 induces ferroptosis by inducing degradation of GPX4. FIN56 also binds to and activates squalene synthase.
|
-
- HY-100534
-
|
IDE 2
|
TGF-beta/Smad
|
Others
|
|
IDE2 is a small molecule cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) by activating the TGF-βsignaling pathway.
|
-
- HY-103322
-
|
6-Bnz-cAMP sodium salt
|
PKA
|
|
|
6-Bnz-cAMP sodium salt is a cell-permeable cAMP analog. 6-Bnz-cAMP selectively activates cAMP-dependent PKA but not Epac signaling pathways.
|
-
- HY-W089835
-
-
- HY-120261
-
-
- HY-147005
-
-
- HY-B0649
-
-
- HY-N2337
-
-
- HY-15675
-
|
AZD1656
|
Glucokinase
|
Metabolic Disease
|
|
AZD1656 is a potent, selective and orally active glucokinase activator with an EC50 of 60 nM. AZD1656 has the potential for type 2 diabetes research.
|
-
- HY-N0436
-
|
Engeletin
|
NF-κB
|
Infection
Inflammation/Immunology
|
|
Engeletin is a flavanonol glycoside isolated from Smilax glabra Roxb. , inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
|
-
- HY-B0021
-
-
- HY-N6046
-
-
- HY-P1314A
-
-
- HY-B0795
-
|
MHY1485
|
mTOR
Autophagy
|
Cancer
|
|
MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
|
-
- HY-N10393
-
|
Vibsanin A
|
PKC
HSP
|
Cancer
|
|
Vibsanin A, a protein kinase C (PKC) activator, exhibits anti-proliferative activity against human cancer cell lines. Vibsanin A is also a HSP90 inhibitor.
|
-
- HY-N2149A
-
-
- HY-15145A
-
-
- HY-P2008
-
-
- HY-135013
-
|
Umbellulone
|
TRP Channel
|
Neurological Disease
|
|
Umbellulone is an active constituent of the leaves of Umbellularia californica. Umbellulone stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.
|
-
- HY-N2149
-
-
- HY-N0826
-
-
- HY-N0050
-
|
Allomatrine
(+)-Allomatrine
|
Others
|
Neurological Disease
|
|
Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors.
|
-
- HY-15145
-
-
- HY-P1562A
-
|
PUMA BH3 TFA
|
Bcl-2 Family
|
Cancer
|
|
PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
|
-
- HY-B1560
-
|
Bismuth subgallate
|
Factor Xa
|
Others
|
|
Bismuth subgallate, a hemostatic agent, acts on coagulation factor XII (Hageman factor), leading to the activation of the coagulation cascade and improving early formation of a fibrin clot.
|
-
- HY-17592
-
|
Bithionol
|
Parasite
Bacterial
|
Cancer
Infection
|
|
Bithionol is an antibacterial, anthelmintic, and algaecide agent. Bithionol is also a potent inhibitor of soluble adenylyl cyclase through binding to the allosteric activator site (IC50: 4 μM).
|
-
- HY-N1469
-
-
- HY-B0926A
-
|
Sodium diatrizoate
Diatrizoic acid sodium salt; Sodium amidotrizoate
|
Apoptosis
|
Inflammation/Immunology
|
|
Sodium diatrizoate (Diatrizoic acid sodium salt) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Sodium diatrizoate induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium.
|
-
- HY-N0014
-
-
- HY-N0233
-
|
Bavachin
Corylifolin
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bavachin, a flavonoid first isolated from seeds of P. corylifolia, acts as a phytoestrogen that activates the estrogen receptors ERα and ERβ with EC50s of 320 and 680 nM, respectively.
|
-
- HY-115767
-
|
(±)-1,2-Diolein
1,2-Dioleoyl-rac-glycerol
|
PKC
|
Others
|
|
(±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) is a PKC activator. (±)-1,2-Diolein increases myotubes Ca 2+ influx.
|
-
- HY-N1208
-
|
Spiradine F
O-Acetylspiradine G; Spiradine G acetate
|
Others
|
Cardiovascular Disease
|
|
Spiradine F is a main alkaloidal component of spiraea japonioa L. fil. Spiradine F derivative can inhibit platelet-activating factor (PAF)-induced platelet aggregation.
|
-
- HY-144813
-
|
Gü2602
|
Cathepsin
|
Cancer
Inflammation/Immunology
|
|
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.
|
-
- HY-B0887S1
-
|
Permethrin-d9
|
Parasite
|
Infection
|
|
Permethrin-d9 is the deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
|
-
- HY-14739
-
|
Choline Fenofibrate
ABT-335
|
PPAR
COX
|
Cardiovascular Disease
|
|
Choline Fenofibrate (ABT-335), a choline salt of Fenofibric acid (HY-B0760), releases free Fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.
|
-
- HY-101255
-
|
ODQ
|
Guanylate Cyclase
Apoptosis
|
Cancer
|
|
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
|
-
- HY-133558
-
|
VII-31
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways.
|
-
- HY-17495
-
-
- HY-N0168A
-
-
- HY-N3245
-
-
- HY-N6018
-
-
- HY-N0486S4
-
-
- HY-138820
-
|
SW02
|
HSP
|
Neurological Disease
|
|
SW02 is a potent activator of ATPase activity of Hsp70, with an EC50 of 150 μM. SW02 leads to accumulation of both total tau and phosphorylated tau (pTau).
|
-
- HY-W011890
-
-
- HY-19770
-
|
GSK2981278
|
ROR
|
Inflammation/Immunology
|
|
GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
|
-
- HY-B0387
-
-
- HY-N0486S
-
-
- HY-15004
-
|
AUZ 454
K03861
|
CDK
|
Cancer
|
|
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
|
-
- HY-N0486S12
-
-
- HY-13595
-
|
Chrysophanol
Chrysophanic acid
|
EGFR
|
Cancer
|
|
Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
|
-
- HY-W034419
-
|
STIMA-1
|
Others
|
Others
|
|
STIMA-1 is an active compound. STIMA-1 can restore the activity of p63. STIMA-1 can activate the proliferation and differentiation of keratinocytes.
|
-
- HY-12212
-
-
- HY-N0486S9
-
-
- HY-121134
-
-
- HY-104073
-
-
- HY-153175
-
|
BT44
|
RET
|
Neurological Disease
|
|
BT44 is a selective RET activator. BT44 can penetrate through the blood-brain barrier and can be used for the research of neurodegenerative disorders and diabetes mellitus.
|
-
- HY-153343
-
|
BAY 2965501
|
DGK
|
Cancer
|
|
BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer.
|
-
- HY-10003
-
|
Alfacalcidol
1-hydroxycholecalciferol; 1.alpha.-Hydroxyvitamin D3
|
VD/VDR
|
Metabolic Disease
|
|
Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis.
|
-
- HY-103640
-
|
Amifostine thiol dihydrochloride
WR-1065 dihydrochloride
|
MDM-2/p53
|
Cancer
|
|
Amifostine thiol (WR-1065) dihydrochloride can protect normal tissues from the toxic effects of certain cancer agents and activate p53 through a JNK-dependent signaling pathway.
|
-
- HY-134001
-
-
- HY-110087
-
-
- HY-10257
-
-
- HY-N0708
-
-
- HY-13851
-
|
PS47
|
PDK-1
|
Others
|
|
PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48.
|
-
- HY-B1899A
-
-
- HY-121160
-
|
Amiprilose
SM1213; Therafectin
|
Bacterial
|
Cancer
Infection
|
|
Amiprilose (SM1213; Therafectin) is a potent inhibitor against Hepatocellular carcinoma (HCC). Amiprilose induces lymphokine-induced macrophage activation directly to kill Listeria monocytogenes.
|
-
- HY-13008
-
-
- HY-100316
-
-
- HY-P0233
-
-
- HY-122808
-
|
(-)-Camphoric acid
|
mGluR
|
Metabolic Disease
|
|
(-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1.
|
-
- HY-135898
-
-
- HY-18286
-
|
NCGC00229600
|
TSH Receptor
|
Endocrinology
|
|
NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
|
-
- HY-B0926
-
|
Diatrizoic acid
Diatrizoate; Amidotrizoic acid
|
Apoptosis
|
Inflammation/Immunology
|
|
Diatrizoic acid (Diatrizoate) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Diatrizoic acid induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium.
|
-
- HY-18936
-
-
- HY-D1056
-
|
Lipopolysaccharides
LPS
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Lipopolysaccharides (LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria. Lipopolysaccharides consists of an antigen O-specific chain, a core oligosaccharide and lipid A. Lipopolysaccharides is a pathogenic associated molecular pattern (PAMP) that activates the immune system. Lipopolysaccharides activates TLR-4 on immune cells. This product is derived from Escherichia coli O55:B5. Lipopolysaccharides induces secretion of cell migrasome.
|
-
- HY-148258
-
-
- HY-111662
-
