Search Result
Results for "
Activators and Inhibitors
" in MedChemExpress (MCE) Product Catalog:
2941
Inhibitors & Agonists
25
Biochemical Assay Reagents
192
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N0277
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- HY-107753
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Ras
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Inflammation/Immunology
Cancer
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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 .
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- HY-130480
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AIM2
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Inflammation/Immunology
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Fructose-arginine, an amino-sugar, is an AIM2 inflammasome activation inhibitor. Fructose-arginine attenuates the secretion of IL-1β, IL-18, and caspase-1, and Asc pyroptosome formation and Gsdmd cleavage resulting from AIM2 inflammasome activation .
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- HY-142163
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Thrombin
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Cardiovascular Disease
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S62798 is a selective and potent inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) with an IC50 value of 6 mM.
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- HY-176427
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ClpP
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Cancer
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HsClpP activator-1 (compound 24) is a potent HsClpP activator with an EC50 of 0.22 μM. HsClpP activator-1 effectively inhibits cancer cell growth with IC50 values of 0.1-1 μM .
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- HY-156081
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Keap1-Nrf2
Apoptosis
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Metabolic Disease
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Nrf2 activator-9 (compound D-36) is an Nrf2 activator that inhibits oxidized low-density lipoprotein (oxLDL) and high glucose (HG)-induced apoptosis in HUVEC cells. Nrf2 activator-9 inhibits oxLDL and HG-induced vascular endothelial cell (VEC) injury and can effectively prevent and treat atherosclerosis .
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- HY-148480
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- HY-N10782
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- HY-172596
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JAK
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Inflammation/Immunology
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TYK2 activator-1 (16b) is a TYK2 activator with anEC50 of 1.78 μM. TYK2 activator-1 inhibits JAK2 and JAK3 with the IC50 values of 6.8 and 6.3 μM, respectively .
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- HY-156375
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Pyruvate Kinase
PDK-1
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Cancer
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PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM) .
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- HY-14754
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S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
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Ras
Autophagy
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Cancer
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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.
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- HY-170918
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Potassium Channel
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Others
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BKCa activator-1 (Compound 51b) is the orally active activator for the calcium-activated potassium channel BKCa with an EC50 of 2.82 μM. BKCa activator-1 increases K+ efflux, leads to cell membrane hyperpolarization, thereby inhibiting smooth muscle contraction. BKCa activator-1 alleviates urinary incontinence in spontaneously hypertensive rat (SHR) model, exhibits antitussive effect in puinea pig cough model .
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- HY-173399
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STING
Interleukin Related
IFNAR
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Inflammation/Immunology
Cancer
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hSTING activator-1 (Compound 68) is a STING agonist. hSTING activator-1 can effectively activate multiple human STING variants (R232, H232, HAQ) with EC50 values of 56 nM, 89 nM and 51 nM, respectively. hSTING activator-1 activates the type I interferon pathway by directly binding to STING protein and stabilizing its conformation, promoting downstream IRF3 phosphorylation and cytokine release. hSTING activator-1 inhibits fibrosarcoma tumor growth and has potential in cancer research .
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- HY-113817
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Phosphatase
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Inflammation/Immunology
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SHIP1 activator 1 is an SH3 domain-containing inositol 5-phosphatase regulator with SHIP1 activating activity. SHIP1 activator 1 retains its SHIA-1 activating ability by removing unnecessary functional groups. SHIP1 activator 1 is able to activate SHIP1 in vitro, inhibit Akt phosphorylation in MOLT-4 cells, and show dose-dependent activity in a mouse model of inflammation. SHIP1 activator 1 is an important chemical tool for evaluating the potential of SHIP1 activators as inhibitors of hematopoietic diseases involving abnormal PI3K cell signaling .
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- HY-114304
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COH000
1 Publications Verification
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E1/E2/E3 Enzyme
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Cancer
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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 .
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- HY-155363
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AMPK
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Metabolic Disease
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AMPK activator 13 is a potent activator of AMPK. AMPK activator 13 inhibits mitotic clonal expansion of 3T3-L1 cells by activating AMPK pathway and enhances cell mitochondrial oxygen consumption rate. AMPK activator 13 can be used in study obesity .
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- HY-154973
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Oxidative Phosphorylation
Mitochondrial Metabolism
AMPK
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Metabolic Disease
Cancer
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AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research .
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- HY-124445
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NF-κB
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Inflammation/Immunology
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APC0576 is an inhibitor for the activation of NF-κB signaling pathway, and inhibits the activation of NF-κB depedent gene (IC50 is 1.0 μM for β-gal). APC0576 inhibits IL-1-induced chemokines release, and can be used in research about pathological endothelial cell activation releted diseases .
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- HY-145879
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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-19635A
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PAK
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Cancer
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G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
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- HY-135825
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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-N4231
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NF-κB
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Inflammation/Immunology
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Lucyoside B inhibits the production of inflammatory mediators via both NF-κB and activator protein-1 pathways in activated macrophages .
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- HY-15723A
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- HY-161929
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Glutathione Peroxidase
Ferroptosis
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Cardiovascular Disease
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GPX4 activator 2 (Compound C3) is an activator of GPX4. GPX4 activator 2 exhibits cardioprotective effects and can inhibit cellular ferroptosis (EC50=7.8 μM). GPX4 activator 2 can be used in the research of myocardial injury .
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- HY-170591
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MDM-2/p53
Apoptosis
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Cancer
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p53 Activator 14 (Compound 7A) is a derivative of Neratinib (HY-32721), that induces DNA damage, activates p53, and inhibits the proliferation of multi cancer cells (IC50=7.21 μM for HCT116 cell). p53 Activator 14 inhibits the adhesion, migration and invasion of HCT116, arrests the cell cycle, and induces apoptosis. p53 Activator 14 inhibits angiogenesis and exhibits antitumor efficacy in chick chorioallantoic membrane (CAM) model .
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- HY-176426
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Deubiquitinase
NF-κB
IFNAR
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Cancer
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Subquinocin is a CYLD inhibitor that inhibits USP family deubiquitinases (DUBs). Subquinocin enhances the activation of NF-κB and IFN pathways by inhibiting CYLD. Subquinocin promotes RIG-I-mediated activation of IRF3 and/or IRF7 in the interferon pathway .
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- HY-101796
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Ras
SOS1
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Cancer
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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 .
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- HY-121896
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SHP2
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Cancer
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DSHN is a potent small heterodimer partner (SHP) activator. DSHN inhibits Ccl2 expression and secretion by inhibiting p65 activation of Ccl2 promoter activity. DSHN can be used in research of cancer .
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- HY-118792
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Endogenous Metabolite
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Cancer
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AHR activator 1 is an aryl hydrocarbon receptor activator with activity regulating fibroblast growth factor-2 (FGF2)-induced branching morphogenesis. AHR activator 1 prevents the formation of cellular branches by inhibiting AHR signaling. AHR activator 1 also associates with adhesion of dissociated linkers, suggesting the importance of dissociated linkers in the inhibition of branching by AHR agonists. Studies of AHR activator 1 reveal its functional role in mammary gland morphogenesis and play a role in inhibiting FGF-induced invasion .
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- HY-131521
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Oxalomalate trisodium
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Isocitrate Dehydrogenase (IDH)
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Cancer
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Oxalomalic acid (Oxalomalate) trisodium is a aconitase and NADP-dependent isocitrate dehydrogenase inhibitor. Oxalomalic acid trisodium inhibits nitrite production and iNOS protein expression in lipopolysaccharide (HY-D1056)-activated J774 macrophages .
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- HY-100472
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Caspase
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Cancer
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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 .
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- HY-173307
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Keap1-Nrf2
Apoptosis
Reactive Oxygen Species (ROS)
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Cardiovascular Disease
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Nrf2 activator 19 is a BBB-penetrable NRF2/HO-1 activator. Nrf2 activator 19 exerts potent antioxidant and neuroprotective effects. Nrf2 activator 19 can also effectively reduce brain damage, reduce Reactive Oxygen Species (ROS) accumulation. Nrf2 activator 19 inhibits neuronal apoptosis. Nrf2 activator 19 promotes the recovery of neurological function and motor ability. Nrf2 activator 19 shows significant potential in ischemic stroke research .
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- HY-P1376
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mAChR
Adrenergic Receptor
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Endocrinology
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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.
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- HY-N10458
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NF-κB
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Inflammation/Immunology
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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 .
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- HY-172901
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AMPK
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Cardiovascular Disease
Metabolic Disease
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AMPK activator 17 (Compound 10g) is an orally active AMPK activator. AMPK activator 17 has significant anti-adipogenic (IC50: 3.4 μM) and dyslipidemia-modifying activities. AMPK activator 17 inhibits the early stages of adipocyte differentiation (mitotic clonal expansion) by activating the AMPK pathway. AMPK activator 17 can enhance mitochondrial function and fatty acid oxidation in mature adipocytes. AMPK activator 17 improves dyslipidemia by promoting reverse cholesterol transport. AMPK activator 17 can be used in the study of obesity and related metabolic diseases (such as type 2 diabetes and cardiovascular disease) .
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- HY-168636
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DNA Methyltransferase
MDM-2/p53
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Cancer
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p53 Activator 13 (compound 11) is a 6mA methyltransferase CamA inhibitor and a p53 activator. p53 Activator 13 intercalates into CamA-bound DNA via the minor groove, causing a conformational shift that moves the catalytic domain away from the DNA and elicits DNA damage response via p53 activation. p53 Activator 13 can be utilized in cancer research .
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- HY-15542A
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PAK
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Cancer
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FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
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- HY-P1918
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Ser/Thr Protease
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Cardiovascular Disease
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Activated Protein C (390-404), human is a peptide of the activated protein C (a vitamin K-dependent serine protease), potently inhibits APC anticoagulant activity .
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- HY-15870
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AP-1
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Inflammation/Immunology
Cancer
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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) .
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- HY-W006230
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Cytochrome P450
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Cancer
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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 .
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- HY-14452
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125B11
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Fatty Acid Synthase (FASN)
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Cancer
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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 .
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- HY-169315
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Keap1-Nrf2
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Cancer
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Nrf2 activator 17 (compound 10) is an Nrf2 activator that inhibits the interaction between Keap1 and Nrf2 with an IC50 of < 0.1 pM. Additionally, Nrf2 activator 17 has an EC50 of < 10 μM in HepG2 cells .
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- HY-168640
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Autophagy
Necroptosis
RIP kinase
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Cancer
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RIP3 activator 1 (compound C8) is a potent RIP3 activator. RIP3 activator 1 inhibits cell growth. RIP3 activator 1 induces necroptosis through the RIP3/p62/Keap1 signaling pathway. RIP3 activator 1 increases the protein expression of p-MLKL. RIP3 activator 1 induces autophagy. RIP3 activator 1 increases accumulation of LC3-II and p62 protein expression .
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- HY-170931
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AMPK
Acetyl-CoA Carboxylase
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Neurological Disease
Metabolic Disease
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AMPK activator 16 (compound 6) is a AMP-activated protein kinase (AMPK) inhibitor. AMPK activator 16 shows the most efficient interactions with the key residues of AMPK and demonstrates significant activation of AMPK. AMPK activator 16 increases the expression of phosphorylated AMPK (p-AMPK) and its downstream signaling proteins, such as phosphorylated ACC (Acetyl-CoA Carboxylase) (p-ACC) and phosphorylated raptor (p-raptor), in N2a cells .
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- HY-N6688
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Potassium Channel
Bacterial
Antibiotic
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Infection
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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 .
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- HY-15027
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- HY-P1918A
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APC
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Cardiovascular Disease
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Activated Protein C (390-404), human TFA, a peptide of the activated protein C (a vitamin K-dependent serine protease), potently inhibits APC anticoagulant activity .
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- HY-110105
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Potassium Channel
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Neurological Disease
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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) .
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- HY-101918
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Thrombin
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Cardiovascular Disease
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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 .
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- HY-14754R
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S-Farnesylthiosalicylic acid (Standard); Farnesyl Thiosalicylic Acid (Standard); FTS (Standard)
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Reference Standards
Ras
Autophagy
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Cancer
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Salirasib (Standard) is the analytical standard of Salirasib. This product is intended for research and analytical applications. 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.
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- HY-124060
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PDK-1
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Cancer
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PS423 is a prodrug of PS210, acting as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K. PS210 is a potent and selective PDK1 activator targeting the PIF binding pocket of PDK1 .
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- HY-N9297
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(+)-Oxyphyllenone A
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NO Synthase
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Inflammation/Immunology
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Oxyphyllenone A is an inhibitor of NO Synthase. Oxyphyllenone A inhibits the NO production in lipopolysaccharide-activated macrophages with an IC50 of 28 μM .
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- HY-N1330
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- HY-15542B
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PAK
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Cancer
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FRAX486 is a p21-activated kinase (PAK) inhibitor with IC50s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.
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- HY-19635
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PAK
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Cancer
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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.
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- HY-N10445
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CD28
CD3
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Inflammation/Immunology
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Maydispenoid A is a potent immunosuppressor. Maydispenoid A can inhibit anti-CD3/anti-CD28 mAbs activated and lipopolysaccharide activated murine splenocyte proliferation .
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- HY-106062
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- HY-168929
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SHP1
Fluorescent Dye
Phosphatase
STAT
Apoptosis
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Cancer
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SHP1 activator 1 (Compound 3n) is an activator for src homology-2 domain-containing protein tyrosine phosphatase 1(SHP1) with an EC50 of 17.66 μM. SHP1 activator 1 inhibits the proliferation of ABC-DLBCL cells, induces apoptosis by inhibiting STAT3 signaling pathway. SHP1 activator 1 emitts blue and green fluorescence signalis in MDA-MB-231 cell, and can be used as a cell imaging agent .
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- HY-N3464
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Phosphodiesterase (PDE)
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Metabolic Disease
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Isopedicin potently and concentration-dependently inhibits superoxide anion (O2 U?) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. Isopedicin increases cAMP formation and PKA activity in FMLP-activated cells by inhibiting phosphodiesterase (PDE) activity .
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- HY-N0896
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1-O-Acetylbritannilactone
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NF-κB
COX
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Inflammation/Immunology
Cancer
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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.
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- HY-18723
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Piezo Channel
Akt
ERK
Potassium Channel
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Cardiovascular Disease
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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 .
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- HY-163445
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NAMPT
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Cancer
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NAMPT activator-6 is a NAMPT activator, a regulatory molecule for the optical control system of NAMPT and NAD+. NAMPT activator-6 can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) to achieve up-down reversible regulation of NAMPT and NAD+ in a light-dependent manner and reduce the toxicity associated with inhibitor-based PS-PROTACs. PS-PROTAC can be used to achieve antitumor activity, NAMPT, and NAD+ modulation in vivo via optical manipulation .
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- HY-N5101
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- HY-13764
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- HY-172944
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Free Fatty Acid Receptor
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Metabolic Disease
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GPR40 Activator 3 (compound SC) is a potent GPR40 activator. GPR40 Activator 3 mitigates pulmonary fibrosis by inhibiting M2 macrophage polarization via the GPR40/PKD1/CD36 axis .
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- HY-161519
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Pyruvate Kinase
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Inflammation/Immunology
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PKM2 activator 7 (Compd B4) is a PKM2 activator with the AC50 of 0.144 μM. PKM2 activator 7 suppresses DSS (HY-116282C)-induced colitis by inhibiting T cell growth in mouse colitis model .
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- HY-N15264
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(-)-Azaspirene
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VEGFR
Raf
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Cancer
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Azaspirene ((-)-Azaspirene) is an angiogenesis and Raf-1 activation inhibitor isolated from the fungus Neosartorya sp. Azaspirene inhibits vascular endothelial growth factor (VEGF)-induced human umbilical vein endothelial cell (HUVEC) migration and Raf-1 activation, but has no effect on the activation of kinase insert domain-containing receptor/fetal liver kinase 1 (VEGF receptor 2) .
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- HY-108356
-
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Apoptosis
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Cancer
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NS3694, a diarylurea compound, is an apoptosome inhibitor. NS3694 inhibits apoptosome formation and caspase activation .
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- HY-143510
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mTOR
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Cancer
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RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.
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- HY-18965
-
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PKC
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Cardiovascular Disease
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TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.
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- HY-120563
-
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Thrombin
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Cardiovascular Disease
|
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LY 135305 is a thrombin activation inhibitor. LY 135305 inhibits spontaneous metastasis and increases animal survival .
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- HY-133987
-
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NF-κB
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Inflammation/Immunology
|
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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-100602
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HJC0152
2 Publications Verification
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STAT
Apoptosis
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Cancer
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HJC0152 is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
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- HY-U00434
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-
- HY-N3054
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- HY-159846
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MEK
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Cancer
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Luvometinib is a mitogen-activated protein kinase (MEK) inhibitor with antitumor activity .
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- HY-N0441
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-
- HY-101214
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-
- HY-18749
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- HY-N10446
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CD28
CD3
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Inflammation/Immunology
|
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Maydispenoid B is a potent immunosuppressor. Maydispenoid B can inhibit anti-CD3/anti-CD28 mAbs activated and lipopolysaccharide activated murine splenocyte proliferation .
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- HY-14452A
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125B11 hydrobromide
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Fatty Acid Synthase (FASN)
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Cancer
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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 .
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- HY-122082
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Apoptosis
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Inflammation/Immunology
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Methopterin inhibits osteoclasts proliferation. Methopterin inhibits the activation and bone resorption function of osteoclasts, and induced osteoclasts apoptosis .
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- HY-153675
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|
|
PIN1
|
Metabolic Disease
|
|
BCPA is a Pin1 regulator without cytotoxicity. BCPA attenuates the reduction of Pin1 protein to inhibit receptor activator of RANKL-induced osteoclastogenesis. BCPA regulates osteoclast activation, used to osteoporosis research .
|
-
- HY-163465
-
|
|
Fluorescent Dye
|
Neurological Disease
|
|
DTNP is a BchE -activated near infrared (NIR) probe with blood-brain permeability. DTNP can be activated by BchE and inhibit its enzyme activity. DTNP can be used in Alzheimer's disease (AD) research .
|
-
- HY-118131
-
|
|
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
-
|
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-P1026
-
-
- HY-149725
-
|
|
MMP
|
Neurological Disease
|
proMMP-9 selective inhibitor-1 (compound 33) is a highly potent and selective inhibitor of proMMP-9 activation .
|
-
- HY-15253
-
|
PAI-039; Tiplasinin
|
PAI-1
Apoptosis
|
Metabolic Disease
Cancer
|
|
Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM .
|
-
- HY-P10048
-
-
- HY-P2606
-
-
- HY-W700638A
-
-
- HY-15300
-
-
- HY-168009
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-45 (D6) is an inhibitor of NLRP3 inflammasome activation, inhibiting the activity of IL-1β (IC50=41.79 nM). NLRP3-IN-45 exerts its effects without affecting the initial stage of NLRP3 inflammasome activation. NLRP3-IN-45 specifically inhibits the activation of NLRP3 inflammasome in the LPS-induced acute lung injury (ALI) mouse model .
|
-
- HY-N9239
-
|
|
Others
|
Others
|
|
Turmeronol A is a sesquiterpenoid compound.
Turmeronol A has anti-inflammatory activity. Turmeronol A prevents macrophage
activation and the production of inflammatory mediators by inhibiting the
activation of NFκB. Turmeronol A can be used to prevent chronic inflammatory
diseases .
|
-
- HY-B1197
-
-
- HY-148712
-
|
|
Apoptosis
Sirtuin
|
Cancer
|
|
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 .
|
-
- HY-128403
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits B cell activation in hWB with an IC50 of 2 nM .
|
-
- HY-108599
-
DCP-LA
5 Publications Verification
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-12762
-
QS11
1 Publications Verification
|
β-catenin
Wnt
Arf Family GTPase
|
Cancer
|
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 μM. QS11 activates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells .
|
-
- HY-136427
-
|
|
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
|
KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity .
|
-
- HY-136172
-
ESI-08
1 Publications Verification
|
Ras
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
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-P0190A
-
|
|
Potassium Channel
|
Others
|
|
Iberiotoxin (TFA) is a selective high conductance high conductance Ca 2+-activated K + channel inhibitor with a Kd of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels .
|
-
- HY-163290
-
|
|
Fluorescent Dye
Monoamine Oxidase
|
Cancer
|
|
HDAC-MB a probe that is activated by HDAC6 and can detect and eliminate glioma cells through activation by HDAC6. HDAC-MB reveals antimetastatic and antiproliferative properties, inhibits glioma invasion and induces cellular apoptosis .
|
-
- HY-123929
-
|
|
MDM-2/p53
Wnt
IKK
Apoptosis
Caspase
|
Cancer
|
|
PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model .
|
-
- HY-P1260
-
-
- HY-100447
-
-
- HY-139858
-
-
- HY-165117
-
|
|
Others
|
Others
|
|
Bactobolamine is an immunosuppressive compound that has synergistic activity with cyclosporine in inhibiting allogeneic lymphocyte activation in vitro.
|
-
- HY-158196
-
|
|
PERK
Apoptosis
|
Cancer
|
|
PERK/eIF2α activator 1 (compound V8) is a flavonoid with an anti-tumor activity. PERK/eIF2α activator 1 induces apoptosis and activates the PERK-eIF2α-ATF4 pathway. PERK/eIF2α activator 1 inhibits HepG2 cell proliferation with an IC50 value of 23 μM .
|
-
- HY-P99371
-
|
AK002; Antolimab
|
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-170532
-
-
- HY-N10227
-
-
- HY-117019
-
|
|
COX
|
Cancer
|
|
LY150310 inhibits thromboxane synthase, cyclooxygenase, and thrombin activation. LY150310 inhibits spontaneous lung metastasis in a dose-dependent manner.
|
-
- HY-170533
-
-
- HY-15870A
-
|
|
AP-1
|
Inflammation/Immunology
Cancer
|
|
(6E)-SR 11302 is a E-isomer of SR 11302. 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-15002
-
AST 487
5 Publications Verification
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-122098
-
|
PAI-749
|
PAI-1
|
Cardiovascular Disease
|
|
Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nM. Diaplasinin has antithrombotic efficacy .
|
-
- HY-126741
-
|
|
Apoptosis
Parasite
NF-κB
Bcl-2 Family
Caspase
|
Infection
Inflammation/Immunology
Cancer
|
|
Azadirachtin is an oral active triterpenoid compound with anticancer, antimalarial, anti-inflammatory, and insecticidal activities. Azadirachtin induces cell apoptosis through the mitochondrial pathway (by inhibiting Bcl-2/Bax ratio or activating Apaf-1 and caspase-3) or through death receptors (by inhibiting TNFR activation). Additionally, Azadirachtin exerts its anti-inflammatory effects by inhibiting NF-кB signaling pathway activation, and it exhibits insecticidal activity by inducing apoptosis in insect cells .
|
-
- HY-N0671
-
|
Rhaponiticin
|
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Rhapontin (Rhaponiticin) is an orally aactive SIRT1 agonist and AMPK activator with anti-inflammatory and anti-fibrotic activities. Rhapontin inhibits NLRP3 inflammasome activation by activating SIRT1 and inhibits TGF-β/Smad signaling via the AMPK pathway. Rhapontin reduces intestinal and lung inflammation, inhibits fibroblast differentiation and extracellular matrix deposition, and enhances tight junction protein expression to repair epithelial barriers. Rhapontin can be used in the study of inflammatory bowel diseases (such as ulcerative colitis) and pulmonary fibrosis .
|
-
- HY-148853
-
|
|
HuR
|
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-A0135
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Enflurane, a volatile anaesthetic, is a potent inhibitor of high conductance Ca 2+-activated K+ channels of Chara australis. Enflurane is an internal standard in monitoring halogenated volatile anaesthetics by headspace gas chromatography-mass spectrometry .
|
-
- HY-N6258
-
|
|
AMPK
Apoptosis
|
Metabolic Disease
Cancer
|
|
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-148189
-
|
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-103697
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
Gardiquimod is an imidazoline TLR7/8 agonist. Gardiquimod inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM.
|
-
- HY-168924
-
|
|
Wnt
β-catenin
|
Metabolic Disease
|
|
Wnt/β-catenin activator 1 (Compound 5m) is the orally active activator for Wnt/β-catenin signaling pathway, that arrests cell cycle at G1 phase, inhibits early proliferation of adipocytes, and inhibits adipogenesis in cell 3T3-L1 with an IC50 of 330 nM. Wnt/β-catenin activator 1 exhibits anti-adipogenic and anti-dyslipidemic activities in high-fat diet fed Syrian golden hamster model .
|
-
- HY-136945
-
|
|
IFNAR
|
Cancer
|
|
StA-IFN-1 is an inhibitor for type I interferon (IFN), that inhibits the activation of IFNβ with an IC50 of 4.1 μM .
|
-
- HY-119582
-
|
|
MMP
|
Inflammation/Immunology
|
|
Safironil is an antifibrotic compound. Safironil is a competitive inhibitor of collagen protein synthesis. Safironil reduces liver fibrogenesis by inhibiting HSC activation .
|
-
- HY-127041
-
|
|
Bacterial
|
Infection
|
|
Virstatin inhibits the pili system synthesis and prevents A. baumannii biofilm formation. Virstatin also inhibits dimerization of the transcriptional activator ToxT .
|
-
- HY-115627
-
|
GPX4-Activator-1d4
|
Glutathione Peroxidase
|
Inflammation/Immunology
|
|
PKUMDL-LC-101-D04 (GPX4-Activator-1d4) is a glutathione peroxidase 4 (GPX4) allosteric activator (pEC50=4.7). PKUMDL-LC-101-D04 can inhibit ferroptosis and inflammation .
|
-
- HY-121667
-
|
|
ROCK
|
Cancer
|
|
Scaff10-8, bound to RhoA, inhibits the AKAP-Lbc-mediated RhoA activation .
|
-
- HY-N1260
-
|
(-)-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-P10877
-
|
|
PAI-1
|
Cancer
|
|
Bicyclic UK18 is a competitive inhibitor for human urokinase-type plasminogen activator (uPA) with a Ki of 53 nM .
|
-
- HY-P1260A
-
-
- HY-105198
-
-
- HY-101214A
-
|
|
PAI-1
|
Others
|
|
UK-371804 hydrochloride (compound 24) is a urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 10 nM .
|
-
- HY-N3425
-
|
|
AMPK
|
Others
|
|
Kazinol U inhibits melanogenesis through the inhibition of tyrosinase-related proteins via AMPK activation .
|
-
- HY-15840
-
|
C24
|
AMPK
|
Cancer
|
|
YLF-466D is a newly developed AMPK activator, which inhibits platelet aggregation.
|
-
- HY-139553
-
|
ATI-450; CDD-450
|
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 .
|
-
- HY-157887
-
|
|
Ras
|
Cancer
|
|
ADT-007 is a potent and orally active pan-RAS inhibitor with strong anticancer effects. ADT-007 binds RAS in a nucleotide-free conformation to block GTP activation. ADT-007 potently and selectively inhibits the growth of cancer cells with mutated or hyper-activated wild-type RAS isozymes .
|
-
- HY-105118A
-
|
CGS-9343B; KW 5617
|
Calmodulin
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM . Zaldaride maleate prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR .
|
-
- HY-110247
-
|
|
TNF Receptor
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
TRAF-STOP inhibitor 6877002 is a selective CD40-TRAF6 interaction inhibitor. TRAF-STOP inhibitor 6877002 exerts anti-atherosclerotic activity by blocking the CD40-TRAF6 signaling pathway, inhibiting classical monocyte activation, leukocyte recruitment, and macrophage activation and migration. TRAF-STOP inhibitor 6877002 reduces the phosphorylation levels of signaling intermediates in the canonical NF-κB pathway .
|
-
- HY-103697B
-
|
|
HIV
Toll-like Receptor (TLR)
|
Infection
Cancer
|
|
Gardiquimod (hydrochloride) is an imidazoline TLR7/8 agonist. Gardiquimod (hydrochloride) inhibits HIV-1 infection of macrophages and activates peripheral blood mononuclear cells (PBMCs). Gardiquimod (hydrochloride) specifically activates TLR7 at concentrations below 10 μM .
|
-
- HY-P4243
-
|
|
Ser/Thr Protease
|
Others
|
|
Dansyl-Glu-Gly-Arg-Chloromethylketone is a protease inhibitor, and inhibits serine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone inhibits activated porcine factor IX .
|
-
- HY-169316
-
|
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-4 (Compound 45) is an inhibitor of YAP/TAZ, exhibiting TEAD transcriptional activation inhibitory activity by suppressing the binding of YAP or TAZ to TEAD .
|
-
- HY-122714
-
|
|
PAI-1
|
Cancer
|
|
SK-216 is a plasminogen activator inhibitor-1 (PAI-1) inhibitor that acts as an anti-metastatic agent for human osteosarcoma and inhibits lung metastasis of human osteosarcoma .
|
-
- HY-101047R
-
|
Erythrosphingosine (Standard); erythro-C18-Sphingosine (Standard); trans-4-Sphingenine (Standard)
|
Reference Standards
PKC
Phosphatase
Endogenous Metabolite
|
Cancer
|
|
D-erythro-Sphingosine (Standard) is the analytical standard of D-erythro-Sphingosine. This product is intended for research and analytical applications. 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-116278
-
|
|
STAT
|
Cancer
|
|
HJC0149 is a potent and orally active inhibitor of signal transducer and activator of transcription 3 (STAT3) .
|
-
- HY-101790
-
-
- HY-U00458
-
K-80003
1 Publications Verification
TX-803
|
Akt
|
Cancer
|
|
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
|
-
- HY-N1147
-
|
Tagitinin D
|
Others
|
Inflammation/Immunology
|
|
Tirotundin (Tagitinin D) is a potent anti-inflammatory agent. Tirotundin inhibits the activation of NF-Kβ .
|
-
- HY-118779
-
-
- HY-17032A
-
|
(rac)-AS1069562 hydrochloride; YM-08054
|
5-HT Receptor
|
Neurological Disease
|
|
Indeloxazine hydrochloride is a 5-HT receptor and norepinephrine (NE) reuptake inhibitor. Indeloxazine hydrochloride is an antidepressant and cerebral activator .
|
-
- HY-15252
-
-
- HY-168709
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Nrf2 activator 18 (Compound 11a) is an orally active activator for Keap1/Nrf2/HO-1 signaling pathway, that promotes the Nrf2 nuclear translocation, and enhances the antioxidant efficacy. Nrf2 activator 18 inhibits the release of IL-6 with an IC50 of 4.816 μM. Nrf2 activator 18 exhibits anti-inflammatory efficacy in mouse PM2.5-induced lung injury model .
|
-
- HY-105118
-
|
CGS-9343B free base; KW 5617 free base
|
Calmodulin
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Zaldaride (CGS-9343B free base) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM . Zaldaride prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR .
|
-
- HY-161242
-
|
|
Bcl-2 Family
|
Cancer
|
|
CBI1 is a covalent BAX inhibitor. CBI1 selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 blocks t-2-hex lipidation and oligomerization of BAX. CBI1 inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .
|
-
- HY-117971
-
|
|
CXCR
Formyl Peptide Receptor (FPR)
|
Others
|
|
BVT173187 is a selective inhibitor of the neutrophil formyl peptide receptor FPR1, with activity that inhibits FPR1 activation. BVT173187 inhibits FPR1 agonist-induced activation in neutrophils, reduces adhesion molecule mobilization and superoxide anion production, and has inhibitory activity on FPR1 similar to that of earlier described peptide antagonists, but also has effects on C5aR and CXCR signaling.
|
-
- HY-103697A
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
Gardiquimod diTFA is an imidazoline TLR7/8 agonist. Gardiquimod diTFA inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 at concentrations below 10 μM.
|
-
- HY-N8041
-
|
|
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-169513
-
|
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
Cancer
|
|
MK2-IN-7 (Compound 144) is a mitogen activated protein kinase-activated protein kinase-2 (MK2) inhibitor. MK2-IN-7 is promising for research of inflammatory diseases, autoimmune diseases and cancer .
|
-
- HY-P10577
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
RAG8 peptide is an antagonist for protease-activated receptor 4 (PAR 4), which inhibits late-stage platelet activation, and reduces thrombosis without altering hemostasis or increasing bleeding risk. RAG8 peptide can be used for atherosclerosis research .
|
-
- HY-101047
-
|
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-N0625A
-
|
|
PPAR
Keap1-Nrf2
Toll-like Receptor (TLR)
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Alpinetin is a flavonoid isolated from cardamom and possesses antitumor, antiinflammation, hepatoprotective, cardiovascular protective, lung protective, antibacterial, antiviral, neuroprotective properties. Alpinetin inhibits lipopolysaccharide (LPS)-induced inflammation, activates PPAR-γ, activates Nrf2, and inhibits TLR4 expression to protect LPS-induced renal injury .
|
-
- HY-137888A
-
|
oATP trisodium salt
|
P2X Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
Oxidized ATP (oATP) trisodium salt is a broad-spectrum P2 receptor inhibitor. Oxidized ATP trisodium salt irreversibly antagonizes P2X7R activation. Oxidized ATP trisodium salt inhibits c-reactive protein (CRP)-induced NLRP3 inflammasome activation. Oxidized ATP trisodium salt can be used for research of atherosclerosis .
|
-
- HY-129390
-
|
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-N0518
-
|
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM .
|
-
- HY-131958
-
|
|
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-155182
-
|
|
HDAC
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
HDAC-IN-62 (Compound 5) a HDAC inhibitor, with IC50s of 0.78, 1.0, 1.2? μM for HDAC6/8/11 respectively. HDAC-IN-62 inhibits-induced microglial activation by the initiation of autophagy, and inhibits nitric oxide production. HDAC-IN-62 has anti-inflammatory and anti-depressant effects. HDAC-IN-62 inhibits microglial activation in mouse brain .
|
-
- HY-15035
-
|
ACS 15; ATB-337
|
MDM-2/p53
JNK
SOD
|
Cardiovascular Disease
Inflammation/Immunology
|
|
S-Diclofenac (ACS 15) is a hybrid molecule of an H2S donor and the NSAID diclofenac. S-Diclofenac activates the p53 signaling pathway, and inhibits the activation of JNK. S-Diclofenac exhibits antioxidant and anti-inflammatory activities .
|
-
- HY-131265
-
|
|
PPAR
PAK
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB .
|
-
- HY-15530
-
-
- HY-N0897
-
|
Corylifol-A; Corylinin
|
UGT
STAT
|
Others
|
|
Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
|
-
- HY-10590
-
-
- HY-162970
-
|
|
Wnt
|
Cancer
|
|
XD23 is a potent osteosarcoma inhibitor that works by downregulating DKK1 and activating the WNT/β-catenin signaling pathway.
|
-
- HY-130789
-
|
|
EBV
|
Infection
|
|
Cimigenol-3-one inhibits Epstein-Barr virus early antigen (EBV-EA) activation .
|
-
- HY-143477
-
-
- HY-N12486
-
-
- HY-128586
-
-
- HY-123399
-
-
- HY-158706
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
SAE-IN-2 (compound 6) is a potent inhibitor of sumo activating enzume (SAE), with the IC50 of 27.8 nM .
|
-
- HY-10249
-
|
|
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-N7563
-
|
|
EBV
|
Infection
Cancer
|
|
α-Toxicarol is a potent inhibitor of EBV.α-Toxicarol significantly inhibits mouse skin tumor in vivo. α-Toxicarol inhibits the TPA-induced EBV-EA activation .
|
-
- HY-P4243A
-
|
|
Ser/Thr Protease
|
Others
|
|
Dansyl-Glu-Gly-Arg-Chloromethylketone TFA is a protease inhibitor, and inhibits serine/threonine proteases. Dansyl-Glu-Gly-Arg-Chloromethylketone TFA inhibits activated porcine factor IX .
|
-
- HY-B0069R
-
|
F-ara-A (Standard); NSC 118218 (Standard)
|
Reference Standards
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
STAT
Apoptosis
|
Cancer
|
|
Fludarabine (Standard) is the analytical standard of Fludarabine. This product is intended for research and analytical applications. 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-77251
-
|
|
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-15027R
-
|
Mesalamine (Standard); 5-ASA (Standard); Mesalazine (Standard)
|
Reference Standards
PPAR
PAK
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
5-Aminosalicylic Acid (Standard) is the analytical standard of 5-Aminosalicylic Acid. This product is intended for research and analytical applications. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
|
-
- HY-136358
-
|
|
Ephrin Receptor
|
Cancer
|
|
LDN-211904 is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 shows good metabolic stability in mouse liver microsomes. LDN-211904 with cetuximab could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab (HY-P9905) resistance in CRC .
|
-
- HY-16511
-
|
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-50714
-
|
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-100965
-
-
- HY-P0190
-
|
|
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-15027S
-
-
- HY-170867
-
|
|
Keap1-Nrf2
Heme Oxygenase (HO)
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
|
|
Nrf2/HO-1 activator 3 (Compound C3a) is the activator for Nrf2 signaling pathway that promotes the Nrf2 translocation into nuclei and upregulates the expression of heme oxygenase-1 HO-1. Nrf2/HO-1 activator 3 inhibits the overespression of ROS and MDA in H2O2- or glucose-stimulated H9c2 cardiomyocytes, inhibits the cell viability and colony formation, thereby exhibiting antioxidant efficacy .
|
-
- HY-N1462
-
|
|
Chloride Channel
Autophagy
mTOR
AMPK
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
|
-
- HY-161242A
-
|
|
Bcl-2 Family
|
Cancer
|
|
CBI1 formic is a covalent BAX inhibitor. CBI1 formic selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 formic blocks t-2-hex lipidation and oligomerization of BAX. CBI1 formic inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .
|
-
- HY-173316
-
|
|
STING
|
Inflammation/Immunology
|
|
STING-IN-12 (compound Y2) is an inhibitor of STING. STING-IN-12 inhibits IFNβ gene expression (IC50=0.75μM) induced by SR717. STING-IN-12 inhibits STING pathway activation induced by the STING agonist SR717 in THP1 cells and MSA-2-induced STING pathway activation in vivo in mice .
|
-
- HY-Z0816
-
|
|
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-108047
-
|
|
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
|
|
MK-0873 is a selective phosphodiesterase-4 (PDE4) inhibitor. MK-0873 increases intracellular levels of cyclic adenosine phosphate (cAMP) by inhibiting the activity of the PDE4 enzyme and subsequently activates protein kinase A (PKA). Activated PKA inhibits the activity of inflammatory cells and leads to direct relaxation of airway smooth muscle. MK-0873 can be used in studies of chronic obstructive pulmonary disease (COPD) .
|
-
- HY-19356
-
|
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-106508
-
|
HP 129; P 71-0129
|
PAI-1
|
Inflammation/Immunology
|
|
Fendosal (HP 129) is an orally active, potent non-steroidal anti-inflammatory agent. Fendosal (HP 129) is also an inhibitor of Plasminogen activator inhibitor-1 (PAI-1) .
|
-
- HY-P3012
-
|
|
Cathepsin
|
Inflammation/Immunology
|
|
Cathepsin G acts as a potent agonist of human platelet activation leading to their aggregation., and can be used for screening of relevant inhibitors .
|
-
- HY-N0516
-
|
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-N1533
-
-
- HY-145944
-
|
|
Apoptosis
|
Cancer
|
|
ASR-488 activates the mRNA-binding protein CPEB1, induces apoptosis and inhibits bladder cancer growth .
|
-
- HY-N2506
-
|
|
Others
|
Cardiovascular Disease
|
|
Ginsenoside Ra1 is a component from ginseng, inhibits protein tyrosine kinase (PTK) activation induced by hypoxia/reoxygenation .
|
-
- HY-14645A
-
|
(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-N1244
-
|
Sarmentosine; Sarmentosine (glycoside)
|
Keap1-Nrf2
mTOR
Apoptosis
|
Cancer
|
|
Sarmentosin is an activator of Nrf2. Sarmentosin inhibits mTOR signaling and induces autophagy-dependent apoptosis in human HCC cells .
|
-
- HY-153671
-
|
|
Fungal
|
Infection
|
|
4'-Methyl-β-naphthoflavone is a metabolite of Naphthoflavones (benzoflavones) in fungal. Naphthoflavones are activators or inhibitors of CYP-450 .
|
-
- HY-135077
-
|
|
Drug Intermediate
|
Others
|
|
Prostaglandin A1 ethyl ester is a prodrug form of Prostaglandin A1. Prostaglandin A1 inhibits the activation of platelets .
|
-
- HY-112125A
-
-
- HY-139401
-
FAPI-34
1 Publications Verification
|
FAP
|
Cancer
|
|
FAPI-34 is a fibroblast-activating protein (FAP) inhibitor with favorable pharmacokinetic and biochemical properties. (patent WO2019154886A1).
|
-
- HY-B0380A
-
|
|
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-B0380
-
|
|
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-N3552
-
|
|
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-13764R
-
-
- HY-101112
-
|
|
HuR
|
Inflammation/Immunology
|
|
Okicenone is a Hu protein R (HuR) inhibitor. Okicenone inhibits HuR oligomerization, interferes with HuR RNA binding, HuR trafficking, cytokine expression and T-cell activation .
|
-
- HY-N3254
-
|
Murpanidin; (+)-Murpanidin
|
HSV
EBV
|
Infection
|
|
Minumicrolin is a plant growth inhibitor. Minumicrolin can be isolated from Murraya paniculata. Minumicrolin inhibits Epstein-Barr virus early antigen (EBV-EA) activation .
|
-
- HY-B1546
-
|
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-142125
-
|
|
Xanthine Oxidase
Reactive Oxygen Species (ROS)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
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-P1929
-
|
|
Thrombin
Interleukin Related
RSV
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
Bivalirudin, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin can be used for the research of thrombotic diseases and others .
|
-
- HY-B1546A
-
|
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-B0111
-
|
Dihydrospirorenone
|
Progesterone Receptor
Androgen Receptor
|
Endocrinology
Cancer
|
|
Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .
|
-
- HY-N0671R
-
|
Rhaponiticin (Standard)
|
Reference Standards
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Rhapontin (Standard) is the analytical standard of Rhapontin (HY-N0671). This product is intended for research and analytical applications. Rhapontin (Rhaponiticin) is an orally aactive SIRT1 agonist and AMPK activator with anti-inflammatory and anti-fibrotic activities. Rhapontin inhibits NLRP3 inflammasome activation by activating SIRT1 and inhibits TGF-β/Smad signaling via the AMPK pathway. Rhapontin reduces intestinal and lung inflammation, inhibits fibroblast differentiation and extracellular matrix deposition, and enhances tight junction protein expression to repair epithelial barriers. Rhapontin can be used in the study of inflammatory bowel diseases (such as ulcerative colitis) and pulmonary fibrosis .
|
-
- HY-N6576
-
|
|
p38 MAPK
ERK
JNK
IAP
PARP
Apoptosis
Caspase
|
Cancer
|
|
Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers .
|
-
- HY-112469
-
|
|
ERK
Insulin Receptor
|
Metabolic Disease
|
|
ERK Inhibitor II (Negative control) is an effective inhibitor of extracellular signal-regulated kinase (ERK). ERK Inhibitor II (Negative control) inhibits the activation of insulin receptor, which can be used in the study of diabetes .
|
-
- HY-W206016
-
|
|
Drug Intermediate
|
Inflammation/Immunology
Cancer
|
|
3-Aminosalicylic acid is the impurity found during the 5-Aminosalicylic acid (HY-15027) production. 5-Aminosalicylic acid is the agonist for PPARγ and the inhibitor for p21-activated kinase 1 (PAK1) and NF-κB .
Crohn's disease, ulcerative proctitis
|
-
- HY-W019721
-
|
|
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-117993
-
|
|
Drug Intermediate
|
Neurological Disease
|
|
MIND4 is a neuroprotective thiozoline compound that inhibits the deacetylase SIRT2. MIND4 is also an inducer and activator of the nuclear factor NRF2. MIND4 can induce NRF2 activation in neurons and non-neuronal cells and reduce the production of reactive oxygen and nitrogen intermediates .
|
-
- HY-138284
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Avenanthramide-C methyl ester is an anti-inflammatory agent and NF-κB inhibitor that inhibits the secretion of pro-inflammatory factors. Avenanthramide-C methyl ester inhibits NF-κB activation by inhibiting IKK and IκB phosphorylation and inhibiting proteasome activity .
|
-
- HY-117102
-
|
|
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
-
|
|
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-108599R
-
|
FR236924 (Standard)
|
Reference Standards
PKC
CaMK
Phosphatase
Apoptosis
|
Neurological Disease
|
|
DCP-LA (Standard) is the analytical standard of DCP-LA. This product is intended for research and analytical applications. 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[1][2][3].
|
-
- HY-134816
-
|
|
Toll-like Receptor (TLR)
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
D-Glucan is an orally effective Dectin-1 receptor immune activator with antioxidant properties (reducing TNF-α). D-Glucan activates macrophages and neutrophils to scavenge free radicals, inhibit oxidative stress and inflammatory responses, and improve insulin sensitivity. D-Glucan promotes glycolysis by enhancing the activity of the antioxidant enzyme glutathione, inhibiting gluconeogenesis and activating GK. D-Glucan can be used in the research of liver damage protection (antagonizing Acetaminophen (HY-66005) toxicity), radiation protection (synergistic with vitamin E) and diabetes (improving glucose metabolism) .
|
-
- HY-14994
-
|
|
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-148553
-
|
|
Others
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 36 is an anti-inflammatory agent. Anti-inflammatory agent 36 inhibits LPS-induced macrophage activation .
|
-
- HY-136352
-
|
|
Taste Receptor
|
Others
|
|
Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin .
|
-
- HY-P9969
-
|
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-12357
-
-
- HY-50910
-
|
CCI-779
|
mTOR
Autophagy
Apoptosis
Bacterial
|
Cancer
|
|
Temsirolimus is an inhibitor of mTOR with an IC50 of 1.76 μM. Temsirolimus activates autophagy and prevents deterioration of cardiac function in animal model .
|
-
- HY-NP134
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
Flagellin from S. typhimurium is a potent TLR5 agonist. Flagellin activates immune cells and inhibits melanoma cells activity .
|
-
- HY-N8759
-
|
|
Others
|
Inflammation/Immunology
|
|
Vogeloside is an iridoid that can be isolated from the roots of Triosteum pinnatifidum. Vogeloside inhibits nitric oxide production in LPS-activated macrophages .
|
-
- HY-15869
-
|
INZ
|
Sirtuin
MDM-2/p53
|
Cancer
|
|
Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an activator p53, used in the research of cancer.
|
-
- HY-126421
-
-
- HY-110074
-
|
|
Others
Wnt
|
Others
|
|
TWS119 TFA is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
|
-
- HY-154924
-
-
- HY-P1615
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Cenupatide (UPARANT) is a Urokinase-type plasminogen activator receptor (uPAR) inhibitor. Cenupatide has anti-angiogenic and anti-inflammatory efficacy .
|
-
- HY-78131B
-
|
(R)-Ibuprofen
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
(R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
|
-
- HY-100407
-
|
|
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-N6946
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Mitraphylline is the major pentacyclic oxindolic alkaloid presented in Uncaria tomentosa. Mitraphylline inhibits lipopolysaccharide-mediated activation of primary human neutrophils .
|
-
- HY-101790A
-
|
|
NEDD8-activating Enzyme
|
Cancer
|
|
ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity .
|
-
- HY-123790
-
|
|
PI3K
|
Inflammation/Immunology
|
|
AS2541019 is a PI3Kδ (p110δ) inhibitor. AS2541019 inhibits B cell activation and proliferation, and suppresses xenograft antibody production .
|
-
- HY-15004
-
AUZ 454
5 Publications Verification
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-125567
-
|
|
CXCR
|
Inflammation/Immunology
|
|
Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury .
|
-
- HY-163497
-
-
- HY-N2117
-
-
- HY-N1990
-
|
|
PPAR
|
Cardiovascular Disease
Inflammation/Immunology
|
|
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-N1419
-
-
- HY-B1221
-
|
|
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-107458
-
|
|
c-Kit
|
Cancer
|
|
AP23848 is an ATP-dependent kinase inhibitor that effectively and selectively targets the Kit activation loop mutation both in vitro and in vivo, showing anti-tumor activity. AP23848 can inhibit the phosphorylation of the activated Kit mutation and tumor growth in mice, making it suitable for targeting diseases with the D816V mutation, such as systemic mastocytosis (SM) and acute myeloid leukemia (AML) research .
|
-
- HY-15027S3
-
|
Mesalamine-d3 disodium; 5-ASA-d3 disodium; Mesalazine-d3 disodium
|
PPAR
NF-κB
Endogenous Metabolite
PAK
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
5-Aminosalicylic acid-d3 disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).
|
-
- HY-107460
-
|
|
Ephrin Receptor
|
Cancer
|
|
LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC .
|
-
- HY-112903A
-
|
|
Protein Arginine Deiminase
MDM-2/p53
PERK
mTOR
Autophagy
|
Cancer
|
|
YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer .
|
-
- HY-160901
-
|
|
Complement System
|
Inflammation/Immunology
|
|
CP-289,503 is an inhibitor of the complement C5a receptor with an IC50 of 1 μM. C5a acts as an activator of leukocytes and phagocytes during complement system activation. The C5a receptor can bind to C5a, which can stimulate the upregulation of cell surface integrins and degranulation of inflammatory cells, leading to endothelial cell damage. C5a receptor inhibitors can block C5a signaling and inhibit a variety of inflammatory diseases .
|
-
- HY-126486
-
|
A293
|
Potassium Channel
|
Cardiovascular Disease
|
|
AVE1231 (A293) is a dual-pore potassium channel TASK-1 inhibitor. AVE1231 blocks carbamoylcholine chloride (HY-B1208)-activated IKACh (IC50=8.4 μM). AVE1231 can be used in the study of arrhythmias and atrial fibrillation .
|
-
- HY-P10414
-
|
KP1 (human)
|
TGF-beta/Smad
p38 MAPK
|
Inflammation/Immunology
|
|
Klotho-derived peptide 1 (KP1 human) blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
|
-
- HY-114398
-
BAY-293
1 Publications Verification
|
SOS1
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-15027S2
-
|
Mesalamine-13C6; 5-ASA-13C6; Mesalazine-13C6
|
PPAR
PAK
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
|
|
5-Aminosalicylic acid- 13C6 is the 13C labeled 5-Aminosalicylic Acid . 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB .
|
-
- HY-15027S1
-
-
- HY-P10414A
-
|
KP1 (human) hydrochloride
|
TGF-beta/Smad
p38 MAPK
|
Inflammation/Immunology
|
|
Klotho-derived peptide 1 (KP1 human) hydrochloride blocks TGF-β/TGF-β receptor 2 interaction, inhibits TGF-β-induced activation of Smad2/3 and mitogen-activated protein kinase (MAPK), and exhibits anti-fibrotic and kidney protective effects in mouse model .
|
-
- HY-156520
-
|
|
Apoptosis
|
Inflammation/Immunology
|
|
Immunosuppressant-1 (Compound 31) inhibits anti-CD3/anti-CD28 co-stimulated T-cell proliferation. Immunosuppressant-1 has immunosuppressive activity, and induces apoptosis by activating caspase-3 and PARP in activated lymph node cells .
|
-
- HY-10119
-
|
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-161043
-
|
|
Pyroptosis
|
Inflammation/Immunology
|
|
ECDD-S16 is a potent inhibitor of pyroptosis. ECDD-S16 inhibits surface and endosomal TLR ligands activated pyroptosis in Raw264.7 cells .
|
-
- HY-13417A
-
|
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
Endogenous Metabolite
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor .
|
-
- HY-118489
-
|
|
iGluR
|
Neurological Disease
Inflammation/Immunology
|
|
L644711 is an anion transport inhibitor that reduces cell swelling by inhibiting potassium-activated D-aspartate release in astrocytes. L644711 can be used in the study of brain injury and neuroprotection .
|
-
- HY-13417
-
|
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
Endogenous Metabolite
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
|
-
- HY-164428
-
|
|
PKC
|
Cancer
|
|
AE 51310 is an OPN4 inhibitor. AE 51310 inhibits the activation of PKC and the downstream BRAF/MEK/ERKs signaling pathway. AE 51310 can be used for cancer research, such as NSCLC .
|
-
- HY-169796
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Panepophenanthrin is a compound that can be isolated from the mushroom strain, Panus rudis Fr. IFO 8994. Panepophenanthrin is a ubiquitin-activating enzyme inhibitor .
|
-
- HY-15723AR
-
|
|
Ras
Apoptosis
|
Cancer
|
|
NSC 23766 (trihydrochloride) (Standard) is the analytical standard of NSC 23766 (trihydrochloride). This product is intended for research and analytical applications. NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.
|
-
- HY-15336
-
|
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-137495A
-
|
|
PAI-1
Ser/Thr Protease
|
Cancer
|
|
GGACK (H-Glu-Gly-Arg-CMK) hydrochloride is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor .
|
-
- HY-15251
-
-
- HY-151631
-
|
|
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-137495
-
|
|
PAI-1
Ser/Thr Protease
|
Cancer
|
|
GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor .
|
-
- HY-161262
-
|
|
FAP
|
Cancer
|
|
SB03178 is a fibroblast activation protein-alpha (FAP) inhibitor. SB03178 can be conjugated with DOTA and can be used for cancer research .
|
-
- HY-N2283
-
|
|
ERK
Akt
Endogenous Metabolite
|
Cancer
|
|
Deltonin, a steroidal saponin, isolated from Dioscorea zingiberensis, has antitumor activity; Deltonin inhibits ERK1/2 and AKT activation.
|
-
- HY-102066
-
|
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-111789
-
|
TAK-981
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
Cancer
|
|
Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities .
|
-
- HY-N10359
-
-
- HY-117962A
-
|
|
Guanylate Cyclase
|
Metabolic Disease
|
|
BI 703704 is a potent soluble guanylate cyclase (sGC) activator. BI 703704 inhibits the progression of diabetic nephropathy in the ZSF1 rat .
|
-
- HY-N1380
-
-
- HY-106504
-
-
- HY-12524
-
Bikinin
1 Publications Verification
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-B0380S2
-
|
|
Isotope-Labeled Compounds
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine-d3 hydrochloride is deuterium labeled Trimebutine hydrochloride. Trimebutine hydrochloride is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine hydrochloride inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine hydrochloride also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine hydrochloride also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine hydrochloride also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-B0380S1
-
|
|
Isotope-Labeled Compounds
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine-d5 fumarate is deuterium labeled Trimebutine fumarate. Trimebutine fumarate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine fumarate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine fumarate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine fumarate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine fumarate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-101180
-
|
Ceramide 2
|
Phosphatase
Mitochondrial Metabolism
Apoptosis
Autophagy
|
Metabolic Disease
Endocrinology
|
|
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-108635
-
|
PAF (C16)
|
p38 MAPK
MEK
ERK
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
|
|
C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability .
|
-
- HY-155477
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Cbl-b-IN-15 (compound 25) is an inhibitor of the RING finger E3 ligase Cbl (IC50: 15 nM). Cbl-b refers to Casitas B-lineage lymphoma proto-oncogene-b, which inhibits T-cell, natural killer (NK) cell, and B-cell activation. Cbl-b-IN-15 activates T cell function with EC50=0.41 μM .
|
-
- HY-114363A
-
|
|
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-P1740
-
|
|
Integrin
Apoptosis
Caspase
|
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-147187
-
|
|
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-159718
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-46 (Compound 3k) activates neuro-immunomodulatory cholinergic anti-inflammatory pathway, and thus inhibits NLRP3 inflammasome activation. NLRP3-IN-46 inhibits Uric acid sodium (HY-B2130A)-induced IL-1β production in THP-1 cells, and can be used in gouty arthritis research .
|
-
- HY-155971
-
|
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
VISTA-IN-2 (Compound 1) is an inhibitor of V-domain Ig suppressor of T-cell activation (VISTA). VISTA-IN-2 induces VISTA degradation in cells through an autophagic mechanism. VISTA-IN-2 rescues VISTA-mediated immunosuppression, and enhances antitumor activity of immune cells. VISTA-IN-2 also activates the antitumor immunity and inhibits tumor growth in a CT26 mouse model .
|
-
- HY-15664
-
|
|
Thrombin
Interleukin Related
RSV
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
Bivalirudin TFA, a hirudin analog and anticoagulant, is a direct thrombin inhibitor. Bivalirudin TFA inhibits thrombin-mediated fibrinogen cleavage, coagulation factor activation, and platelet activation by reversibly binding to thrombin. In addition, Bivalirudin TFA also has certain effects of anti-virus, anti-inflammation, and vascular endothelial barrier function protection. Bivalirudin TFA can be used for the research of thrombotic diseases and others .
|
-
- HY-P5154
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Tamapin is a venom peptide, targeting to small conductance Ca(2+)-activated K(+) (SK) channels. Tamapin is a selctive blocker of SK2 (Potassium Channel). Tamapin inhibits SK channel-mediated currents in pyramidal neurons of the hippocampus. Tamapin can be isolated from the Indian red scorpion (Mesobuthus tamulus) .
|
-
- HY-N6051
-
|
|
Fungal
NOD-like Receptor (NLR)
NF-κB
|
Infection
Inflammation/Immunology
|
|
(-)-Maackiain is a pterocarpan phytoalexin produced from Sophora flavescens. (-)-Maackiain is toxic to several genera of fungal pathogens of legume and non legume hosts. (-)-Maackiain enhances the activation of NLRP3 inflammasome, inhibits the activation of NF-κB pathway, exhibiting thereby immunostimulatory and anti-inflammatory activities. (-)-Maackiain is orally active .
|
-
- HY-103697R
-
|
|
Toll-like Receptor (TLR)
Reference Standards
|
Cancer
|
|
Gardiquimod (Standard) is the analytical standard of Gardiquimod. This product is intended for research and analytical applications. Gardiquimod is an imidazoline TLR7/8 agonist. Gardiquimod inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM.
|
-
- HY-N6258R
-
|
|
Reference Standards
AMPK
Apoptosis
|
Metabolic Disease
|
|
Kahweol (Standard) is the analytical standard of Kahweol. This product is intended for research and analytical applications. 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-10119A
-
|
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-P10850
-
|
|
TNF Receptor
NF-κB
Apoptosis
|
Inflammation/Immunology
|
|
PIYLGGVFQ is a peptide inhibitor for TNF-α. PIYLGGVFQ inhibits TNF-α-mediated apoptosis, NF-κB nuclear translocation and activation. PIYLGGVFQ exhibits anti-arthritic activity in the CIA mouse model .
|
-
- HY-163939
-
|
|
SOS1
Ras
|
Cancer
|
|
RGT-018 is a potent and orally active SOS1 inhibitor with anti-tumor effects. RGT-018 exerts anti-cancer cell proliferation activity by inhibiting KRAS activation .
|
-
- HY-122082R
-
|
|
Apoptosis
Reference Standards
|
Inflammation/Immunology
|
|
Methopterin (Standard) is the analytical standard of Methopterin. This product is intended for research and analytical applications. Methopterin inhibits osteoclasts proliferation. Methopterin inhibits the activation and bone resorption function of osteoclasts, and induced osteoclasts apoptosis .
|
-
- HY-165529
-
|
|
Ser/Thr Protease
|
Inflammation/Immunology
|
Camostat is an orally active trypsin inhibitor. Camostat can reduce pancreatic fibrosis induced by repeated administration of superoxide dismutase inhibitors in rats, and decrease the proliferation and activation of pancreatic stellate cells (PSCs) .
|
-
- HY-17602
-
|
BBI503
|
Apoptosis
|
Cancer
|
|
Amcasertib (BBI503) is an orally activate cancer stemness kinase inhibitor that enhances apoptosis. Amcasertib inhibits the expression of NANOG and CD133 and cell viability in PC-9/GR cells.
|
-
- HY-17376
-
-
- HY-N2065
-
|
|
NF-κB
Ferroptosis
|
Inflammation/Immunology
Cancer
|
|
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-18935A
-
|
Curaxin-137 hydrochloride; CBL-C137 hydrochloride
|
MDM-2/p53
NF-κB
|
Cancer
|
|
CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 μM, respectively.
|
-
- HY-103097
-
|
|
Phospholipase
|
Others
|
|
ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
|
-
- HY-110228
-
|
1,1-Dimethylbiguanide-d6 hydrochloride
|
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
|
|
Metformin-d6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-134975
-
|
|
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-13694
-
-
- HY-P2271
-
|
|
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-N8816
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Stipuleanoside R2 inhibits NF-κB activation stimulated by TNFα in a dose-dependent manner with IC50 value of 4.1 μM .
|
-
- HY-W668749
-
|
|
FAP
|
Cancer
|
|
3BP-3580 is a fibroblast activation protein (FAP) inhibitor (pIC50: 8.6), and can be used for cancer research .
|
-
- HY-161293
-
|
|
p38 MAPK
|
Cancer
|
|
p38-α MAPK-IN-6 (compound 3a) is a p38α mitogen-activated protein kinase inhibitor .
|
-
- HY-148507
-
|
|
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-B0809S
-
-
- HY-122486
-
|
Lophirochalcone
|
EBV
|
Cancer
|
|
Lophirachalcone (Lophirochalcone) is an inhibitor of the activation of EB virus (EBV) induced by tumor promoter teleocidin B-4. Lophirachalcone has antitumor activity .
|
-
- HY-120491
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
L 722151 is a competitive inhibitor for factor XIIIa with Ki of 49 µM. L 722151 accelerates tissue plasminogen activator-catalyzed clot dissolution, and exhibits antithrombotic efficacy .
|
-
- HY-N10926
-
|
|
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-B0099
-
|
MCI-186
|
MMP
Apoptosis
|
Neurological Disease
|
|
Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
|
-
- HY-121006
-
|
|
Mitochondrial Metabolism
AMPK
Insulin Receptor
|
Metabolic Disease
Cancer
|
|
Biguanide is an orally active antihyperglycemic agent. Biguanide inhibits mitochondrial ATP production, activates the LKB1-AMPK signaling pathway, and damages the energy homeostasis. Biguanide enhances insulin-receptor activation and downstream signaling. Biguanide exhibits potential in ameliorating the type 2 diabetes and the insulin-associated cancers[1].
|
-
- HY-108586
-
|
|
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-139553A
-
|
(R)-ATI-450; (R)-CDD-450
|
Drug Isomer
|
Inflammation/Immunology
|
|
(R)-Zunsemetinib is the isomer of Zunsemetinib (HY-139553), and can be used as an experimental control. 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 .
|
-
- HY-N6641
-
|
|
Keap1-Nrf2
PPAR
|
Inflammation/Immunology
Cancer
|
|
Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor). Monascin is a Nrf2 activator and PPARγ agonist .
|
-
- HY-50694
-
|
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-N8847
-
|
alpha-Ionone
|
Hippo (MST)
YAP
Olfactory Receptor
Apoptosis
|
Cancer
|
|
α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
|
-
- HY-Y0152
-
|
(8R,9S)-Cinchonine; LA40221
|
Apoptosis
Parasite
Autophagy
Caspase
Calcium Channel
|
Others
Inflammation/Immunology
Cancer
|
|
Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells .
|
-
- HY-N1504
-
|
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-N0625AR
-
|
|
Reference Standards
PPAR
Keap1-Nrf2
Toll-like Receptor (TLR)
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Alpinetin (Standard) is the analytical standard of Alpinetin. This product is intended for research and analytical applications. Alpinetin is a flavonoid isolated from cardamom and possesses antitumor, antiinflammation, hepatoprotective, cardiovascular protective, lung protective, antibacterial, antiviral, neuroprotective properties. Alpinetin inhibits lipopolysaccharide (LPS)-induced inflammation, activates PPAR-γ, activates Nrf2, and inhibits TLR4 expression to protect LPS-induced renal injury .
|
-
- HY-155516
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
KV1.3-IN-1 (Compound trans-18) is a KV1.3 channel inhibitor (IC50: 230 nM and 26.12 nM in Ltk? cells and PHA-activated T-lymphocytes respectively). KV1.3-IN-1 impairs intracellular Ca 2+ signaling. KV1.3-IN-1 inhibits T-cell activation, proliferation, and colony formation .
|
-
- HY-156677
-
|
|
METTL3
|
Cancer
|
|
STC-15 is an orally active RNA methyltransferase METTL3 inhibitor with the activity of activating anti-tumor immunity and reshaping the tumor microenvironment. STC-15 inhibits tumor growth by activating anti-cancer immune responses associated with increased interferon signaling and synergizes with T-cell checkpoint blockade. STC-15 can be used in the study of proliferative diseases such as cancer and autoimmune diseases .
|
-
- HY-169509
-
|
|
PARP
Necroptosis
Topoisomerase
RIP kinase
Mixed Lineage Kinase
|
Cancer
|
|
Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment .
|
-
- HY-13559A
-
|
Azaspirane dimaleate; SKF 106615-12 dimaleate; SKF 106615A12 dimaleate
|
Apoptosis
Caspase
STAT
Interleukin Related
|
|
|
Atiprimod (Azaspirane) (dimaleate) is an anti-proliferative and anti-angiogenic agent that inhibits proliferation of cancer cell lines. Atiprimod (dimaleate) also induces Apoptosis and activates both caspase-9 and caspase-3 in T84 colon carcinoma cells. Atiprimod (dimaleate) inhibits both bFGF and VEGF induced proliferation and migration of human umbilical vein endothelial cells, resulting in disruption of cord formation. Atiprimod (dimaleate) reduces production of IL-6, VEGF and inhibits activation of Stat3 .
|
-
- HY-12364
-
|
|
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-A0042
-
|
CGP 33101; E 2080; RUF 331
|
Sodium Channel
|
Neurological Disease
|
|
Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
|
-
- HY-12808
-
|
|
NAMPT
AMPK
mTOR
|
Cancer
|
|
STF-118804 is a highly specific NAMPT inhibitor. STF-118804 activates AMPK and inhibits mTOR pathways. STF-118804 has antitumor activity against pancreatic cancer .
|
-
- HY-N0773
-
|
Saponaretin; Homovitexin
|
JNK
NF-κB
|
Inflammation/Immunology
|
|
Isovitexin is a flavonoid isolated from passion flower, Cannabis and, and the palm, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
|
-
- HY-145263
-
|
|
Ser/Thr Protease
|
Cancer
|
|
VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer .
|
-
- HY-159643
-
|
|
MAP4K
|
Cancer
|
|
NDI-101150 is an orally active, potent and selective hematopoietic progenitor cell kinase 1 (HPK1) inhibitor. NDI-101150 enhances T cell activation and inhibits tumor growth .
|
-
- HY-N2119
-
|
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Sciadopitysin is a type of biflavonoids in leaves from ginkgo biloba . Sciadopitysi inhibits RANKL-induced osteoclastogenesis and bone loss by inhibiting NF-κB activation and reducing the expression of c-Fos and NFATc1 .
|
-
- HY-P1281
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Kaliotoxin is a peptidyl inhibitor of neuronal BK-Type. Kaliotoxin can specific inhibit Kv channels and calcium-activated potassium channels. Kaliotoxin can be used for the research of the regulation of membrane potential and neuron excitability .
|
-
- HY-173618
-
-
- HY-N7452
-
|
|
JAK
Bacterial
Orthopoxvirus
|
Metabolic Disease
|
|
Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria. Coumermycin A1 shows anti-orthopoxvirus activity.
|
-
- HY-121434
-
|
|
Microtubule/Tubulin
|
|
|
N-Deacetylcolchicine is a microtubule polymerization inhibitor with an IC50 of 3 μM against bovine brain microtubules. It is a derivative of the microtubule polymerization inhibitor Colchicine (HY-16569) and activates the GTPase activity of microtubules [1][2].
|
-
- HY-170485
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
Thrombin inhibitor 13 (Compound 13a) is a covalent and reversible inhibitor for thrombin (FIIa) with an IC50 of 0.7 nM. Thrombin inhibitor 13 prolongs the activated partial thromboplastin time (aPTT) and prothrombin time (PT), exhibits antithrombotic and anticoagulant activities .
|
-
- HY-15477
-
|
|
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-113224
-
-
- HY-15477A
-
|
|
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-N0826
-
-
- HY-132878
-
|
|
p38 MAPK
|
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-138558
-
-
- HY-P3065
-
|
|
Calcium Channel
|
Neurological Disease
|
|
Calcicludine is a protein toxin from the venom of the green mamba that inhibits high-voltage-activated calcium channel, especially L-type calcium channel .
|
-
- HY-15718A
-
-
- HY-149860
-
|
|
FAP
|
Cancer
|
|
FAP-IN-1 is a fibroblast activation protein (FAP) inhibitor with an IC50 value of 3.3 nM. FAP-IN-1 can be used for the research of cancer .
|
-
- HY-B0167
-
-
- HY-19205A
-
|
LDP-392
|
Lipoxygenase
|
Inflammation/Immunology
|
|
CMI-392 is a dual 5-lipoxygenese inhibitor and platelet-activating factor (PAF) receptor antagonist with IC50s of 100 and 10 nM, respectively.
|
-
- HY-47979
-
|
|
FAP
|
Others
Cancer
|
|
FAP-IN-2 is a derivative of 99mTc-labeled isonitrile-containing fibroblast activation protein (FAPI) inhibitor, that can be used for tumor imaging .
|
-
- HY-10072
-
|
|
NF-κB
AP-1
|
Inflammation/Immunology
|
|
SPC 839 (compound 10) is an orally active inhibitor of AP-1 and NF-kB mediated transcriptional activation with IC50 of 0.008 μM .
|
-
- HY-118019
-
-
- HY-167719
-
-
- HY-100611
-
-
- HY-B0380AR
-
|
|
Reference Standards
Opioid Receptor
Apoptosis
Potassium Channel
NF-κB
Akt
IRAK
JNK
Toll-like Receptor (TLR)
ERK
Calcium Channel
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine maleate (Standard) is the analytical standard of Trimebutine maleate (HY-B0380A). This product is intended for research and analytical applications. Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-B0380R
-
|
|
Opioid Receptor
Toll-like Receptor (TLR)
Calcium Channel
Potassium Channel
IRAK
ERK
JNK
NF-κB
Akt
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Trimebutine (Standard) is the analytical standard of Trimebutine (HY-B0380). This product is intended for research and analytical applications. Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
|
-
- HY-168034
-
|
|
STING
|
Infection
Inflammation/Immunology
|
|
diABZI-4 is an oral active STING agonist with broad-spectrum antiviral activity. diABZI-4 induces the production of pro-inflammatory cytokines and lymphocyte activation by activating STING, thereby inhibiting the replication of influenza A virus (IAV), SARS-CoV-2, and human rhinovirus (HRV), with an EC50 range of 11.8-199 nM .
|
-
- HY-P5154A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Tamapin TFA is a venom peptide, targeting to small conductance Ca(2+)-activated K(+) (SK) channels. Tamapin TFA is a selctive blocker of SK2 (Potassium Channel). Tamapin TFA inhibits SK channel-mediated currents in pyramidal neurons of the hippocampus. Tamapin TFA can be isolated from the Indian red scorpion (Mesobuthus tamulus) .
|
-
- HY-101047S
-
|
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 .
|
-
- HY-14569
-
CDPPB
1 Publications Verification
|
mGluR
Akt
ERK
Caspase
Mitochondrial Metabolism
|
Neurological Disease
|
|
CDPPB is a selective, orally active mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNF mRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease .
|
-
- HY-120760
-
|
|
Lipoxygenase
|
Others
|
|
L-691831 is a ligand for 5-lipoxygenase activating protein binding assays that has utility as a tool for studying 5-lipoxygenase activating protein (FLAP) related activities. L-691831 can be used to measure the affinity of FLAP on the leukocyte membrane for leukotriene synthesis inhibitors, with binding being correlated with inhibition of leukotriene synthesis.
|
-
- HY-124822
-
COH-SR4
1 Publications Verification
|
AMPK
|
Metabolic Disease
Cancer
|
|
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-121629
-
|
|
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
-
|
|
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-124748
-
|
|
Protease Activated Receptor (PAR)
Apoptosis
|
Inflammation/Immunology
|
|
ENMD-1068 is a selective protease-activated receptor 2 (PAR2) antagonist. ENMD-1068 reduces hepatic stellate cell activation and collagen expression by inhibiting TGF-β1/Smad signaling. ENMD-1068 also inhibits the proliferation of endometrial cells and induces apoptosis of epithelial cells in the lesion. ENMD-1068 can be used in the study of endometriosis and liver fibrosis .
|
-
- HY-124748A
-
|
|
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-100684
-
|
|
Prolyl Endopeptidase (PREP)
FAP
|
Cancer
|
|
UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 3.2 nM. UAMC-1110 also inhibits prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM .
|
-
- HY-10999
-
|
GSK1120212; JTP-74057
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
|
-
- HY-107415
-
|
|
Raf
|
Cancer
|
|
PLX7922, a RAF inhibitor, can bind with BRAF V600E. PLX7922 inhibits pERK in BRAF V600E cell lines, and activates pERK in mutant NRAS cell lines .
|
-
- HY-110367A
-
|
|
Src
|
Others
|
|
LCB 03-0110, a thienopyridine derivative, is a potent pan-discoidin domain receptor/c-Src family tyrosine kinase inhibitor. LCB 03-0110 suppresses scar formation by inhibiting fibroblast and macrophage activation .
|
-
- HY-18849
-
|
|
ERK
|
Cancer
|
|
ERK2-IN-3 (compound 2) is a inhibitor of ERK2, and inhibits Erk2 WT and Erk2 DS1 activation loop phosphorylation, with IC50 of 5 μM and 42 nM, respectively .
|
-
- HY-N4171
-
|
|
Apoptosis
|
Inflammation/Immunology
|
|
Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity .
|
-
- HY-14165
-
-
- HY-123506
-
|
|
Src
|
Neurological Disease
Inflammation/Immunology
|
|
Fenlean, a natural squamosamide derivative, is a Src tyrosine kinase inhibitor. Fenlean can inhibit over-activated microglia and protect dopaminergic neurons. Fenlean can attenuate neuroinflammation in Parkinson's disease models .
|
-
- HY-P2333
-
LCKLSL
5 Publications Verification
|
Annexin A
|
Cardiovascular Disease
|
|
LCKLSL is a N-terminal hexapeptide and a competitive annexin A2 (AnxA2) inhibitor. LCKLSL potently inhibits the binding of tissue plasminogen activator (tPA) to AnxA2. LCKLSL also inhibits the generation of plasmin and has anti-angiogenic roles .
|
-
- HY-120231
-
|
|
MALT1
|
Cancer
|
|
Z-VRPR-FMK is an irreversible MALT1 protein inhibitor. Z-VRPR-FMK inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression .
|
-
- HY-100227
-
E 64c
2 Publications Verification
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-P2333A
-
|
|
Annexin A
|
Cardiovascular Disease
|
|
LCKLSL hydrochloride is a N-terminal hexapeptide and a competitive annexin A2 (AnxA2) inhibitor. LCKLSL hydrochloride potently inhibits the binding of tissue plasminogen activator (tPA) to AnxA2. LCKLSL hydrochloride also inhibits the generation of plasmin and has anti-angiogenic roles .
|
-
- HY-120149
-
|
|
Toll-like Receptor (TLR)
MDM-2/p53
MMP
Caspase
SOD
p38 MAPK
NF-κB
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Inotodiol activates p53 signaling pathway, inhibits MMP-2/9, and exhibits antitumor activity in cancer cell HeLa. Inotodiol inhibits the generation of ROS and exhibits antioxidant and neuroprotective effects. Inotodiol inhibits the activation of MAPK and NF-κB signaling pathway, and exhibits anti-inflammatory activity. Inotodiol inhibits TLR-4 mediated TNF-α production (IC50s in BMMC and BMDM is 0.7 μM and 3.0 μM), inhibits the degranulation in mast cell, exhibits anti-allergic activity. Inotodiol is orally active .
|
-
- HY-149989
-
|
|
Ack1
Akt
|
Cancer
|
|
Ack1 inhibitor 1 is a potent, selective, and orally active inhibitor of ACK1 kinase with an IC50 value of 2.1 nM. Ack1 inhibitor 1 inhibits the phosphorylation of ACK1 and activation of downstream AKT. Ack1 inhibitor 1 has anti-tumor activity .
|
-
- HY-B0627
-
|
1,1-Dimethylbiguanide
|
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Metformin (1,1-Dimethylbiguanide) inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-17471A
-
|
1,1-Dimethylbiguanide hydrochloride
|
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-N1462R
-
|
|
Reference Standards
Chloride Channel
Autophagy
mTOR
AMPK
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for use in research and analytical applications. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
|
-
- HY-N8617
-
|
|
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-122908
-
|
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
-
|
|
Phosphodiesterase (PDE)
|
Infection
Cancer
|
|
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-15098
-
|
Apoptosis Activator VII
|
HSP
Apoptosis
|
Cancer
|
|
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.
|
-
- HY-161392
-
|
|
CRM1
|
Cancer
|
|
CW2158 (Compound 13) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
|
-
- HY-N0754
-
|
|
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-155646
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 48 is an anti-inflammatory agent based on its role in inhibiting the NF-κB signaling pathway and activating HO-1 expression .
|
-
- HY-I0352
-
-
- HY-16642A
-
-
- HY-N7314
-
|
|
Syk
|
Inflammation/Immunology
|
|
Asebogenin has antimalarial activity in vitro . Asebogenin can inhibit the phosphorylation of Syk, thereby effectively suppressing platelet activation and the formation of neutrophil extracellular traps .
|
-
- HY-161391
-
|
|
CRM1
|
Cancer
|
|
CW0134 (Compound 12) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells .
|
-
- HY-139303
-
|
|
GnRH Receptor
|
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-120261
-
-
- HY-147005
-
|
|
CRAC Channel
|
Cardiovascular Disease
|
|
piCRAC-1 is a potent, photoinducible Ca 2+ release-activated Ca 2+ (CRAC) channel inhibitor. piCRAC-1 alleviates thrombocytopenia and hemorrhage .
|
-
- HY-B0649
-
-
- HY-19700
-
|
|
MEK
ERK
Endogenous Metabolite
|
Others
|
|
trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
|
-
- HY-156769
-
-
- HY-13296
-
|
|
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-B0795
-
|
|
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
-
|
|
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-19084
-
-
- HY-N0629
-
-
- HY-120459
-
|
|
Na+/K+ ATPase
|
Others
|
|
Rs-029 is an inhibitor Na+/K+ ATPase and an activator for Mg2+ ATPase. Rs-029 decreases the ATP level in red blood cells .
|
-
- HY-N9921
-
|
|
Pyroptosis
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
Antcin A is a potent NLRP3 inhibitor that inhibits the assembly and activation of the NLRP3 inflammasome. Antcin A can inhibit Kupffer cell pyroptosis and has liver protective activity. Antcin A can be used to study inflammation, such as non-alcoholic fatty liver disease .
|
-
- HY-126754
-
-
- HY-121377
-
-
- HY-120675
-
SSTC3
2 Publications Verification
|
Casein Kinase
Wnt
|
Cancer
|
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors .
|
-
- HY-18965R
-
|
|
PKC
|
Cardiovascular Disease
|
|
TAS-301 (Standard) is the analytical standard of TAS-301. This product is intended for research and analytical applications. TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.
|
-
- HY-107002A
-
|
|
Dopamine Receptor
|
Neurological Disease
Endocrinology
|
|
Lergotrile mesylate is a potent and orally active dopamine agonist and a prolactin secretion inhibitor. Lergotrile mesylate inhibits prolactin release from pituitaries by activating an adenohypophyseal dopamine receptor. Lergotrile mesylate has the potential for the research of Parkinson's disease .
|
-
- HY-N0141
-
|
(-)-Parthenolide
|
NF-κB
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
|
-
- HY-137974
-
|
|
STAT
Apoptosis
|
Cancer
|
|
8-Epixanthatin is a potential colchicine binding site inhibitor isolated from Xanthium chinese Mill. 8-Epixanthatin can inhibit the activation of STAT3, induce apoptosis, and has anti-tumor activity .
|
-
- HY-W404002
-
|
|
Prolyl Endopeptidase (PREP)
|
Metabolic Disease
|
|
BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC50 of 49.00 μM. BR102910 can be used for the researchof type 2
|
-
- HY-119160
-
|
|
PAI-1
|
Inflammation/Immunology
Cancer
|
|
TM5007 is a poent and orally active inhibitor of plasminogen activator inhibitor-1 (PAI-1) with an IC50 of 29 μM. TM5007 enhance fibrinolysis activity and inhibits coagulation. TM5007 also prevents the fibrotic process initiated by bleomycin in mouse lung .
|
-
- HY-P4136
-
|
|
ERK
|
Cancer
|
|
Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits ERK activation with an IC50 of 10 μM .
|
-
- HY-111662
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium (DSS; HY-116282C)-induced murine experimental colitis .
|
-
- HY-B1221R
-
|
|
Reference Standards
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
|
Flufenamic acid (Standard) is the analytical standard of Flufenamic acid. This product is intended for research and analytical applications. 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-B1221S1
-
|
|
Isotope-Labeled Compounds
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
|
Flufenamic acid- 13C6 is the 13C6 labeled Flufenamic acid. 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-15186
-
|
GDC-0068; RG7440
|
Organoid
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-14162
-
|
|
FLAP
|
Inflammation/Immunology
|
AM103 (free acid) is a selective FLAP inhibitor that can block the first step of the LT pathway, which is 5-LO activation. AM103 (free acid) can inhibit the production of LTB4 and cysteinyl leukotrienes (CysLT). AM103 (free acid) has anti-inflammatory activity in a mouse model of chronic lung inflammation and can extend the survival time of mice injected with platelet-activating factor. AM103 (free acid) can be used for research on respiratory diseases such as asthma .
|
-
- HY-123936
-
|
|
NF-κB
IKK
|
Neurological Disease
Inflammation/Immunology
|
|
SR12343, an IKK/NF-κB inhibitor, is a NF-κB essential modulator (NEMO)-binding domain (NBD) mimetic. SR12343 inhibits TNF-α- and LPS-induced NF-κB activation by blocking the interaction between IKKβ and NEMO, with an IC50 of 37.02 μM for TNF-α-mediated NF-κB activation. SR12343 suppresses LPS-induced acute pulmonary inflammation in mice. SR12343 can be used for research of inflammatory and degenerative diseases .
|
-
- HY-15186C
-
|
GDC-0068 tosylate; RG7440 tosylate
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) tosylate 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 tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-N3807
-
|
|
Acyltransferase
ERK
NF-κB
|
Infection
Cardiovascular Disease
Cancer
|
|
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-B1221S
-
|
|
Isotope-Labeled Compounds
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
|
Flufenamic acid-d4 is deuterium labeled Flufenamic acid. 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-15027S4
-
|
5-ASA-d7; Mesalamie-d7; Mesalazie-d7
|
Isotope-Labeled Compounds
PPAR
PAK
Endogenous Metabolite
NF-κB
|
Inflammation/Immunology
Cancer
|
|
5-Aminosalicylic acid-d7 (5-ASA-d7; Mesalamie-d7; Mesalazie-d7) is deuterium labeled 5-Aminosalicylic Acid. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN) .
|
-
- HY-167692
-
|
|
STAT
|
Others
|
|
JI069 is a novel JAK-STAT inhibitor that demonstrates potent activity in suppressing Th1, Th2, and Th17 differentiation while promoting iTreg differentiation. JI069 effectively inhibits STAT3 activation as well as the activation of other STATs, including STAT1, STAT5, and STAT6. JI069 has shown significant therapeutic potential in alleviating symptoms of collagen-induced arthritis in mice while inhibiting cytokine production from T cells and the phosphorylation of STAT3 in synovial cells.
|
-
- HY-P10854
-
|
|
NF-κB
Interleukin Related
STAT
Akt
|
Neurological Disease
Inflammation/Immunology
|
|
TAT-N15 is a p55PIK inhibitor with remarkable anti-inflammatory activity and neuroprotective effects. TAT-N15 can significantly inhibit the activation of IL-6, IL-8, Akt, and NF-κB pathways, as well as suppress the protein expression of phosphorylated STAT3 and NF-κB. By inhibiting the activation of Akt, STAT3, and NF-κB pathways, TAT-N15 is used in research on acute conjunctivitis, allergic rhinitis, chronic obstructive pulmonary disease (COPD), and stroke .
|
-
- HY-10484
-
|
MLN4924 hydrochloride
|
NEDD8-activating Enzyme
Apoptosis
|
Cancer
|
|
Pevonedistat (MLN4924) hydrochloride is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM. Pevonedistat hydrochloride induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat hydrochloride suppresses the growth of human tumour xenografts in mice .
|
-
- HY-15035R
-
|
|
MDM-2/p53
JNK
SOD
|
Cardiovascular Disease
Inflammation/Immunology
|
|
S-Diclofenac (Standard) is the analytical standard of S-Diclofenac. This product is intended for research and analytical applications. S-Diclofenac (ACS 15) is a hybrid molecule of an H2S donor and the NSAID diclofenac. S-Diclofenac activates the p53 signaling pathway, and inhibits the activation of JNK. S-Diclofenac exhibits antioxidant and anti-inflammatory activities .
|
-
- HY-139504
-
|
CC-99677
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
|
Gamcemetinib (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). Gamcemetinib is extracted from patent WO2020236636, compound 1 .
|
-
- HY-103697AR
-
|
|
Toll-like Receptor (TLR)
Reference Standards
|
Cancer
|
|
Gardiquimod (diTFA) (Standard) is the analytical standard of Gardiquimod (diTFA). This product is intended for research and analytical applications. Gardiquimod diTFA is an imidazoline TLR7/8 agonist. Gardiquimod diTFA inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 at concentrations below 10 μM.
|
-
- HY-119039
-
RU-301
1 Publications Verification
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
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-118828
-
|
12-OPDA
|
NF-κB
p38 MAPK
|
Neurological Disease
Inflammation/Immunology
|
|
12-Oxo phytodienoic acid (12-OPDA) is a plant lipid-derived anti-inflammatory compound. 12-Oxo phytodienoic acid suppresses neuroinflammation by inhibiting Nf-κB and p38 MAPK signaling in Lipopolysaccharides (LPS) (HY-D1056)-activated cells. 12-Oxo phytodienoic acid can be used for neurodegenerative diseases research .
|
-
- HY-12496
-
NS-1619
3 Publications Verification
|
Potassium Channel
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
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-103308
-
|
|
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-13868
-
|
|
Ras
|
Cancer
|
|
SCH-53870 is a Ras activation inhibitor that binds to the Ras-GDP complex, keeping the Ras protein in an inactive GDP-bound state and preventing it from switching to an active GTP-bound state. SCH-53870 affects cell signaling and cell proliferation by preventing the activation of Ras protein. SCH-53870 can be used in cancer research .
|
-
- HY-70062
-
|
MLN4924
|
NEDD8-activating Enzyme
Apoptosis
|
Cancer
|
|
Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM. Pevonedistat induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat suppresses the growth of human tumour xenografts in mice .
|
-
- HY-14993R
-
|
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 (Standard) is the analytical standard of SCH79797. This product is intended for research and analytical applications. 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-133233
-
|
1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
|
Endogenous Metabolite
Phospholipase
|
Metabolic Disease
|
|
Thioetheramide-PC (1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine) is a structurally modified phospholipid that acts as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). Thioetheramide-PC has an IC50 value of 2 μM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, Thioetheramide-PC also binds to the activation site of the enzyme. Thioetheramide-PC binds more tightly to the activation site than to the catalytic site. As a result of this dual interaction, at low concentrations, Thioetheramide-PC may activate phospholipase activity rather than inhibit it.
|
-
- HY-14994R
-
|
|
Protease Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
|
SCH79797 (dihydrochloride) (Standard) is the analytical standard of SCH79797 (dihydrochloride). This product is intended for research and analytical applications. 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-151619
-
|
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
sEH inhibitor-12 (compound 34) is a sEH inhibitor with an IC50 value of 0.7 μM. sEH inhibitor-12 inhibits the 5-lipoxygenase-activating protein (FLAP)-mediated leukotriene (LT) biosynthesis with an IC50 value of 2.9 μM. sEH inhibitor-12 can be used for the research of inflammation .
|
-
- HY-132243
-
|
|
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
|
NFAT Inhibitor-3 (Compound 10) is a factor nuclear factor of activated T cells (NFAT) inhibitor. NFAT Inhibitor-3 inhibits IL-2 production. NFAT Inhibitor-3 binds in a sequence-selective manner directly to DNA. NFAT Inhibitor-3 can be used for the research of transcription factor dysregulation .
|
-
- HY-P4133
-
|
|
ERK
MEK
|
Cancer
|
|
MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of ERK2 by MEK1 with an IC50 value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable .
|
-
- HY-112391
-
SD-1029
1 Publications Verification
|
JAK
STAT
|
Cancer
|
|
SD-1029 is a JAK2/STAT3 inhibitor . SD-1029 inhibits STAT3 nuclear translocation. SD-1029 is an inhibitor of STAT3 activation due to inhibition of JAK2 phosphorylation .
|
-
- HY-N0518R
-
|
|
Reference Standards
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone (Standard) is the analytical standard of Toddalolactone. This product is intended for research and analytical applications. Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM .
|
-
- HY-10255A
-
|
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-163666
-
|
|
HIV
PKC
|
Infection
|
|
HIV-1 inhibitor-68 (compound 26) is a protein kinase C (PKC) activator derivative with reversal activity in HIV-1 latency. HIV-1 inhibitor-68 may be able to eliminate cells latently infected with HIV-1, .
|
-
- HY-119931
-
-
- HY-108534
-
|
AW 464
|
TrxR
|
Inflammation/Immunology
Cancer
|
|
PMX464 (AW 464), a thiol-reactive quinol, is the inhibitor of thioredoxin-thioredoxin reductase (Trx/TrxR) system. PMX464 can inhibit NF-κB-mediated proinflammatory activation of human type II alveolar epithelial cells .
|
-
- HY-125305
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
Z-AEVD-FMK is a caspase-10 inhibitor. Z-AEVD-FMK can inhibit the activation of Bid and the release of apoptosis-inducing factor (AIF) in mitochondria in cells, resulting in a significant decrease in the number of apoptotic cells .
|
-
- HY-163275
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MDM2-IN-24 (compound A3f) exhibits MDM2-inhibiting and MDMX-activating properties in triple-negative breast cancer (TNBC) cells, with apoptotic and anti-proliferative activities .
|
-
- HY-157430
-
|
|
Epigenetic Reader Domain
|
Neurological Disease
|
|
BET-IN-21 (compound 16) is a blood-brain barrier-permeable extra terminal domain (BET) inhibitor with the Ki of 230 nM. BET-IN-21 inhibits microglia activation and has ameliorative effects on experimental autoimmune encephalomyelitis mice .
|
-
- HY-110031
-
|
|
Apoptosis
Bcl-2 Family
|
Cancer
|
|
BAI1 hydrochloride is a selective apoptosis factor BAX allosteric inhibitors. BAI1 hydrochloride binds BAX and allosterically inhibits its activation. BAI1 hydrochloride has the potential to be used in the study of BAX dependent cell death-mediated diseases .
|
-
- HY-168561
-
-
- HY-103269
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death .
|
-
- HY-121160
-
|
SM1213; Therafectin
|
Bacterial
|
Infection
Cancer
|
|
Amiprilose (SM1213; Therafectin) is a potent inhibitor against Hepatocellular carcinoma (HCC). Amiprilose induces lymphokine-induced macrophage activation directly to kill Listeria monocytogenes .
|
-
- HY-N9753
-
|
|
Others
|
|
|
Tsukubamycin B is discovered from Streptomyces tsukubaensis and exhibits immunosuppressive activity by inhibiting T-cell activation. Tsukubamycin B can be used for immune rejection reaction research .
|
-
- HY-N1490
-
|
14-dehydro andrographolide; AP10
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
14-Deoxy-11,12-didehydroandrographolide is an analogue of Andrographolide. 14-Deoxy-11,12-didehydroandrographolide inhibits NF-κB activation.
|
-
- HY-17592
-
|
|
Parasite
Bacterial
|
Infection
Cancer
|
|
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-139132
-
|
|
Apoptosis
|
Cancer
|
|
Met-F-AEA is a metabolically stable anandamine analogue. Met-F-AEA inhibits cell growth by activating apoptosis. Met-F-AEA has antitumor activity .
|
-
- HY-N3436
-
-
- HY-13772
-
|
AD-32
|
PKC
Antibiotic
|
Inflammation/Immunology
Cancer
|
|
Valrubicin is a chemotherapy agent, inhibits TPA- and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
|
-
- HY-N1208
-
|
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
-
|
|
Cathepsin
|
Inflammation/Immunology
Cancer
|
|
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-151196
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki of 0.17 nM. FXIa-IN-10 has good oral bioavailability .
|
-
- HY-161074
-
|
|
FAP
|
Cancer
|
|
PNT6555 is a fibroblast activation protein-α (FAP) inhibitor. PNT6555 has antitumor activity. PNT6555 can be used for imaging of FAP-positive tumors .
|
-
- HY-101255
-
ODQ
3 Publications Verification
|
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
1 Publications Verification
|
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-N4182
-
|
|
Akt
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Licochalcone E, a flavonoid compound isolated from Glycyrrhiza uralensis, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation .
|
-
- HY-N3245
-
-
- HY-B0289
-
-
- HY-N11004
-
-
- HY-19770
-
|
|
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-155657
-
|
|
Src
|
Inflammation/Immunology
|
|
BT424 is a specific HCK inhibitor. BT424 can regulate macrophage activation and autophagy in vitro. BT424 ameliorates inflammation and kidney fibrosis in UUO model .
|
-
- HY-12825
-
-
- HY-121134
-
|
|
Reactive Oxygen Species (ROS)
|
Neurological Disease
Cancer
|
|
Decylubiquinone is an analog of ubiquinone (coenzyme Q10). Decylubiquinone blocks reactive oxygen species (ROS) production in response to glutathione depletion and inhibits activation of the mitochondrial permeability transition .
|
-
- HY-153343
-
|
|
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-N2337
-
|
11β-Hydroxyprogesterone
|
11β-HSD
|
Cardiovascular Disease
|
|
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
|
-
- HY-N0436
-
|
|
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-122041
-
|
|
Apoptosis
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Cancer
|
|
Ethacridine is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor and an activator of the transcriptional coactivator. Ethacridine induces thyroid cancer cells apoptosis and promotes differentiation in thyroid follicular cells .
|
-
- HY-10257
-
|
BAY 11-7083
|
NF-κB
Ferroptosis
Apoptosis
|
Cancer
|
|
BAY 11-7085 (BAY 11-7083) is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM .
|
-
- HY-N3720
-
|
6-Demethoxycapillarisin
|
PEPCK
|
Metabolic Disease
|
|
Demethoxycapillarisin (6-Demethoxycapillarisin) inhibits PEPCK mRNA levels (IC50: 43 μM) by activation of the PI3K pathway. Demethoxycapillarisin decreases glucose production .
|
-
- HY-14974
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
R 1487 is an orally active and highly selective p38α mitogen-activated protein kinase inhibitor. R 1487 can be used in the study of rheumatoid arthritis .
|
-
- HY-N0708
-
-
- HY-121944
-
|
|
Casein Kinase
Wnt
|
Others
|
|
Ricinine exhibits hepatoprotection in CCl4-induced liver damage. Ricinine is also a CK1α inhibitor, and may activate Wnt pathway .
|
-
- HY-W168754
-
|
|
MHC
|
Others
|
|
DB28 is a novel MR1 ligand. DB28 decreases cell surface expression of MR1 and competitively inhibits activation of MAIT cells by agonist ligands .
|
-
- HY-18286
-
|
|
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-118934
-
|
|
Others
|
Neurological Disease
Metabolic Disease
|
|
Novocebrin is a central nervous system activator that effectively increases brain and femoral blood flow in dogs. In addition, Novocebrin inhibits triglyceride biosynthesis in porcine adipose tissue .
|
-
- HY-172778
-
|
|
NOD-like Receptor (NLR)
URAT1
|
Metabolic Disease
Inflammation/Immunology
|
|
HNW005 is a dual inhibitor of NLRP3 inflammasome and urate transporter 1 (URAT1). It has a KD value of 204.6 nM and an IC50 of 1.7 μM for inhibiting NLRP3 inflammasome activation, and an IC50 of 6.4 μM for inhibiting uric acid transmembrane transport. When administered at a dose of 2 mg/kg in vivo, HNW005 can achieve a uric acid reduction rate of 64.8%. It can exert anti - inflammatory, analgesic, and uric acid - lowering activities by inhibiting the activation of NLRP3 inflammasome and uric acid transmembrane transport. HNW005 can be used in the research of gouty arthritis .
|
-
- HY-B0627A
-
|
1,1-Dimethylbiguanide (glycinate)
|
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Metformin (1,1-Dimethylbiguanide) glycinate inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin glycinate also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin glycinate regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-118532
-
|
AG30
|
EGFR
|
Cancer
|
|
Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts .
|
-
- HY-116868
-
|
Anecortave
|
PAI-1
|
Cardiovascular Disease
|
|
Anecortave acetate is a potent ocular angiostatic agent. Anecortave acetate inhibits neovascularization which is induced by many different angiogenic factors, and increases plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate can be used to research ocular neovascular diseases .
|
-
- HY-13412
-
|
HOE-642
|
Potassium Channel
Sodium Channel
|
Cardiovascular Disease
|
|
Cariporide is a Na+/H+ Exchanger 1 (NHE-1) inhibitor. Cariporide inhibits the expression of monocyte endothelial cell adhesion and intercellular adhesion molecule-1 (ICAM-1) mediated by high glucose (HG) by inhibiting the activation of NHE-1 .
|
-
- HY-112800
-
|
|
Phosphatase
|
Metabolic Disease
|
|
cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity .
|
-
- HY-12557
-
|
|
CaSR
Wnt
TNF Receptor
|
Inflammation/Immunology
|
|
γ-Glutamylvaline is an activator of CaSR with anti-inflammatory activity. γ-Glutamylvaline inhibits TNF-α-induced proinflammatory cytokine production and increases Wnt5a expression. γ-Glutamylvaline activates calcium-sensing receptor pathways in adipocytes of 3T3-L1 mice and prevents low-grade chronic inflammation .
|
-
- HY-N7018
-
|
|
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-B0700
-
|
BRL 49653 sodium
|
PPAR
TRP Channel
Autophagy
|
Metabolic Disease
Inflammation/Immunology
|
|
Rosiglitazone sodium is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone sodium is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
|
-
- HY-107818
-
|
|
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
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-130354
-
|
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-121516
-
|
|
Potassium Channel
|
Others
|
|
CM-TPMF is a K(Ca)2 channel modulator with selective activation and inhibition of K(Ca)2.1 subtypes. CM-TPMF can act on K(Ca)2.1 channels as an activator or inhibitor, and its activity is affected by the stereochemical structure. It can be used to study the physiological or pathophysiological effects of K(Ca)2.1 channels.
|
-
- HY-107547
-
|
|
Guanylate Cyclase
Adenylate Cyclase
|
Metabolic Disease
|
|
BPIPP is a guanylyl cyclase type C (GC-C) and adenylyl cyclase inhibitor that can suppress cyclic nucleotide synthesis. BPIPP inhibits chloride-ion transport stimulated by activation of guanylyl or adenylyl cyclases, and has the potential for diarrhea research .
|
-
- HY-119264
-
|
|
HIF/HIF Prolyl-Hydroxylase
Ras
|
Cancer
|
|
PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma .
|
-
- HY-P6440
-
|
|
Apoptosis
Caspase
|
Others
|
|
Met-12 is a small peptide inhibitor of the Fas receptor. Met-12 can inhibit Fas receptor-mediated photoreceptor cell apoptosis, reduce Caspase activation. Met-12 can be used in the research of photoreceptor .
|
-
- HY-109079A
-
|
DWP14012 hydrochloride; Fexuprazan hydrochloride
|
Proton Pump
|
Metabolic Disease
|
|
Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
|
-
- HY-10219
-
|
Sirolimus; AY-22989
|
mTOR
FKBP
Fungal
Autophagy
Endogenous Metabolite
Antibiotic
Bacterial
|
Cancer
|
|
Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
|
-
- HY-100278
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
AKP-001 is an inhibitor of p38 mitogen-activated protein kinase (p38 MAPK). AKP-001 can inhibit the production of inflammatory cytokines and can be used for research in rheumatoid arthritis and inflammatory bowel disease .
|
-
- HY-145034
-
|
|
Kinesin
|
Cancer
|
|
KIF18A-IN-1 is an inhibitor of the mitotic kinesin KIF18A with anti-tumor activity. KIF18A targeted inhibitors may activate mitotic checkpoints and selectively kill chromosomally unstable cancer cells .
|
-
- HY-127002A
-
|
|
Src
|
Cancer
|
|
Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells .
|
-
- HY-109079
-
|
DWP14012; Fexuprazan
|
Proton Pump
|
Metabolic Disease
|
|
Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
|
-
- HY-119264A
-
|
|
HIF/HIF Prolyl-Hydroxylase
Ras
|
Cancer
|
|
PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma .
|
-
- HY-P3452
-
|
|
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-144366
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel .
|
-
- HY-P2641
-
|
|
MMP
|
Cancer
|
|
Peptide 74 is a synthetic peptide containing the prodomain sequence of matrix metalloproteinase (MMP). Peptide 74 inhibits the activated form of the 72-kDa type IV collagenase in vitro .
|
-
- HY-N0014
-
-
- HY-P3617
-
|
|
GCGR
|
Metabolic Disease
|
|
Glucagon (22-29) is partial agonist of Glucagon (19–29). Glucagon specifically inhibits the Ca 2+ pump in liver plasma membranes independently of adenylate cyclase activation .
|
-
- HY-19634
-
|
|
Sirtuin
|
Cancer
|
|
YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells .
|
-
- HY-114481
-
|
IKE
|
Ferroptosis
|
Cancer
|
|
Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc - and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity .
|
-
- HY-13595
-
|
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-12212
-
|
RTA 408
|
Keap1-Nrf2
STING
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
|
-
- HY-161605
-
-
- HY-N10062
-
|
|
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 RAW264.7 cells.
|
-
- HY-148052
-
|
|
RIP kinase
|
Cancer
|
|
RIPK3-IN-2 is a RIP3 inhibitor. RIPK3-IN-2 can be used in diseases caused by or associate with activated necrotic pathways research .
|
-
- HY-W874892
-
|
CBDP
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Cannabidiphorol (CBDP) is a phytocannabinoid that increases the production of reactive oxygen species (ROS) and activates cellular pathways related to ROS signaling. Cannabidiphorol inhibits cell viability of breast cancer cells .
|
-
- HY-N11768
-
|
|
NF-κB
Interleukin Related
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
4-Methoxylonchocarpin is an orally active anti-inflammatory agent. 4-methoxylonchocarpin inhibits the binding of LPS to Toll-like Receptor (TLR) TLR4 to inhibit NF-κB activation and TNF Receptor and IL-6 expression. 4-Methoxylonchocarpin also inhibits the phosphorylation of TGF-beta activated kinase 1 and TNBS-induced expression of IL-1β, IL-17A, and TNF. 4-methoxylonchocarpin can improve 2,4, 6-trinitrobenzene sulfonic acid (TNBS)-induced colitis mouse model .
|
-
- HY-122542
-
|
|
Thrombin
PAI-1
|
Cardiovascular Disease
|
|
PPACK is potent, selective and irreversible thrombin inhibitor. PPACK can be used an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole-blood electrolyte analyses. PPACK is also a plasminogen activator (rt-PA) inhibitor. PPACK can inhibit the binding of rt-PA to plasma protease inhibitors .
|
-
- HY-122542A
-
|
Pebac; D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone; D-Phe-Pro-Arg-CH2Cl
|
Thrombin
PAI-1
|
Cardiovascular Disease
|
|
PPACK dihydrochloride is potent, selective and irreversible thrombin inhibitor. PPACK dihydrochloride can be used an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole-blood electrolyte analyses. PPACK dihydrochloride is also a plasminogen activator (rt-PA) inhibitor. PPACK dihydrochloride can inhibit the binding of rt-PA to plasma protease inhibitors .
|
-
- HY-N2006
-
|
|
EBV
HIV Protease
|
Infection
Inflammation/Immunology
|
|
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease (IC50: 170 μM) .
|
-
- HY-158104
-
|
|
ATF6
|
Others
|
|
LPPM-8 is a ligand of Med25 and an inhibitor of Med25 protein-protein interactions (PPIs). LPPM-8 engages Med25 through interaction with the H2 face of its Activator Interaction Domain and stabilizes full-length protein in the cellular proteome. LPPM-8 is an orthosteric inhibitor of H2-binding transcriptional activators (such as ATF6a). LPPM-8 can be used for studying Med25 and Mediator complex biology .
|
-
- HY-120265
-
|
|
PI3K
|
Cardiovascular Disease
|
|
MIPS-9922 is a potent and selective PI3Kβ inhibitor with an IC50 of 63 nM. MIPS-9922 inhibits PI3Kβ with >30-fold higher potency than PI3Kδ. MIPS-9922 blocks PI3K mediated activation of platelet glycoprotein αIIbβ3 activation and platelet adhesion in vitro. MIPS-9922 shows anti-platelet and anti-thrombotic activities .
|
-
- HY-161838
-
|
|
ATM/ATR
|
Cancer
|
|
ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.
|
-
- HY-124122
-
|
|
VEGFR
Checkpoint Kinase (Chk)
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases .
|
-
- HY-50662
-
|
|
AMPK
|
Metabolic Disease
|
|
A-769662 is a AMP-activated protein kinase (AMPK) activator. A-769662 inhibits the function of the 26S proteasome by an AMPK-independent mechanism and leads to cell cycle arrest. A-769662 directly stimulates partially purified rat liver AMPK (EC50 = 0.8 μM) and inhibits fatty acid synthesis in primary rat hepatocytes (IC50 = 3.2 μM). A-769662 can alleviate the symptoms of metabolic diseases such as type 2 diabetes .
|
-
- HY-B0151
-
|
3β-Hydroxy-5-pregnen-20-one
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
|
-
- HY-144765
-
|
|
NF-κB
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research .
|
-
- HY-163362
-
|
|
Reverse Transcriptase
PKC
HIV
|
Infection
|
|
HIV-1 inhibitor-65 (compound 3c) is an inhibitor of HIV-1 (EC50: 2.9 nM) and an activator of protein kinase C (PKC). HIV-1 inhibitor-65 inhibits syncytium formation (EC50: 7.0 nM) and inhibits HIV-1 entry and HIV-1 reverse transcriptase .
|
-
- HY-160765
-
|
APS-8-100-2
|
Wnt
Apoptosis
|
Cancer
|
|
WNTinib (APS-8-100-2) is a multi-kinase inhibitor that selectively antagonizes β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC). WNTinib downregulates oncogenicWntsignaling by inhibiting KIT/MAPK and downstream EZH2 activation .
|
-
- HY-50714R
-
|
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
|
Quiflapon (sodium) (Standard) is the analytical standard of Quiflapon (sodium). This product is intended for research and analytical applications. 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-173326
-
|
|
STING
|
Inflammation/Immunology
|
|
STING-IN-14 is an inhibitor of STING (IC50: 0.6 nM). STING-IN-14 inhibits the activation of the IRF pathway in THP1-Dual TM cells. STING-IN-14 can be used in autoimmune diseases research .
|
-
- HY-100164
-
|
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-145849
-
|
|
VEGFR
|
Cancer
|
|
VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition .
|
-
- HY-18982
-
|
Flagecidin; Wuningmeisu C
|
DNA/RNA Synthesis
JNK
Bacterial
Apoptosis
Antibiotic
Parasite
|
Infection
Cancer
|
|
Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system . Anisomycin is a JNK activator, which increases phospho-JNK . Anisomycin is a bacterial antibiotic .
|
-
- HY-138683
-
|
|
STING
|
Inflammation/Immunology
|
|
STING-IN-3 is an inhibitor of stimulator of interferon genes (STING). STING-IN-3 efficiently inhibits both hsSTING and mmSTING through covalently target the predicted transmembrane cysteine residue 91 and thereby block the activation-induced palmitoylation of STING .
|
-
- HY-N0039
-
-
- HY-100016
-
|
|
ATM/ATR
Apoptosis
|
Cancer
|
|
AZD0156 is a potent, selective and orally active ATM inhibitor with an IC50 of 0.58 nM. AZD0156 inhibits the ATM-mediated signaling, prevents DNA damage checkpoint activation, disrupts DNA damage repair, and induces tumor cell apoptosis .
|
-
- HY-N10079
-
|
Jatrophan
|
SHP2
|
Cancer
|
|
Suchilactone (Jatrophan) is a lignan extracted from Monsonia angustifolia E.Mey. Suchilactone binds to SHP2 and inhibits SHP2 activation, thereby inhibiting ERK-mediated cell proliferation. Suchilactone can be ued in acute myeloid leukaemia (AML) .
|
-
- HY-N0883
-
|
Gamabufagin
|
VEGFR
|
Cancer
|
|
Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.
|
-
- HY-12372
-
|
|
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-157518
-
|
|
Bacterial
|
Infection
|
|
OJT008 is an inhibitor of MtMetAP1c. OJT008 inhibits NiCl2- and CoCl2 activated MtMetAP1c with IC50s of 11 and 40 μM, respectively. OJT008 can used to study tuberculosis .
|
-
- HY-10119S
-
|
SCH 530348-d5
|
Protease Activated Receptor (PAR)
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Vorapaxar-d5 is deuterated labeled Vorapaxar (HY-10119). 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-N1990R
-
|
|
Reference Standards
PPAR
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Gypenoside XLIX (Standard) is the analytical standard of Gypenoside XLIX. This product is intended for research and analytical applications. 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-16124
-
|
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-10119R
-
|
SCH 530348 (Standard)
|
Reference Standards
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (Standard) is the analytical standard of Vorapaxar. This product is intended for research and analytical applications. 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-14600
-
|
BRL 49653C
|
PPAR
TRP Channel
Autophagy
Ferroptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
|
-
- HY-W019721R
-
|
|
Reference Standards
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
|
Cyclosporin D (Standard) is the analytical standard of Cyclosporin D. This product is intended for research and analytical applications. 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-B1816
-
|
M&B 22948
|
Phosphodiesterase (PDE)
GPR35
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
|
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects .
|
-
- HY-130723
-
|
|
AMPK
|
Cancer
|
|
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) .
|
-
- HY-130723A
-
|
|
AMPK
|
Cancer
|
|
AMPK activator 2 (compound 7a) hydrochloride, a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 hydrochloride inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549) .
|
-
- HY-W027751R
-
|
|
Drug Intermediate
Reference Standards
|
Others
|
|
Gypenoside XLIX (Standard) is the analytical standard of Gypenoside XLIX. This product is intended for research and analytical applications. 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-103238
-
RSVA405
1 Publications Verification
|
AMPK
STAT
Autophagy
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
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-118828B
-
|
12-OPDA (≥90%)
|
NF-κB
p38 MAPK
|
Neurological Disease
Inflammation/Immunology
|
|
12-Oxo phytodienoic acid (≥90%) (12-OPDA (≥90%)) is a plant lipid-derived anti-inflammatory compound. 12-Oxo phytodienoic acid (≥90%) suppresses neuroinflammation by inhibiting Nf-κB and p38 MAPK signaling in Lipopolysaccharides (LPS) (HY-D1056)-activated cells. 12-Oxo phytodienoic acid (≥90%) can be used for neurodegenerative diseases research .
|
-
- HY-100487
-
|
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-168078
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
PD-1/PD-L1-IN-50 (Compound LG-12) is a PD-1/PD-L1 inhibitor. PD-1/PD-L1-IN-50 increases the secretion of IFN-γ to promote CD8 + T cell activation, and activates the antitumor immunity of T cells .
|
-
- HY-N6051R
-
|
|
Reference Standards
Fungal
NOD-like Receptor (NLR)
NF-κB
|
Infection
Inflammation/Immunology
|
|
(-)-Maackiain (Standard) is the analytical standard of (-)-Maackiain. This product is intended for research and analytical applications. (-)-Maackiain is a pterocarpan phytoalexin produced from Sophora flavescens. (-)-Maackiain is toxic to several genera of fungal pathogens of legume and non legume hosts. (-)-Maackiain enhances the activation of NLRP3 inflammasome, inhibits the activation of NF-κB pathway, exhibiting thereby immunostimulatory and anti-inflammatory activities. (-)-Maackiain is orally active .
|
-
- HY-156120
-
|
|
CD38
|
Metabolic Disease
|
|
CD38 inhibitor 3 (compound 1) is the orally active inhibitor for CD38 (IC50=11 nM). CD38 inhibitor 3 increases intracellular NAD + levels, activates the Nrf2 signaling pathway, and promotes mitochondrial biogenesis. CD38 inhibitor 3 improves muscle function .
|
-
- HY-10255
-
|
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-D2360
-
|
|
HIF/HIF Prolyl-Hydroxylase
HSP
|
Cancer
|
|
O-Carboranylphenoxyacetanilide is a HIF-1α inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC50: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity .
|
-
- HY-N2117R
-
|
|
Reference Standards
MMP
Akt
NF-κB
Proteasome
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Isoginkgetin (Standard) is the analytical standard of Isoginkgetin. This product is intended for research and analytical applications. Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy .
|
-
- HY-17471AR
-
|
1,1-Dimethylbiguanide hydrochloride (Standard)
|
Reference Standards
AMPK
Autophagy
Mitophagy
Apoptosis
mTOR
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Metformin hydrochloride (Standard) is the analytical standard of Metformin (hydrochloride). This product is intended for research and analytical applications. Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo .
|
-
- HY-169973
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
PhoPS is the photocaged inhibitor for β-lactamase. PhoPS is activated upon light irradiation, and active β-lactamase inhibitor Sulbactam (HY-B0334) is released. PhoPS inhibits the synthesis of bacterial cell wall and the formation of E. coli biofilm, exhibits antimicrobial activity .
|
-
- HY-126055A
-
|
|
Adenylate Cyclase
|
Others
|
|
Hadacidin sodium is a competitive inhibitor of adenylate synthase. Hadacidin sodium binds to the active site of adenylate synthase, competitively inhibiting L-aspartate binding. Hadacidin sodium can be used in drug design, to help develop new inhibitors or activators to regulate adenylate synthase activity, and to play a role in the study of related diseases .
|
-
- HY-126055
-
|
|
Adenylate Cyclase
|
Others
|
|
Hadacidin is a competitive inhibitor of adenylate synthase. Hadacidin binds to the active site of adenylate synthase, competitively inhibiting L-aspartate binding. Hadacidin can be used in drug design, to help develop new inhibitors or activators to regulate adenylate synthase activity, and to play a role in the study of related diseases .
|
-
- HY-N0112
-
|
Ampelopsin; Ampeloptin
|
mTOR
Influenza Virus
DNA/RNA Synthesis
Autophagy
|
Infection
Cancer
|
|
Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
|
-
- HY-144812
-
|
|
Cathepsin
|
Inflammation/Immunology
Cancer
|
|
Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen .
|
-
- HY-157147
-
-
- HY-135715
-
|
|
PAI-1
|
Others
|
|
(E)-UK122 TFA is the isomer of UK122 TFA. UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM .
|
-
- HY-101860
-
-
- HY-P2228
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. Chlamydocin exhibits potent antiproliferative and anticancer activities. Chlamydocin induces apoptosis by activating caspase-3 .
|
-
- HY-139701
-
|
|
HDAC
|
Cancer
|
|
NI-Pano (CH-03) is a novel hypoxia-activated KDAC inhibitor. NI-Pano (CH-03) is reduced in an O2-dependent manner to release panobinostat.
|
-
- HY-P1430
-
-
- HY-N12941
-
-
- HY-B1104
-
|
(±)-Indoprofe
|
Akt
AMPK
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
|
Indoprofen ((±)-Indoprofe) activates AKT-AMPK signaling pathway, inhibits NF-κB/MAPK signaling pathway. Indoprofen exhibits anti-inflammatory and immunomodulatory activities. Indoprofen is orally active .
|
-
- HY-12074
-
|
|
GSK-3
|
Metabolic Disease
|
|
Cazpaullone is a glycogen synthase kinase-3 (GSK-3) inhibitor. Cazpaullone can activate pancreatic beta cell protection and replication. Cazpaullone can be used for the research of diabetes .
|
-
- HY-156194
-
|
|
FLAP
|
Cardiovascular Disease
|
|
FLAP-IN-1 (Intermediate 14) is a 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 654 nM. FLAP-IN-1 can be used in cardiovascular disease research .
|
-
- HY-W001174
-
|
|
ERK
NF-κB
|
Inflammation/Immunology
|
|
2,5-Dihydroxyacetophenone, isolated from Rehmannia glutinosa, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways .
|
-
- HY-N10865
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
Chloranthalactone E (compound 6), a labdane diterpene, can be isolated from the aerial parts of Chloranthus serratus. Chloranthalactone E inhibits NO production in LPS-activated RAW 264.7 macrophages .
|
-
- HY-N0385
-
|
|
NO Synthase
AMPK
CaMK
NF-κB
Keap1-Nrf2
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Gomisin J is a Schisandra chinensis-derived lignan that can inhibit multiple targets such as eNOS, AMPK (LKB1, CaMKIIβ), fetuin-A, NF-κB, Nrf2/HO-1, and can pass through the blood-brain barrier. Gomisin J increases NO bioavailability by activating eNOS, regulates lipid metabolism by activating the AMPK pathway, inhibits fetuin-A and NF-κB to exert anti-inflammatory effects, and activates Nrf2/HO-1 to enhance antioxidant capacity. Gomisin J has the activities of anti-hypertension, regulating liver lipid metabolism, and reducing cerebral ischemia-reperfusion injury, and can be used for research on hypertension, non-alcoholic fatty liver disease, cerebral ischemia-reperfusion injury, etc .
|
-
- HY-135388
-
|
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-N10358
-
|
|
NF-κB
|
Others
|
|
3-(2-Hydroxyethyl) thio withaferin A is a Withaferin A derivative. Withaferin A, a steroidal lactone, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding .
|
-
- HY-122881A
-
|
(E/Z)-JTP-0819958
|
IKK
|
Cancer
|
|
(E/Z)-HOIPIN-1 ((E/Z)-JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 value >2.8 μM. HOIPIN-1 inhibits LUBAC-mediated NF-kB activation.
|
-
- HY-137992
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Aucuparin, a natural product found in Sorbus aucuparia, inhibits pulmonary fibrosis in a bleomycin (HY-108345)-induced lung fibrosis mouse model. Aucuparin has anti-inflammatory activity and can inhibit the activation of inflammatory factors by TGF-β .
|
-
- HY-151970
-
|
|
STING
|
Inflammation/Immunology
|
|
STING-IN-4 (Compound 1) is a STING inhibitor that inhibits STING expression and hence reducing activation of STING and nuclear factor-κB (NF-κB) signaling. STING-IN-4 shows anti-inflammatory activity and can be used for the research of sepsis .
|
-
- HY-19706
-
ARS-853
4 Publications Verification
|
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
-
|
|
Keap1-Nrf2
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator .
|
-
- HY-10508
-
|
|
MEK
|
Cancer
|
|
(R)-PD 0325901CL is an isomer of PD 0325901CL. PD 0325901CL is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) involved in cancer research. PD 0325901CL inhibits the growth of cancer cells in vitro and in vivo .
|
-
- HY-122052
-
|
|
Thrombin
|
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-10255AS
-
|
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 . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-B0167A
-
-
- HY-149710
-
|
|
ICMT
ERK
|
Cancer
|
|
POP-3MB (compound 1b) is an ICMT inhibitor (IC50: 2.5 μM). POP-3MB changes the subcellular localization of K-Ras and inhibits Ras activation. POP-3MB also inhibits Erk phosphorylation .
|
-
- HY-W013375
-
|
|
Neprilysin
|
Neurological Disease
|
|
Thiorphan is a selective neprilysin (NEP) inhibitor with an IC50 of 6.9 nM. Thiorphan competitively binds to NEP and blocks its activity, preventing the degradation of neuropeptides such as substance P (SP) and neurokinin NKA. In the field of neonatal brain injury research, Thiorphan can increase the levels of SP and NKA, activate NK1 and NK2 receptors and downstream transduction pathways, and inhibit excessive activation of NMDA receptors. Thus, Thiorphan can protect neocortical neurons from excitotoxic cell death. Thiorphan may also inhibit NEP from enhancing bronchoconstriction and can be used in the study of respiratory diseases .
|
-
- HY-134205A
-
|
|
Keap1-Nrf2
|
Neurological Disease
Metabolic 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-10119AR
-
|
SCH 530348 sulfate (Standard)
|
Reference Standards
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Vorapaxar (sulfate) (Standard) is the analytical standard of Vorapaxar (sulfate). This product is intended for research and analytical applications. 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-170930
-
|
|
GABA Receptor
Sodium Channel
|
Neurological Disease
|
|
Anticonvulsant agent 9 (compound 4f) is an α1β2γ2 GABAA receptors activator. Anticonvulsant agent 9 activatesα1β2γ2 GABAA receptors with an EC50 of 1.24 μM. Anticonvulsant agent 9 inhibits the inactivation of Nav1.2 channels. Anticonvulsant agent 9 exhibits significant anticonvulsant activities .
|
-
- HY-N6641R
-
|
|
Reference Standards
Keap1-Nrf2
PPAR
|
Inflammation/Immunology
Cancer
|
|
Monascin (Standard) is the analytical standard of Monascin. This product is intended for research and analytical applications. Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor). Monascin is a Nrf2 activator and PPARγ agonist .
|
-
- HY-Y0152R
-
|
(8R,9S)-Cinchonine (Standard); LA40221 (Standard)
|
Reference Standards
Apoptosis
Parasite
Autophagy
Caspase
Calcium Channel
|
Others
Inflammation/Immunology
Cancer
|
|
Cinchonine (Standard) is the analytical standard of Cinchonine. This product is intended for research and analytical applications. Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells .
|
-
- HY-P3412
-
|
|
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-150587
-
|
|
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-W017158R
-
|
|
Reference Standards
Endogenous Metabolite
|
Metabolic Disease
|
|
Vorapaxar (sulfate) (Standard) is the analytical standard of Vorapaxar (sulfate). This product is intended for research and analytical applications. 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-101047S1
-
|
Erythrosphingosine-13C2,d2; erythro-C18-Sphingosine-13C2,d2; trans-4-Sphingenine-13C2,d2
|
Isotope-Labeled Compounds
PKC
Endogenous Metabolite
Phosphatase
|
Cancer
|
|
D-erythro-Sphingosine-13C2,d2 is a deuterated 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 .
|
-
- HY-113224R
-
|
|
Reference Standards
Endogenous Metabolite
LXR
Fatty Acid Synthase (FASN)
Interleukin Related
Reactive Oxygen Species (ROS)
NOD-like Receptor (NLR)
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Desmosterol (Standard) is the analytical standard of Desmosterol. This product is intended for research and analytical applications. Desmosterol is a cholesterol-like molecule. In the Bloch pathway of cholesterol biosynthesis, Desmosterol is a direct precursor of cholesterol. As an endogenous metabolite, Desmosterol is used to study cholesterol metabolism [1]. Desmosterol is an LXR activator and SREBP inhibitor, which can suppress macrophage inflammasome activation and prevent vascular inflammation and atherosclerosis. A reduction in Desmosterol promotes the production of mitochondrial reactive oxygen species (ROS) in macrophages and pyrin domain-dependent inflammasome activation of NLRP3. Desmosterol holds potential for research in inflammation, metabolism, and cardiovascular diseases [1][2][3].
|
-
- HY-13757A
-
|
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Endocrinology
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 transgenic mouse .
|
-
- HY-126361A
-
|
|
Ser/Thr Protease
PAI-1
|
Inflammation/Immunology
|
|
ZK824190 hydrochloride is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively .
|
-
- HY-14256
-
-
- HY-111789A
-
|
(S)-TAK-981
|
Drug Isomer
|
Inflammation/Immunology
Cancer
|
|
(S)-Subasumstat is the isomer of Subasumstat (HY-111789). Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities .
|
-
- HY-17376S
-
-
- HY-112473
-
|
|
Ras
|
Cancer
|
|
NAV-2729 is a dual Arf1/Arf6 activation inhibitor. ADP ribosylation factors (Arfs) are members of the Arf family of GTP-binding proteins of the Ras superfamily.
|
-
- HY-114330A
-
|
|
PAI-1
Ser/Thr Protease
|
Inflammation/Immunology
|
|
ZK824859 hydrochloride is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively .
|
-
- HY-N11548
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
Inflexuside A, an abietane diterpenoid, can be isolated from the aerial parts of Isodon inflexus. Inflexuside B strongly inhibits lipopolysaccharide (LPS)-activated NO production (NO Synthase) in RAW264.7 macrophages .
|
-
- HY-146334
-
|
|
Chloride Channel
|
Inflammation/Immunology
|
|
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain .
|
-
- HY-75247
-
-
- HY-12357S2
-
|
ETC-1002-d4; ESP-55016-d4
|
ATP Citrate Lyase
AMPK
|
Others
|
|
Bempedoic acid-d4 is the deuterium labeled Bempedoic acid. Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor. Bempedoic acid (ETC-1002) activates AMPK .
|
-
- HY-13324
-
|
RTA 402; NSC 713200; CDDO Methyl ester
|
Keap1-Nrf2
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.
|
-
- HY-126361
-
|
|
Ser/Thr Protease
PAI-1
|
Inflammation/Immunology
|
|
ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively .
|
-
- HY-147287
-
|
|
PSMA
|
Cancer
|
|
Glu-urea-Glu-NHS ester (compound 21) is an activated N-hydroxysuccinamide (NHS) ester of Glu-urea-Glu which can be used as a pharmacophore for linking with prostate specific membrane antigen (PSMA) inhibitors .
|
-
- HY-123963
-
|
|
STING
|
Inflammation/Immunology
|
|
C-178 is a potent and selective covalent inhibitor of STING. C-178 binds to Cys91 and suppresses the STING responses elicited by distinct bona fide activators in mouse but not human .
|
-
- HY-32735
-
|
PG490
|
NF-κB
Apoptosis
|
Cancer
|
|
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor .
|
-
- HY-114330
-
|
|
PAI-1
Ser/Thr Protease
|
Inflammation/Immunology
|
|
ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79 nM, 1580 nM and 1330 nM for human uPA, tPA, and plasmin, respectively .
|
-
- HY-P10878
-
|
|
PAI-1
|
Cancer
|
|
UK140 is the inhibitor for urokinase-type plasminogen activator (uPA) with Ki of 0.20 µM and 2.79 µM for huPA anf muPA. UK140 can be used in metastasis-related research .
|
-
- HY-B0649S
-
|
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Propofol-d17 is the deuterium labeled Propofol. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties .
|
-
- HY-148973
-
|
|
ATP Synthase
|
Metabolic Disease
|
|
ZW290 is a compound to activate brown adipose tissue (BAT) thermogenic function. ZW290 increases the expression of uncoupling Protein 1 (UCP1) protein and inhibits ATP synthesis in BAT .
|
-
- HY-N11544
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
Inflexuside B, an abietane diterpenoid, can be isolated from the aerial parts of Isodon inflexus. Inflexuside B strongly inhibits lipopolysaccharide (LPS)-activated NO Synthase in RAW264.7 macrophages .
|
-
- HY-126046
-
|
|
ClpP
Bacterial
|
Infection
|
|
ACP1b is an activator for ClpP protease with Kd of 3.2 μM, and exhibits antibacterial activity. ACP1b inhibits N. meningitidis and H. influenzae with MBC of 16 and 8 μg/mL .
|
-
- HY-N0897R
-
|
Corylifol-A (Standard); Corylinin (Standard)
|
UGT
Reference Standards
STAT
|
Others
|
|
Corylifol A (Standard) is the analytical standard of Corylifol A. This product is intended for research and analytical applications. Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
|
-
- HY-U00441
-
DPBQ
1 Publications Verification
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells .
|
-
- HY-N4053
-
-
- HY-16031B
-
|
NSC710464 dihydrochloride
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
AFP464 (dihydrochloride) (NSC710464 (dihydrochloride)) is the hydrochloride form of AFP464 and is a potent HIF-1α inhibitor with an IC50 value of 0.25 μM. It is also an activator of aryl hydrocarbon receptor (AhR).
|
-
- HY-50733A
-
|
|
Casein Kinase
Ras
Apoptosis
|
Cancer
|
|
CX-5011 is a CK2 inhibitor. CX-5011 also induces Rac1 activation. CX-5011 induces apoptosis and induces cancer cell death .
|
-
- HY-155954
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
UCM-1336 is a potent ICMT inhibitor, with an IC50 of 2 μM. UCM-1336 induces mislocalization of endogenous Ras, decreases Ras activation and induces cell death by autophagy and apoptosis .
|
-
- HY-162081
-
|
|
Btk
|
Cancer
|
|
BTK-IN-32 (compound C2) is a potent inhibitor of BTK. BTK-IN-32 activates full-length BTK and smaller multidomain BTK fragments instead of the isolated kinase domain .
|
-
- HY-P1288
-
|
PKC fragment (530-558)
|
PKC
|
Others
|
|
Protein Kinase C (530-558), a peptide fragment of protein kinase C (PKC), is a potent PKC activator. Protein Kinase C (530-558) significantly inhibits osteoclastic bone resorption .
|
-
- HY-161100
-
|
|
Apoptosis
|
Cancer
|
|
BDM19 binds and activates cytosolic BAX dimers, and prompts cell apoptosis either alone or in combination with BCL-2/BCL-XL inhibitor Navitoclax (HY-10087) .
|
-
- HY-123632
-
|
|
Cytochrome P450
|
Others
|
|
(3S,5S)-Atorvastatin sodium salt is a pregnane X receptor (PXR) activator and the inactive enantiomer of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor with lipid-lowering capabilities .
|
-
- HY-164364A
-
|
|
FAP
|
Cancer
|
|
DOTAGA.(SA.FAPi)2 TFA is a potent dimeric fibroblast-activation protein inhibitor (FAPi). DOTAGA.(SA.FAPi)2 TFA has the potential for cancer diagnosis research .
|
-
- HY-N0103A
-
|
|
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MEK
ERK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Sophocarpine monohydrate is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine monohydrate upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine monohydrate inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine monohydrate can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine monohydrate has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage .
|
-
- HY-N0103
-
|
|
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MEK
ERK
PTEN
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage .
|
-
- HY-B0130
-
-
- HY-150073
-
|
|
PKA
|
Cancer
|
|
DS01080522 is a Protein Kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor. DS01080522 inhibits PRKACA kinase activity and CREB phosphorylation with IC50s of 0.8 nM and 66 nM, respectively. DS01080522 can be used for the research of cancer .
|
-
- HY-B0130A
-
|
Perindopril tert-butylamine salt; S-9490 erbumine
|
Sirtuin
NF-κB
STAT
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure .
|
-
- HY-14530
-
|
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-12364B
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
( )-C75 is a isoform of C75 (HY-12364), which 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-17376S1
-
|
SCH 58235-d4-1
|
Keap1-Nrf2
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Ezetimibe-d4-1 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
|
-
- HY-103666
-
|
|
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-111249
-
|
|
FLT3
|
Cancer
|
|
TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research .
|
-
- HY-137561
-
|
PLN-74809
|
Integrin
|
Inflammation/Immunology
|
|
Bexotegrast (PLN-74809) is an orally active, potent dual αvβ6/αvβ1 integrin inhibitor with Kd of 5.7 nM and 3.4 nM, respectively. Bexotegrast inhibits αvβ6- and αvβ1-induced TGF-β activation with IC50 values of 29.8 nM and 19.2 nM, respectively. Bexotegrast has antifibrogenic effects and block multiple avenues of TGF-β activation in the fibrotic lung .
|
-
- HY-14759
-
|
PAZ-417
|
PAI-1
Amyloid-β
|
Neurological Disease
|
|
Aleplastinin (PAZ-417) is an orally active, blood-brain barrier permeable, selective SERPINE1 (PAI-1) inhibitor (IC50=655 nM). Aleplastinin activates the tissue type plasminogen activator (tPA)/fibrinolysis cascade by inhibiting PAI-1, thereby promoting the degradation of amyloid-β (Aβ) oligomers and monomers. Aleplastinin can significantly reduce plasma and brain Aβ levels, improve memory impairment, and reverse cognitive impairment. Aleplastinin can be used for research on Alzheimer's disease .
|
-
- HY-121787
-
|
OLC20
|
Olfactory Receptor
|
Others
|
|
OX1a (OLC20) is an Orco antagonist with non-competitive activity that inhibits the activation of oxygen odor receptors (ORs). OX1a is able to reduce the activation of ORs by competitively inhibiting the effects of Orco agonists. OX1a also shows non-competitive inhibition of odor molecules, which may affect the olfactory-mediated behavior of insects. Through structural optimization, OX1a analogs have shown higher antagonistic potency, indicating that this type of compound may have application potential in a wide range of insect species .
|
-
- HY-19486
-
|
|
Nuclear Factor of activated T Cells (NFAT)
CD3
CD28
Interleukin Related
|
Inflammation/Immunology
|
UR-1505 is a nuclear factor of activated T cells (NF-AT) inhibitor. UR-1505 can suppress CD3/CD28 induced T cell proliferation, increase p27 KIP levels, and induce G1/S cell cycle arrest. UR-1505 can also inhibit the production of IL-5 and IFN-γ in activated T cells. UR-1505 has immunomodulatory properties and can be used in the study of atopic dermatitis .
|
-
- HY-113205
-
|
15-keto-PGE2
|
Endogenous Metabolite
Prostaglandin Receptor
STAT
PPAR
|
Cancer
|
|
15-keto-Prostaglandin E2 is an endogenous metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to its Cys259 residue. 15-keto-Prostaglandin E2 can bind and stabilize EP2 and EP4 receptor. 15-keto-Prostaglandin E2 inhibits breast cancer cell growth and progression. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth .
|
-
- HY-122700
-
|
|
Complement System
|
Inflammation/Immunology
|
|
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases .
|
-
- HY-100431
-
IMR-1
5 Publications Verification
|
Notch
|
Cancer
|
|
IMR-1 is a novel class of Notch inhibitor targeting the transcriptional activation with an IC50 of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth .
|
-
- HY-P2413
-
|
|
Androgen Receptor
Src
|
Others
|
|
Ac-PPPHPHARIK-NH2 (compound S1) is a compound that inhibits the interaction between androgen receptor and Src. It can inhibit the binding of androgen or estrogen-induced receptor and Src in cancer cells, as well as the activation of related signaling pathways, and can also inhibit cell cycle progression and tumor growth.
|
-
- HY-122542B
-
|
|
Thrombin
PAI-1
|
Cardiovascular Disease
|
|
PPACK TFA is potent, selective and irreversible thrombin inhibitor. PPACK TFA can be used an alternative anticoagulant to lithium heparin (LiHep) for blood gas and whole-blood electrolyte analyses. PPACK TFA is also a plasminogen activator (rt-PA) inhibitor. PPACK TFA can inhibit the binding of rt-PA to plasma protease inhibitors .
|
-
- HY-10255AS1
-
|
|
Isotope-Labeled Compounds
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 . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-N6031
-
-
- HY-158326
-
|
|
FAP
|
Cancer
|
|
FAP-IN-4 (Comp 10) is a fibroblast activation protein (FAP) inhibitor and a 18F-labeled PET tracer targeting FAP. FAP-IN-4 can be used for cancer research .
|
-
- HY-N0516R
-
|
Vitexicarpin (Standard)
|
Reference Standards
STAT
|
Inflammation/Immunology
|
|
Casticin (Standard) is the analytical standard of Casticin. This product is intended for research and analytical applications. Casticin is a methyoxylated flavonol isolated from Vitex rotundifolia, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
|
-
- HY-P2012
-
|
|
Caspase
Bcl-2 Family
|
Others
|
|
TRP-601 is a caspase inhibitor. TRP-601 reversed the increased expression of active caspase-2, the activation of endogenous apoptotic pathway and the up-regulation of key protein triggered by hyperoxia .
|
-
- HY-117393
-
|
|
PKC
|
Cancer
|
|
Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases .
|
-
- HY-N1380S
-
-
- HY-78131BS
-
|
(R)-Ibuprofen-d3
|
NF-κB
|
Inflammation/Immunology
Cancer
|
|
(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
|
-
- HY-N0139
-
-
- HY-162669
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Mu opioid receptor antagonist 8 (368) is a μ-opioid receptor antagonist. Mu opioid receptor antagonist 8 (368) significantly inhibits met-enkephalin-induced µOR activation of Gi .
|
-
- HY-N6261
-
|
|
Others
|
Inflammation/Immunology
|
|
Epimagnolin B is a bisepoxylignan isolated from Magnolia fargesii, with anti-inflammatory activity and antiallergic effects. Epimagnolin B inhibits NO production in LPS-activated microglia. Epimagnolin B exhibited antiallergic effects .
|
-
- HY-69359
-
|
(±)-β-Homoproline; Hexahydronicotinic acid; 3-Carboxypiperidine
|
GABA Receptor
|
Neurological Disease
|
|
Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM .
|
-
- HY-16031
-
|
NSC710464 free base
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
|
-
- HY-135145
-
|
CB-103
|
Notch
|
Cancer
|
|
Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity .
|
-
- HY-N1380S1
-
-
- HY-18937
-
|
|
RIP kinase
|
Cancer
|
|
WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation .
|
-
- HY-P1430A
-
-
- HY-N10083
-
|
|
Reactive Oxygen Species (ROS)
Sirtuin
|
Cancer
|
|
Selaginellin is an inhibitor of Reactive Oxygen Species and an activator of SIRT1. Selaginellin protects endothelial cells against homocysteine-induced senescence by inhibitng reactive oxygen species and upregulating SIRT1 gene expression .
|
-
- HY-N8129
-
|
|
Others
|
Others
|
|
Rhaponticin 6′′-O-gallate is a stilbene glucoside gallate that can be found in rhizome of Rheum undulatum L. Rhaponticin 6′′-O-gallate inhibits nitric oxide production in lipopolysaccharide-activated macrophages .
|
-
- HY-W015300
-
|
Octanedioic acid
|
Endogenous Metabolite
Akt
TGF-β Receptor
p38 MAPK
|
Metabolic Disease
|
|
Suberic acid (Octanedioic acid) is an orally active crystalline dibasic acid. Suberic acid activates the Akt signaling pathway and regulates the expression of molecules related to the TGF-β and MAPK signaling pathways. Suberic acid inhibits skin dryness .
|
-
- HY-158201
-
-
- HY-12357S
-
|
ETC-1002-d5; ESP-55016-d5
|
ATP Citrate Lyase
AMPK
|
Metabolic Disease
|
|
Bempedoic acid-d5 is the deuterium labeled Bempedoic acid . Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor . Bempedoic acid (ETC-1002) activates AMPK .
|
-
- HY-N1380S3
-
-
- HY-18711A
-
|
Metatinib anhydrous; c-Met inhibitor 2
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
SCR-1481B1 (Metatinib anhydrous) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.
|
-
- HY-13735E
-
|
Mepacrine methanesulfonate; SN-390 methanesulfonate
|
Parasite
Apoptosis
Autophagy
Mitophagy
|
Infection
Cancer
|
|
Quinacrine (Mepacrine) methanesulfonate is a potent, orally active antimalarial agent with antitumor effects in vitro and in vivo. Quinacrine dihydrochloride inhibits NF-κB and activates p53 signaling, inducing apoptosis in tumor cells .
|
-
- HY-78869
-
|
Osimertinib analog
|
EGFR
|
Cancer
|
|
Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
|
-
- HY-159885
-
|
|
Apoptosis
|
Cancer
|
|
MG-B-28 is an inhibitor of BTLA-HVEM with an IC50 value of 906 nM. MG-B-28 promotes T-cell activation in a dose-dependent manner by blocking the BTLA-HVEM interaction .
|
-
- HY-13694S
-
-
- HY-112125
-
-
- HY-126420
-
-
- HY-162348
-
|
|
Necroptosis
|
Cancer
|
|
Antitumor agent-145 (Compound Ir5) is a tumor inhibitor with remarkable fluorescence and mitochondrial targeting, which exerts anti-cancer effects by inducing necroptosis and activating the necroptosis-related immune response .
|
-
- HY-135898
-
|
|
DGK
|
Inflammation/Immunology
Cancer
|
|
DGK-IN-1 is a DGK inhibitor (DGKa/DGKz IC50: 0.65/0.25 μM). DGK-IN-1 is a T cell activator that can be used in cancer and viral infection research .
|
-
- HY-13694S1
-
|
MRX-1024-d4; D-Methionine-d4
|
GABA Receptor
Endogenous Metabolite
|
Cancer
|
|
Methionine-d4 is the deuterium labeled Methionine. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
|
-
- HY-137552
-
|
MASTL Kinase Inhibitor-1
|
MASTL
|
Cancer
|
|
MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer .
|
-
- HY-13417R
-
|
Acadesine (Standard); AICA Riboside (Standard)
|
Reference Standards
AMPK
Autophagy
YAP
Mitophagy
Endogenous Metabolite
|
Cancer
|
|
AICAR (Standard) is the analytical standard of AICAR. This product is intended for research and analytical applications. AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor .
|
-
- HY-13417AR
-
|
|
AMPK
Autophagy
YAP
Mitophagy
Endogenous Metabolite
|
Cancer
|
|
AICAR (phosphate) (Standard) is the analytical standard of AICAR (phosphate). This product is intended for research and analytical applications. AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor .
|
-
- HY-163358
-
-
- HY-139576A
-
|
DUR-928 sodium
|
LXR
Endogenous Metabolite
|
Metabolic Disease
|
|
Larsucosterol (DUR-928) sodium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol sodium as a potent endogenous regulator decreases lipogenesis. Larsucosterol sodium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1 .
|
-
- HY-162607
-
|
|
STAT
|
Inflammation/Immunology
|
|
STAT3-IN-28 (compound 18) is a STAT3 inhibitor. STAT3-IN-28 can inhibit the activation of microglia and has anti-neuroinflammatory effects. STAT3-IN-28 can cross the blood-brain barrier .
|
-
- HY-139667
-
|
|
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-12995
-
|
|
FLAP
|
Cardiovascular Disease
Inflammation/Immunology
|
|
BI 665915 is an orally active and potent 5-lipoxygenase-activating protein (FLAP) inhibitor. BI 665915 inhibits FLAP production that blocks LTB4 biosynthesis in mice. BI 665915 is promising for research of various inflammatory diseases, including respiratory and cardiovascular diseases .
|
-
- HY-10219S
-
|
Sirolimus-d3; AY-22989-d3
|
Isotope-Labeled Compounds
mTOR
FKBP
Autophagy
|
Cancer
|
|
Rapamycin-d3 is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .
|
-
- HY-158093
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NIC-12 is a potent NLRP3 inhibitor. NIC-12 selectively reduces circulating IL-1ß levels in the LPS-endotoxemia mice model. NIC-12 inhibits NLRP3 inflammasome activation in mouse macrophages .
|
-
- HY-N10754
-
|
|
mTOR
Cytochrome P450
|
Infection
Cardiovascular Disease
Cancer
|
|
Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca 2+-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme .
|
-
- HY-10999S
-
|
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib-d4 is the deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
|
-
- HY-150761
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity .
|
-
- HY-133114
-
|
EZM-K
|
Keap1-Nrf2
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor .
|
-
- HY-139576
-
|
DUR-928
|
LXR
Endogenous Metabolite
|
Metabolic Disease
|
|
Larsucosterol (DUR-928), a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol as a potent endogenous regulator decreases lipogenesis. Larsucosterol inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1 .
|
-
- HY-P3785
-
|
|
PKA
|
Neurological Disease
|
|
PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors .
|
-
- HY-N6033
-
|
(+)-Ferruginol
|
EBV
HSV
Apoptosis
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Ferruginol ((+)-Ferruginol), a natural diterpenoid, is an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). Ferruginol inhibits the growth of thyroid cancer cells through the induction of mitochondrial apoptosis. Ferruginol has antitumor, cardioprotective, antioxidant, gastroprotective, and neuroprotective activities .
|
-
- HY-N10312
-
-
- HY-N3255
-
|
|
CXCR
STAT
|
Inflammation/Immunology
Cancer
|
|
Minecoside is a CXCR4/STAT3 inhibitor with anticancer and anti-inflammatory activity. Minecoside decreases CXCR4 expression and suppresses STAT3 activation, thus to inhibit CXCL 12-induced invasion. Minecoside potently inhibits cancer metastasis and promotes apoptotic progression .
|
-
- HY-111549
-
|
|
Arf Family GTPase
|
Cancer
|
|
Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity .
|
-
- HY-170453
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .
|
-
- HY-108900
-
|
|
Aminoacyl-tRNA Synthetase
Bacterial
|
Infection
Cancer
|
|
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria .
|
-
- HY-137638
-
|
|
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-117958
-
HJC0197
1 Publications Verification
|
Ras
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
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-100939
-
|
|
Sodium Channel
|
Neurological Disease
|
|
4-Chlorophenylguanidine hydrochloride is an urokinase-type plasminogen activator inhibitor. 4-Chlorophenylguanidine hydrochloride is a potent ASIC3 positive allosteric modulator and reverses the effects of ASIC3 desensitization. 4-Chlorophenylguanidine hydrochloride influences ASIC3 activity through directly activating the channel and increasing proton sensitivity. 4-Chlorophenylguanidine hydrochloride offers a chemical backbone for the design of new ASIC3 ligands to study ASIC3 in vivo .
|
-
- HY-P1823
-
|
|
Akt
mTOR
Caspase
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
C-Reactive Protein (CRP) is an anti-pneumococcal plasma protein that can serve as an inflammatory marker. C-Reactive protein can protect mice from pneumococcal infection by activating complement. C-Reactive protein can inhibit the activation of caspase-3/9 through the CD64/AKT/mTOR pathway, thereby promoting chemotherapy resistance in mice with tongue squamous cell carcinoma .
|
-
- HY-148368
-
|
|
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
-
|
|
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-50694R
-
|
|
Potassium Channel
|
Others
|
|
Senicapoc (Standard) is the analytical standard of Senicapoc. This product is intended for research and analytical applications. Senicapoc (ICA-17043) is a potent and selective Gardos channel (Ca2+-activated K+ channel; KCa3.1) blocker with an IC50 of 11 nM. Senicapoc blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 nM and inhibits RBC dehydration with IC50 of 30 nM .
|
-
- HY-121693
-
|
MDL101114ZA free base
|
VDAC
RAD51
|
Cancer
|
|
DIDS is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research .
|
-
- HY-108635R
-
|
|
p38 MAPK
MEK
ERK
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
|
|
C16-PAF (Standard) is the analytical standard of C16-PAF. This product is intended for research and analytical applications. C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability .
|
-
- HY-138844
-
|
|
Eukaryotic Initiation Factor (eIF)
p38 MAPK
JNK
Apoptosis
|
Cancer
|
|
3-AP-Me is a dimethyl derivative of the nucleotide reductase inhibitor 3-AP (SML0568). 3-AP-Me can activate the endoplasmic reticulum (ER) stress pathway by promoting the phosphorylation of eIF2α and increasing the gene expression of transcription factors ATF4 and ATF6, leading to cell apoptosis. Additionally, 3-AP-Me can activate the stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinases. 3-AP-Me also leads to the upregulation of the spliced mRNA variant XBP1, can be used in cancer research .
|
-
- HY-19151
-
|
IS-741
|
Integrin
Phospholipase
|
Inflammation/Immunology
|
|
Fuzapladib (IS-741), an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
|
-
- HY-115537
-
|
|
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-110315
-
|
|
Apoptosis
MDM-2/p53
Epigenetic Reader Domain
|
Cardiovascular Disease
|
|
Ischemin sodium is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin sodium salt inhibits p53-induced p21 activation with an IC50 value of 5 µM. Ischemin sodium salt also prevents apoptosis in ischemic cardiomyocytes. Ischemin sodium salt can be used in the study of cardiovascular diseases (such as myocardial ischemia) .
|
-
- HY-19151A
-
|
IS-741 sodium
|
Integrin
Phospholipase
|
Inflammation/Immunology
|
|
Fuzapladib (IS-741) sodium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib sodium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib sodium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
|
-
- HY-125669
-
|
|
Farnesyl Transferase
|
Cancer
|
|
XR 3054 is an inhibitor for Farnesyl Transferase, that inhibits farnesylation of CAAX recognition peptide with IC50 of 50 μM. XR 3054 suppresses the farnesylation of p21 ras and activation of MAP kinase. XR 3054 inhibits the proliferation of prostate cancer cell and colon cancer cell, with IC50 of 8.8-21.4 μM .
|
-
- HY-163176
-
|
|
STAT
|
Inflammation/Immunology
|
|
WB518 is a potent STAT3 inhibitor. WB518 effectively inhibits STAT3 activation and Keratin 17 expression. WB518 effectively alleviates imiquimod (HY-B0180) and TPA (HY-18739)-induced animal psoriasis by inhibiting STAT3 phosphorylation and Keratin 17 .
|
-
- HY-19151B
-
|
IS-741 potassium
|
Integrin
Phospholipase
|
Inflammation/Immunology
|
|
Fuzapladib (IS-741) potassium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib potassium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib potassium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
|
-
- HY-W015445
-
|
|
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-100415
-
|
WX-UK1; UKI-1C
|
PAI-1
Ser/Thr Protease
|
Cancer
|
|
UKI-1 (WX-UK1) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells .
|
-
- HY-19151C
-
|
IS-741 calcium
|
Integrin
Phospholipase
|
Inflammation/Immunology
|
|
Fuzapladib calcium, an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib calcium is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib calcium exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site .
|
-
- HY-17537
-
|
|
IRE1
|
Cancer
|
|
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .
|
-
- HY-N0592A
-
|
|
NF-κB
AMPK
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Demethyleneberberine chloride is a natural mitochondria-targeted antioxidant. Demethyleneberberine chloride alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine chloride could serve as a AMPK activator for researching non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-155785
-
|
|
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
JAK
|
Cancer
|
|
MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma .
|
-
- HY-N0177
-
|
|
STAT
MicroRNA
|
Metabolic Disease
|
|
Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway . Diosgenin is an exogenous activator of Pdia3/ERp57 . Diosgenin inhibits aortic atherosclerosis progression by suppressing macrophage miR-19b expression .
|
-
- HY-N2065R
-
|
|
Reference Standards
NF-κB
Ferroptosis
|
Inflammation/Immunology
Cancer
|
|
Withaferin A (Standard) is the analytical standard of Withaferin A. This product is intended for research and analytical applications. Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-145358
-
|
|
PI3K
|
Cancer
|
|
FAP-PI3KI1 is a fibroblast-activated protein (FAP)-targeted PI3K inhibitor that selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells and effectively inhibits collagen synthesis and reduces collagen deposition .
|
-
- HY-169566
-
|
|
EGFR
AMPK
|
Metabolic Disease
|
|
EGFR-IN-146 is an EGFR inhibitor that can inhibit the EGFR signaling pathway and improve insulin sensitivity by activating the AMPK pathway, which can effectively reduce blood sugar levels and body weight. EGFR-IN-146 has great potential in the study of diabetes and obesity .
|
-
- HY-17376R
-
|
SCH 58235 (Standard)
|
Reference Standards
Keap1-Nrf2
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Ezetimibe (Standard) is the analytical standard of Ezetimibe. This product is intended for research and analytical applications. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
|
-
- HY-112384B
-
|
|
ERK
|
Inflammation/Immunology
|
|
DL-threo-Dihydrosphingosine is a extracellular signal-regulated kinase(ERK) signalling cassette inhibitor and is effective against both growth factor- and G-protein-dependent activation of ERK. DL-threo-Dihydrosphingosine inhibits smooth muscle cell proliferation and can be used for study of asthma .
|
-
- HY-135815
-
|
TAK-788; AP32788
|
EGFR
|
Cancer
|
|
Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research .
|
-
- HY-P1507
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Fibrinogen Binding Inhibitor Peptide is a dodecapeptide (HHLGGAKQAGDV, H12), which is a fibrinogen γ-chain carboxy-terminal sequence (γ400-411). Fibrinogen Binding Inhibitor Peptide is a specific binding site of the ligand for activated glycoprotein (GP) IIb/IIIa.
|
-
- HY-B0466A
-
-
- HY-13297
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells .
|
-
- HY-109897
-
-
- HY-B0466
-
|
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Cloxacillin sodium monohydrate is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 µM. Cloxacillin sodium monohydrate can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins .
|
-
- HY-135815B
-
|
TAK-788 mesylate; AP32788 mesylate
|
EGFR
|
Cancer
|
|
Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research .
|
-
- HY-124739
-
|
|
Deubiquitinase
|
Cancer
|
|
HBX 28258 is a selective USP7 inhibitor, with an IC50 of 22.6 μM. HBX 28258 can covalently binds to Cys223 located in the catalytic core of USP7, inhibits its deubiquitinating activity, promotes MDM2 protein degradation, and activates p53 .
|
-
- HY-163108
-
-
- HY-B0466B
-
-
- HY-N0592
-
|
|
NF-κB
AMPK
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-152265
-
|
|
PINK1/Parkin
Mitophagy
|
Neurological Disease
|
|
PARL-IN-1 is a potent PARL inhibitor with an IC50 value of 28 nM. PARL-IN-1 inhibits PARL and leads to a robust activation of the PINK1/Parkin pathway. PARL-IN-1 promotes PINK1/Parkin-dependent mitophagy .
|
-
- HY-P2913
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Vitronectin is a multifunctional glycoprotein present in blood and in the extracellular matrix. Vitronectin binds glycosaminoglycans, collagen, plasminogen and the urokinase-receptor. Vitronectin also stabilizes the inhibitory conformation of plasminogen activation inhibitor-1 (PAI-1). Vitronectin can be used for researching wound healing and in tumorprogression .
|
-
- HY-P5786
-
-
- HY-18764
-
|
|
PTEN
|
Metabolic Disease
|
|
BpV(pic) potassium hydrate is a PTEN inhibitor with IC50 31 nM. BpV(pic) potassium hydrate is also an insulin simulator that activates insulin receptor kinase in cultured liver cancer cells, stimulates adipogenesis in adipocytes, and inhibits the dephosphorylation of autophosphorylated insulin receptors and epidermal growth factor receptors in rat hepatosomes .
|
-
- HY-16785B
-
|
INXN-1001 (S enantiomer); RG-115932 (S enantiomer)
|
Interleukin Related
|
Cancer
|
|
Veledimex S enantiomer (INXN-1001 S enantiomer) is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5 .
|
-
- HY-116010
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Oleandomycin is a macrolide antibiotic structurally closely related to Erythromycin. Oleandomycin is similar to Erythromycin with antimicrobial activity. Oleandomycin inhibits protein synthesis by interference with translation of activated amino acids to nascent peptide chains on the ribosomes .
|
-
- HY-N6681
-
|
|
Caspase
Bacterial
Apoptosis
Antibiotic
|
Infection
|
|
15-acetoxyscirpenol, one of acetoxyscirpenol moiety mycotoxins (ASMs), strongly induces apoptosis and inhibits Jurkat T cell growth in a dose-dependent manner by activating other caspases independent of caspase-3 .
|
-
- HY-W067427
-
|
|
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-P99842A
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
Dapirolizumab is a monoclonal antibodi against CD40 ligand. Dapirolizumab targets CD40L, blocks its interaction with CD40 receptors, and inhibits adaptive immune activation. Dapirolizumab attenuates systemic lupus erythematosus .
|
-
- HY-N1380S4
-
-
- HY-116010A
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Oleandomycin phosphate is a macrolide antibiotic structurally closely related to Erythromycin. Oleandomycin is similar to Erythromycin with antimicrobial activity. Oleandomycin inhibits protein synthesis by interference with translation of activated amino acids to nascent peptide chains on the ribosomes .
|
-
- HY-161669
-
-
- HY-N15305
-
|
|
FXR
|
Inflammation/Immunology
|
|
Ferolin is the agonist for farnesoid X receptor (FXR) with an EC50 of 0.56 µM. Ferolin inhibits the expression of inflammatory genes (such as iNOS, IL-1β and TNFα) upon the FXR activation .
|
-
- HY-Q25865
-
|
|
VISTA
|
Cancer
|
|
MG-V-53 is a potent small molecule V domain T-cell activating immunoglobulin suppressor (VISTA) inhibitor with IC50 value of 121 nM. MG-V-53 has antitumor activity .
|
-
- HY-N6946R
-
|
|
NF-κB
Reference Standards
|
Inflammation/Immunology
|
|
Mitraphylline (Standard) is the analytical standard of Mitraphylline. This product is intended for research and analytical applications. Mitraphylline is the major pentacyclic oxindolic alkaloid presented in Uncaria tomentosa. Mitraphylline inhibits lipopolysaccharide-mediated activation of primary human neutrophils .
|
-
- HY-50910R
-
|
|
mTOR
Autophagy
Apoptosis
Bacterial
|
Cancer
|
|
Temsirolimus (Standard) is the analytical standard of Temsirolimus. This product is intended for research and analytical applications. Temsirolimus is an inhibitor of mTOR with an IC50 of 1.76 μM. Temsirolimus activates autophagy and prevents deterioration of cardiac function in animal model .
|
-
- HY-N1380S2
-
-
- HY-112906
-
|
|
STING
|
Inflammation/Immunology
|
|
C-176 is a selective and blood-brain barrier permeable STING inhibitor. C-176 covalently targets transmembrane cysteine residue 91 and thereby blocking activation-induced palmitoylation of STING .
|
-
- HY-12357R
-
|
ETC-1002 (Standard); ESP-55016 (Standard)
|
ATP Citrate Lyase
AMPK
|
Metabolic Disease
|
|
Bempedoic acid (Standard) is the analytical standard of Bempedoic acid. This product is intended for research and analytical applications. Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor . Bempedoic acid (ETC-1002) activates AMPK .
|
-
- HY-N0220
-
-
- HY-N3260
-
-
- HY-123414
-
|
PF-05196233
|
Sodium Channel
|
Neurological Disease
|
|
GX-936 (PF-05196233), a potent and Nav1.7-subtype selective inhibitor, binds to the activated state of voltage-sensor domain IV (VSD4) .
|
-
- HY-106038
-
|
Dacopafant; RP 55778
|
HIV
Platelet-activating Factor Receptor (PAFR)
|
Infection
|
|
Acopafant (Dacopafant; RP 55778) is a potent platelet-activating factor antagonist. Acopafant inhibits the induction of human immunodeficiency virus (HIV) expression in chronically infected cells. Acopafant has the potential for the research of HIV infection .
|
-
- HY-13812
-
-
- HY-162059
-
|
|
Pim
Apoptosis
Caspase
|
Cancer
|
|
Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7 activation .
|
-
- HY-N1504R
-
|
|
Reference Standards
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B (Standard) is the analytical standard of Loureirin B. This product is intended for research and analytical applications. Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-170431
-
|
|
Phosphodiesterase (PDE)
Parasite
|
Infection
|
|
SAL-0010042 is the inhibitor for Plasmodium phosphodiesterase β (PDEβ), that inhibits the hydrolysis of cAMP and cGMP (IC50=48.9 nM) in gametocytes, activates PKG, and inhibits the growth and development of Plasmodium (IC50 for 3D7 and Dd2 is 142 nM and 218 nM). SAL-0010042 inhibits hPDE5 and hPDE6 with IC50 of 632 nM and 73 nM .
|
-
- HY-B0151S2
-
|
3β-Hydroxy-5-pregnen-20-one-d4-1
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone-d4-1 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
|
-
- HY-B0151S1
-
|
3β-Hydroxy-5-pregnen-20-one-13C2,d2
|
Isotope-Labeled Compounds
Autophagy
Cannabinoid Receptor
Endogenous Metabolite
TRP Channel
|
Neurological Disease
|
|
Pregnenolone- 13C2,d2 is the deuterium and 13C labeled Pregnenolone (HY-B0151). Pregnenolone is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
|
-
- HY-P99638
-
|
ALXN-1720
|
Complement System
|
Inflammation/Immunology
|
|
Gefurulimab (ALXN-1720) is a high-affinity antibody inhibitor targeting complement protein C5, which can specifically bind to C5 and inhibit its cleavage into C5a and C5b. Gefurulimab can block the activation of the terminal complement pathway and reduce inflammatory damage. Gefurulimab can effectively reduce the formation of membrane attack complex (MAC) and has good pharmacokinetic properties. Gefurulimab can be used to study kidney and autoimmune diseases related to abnormal activation of the complement system, such as IgA nephropathy, lupus nephritis, and myasthenia gravis .
|
-
- HY-B0151S
-
|
3β-Hydroxy-5-pregnen-20-one-d4
|
Isotope-Labeled Compounds
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
|
-
- HY-B1739
-
|
3β-Hydroxy-5-pregnen-20-one monosulfate
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication . Pregnenolone monosulfate is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
|
-
- HY-111673
-
|
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
-
|
|
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-110189
-
|
3β-Hydroxy-5-pregnen-20-one monosulfate sodium
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
|
-
- HY-19044
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
SKF 95601 is a modulator of small conductive Ca2+-activated K+ channels with anti-atrial fibrillation (AF) activity. SKF 95601 may play a role in inhibiting atrial fibrillation by affecting the interaction between intracellular Ca2+ concentration and membrane potential. SKF 95601 has become a potential inhibitory target against atrial fibrillation due to its significant expression in various species, especially human atria .
|
-
- HY-155974
-
|
|
MDM-2/p53
|
Cancer
|
|
MeOIstPyrd is an anti-skin cancer agent. MeOIstPyrd inhibits cell proliferation, migration, and spheroid formation by activating the mitochondrial intrinsic apoptotic pathway. MeOIstPyrd induces DNA damage. MeOIstPyrd activates p53, and increases the half-life of p53 and stabilizes p53 by phosphorylating it at ser15. MeOIstPyrd binds to MDM2 in the p53 sub-pocket and blocks p53-MDM2 interaction .
|
-
- HY-P1241
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
Inflammation/Immunology
|
|
BAM(8-22), a proteolytically cleaved product of proenkephalin A and sensory neuron-specific receptor (SNSR) agonist, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM(8-22) induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) has an analgesic effect and can also inhibit the activation of microglia .
|
-
- HY-N8847R
-
|
alpha-Ionone (Standard)
|
Reference Standards
Hippo (MST)
YAP
|
Cancer
|
|
α-Ionone (Standard) is the analytical standard of α-Ionone. This product is intended for research and analytical applications. α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
|
-
- HY-E70390
-
|
masp-2, c1 esterase, c1-esterase
|
Wnt
|
Cardiovascular Disease
Inflammation/Immunology
|
|
C1s Enzyme is a subunit of the complement C1 complex, which activates the complement as a serine protease. C1s Enzyme cleaves LRP5 and LRP6, and thus activates the Wnt/β-Catenin signaling pathway. C1s Enzyme promotes the macrophage M2 polarization and inhibits M1 polarization. C1s Enzyme enhances efferocytosis, exhibits anti-inflammatory activity .
|
-
- HY-112671
-
|
RTA dh404
|
Keap1-Nrf2
NF-κB
Apoptosis
|
Cardiovascular Disease
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-P1241A
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
Inflammation/Immunology
|
|
BAM(8-22) TFA, a proteolytically cleaved product of proenkephalin A and sensory neuron-specific receptor (SNSR) agonist, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM(8-22) TFA induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) TFA has an analgesic effect and can also inhibit the activation of microglia .
|
-
- HY-N1970
-
|
|
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-P10869
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Inflammation/Immunology
Cancer
|
|
dCNP binds to NPR-B/C receptor, activates cGMP signaling pathway, and regulates vascular function. dCNP exhibits anti-hypoxia property through downregulation of hypoxia-related genes expressions like HIF1α and HIF2α. dCNP inhibits the induction of tumor stroma and exhibits anti-fibrosis activity. dCNP upregulates CTLs, NK cells, and conventional type 1 dendritic cells in tumors, and activates immune responses .
|
-
- HY-70062R
-
|
|
NEDD8-activating Enzyme
Apoptosis
|
Cancer
|
|
Pevonedistat (Standard) is the analytical standard of Pevonedistat. This product is intended for research and analytical applications. Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM. Pevonedistat induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat suppresses the growth of human tumour xenografts in mice .
|
-
- HY-136179
-
|
|
Tyrosinase
|
Inflammation/Immunology
|
|
ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs) .
|
-
- HY-N0773R
-
|
Saponaretin (Standard); Homovitexin (Standard)
|
Reference Standards
JNK
NF-κB
|
Inflammation/Immunology
|
|
Isovitexin (Standard) is the analytical standard of Isovitexin. This product is intended for research and analytical applications. Isovitexin is a flavonoid isolated from passion flower, Cannabis and, and the palm, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
|
-
- HY-13418
-
|
Compound C dihydrochloride; BML-275 dihydrochloride
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
|
-
- HY-149604
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-21 (compound L38) is a NLRP3 inflammasome inhibitor with inflammatory properties. NLRP3-IN-21 inhibits NLRP3 inflammasome activation and pyroptosis by suppressing gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly .
|
-
- HY-10999S1
-
|
|
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib- 13C6 is the 13C-labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
|
-
- HY-N0859B
-
|
|
NO Synthase
|
Neurological Disease
|
|
Schisanchinin D is an NO release inhibitor found in the fruits of Schisandra chinensis. Schisanchinin D can inhibit the release of nitric oxide (NO) by lipopolysaccharide (LPS)-activated microglia in primary murine BV2 microglia cells. Schisanchinin D is promising for research of neurodegenerative diseases such as Alzheimer's disease (AD) .
|
-
- HY-N2119R
-
|
|
TNF Receptor
Reference Standards
NF-κB
|
Inflammation/Immunology
|
|
Sciadopitysin (Standard) is the analytical standard of Sciadopitysin. This product is intended for research and analytical applications. Sciadopitysin is a type of biflavonoids in leaves from ginkgo biloba . Sciadopitysi inhibits RANKL-induced osteoclastogenesis and bone loss by inhibiting NF-κB activation and reducing the expression of c-Fos and NFATc1 .
|
-
- HY-134969
-
|
|
LXR
|
Metabolic Disease
|
|
TFCA is a liver X receptor α (LXRα) antagonist. TFCA inhibits ligand-activated LXRα coactivation and transcriptional expression of the downstream target genes involved in fatty acid synthesis. TFCA attenuates ligand-induced lipogenesis and fatty liver by selectively inhibiting LXRα in the liver .
|
-
- HY-149816
-
-
- HY-170327
-
|
|
Ras
|
Cancer
|
|
ZCL279 is a small molecule modulator (SMM) that inhibits Cdc42-intersectin (ITSN) interaction. ZCL279 can activate Cdc42 (a cytoplasmic small GTPase in the Ras superfamily) at lower concentrations (<10 μM) and significantly inhibit it at higher concentrations (<10 μM) .
|
-
- HY-163461
-
|
|
PARP
|
Cancer
|
|
4F-DDC is a novel PARP1 inhibitor with an IC50 value of 82 nM. 4F-DDC induces DNA damage and activates the cGAS–STING pathway. 4F-DDC inhibits the growth of HCC-1937-derived tumor xenografts .
|
-
- HY-10999A
-
|
GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)
|
MEK
Apoptosis
|
Cancer
|
|
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis .
|
-
- HY-N0103R
-
|
|
Reference Standards
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MEK
ERK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Sophocarpine (Standard) is the analytical standard of Sophocarpine (HY-N0103). This product is intended for research and analytical applications. Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage .
|
-
- HY-D0086
-
|
MDL101114ZA
|
VDAC
RAD51
|
Cancer
|
|
DIDS sodium salt (MDL101114ZA) is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research .
|
-
- HY-N3643
-
-
- HY-N0250
-
-
- HY-112108
-
|
COS
|
AMPK
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
|
-
- HY-P3204
-
POT-4
1 Publications Verification
AL-78898A
|
Complement System
|
Metabolic Disease
|
|
POT-4 (AL-78898A), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 can be used for age-related macular degeneration research
|
-
- HY-163756
-
-
- HY-15272
-
|
|
mTOR
|
Inflammation/Immunology
Cancer
|
|
WAY-600 is a potent, ATP-competitive, and selective mTOR inhibitor with an IC50 of 9 nM for recombinant mTOR enzyme. WAY-600 blocks mTOR complex 1/2 (mTORC1/2) assemble and activation.
|
-
- HY-13255A
-
|
|
APC
|
Cancer
|
|
TAME hydrochloride is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest. TAME hydrochloride is not cell permeable .
|
-
- HY-P0318
-
-
- HY-N0802
-
|
Senegenin
|
NF-κB
Bacterial
|
Infection
Inflammation/Immunology
|
|
Tenuigenin is a major active component isolated from the root of the Chinese herb Polygala tenuifolia. Tenuigenin protects against S.aureus-induced pneumonia by inhibiting NF-κB activation. Tenuigenin has anti-inflammatory effect .
|
-
- HY-102092
-
|
PD 147953
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
FR139317 (PD 147953) is a selective ETA receptor antagonist. FR139317 inhibits cerebral activation by intraventricular endothelin-1 in conscious rats. FR139317 also ameliorates cerebral vasospasm in dogs .
|
-
- HY-13255
-
TAME
1 Publications Verification
|
APC
|
Cancer
|
|
TAME is an inhibitor of anaphase-promoting complex/cyclosome (APC/C or APC), which binds to APC/C and prevents its activation by Cdc20 and Cdh1, produces mitotic arrest. TAME is not cell permeable .
|
-
- HY-126133
-
|
|
Ras
|
Cardiovascular Disease
Others
|
|
AM-001 is a non-competitive inhibitor of Epac1 that blocks the activation of Rap1, a downstream effector of Epac1, in cultured cells. AM-001 can be used in heart disease-related research .
|
-
- HY-15251R
-
|
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
Reparixin (Standard) is the analytical standard of Reparixin. This product is intended for research and analytical applications. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
|
-
- HY-16696
-
SN 2
3 Publications Verification
|
Flavivirus
Dengue Virus
TRP Channel
|
Infection
|
|
SN 2 is a potent activator of TRPML3 ion channel with an EC50 of 1.8 μM .
SN 2 also acts as a potent inhibitor of Dengue virus 2 (DENV2) and Zika virus (ZIKV) .
|
-
- HY-129496
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
NP-313 is a potent antithrombotic agent that inhibits platelet aggregation and activation. NP-313 has dual inhibition of thromboxane A 2 synthesis and selective inhibition of SOCC-mediated Ca 2+ inward flow .
|
-
- HY-B0285
-
-
- HY-162586
-
|
|
PDHK
|
Cancer
|
|
PDHK-IN-7 (compound 32) is an inhibitor of pyruvate dehydrogenase kinase with an IC50 value of 17 nM.PDHK-IN-7 activates PDH in rat livers and has a glucose-lowering effect in Zucker fatty rats .
|
-
- HY-N0020
-
|
|
Wnt
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche deserticola, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity .
|
-
- HY-10162
-
|
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-10590R
-
-
- HY-B0285A
-
-
- HY-N1380R
-
-
- HY-15880
-
|
|
Phosphatase
Apoptosis
Autophagy
|
Cancer
|
|
CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy .
|
-
- HY-124956
-
|
|
Taste Receptor
|
Others
|
|
GIV3727 is a bitter taste receptor hTAS2R antagonist, which can inhibit the activation of hTAS2R31 by saccharin and acesulfame potassium, and can effectively reduce the bitter quality of food, beverage and medicine .
|
-
- HY-108963
-
|
|
PKC
Leukotriene Receptor
|
Cancer
|
|
LY 170198 is a protein kinase C inhibitor and a LTD4 antagonist. LY 170198 is promising for research of tumor promotion, oncogene activation, protein phosphorylation, feedback mechanisms in signal transduction and cellular responses to growth factors .
|
-
- HY-155978
-
|
|
Tyrosinase
|
Inflammation/Immunology
|
|
RDN2150 (Compound 25) is a ZAP-70 inhibitor (IC50: 14.6 nM). RDN2150 covalently binds to the C346 residue of ZAP-70. RDN2150 inhibits the expression of CD25 and CD69, and inhibits CD4 + T cell activation. RDN2150 can be used for research of psoriasis .
|
-
- HY-15271
-
WYE-687
3 Publications Verification
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
|
-
- HY-B0689
-
|
MK-639 free base; L-735524 free base
|
HIV
HIV Protease
Apoptosis
MMP
SARS-CoV
|
Inflammation/Immunology
Cancer
|
|
Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CL pro inhibitor .
|
-
- HY-133015
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity ..
|
-
- HY-138537
-
|
|
IKK
|
Cancer
|
|
NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells .
|
-
- HY-138956
-
|
|
NF-κB
RSV
|
Infection
|
|
MAY0132 is a potent and selective EPAC2 inhibitor with an IC50 of 0.4 μM. MAY0132 significantly inhibits replication of HMPV, AdV and RSV, reduces viral infection-induced cytokine/chemokine production, and inhibits NF-κB activation. MAY0132 has antiviral activity and can be used in the study of respiratory virus infection .
|
-
- HY-10255AR
-
|
SU 11248 (Standard)
|
Reference Standards
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. 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-13757
-
|
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 transgenic mouse .
|
-
- HY-P990091
-
|
SAR 445088
|
Complement System
|
Inflammation/Immunology
|
|
Riliprubart (SAR 445088) is an anti-C1s humanized IgG4 monoclonal antibody that inhibits activated C1s in the proximal portion of the classical complement system. Riliprubart selectively inhibits activated C1s and prevents the enzymatic action of C1 on its substrates C4 and C2, thus inhibiting the formation of the classical pathway C3 convertase, C4b2a. Riliprubart can be used to study complement-mediated diseases such as systemic lupus erythematosus. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
|
-
- HY-N7046
-
|
Silibinin B
|
Amyloid-β
Apoptosis
JNK
p38 MAPK
|
Neurological Disease
Cancer
|
|
Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator, that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity .
|
-
- HY-121435
-
|
|
RAR/RXR
PI3K
Akt
Apoptosis
|
Cancer
|
|
K-8012, a sulindac (HY-B0008) analog, is a potent antagonist of RXRa. The IC50 value for K-8012 to inhibit 9-cis-RA-induced Gal4-RXRa-LBD trans-activation were about 9.2 μM. K-8012 exerts improved anticancer activity over sulindac in a RXRa-dependent manner. K-8012 exhibits activity in inhibiting the tRXRa-mediated PI3K/AKT signaling pathway. K-8012 induces apoptosis and inhibits AKT activation by preventing tRXRa from binding to p85a .
|
-
- HY-170570
-
|
|
LXR
Stearoyl-CoA Desaturase (SCD)
Fatty Acid Synthase (FASN)
|
Cancer
|
|
PFM046 is the antagonist for liver X receptor (LXR), that inhibits the activation of LXRα and LXRβ with IC50 of 2.04 μM and 1.58 μM. PFM046 inhibits the expression of SCD1 and FASN, upregulates the expression of ABCA1, and exhibits antitumor efficacy in mouse models .
|
-
- HY-100345
-
|
|
TRP Channel
|
Neurological Disease
Cancer
|
|
AMTB hydrochloride is a selective TRPM8 channel blocker. AMTB hydrochloride inhibits icilin-induced TRPM8 channel activation with a pIC50 of 6.23. AMTB hydrochloride can be used for the research of the overactive bladder and painful bladder syndrome. AMTB hydrochloride is a non-selective inhibitor of voltage-gated sodium channels (NaV) .
|
-
- HY-139576C
-
|
DUR-928 ammonium
|
LXR
Endogenous Metabolite
|
Metabolic Disease
|
|
Larsucosterol (DUR-928) ammonium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol ammonium as a potent endogenous regulator decreases lipogenesis. Larsucosterol ammonium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1 .
|
-
- HY-148591
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
GSK761 is a selective inhibitor of speckled 140 kDa (SP140) with an IC50 value of 77.79 nM. GSK761 reduces monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation. GSK761 induces the production of CD206 + regulatory macrophages by inhibiting SP140 .
|
-
- HY-139576B
-
|
DUR-928 (trimethylamine)
|
LXR
Endogenous Metabolite
|
Metabolic Disease
|
|
Larsucosterol (DUR-928) trimethylamine, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol trimethylamine as a potent endogenous regulator decreases lipogenesis. Larsucosterol trimethylamine inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1 .
|
-
- HY-101246
-
|
|
RET
|
Cancer
|
|
RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .
|
-
- HY-127149
-
|
Ro 40-8757
|
Apoptosis
Reactive Oxygen Species (ROS)
Caspase
|
Cancer
|
|
Mofarotene (Ro 40-8757), an arotinoid, is anticancer compound. Mofarotene induces apoptosis, associated with mitochondrial membrane depolarization, activation of caspase-3 and -9, and enhanced production of reactive oxygen species. Mofarotene inhibits hematopoiesis in vitro by inhibiting maturation from primitive progenitor cells .
|
-
- HY-130369
-
|
|
Bacterial
Necroptosis
HSV
|
Infection
Cancer
|
|
NSC10010 hydrochloride inhibits gammaherpesvirus associated B-lymphomas growth through activation of NF-kB and c-Myc-mediated signaling pathways. NSC10010 hydrochloride induces necrotic cell death in gammaherpesvirus infected B-cells. NSC10010 hydrochloride is also an inhibitor of Mtb ClpC1 ATPase .
|
-
- HY-N0191
-
-
- HY-10999R
-
|
GSK1120212 (Standard); JTP-74057 (Standard)
|
Reference Standards
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib (Standard) is the analytical standard of Trametinib. This product is intended for research and analytical applications. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
|
-
- HY-12467
-
|
|
TOPK
CDK
Apoptosis
|
Cancer
|
|
OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM . OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM .
|
-
- HY-103639A
-
|
|
Toll-like Receptor (TLR)
|
Infection
|
|
M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis .
|
-
- HY-14600R
-
|
BRL 49653C (Standard)
|
Reference Standards
PPAR
TRP Channel
Autophagy
Ferroptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Rosiglitazone (maleate) (Standard) is the analytical standard of Rosiglitazone (maleate). This product is intended for research and analytical applications. Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
|
-
- HY-107661
-
|
ONO-2506; (R)-2-Propyloctanoic acid
|
Others
|
Neurological Disease
|
|
Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid also increases the expression level of EAAT1 by activating the Akt, ERK, and NF-κB signaling pathways, which has the potential to eliminate excess glutamate and inhibit excitotoxic brain damage or death. Arundic acid has the potential for stroke and Alzheimer’s disease research .
|
-
- HY-113843
-
|
|
MDM-2/p53
|
Cancer
|
|
RETRA (hydrobromide) is a mutant p53-dependent activator of p73 that can inhibit cancer cells carrying mutant p53. RETRA (hydrobromide) increases the expression level of p73, induces transcriptional activation of several common to transcriptional targets p53 and p73, which leads to mutant p53- and p73-dependent inhibition of tumor growth, reduction of colony formation and induction of effector caspases .
|
-
- HY-111866
-
|
|
PROTACs
RIP kinase
|
Metabolic Disease
Cancer
|
|
PROTAC RIPK degraders -2 is a non-peptide PROTAC based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes .
|
-
- HY-135110
-
|
Rp-8-bromo-Cyclic GMPS sodium
|
Calcium Channel
PKG
HCN Channel
|
Metabolic Disease
|
|
Rp-8-Br-cGMPS (Rp-8-bromo-Cyclic GMPS) sodium salt is a potent Ca 2+-ATPase activator. Rp-8-Br-cGMPS is also an agonist of the rod CNG channel and an inhibitor of PKG. Rp-8-Br-cGMPS sodium salt mediates cytosolic Ca 2+ reduction by activating Ca 2+-ATPase and subsequently removing Ca 2+ from the cell .
|
-
- HY-152860
-
|
HRX-0215
|
p38 MAPK
JNK
NF-κB
MDM-2/p53
|
Cancer
|
|
Darizmetinib (HRX-0215) is an orally active, potent and selective inhibitor of mitogen-activated protein kinase kinase 4 (MKK4). Darizmetinib leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration. Darizmetinib is promising for research of preventing liver failure after extensive oncological liver resections or transplantation of small liver grafts .
|
-
- HY-N0106
-
|
(Rac)-Danshensu sodium; (Rac)-Tanshinol sodium
|
Keap1-Nrf2
NF-κB
Mitochondrial Metabolism
Apoptosis
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
(Rac)-Salvianic acid A sodium is the racemic form of Salvianic acid A (HY-N1913). Salvianic acid A is an orally active phenolic compound that induces Nrf2/HO-1 activation and inhibits the NF-κB pathway, and it also activates the mitochondrial antioxidant defense system (Mitochondrial Metabolism). Salvianic acid A exhibits anti-inflammatory, antioxidant, and anti-apoptotic properties (Apoptosis), demonstrating potential for research into inflammation and cardiovascular diseases .
|
-
- HY-137638A
-
|
Sp-5,6-DCI-cBIMPS
|
PKA
|
Metabolic Disease
|
|
Sp-5,6-DCl-cBIMPS sodium is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS sodium stimulates insulin release. Sp-5,6-DCl-cBIMPS sodium inhibits U-46619 (HY-108566)-induced activation of Rho, Gq and G12/G13 in platelets .
|
-
- HY-12496R
-
|
|
Potassium Channel
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
NS-1619 (Standard) is the analytical standard of NS-1619. This product is intended for research and analytical applications. NS-1619 is an opener of large conductance Ca2+-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-135110A
-
|
Rp-8-bromo-Cyclic GMPS
|
Calcium Channel
PKG
HCN Channel
|
Metabolic Disease
|
|
Rp-8-Br-cGMPS (Rp-8-bromo-Cyclic GMPS) sodium salt is a potent Ca 2+-ATPase activator. Rp-8-Br-cGMPS is also an agonist of the rod CNG channel and an inhibitor of PKG. Rp-8-Br-cGMPS sodium salt mediates cytosolic Ca 2+ reduction by activating Ca 2+-ATPase and subsequently removing Ca 2+ from the cell .
|
-
- HY-120026
-
|
KB015
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 opens large-conductance Ca 2+-activated K + channels and relaxes vascular smooth muscle .
|
-
- HY-153225
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
PYR01 is a non-nucleoside reverse transcriptase inhibitor and a killing activator targeting HIV infected cells. PYR01 has cytokilling and antiviral properties of HIV-1 infection with the IC50 values of 27.5nM and 39.7nM, respectively. PYR01 leads to selective cytotoxicity by promoting HIV-1 Gag-Pol dimerization and HIV-1 protease intracellular activation. PYR01 can be used in the study of HIV .
|
-
- HY-100539
-
|
|
Dopamine Receptor
|
Others
|
|
PD 128907 is a D3 receptor ligand with activities of activating dopamine receptors, inhibiting cell firing, and inhibiting dopamine release. The active (+) enantiomer of PD 128907 has high affinity and selectivity for rat D3 dopamine receptors. PD 128907 inhibits cell firing in the ventral tegmental area and substantia nigra pars compacta with EC50 values of 33nM and 38nM, respectively. PD 128907 also inhibits dopamine release in the caudate putamen with an EC50 of 66nM. However, the selective D2 receptor antagonist L-741,626 has high affinity for receptors activated by PD 128907, indicating that the effects of PD 128907 are more likely on D2 autoreceptors rather than D3 dopamine receptor subtypes.
|
-
- HY-N2157
-
|
(+)-Pteryxin
|
Cholinesterase (ChE)
NF-κB
NOD-like Receptor (NLR)
Keap1-Nrf2
Reactive Oxygen Species (ROS)
Nuclear Factor of activated T Cells (NFAT)
p38 MAPK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Pteryxin ((+)-Pteryxin) is an orally active multi-target inhibitor that targets NF-κB, MAPK, NLRP3 inflammasome, and Nrf2/ARE pathways. Pteryxin is also a BChE inhibitor (IC50=12.96 μg/mL) with a low inhibitory efficiency on AChE. Pteryxin inhibits the Ca 2+-calcineurin-NFATc1 pathway by blocking NF-κB/MAPK signaling, inhibiting NLRP3 inflammasome activation, and reducing ROS generation, and activates Nrf2-mediated antioxidant enzyme expression. Pteryxin has anti-inflammatory, antioxidant, and osteoclastogenesis inhibitory activities. Pteryxin can be used in the study of inflammatory diseases, osteoporosis, diabetes, and Alzheimer's disease .
|
-
- HY-116806
-
|
|
CFTR
|
Endocrinology
|
|
AF-2785 is a potent CFTR blocker. AF-2785 inhibits the cAMP-activated chloride current in rat epididymal cells with an IC50 of 170.6 μM. AF-2785 can be used in research related to contraceptives .
|
-
- HY-151626
-
|
|
Bacterial
|
Infection
|
|
MRV03-037 is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-037 prevents gut bacterial genotoxin production .
|
-
- HY-B0099R
-
|
MCI-186 (Standard)
|
Reference Standards
MMP
Apoptosis
|
Neurological Disease
|
|
Edaravone (Standard) is the analytical standard of Edaravone. This product is intended for research and analytical applications. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
|
-
- HY-P10827A
-
|
|
Complement System
|
Inflammation/Immunology
|
|
PIC1 PA TFA is the trifluoroacetate salt form of PIC1 PA (HY-P10827). PIC1 PA TFA is a 15-amino acid peptide that is a potent PIC1 analog that inhibits classical complement activation .
|
-
- HY-111447
-
|
|
NADPH Oxidase
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
VAS 3947, a specific NADPH oxidase (NOX) inhibitor, exerts a potent antiplatelet effect. VAS3947 induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins .
|
-
- HY-N3828
-
|
|
Apoptosis
ERK
JNK
|
Cancer
|
|
epi-Eriocalyxin A (Epieriocalyxin A), a diterpenoid isolated from Isodon eriocalyx, induces colon cancer apoptosis. epi-Eriocalyxin A also inhibits ERK1/2 and JNK activation, which suppresses Bcl-2 expression .
|
-
- HY-153098
-
-
- HY-15874A
-
|
GSK2190915 sodium salt; AM-803 sodium
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood .
|
-
- HY-N0109
-
|
Rhodioloside
|
PINK1/Parkin
mTOR
Apoptosis
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Salidroside (Rhodioloside) is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
|
-
- HY-109011
-
|
AQX-1125
|
Phosphatase
|
Cancer
|
|
Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro .
|
-
- HY-P2020
-
|
|
Bacterial
|
Infection
|
|
Berninamycin A is a cyclic thiopeptide antibiotic first isolated from S. bernensis. It inhibits protein biosynthesis in Gram positive bacteria through binding with ribosomal subunits. Cyclic thiopeptide antibiotics, including berninamycin A, induce the transcriptional activator TipA in Streptomyces.
|
-
- HY-18952A
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3 .
|
-
- HY-136641
-
|
|
Radionuclide-Drug Conjugates (RDCs)
FAP
|
Cancer
|
|
NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor. NOTA-FAPI can be used as a probe for FAP-targeted tumour imaging. NOTA-FAPI has good tumour detection efficacy and excellent imaging quality .
|
-
- HY-157554
-
-
- HY-162516
-
|
|
AMPK
Mitochondrial Metabolism
|
Cancer
|
|
DBI-2 is an AMPK activator targeting mitochondrial complex I. DBI-2 disrupts the OXPHOS process, and reduces ATP generation in mitochondria. DBI-2 inhibits the proliferation of colorectal cancer (CRC) cells .
|
-
- HY-N0589
-
|
|
NF-κB
COX
Bacterial
|
Infection
Inflammation/Immunology
|
|
Dehydrodiisoeugenol is isolated from Myristica fragrans Houtt, shows anti-inflammatory and anti-bacterial actions . Dehydrodiisoeugenol inhibits LPS- stimulated NF-κB activation and cyclooxygenase (COX)-2 gene expression in murine macrophages .
|
-
- HY-W041892
-
-
- HY-109011A
-
|
AQX-1125 acetate
|
Phosphatase
|
Cancer
|
|
Rosiptor (AQX-1125) acetate is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor acetate (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro .
|
-
- HY-N13098
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Elatoside F is a triterpenoid saponin with anti-inflammatory activity. Elatoside F inhibits lipopolysaccharide-induced nitric oxide production and nuclear factor NF-κB activation. Elatoside F can be isolated from Aralia elata in one step.
|
-
- HY-169817
-
-
- HY-N12283
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-13 (compound 12) can significantly inhibit LPS-induced NF-κB activation and NO production in RAW264.7 macrophages. NF-κB-IN-13 has anti-inflammatory effects .
|
-
- HY-N0375
-
-
- HY-102004
-
|
SB 659032
|
Phospholipase
|
Neurological Disease
Inflammation/Immunology
|
|
Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM . Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist .
|
-
- HY-122813
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Dabigatran acyl-β-D-glucuronide is an active metabolite of the thrombin inhibitor Dabigatran (HY-10163). Dabigatran acyl-β-D-glucuronide increases activated partial thromboplastin time (aPTT) in isolated human platelet-poor plasma.
|
-
- HY-15251A
-
|
(Rac)-Repertaxin; (Rac)-DF 1681Y
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
(Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
|
-
- HY-B0621
-
|
CGA89317
|
Parasite
Caspase
Bcl-2 Family
PARP
Pyroptosis
|
Infection
|
|
Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica .
|
-
- HY-168516
-
|
|
FXR
|
Others
|
|
FXR/CES2 modulator 1 (compound LE-77) is a doul modulator that activates FXR and inhibits CES2. FXR/CES2 modulator 1 effectively mitigates the intestinal toxicity of irinotecan .
|
-
- HY-13694R
-
|
MRX-1024 (Standard); D-Methionine (Standard)
|
Reference Standards
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Methionine (Standard) is the analytical standard of Methionine. This product is intended for research and analytical applications. Methionine (MRX-1024; D-Methionine) is an effective chemoprotective agent which can also inhibit the neuronal activity through GABAA receptor activation.
|
-
- HY-P99462
-
|
CDX-0159; CDX-0158
|
c-Kit
|
Inflammation/Immunology
|
|
Barzolvolimab (CDX 0159) is a humanized anti-KIT IgG1 monoclonal antibody. Barzolvolimab specificity and potently inhibits KIT activation by SCF. Barzolvolimab can reduce skin mast cells and disease activity in chronic inducible urticaria .
|
-
- HY-15874
-
|
GSK2190915; AM-803
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
|
Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood .
|
-
- HY-B0167S
-
-
- HY-B1240
-
|
Dehydrobenzperidol
|
Dopamine Receptor
GABA Receptor
nAChR
|
Neurological Disease
|
|
Droperidol (Dehydrobenzperidol) is a butyrophenone pamine-2 receptor antagonist that inhibits the activation of GABA(A) and neuronal nicotinic receptors (nAChR), with IC50 values of 12.6 nM and 5.8 μM. Droperidol has anesthetic and sedative properties .
|
-
- HY-153098A
-
|
|
Complement System
|
Inflammation/Immunology
|
|
ARC186 (sodium) is an unconjugated 40KDa PEG aptamer with a sequence identical to HY-147080 Avacincaptad pegol (ARC1905) sodium. ARC1905 is highly potent complement inhibitors that function by blocking the convertase-catalyzed activation of C5.
|
-
- HY-P99196
-
|
|
c-Met/HGFR
|
Cancer
|
|
Ficlatuzumab is a monoclonal antibody (McAb) targeting human hepatocyte growth factor (HGF). Ficlatuzumab blocks the activation of the HGF/c-Met signaling pathway, and inhibits c-Met receptor-mediated cancer cell proliferation, migration, and invasion .
|
-
- HY-162325
-
-
- HY-135808
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases .
|
-
- HY-N6985
-
|
|
Others
|
Cancer
|
|
Baccatin III is an orally available, selective inhibitor of the TGF-β1 signaling pathway and myeloid-derived suppressor cell (MDSC) activation. Baccatin III targets the AKT/STAT6 and Smad2/3 pathways, blocking TGF-β1-induced fibroblast differentiation and MDSC-mediated immunosuppression. Baccatin III exerts anti-inflammatory and anti-fibrotic effects by inhibiting macrophage activation and extracellular matrix deposition, and shows potential in the treatment of pulmonary fibrosis and cancer in terms of regulating the tumor immune microenvironment[1][2].
|
-
- HY-169703
-
|
|
RANKL/RANK
p38 MAPK
Akt
NF-κB
|
Inflammation/Immunology
|
|
SPA0355 is a thiourea derivative that has antioxidant and anti-inflammatory properties. SPA0355 inhibits the RANKL (receptor activator of nuclear factor κB ligand) induced osteoclast formation in primary bone marrow-derived macrophages. SPA0355 also suppresses the activation of the MAPKs, Akt, and NF-κB pathways. Additionally, SPA0355 promotes osteoblast differentiation, increases alkaline phosphatase activity, and enhances mineral nodule formation. SPA0355 can protect ovariectomized mice from bone loss by stimulating osteoblast differentiation and inhibiting osteoclast resorption, making it useful for studying postmenopausal osteoporosis .
|
-
- HY-134356
-
|
AICAR-5'-MP
|
Endogenous Metabolite
|
Others
|
|
AICA-riboside, 5′-phosphate is AICA riboside with a phosphate group. The functions of AICA riboside include: 1) conversion into AMP mimetic to selectively activate AMPK; 2) competition with adenosine for the uptake of nucleoside transporters, reversible blocking of adenosine reuptake, increasing extracellular adenosine concentration, and indirectly activating adenosine A1 receptors. AICA riboside is involved in metabolic regulation (promoting catabolism and inhibiting anabolism) and adenosine-dependent neuroprotection (inhibiting excitatory synaptic transmission). AICA riboside can be used in the study of metabolic diseases (such as diabetes and obesity) and neurological diseases (such as ischemia and epilepsy), and has central nervous system protective activity .
|
-
- HY-174437
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-32 is a potent FLT3 inhibitor. FLT3-IN-32 shows high selectivity for FLT3 and efficiently inhibits FLT3-activating mutations and induces apoptosis. FLT3-IN-32 shows good tolerability in non-tumor bearing mice. FLT3-IN-32 demonstrates outstanding anti-tumor efficacy in MV4-11 bearing NOD/SCID mice, prolonging the survival noticeably. FLT3-IN-32 can be used for the research of acute myeloid leukemia .
|
-
- HY-19959
-
Mirin
5 Publications Verification
|
ATM/ATR
Apoptosis
|
Cancer
|
|
Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells .
|
-
- HY-B0151R
-
|
3β-Hydroxy-5-pregnen-20-one (Standard)
|
Reference Standards
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone (Standard) is the analytical standard of Pregnenolone. This product is intended for research and analytical applications. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication . Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
|
-
- HY-136093B
-
|
IM156 free base; HL156A free base; HL271 free base
|
Mitochondrial Metabolism
|
Cancer
|
|
Lixumistat (IM156) is a novel biguanide mitochondrial protein complex 1 inhibitor of oxidative phosphorylation (OXPHOS) with anti-tumor activity. Lixumistat regulates OXPHOS to attenuate mitochondrial metabolic reprogramming and inhibit lung fibrosis. Lixumistat also suppresses B-cell activation to alleviate systemic lupus erythematosus .
|
-
- HY-126390
-
|
NSC 150117
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway .
|
-
- HY-152265A
-
|
|
PINK1/Parkin
Mitophagy
|
Neurological Disease
|
|
PARL-IN-1 TFA is a potent PARL inhibitor with an IC50 value of 28 nM. PARL-IN-1 TFA inhibits PARL and leads to a robust activation of the PINK1/Parkin pathway. PARL-IN-1 TFA promotes PINK1/Parkin-dependent mitophagy .
|
-
- HY-149700
-
|
|
ROCK
MMP
STAT
|
Others
|
|
ROCK2-IN-7 is a kinase inhibitor targeting to ROCK2. ROCK2-IN-7 inhibits ROCK2/pSTAT3 Signaling. ROCK2-IN-7 suppresses systemic immunity activation and attenuates inflammation in psoriasis model .
|
-
- HY-148606
-
|
|
STING
|
Cancer
|
|
STING modulator-3 is a STING inhibitor. STING modulator-3 inhibits R232 STING with an Ki value of 43.1 nM in scintillation proximity assay. STING modulator-3 has no effect on IRF-3 activation or TNF-β induction in THP-1 cells .
|
-
- HY-13965
-
|
ML161
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM . Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo .
|
-
- HY-100612
-
|
|
Chloride Channel
|
Others
|
|
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC) .
|
-
- HY-135815A
-
|
TAK-788 succinate; AP32788 succinate
|
EGFR
|
Cancer
|
|
Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research .
|
-
- HY-P10875
-
|
|
Hedgehog
|
Cancer
|
|
HL2-m5 is the inhibitor for the interaction between sonic hedgehog/patched (Shh/PTCH1) with Kd of 170 nM for Shh. HL2-m5 inhibits activation of Hedgehog signaling pathway and transcription of Gli-controlled gene with an IC50 of 230 nM .
|
-
- HY-12364R
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
C75 (Standard) is the analytical standard of C75. This product is intended for research and analytical applications. 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-N0141R
-
|
(-)-Parthenolide (Standard)
|
Reference Standards
NF-κB
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Parthenolide (Standard) is the analytical standard of Parthenolide. This product is intended for research and analytical applications. Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
|
-
- HY-W018723
-
|
p-Aminobenzamidine dihydrochloride
|
Ser/Thr Protease
PAI-1
|
Cardiovascular Disease
Cancer
|
|
4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor. 4-Aminobenzamidine dihydrochloride acts as an orally active urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine dihydrochloride can be used for cardiovascular diseases and anti-tumor study .
|
-
- HY-108022
-
-
- HY-120111
-
|
MW01-18-150SRM
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
|
-
- HY-W395779
-
|
|
Filovirus
|
Infection
|
|
EBOV-IN-1 (com 3.47) is an adamantane dipeptide piperazine and an inhibitor of Ebola virus (EBOV). EBOV-IN-1 targets Niemann-Pick C1 (NPC1) and inhibits its binding to the EBOV glycoprotein (GP) that activates and mediates viral penetration into host cells, thereby inhibiting EBOV infection. EBOV-IN-1 inhibits pseudotyped EBOV infection with an IC50 of 13 nM .
|
-
- HY-N3548
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Catalpalactone has anti-inflammatory effect. Catalpalactone inhibits LPS-induced NO production and iNOS expression in RAW264.7 cells, and also inhibits IRF3, NF-κB, and IFN-β/STAT-1 activation. Catalpalactone also inhibits dopamine biosynthesis by reducing tyrosine hydroxylase (TH) and aromatic-l-amino acid decarboxylase (AADC) activities .
|
-
- HY-103347
-
|
|
Apoptosis
|
Inflammation/Immunology
|
|
M50054 is a potent inhibitor of apoptosis. M50054 inhibits Etoposide-induced caspase-3 activation of U937 cells with an IC50 of 79 μg/mL. M50054 does not directly inhibit the enzymatic activity of caspase-3. M50054 can be used for the research anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia .
|
-
- HY-132304
-
|
|
PKC
|
Inflammation/Immunology
|
|
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by inhibiting IL-2 expression .
|
-
- HY-172204
-
|
|
Sirtuin
Apoptosis
Autophagy
MDM-2/p53
|
Cancer
|
|
SIRT-IN-7 (Compound 7ba) is a SIRT inhibitor. SIRT-IN-7 can inhibit the expression of SIRT1, SIRT2, and SIRT3, and increase the acetylation and activation of p53. SIRT-IN-7 can inhibit the proliferation, and induce apoptosis and autophagy of breast cancer cells. SIRT-IN-7 has anti-tumor activity .
|
-
- HY-B0689A
-
|
MK-639; L735524
|
HIV
HIV Protease
SARS-CoV
Apoptosis
MMP
|
Infection
Cancer
|
|
Indinavir sulfate (MK-639) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate is also a SARS-CoV 3CL pro inhibitor .
|
-
- HY-B2145
-
|
IY-81149 sodium
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-15271A
-
|
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM . WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2 . WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively .
|
-
- HY-123870
-
|
|
Survivin
IAP
NF-κB
|
Inflammation/Immunology
Cancer
|
|
MX107 is a selective and potent survivin inhibitor that suppresses triple-negative breast cancer (TNBC) cell proliferation. MX107 induces degradation of survivin and inhibitor-of-apoptosis proteins (IAPs), which inhibits nuclear factor κB (NF-κB) activation induced by DNA damage. MX107 enhances tumoricidal efficacy of genotoxic treatments synergized with chemotherapeutic drugs .
|
-
- HY-B2145A
-
|
IY-81149 sodium hydrate
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor. Ilaprazole sodium hydrate irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium hydrate is used for the research of gastric ulcers. Ilaprazole sodium hydrate is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-150617
-
|
M4076; ATM Inhibitor-5
|
ATM/ATR
STING
PD-1/PD-L1
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .
|
-
- HY-139486
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
AM-8123 is an orally active and potent APJ agonist. AM-8123 inhibits Forskolin-stimulated cAMP production and promotes Gα protein activation. AM-8123 can be used for the research of cardiovascular disease .
|
-
- HY-P5762
-
|
PNX-14
|
GnRH Receptor
|
Neurological Disease
|
|
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia .
|
-
- HY-B1505
-
-
- HY-100911
-
|
|
Calmodulin
|
Neurological Disease
|
|
W-5 hydrochloride is a calmodulin antagonist. W-5 hydrochloride inhibits phosphodiesterase activation with an IC50 value of 240 µM. W-5 hydrochloride can be used as a negative control for W-7 (HY-100912) .
|
-
- HY-P5321
-
|
|
FGFR
|
Others
|
|
bFGF (119-126) is a biological active peptide. (This peptide corresponds to human, bovine (119-126), mouse, rat (118-125) and Heparin-Binding Growth Factor 2 (118-125) residues of bFGF. It inhibits dimerization and activation of bFGF receptors.)
|
-
- HY-134885
-
|
RM-023
|
SHP2
SOS1
Ras
|
Cancer
|
|
RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction .
|
-
- HY-137813
-
|
|
PERK
|
Neurological Disease
Metabolic Disease
Cancer
|
|
PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC 50 of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states .
|
-
- HY-B0099S
-
-
- HY-P1396A
-
|
|
G Protein-coupled Receptor Kinase (GRK)
|
Others
|
|
GRK2i TFA is a GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. GRK2i TFA corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist .
|
-
- HY-B0167R
-
-
- HY-155765
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 51 (compound 11d) is an amide/sulfonamide derivative with anti-inflammatory activities. Anti-inflammatory agent 51 inhibits NF-κB activation, has the potential for acute lung injury and ulcerative colitis research .
|
-
- HY-125354
-
|
|
Caspase
|
Cancer
|
|
Limonin glucoside can be isolated from seeds of Citrus reticulata. Limonin glucoside induces activation of caspase-3. Limonin glucoside inhibits the proliferation of human colon adenocarcinoma (SW480) cells (IC50: 37.39 μM) .
|
-
- HY-122881
-
|
JTP-0819958
|
IKK
|
Cancer
|
|
HOIPIN-1 (JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM . HOIPIN-1 suppress LUBAC-mediated NF-kB activation in vitro .
|
-
- HY-15214
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
|
-
- HY-161604
-
-
- HY-15214A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
|
-
- HY-N6748
-
-
- HY-153967
-
BLU0588
1 Publications Verification
|
PKA
|
Cancer
|
|
BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research .
|
-
- HY-N0003
-
|
NSC 293100
|
Akt
Autophagy
HCV
ERK
|
Cancer
|
|
Honokiol is a bioactive, biphenolic phytochemical that possesses potent antioxidative, anti-inflammatory, antiangiogenic, and anticancer activities by targeting a variety of signaling molecules. It inhibits the activation of Akt. Honokiol can readily cross the blood brain barrier .
|
-
- HY-173272
-
|
|
PAI-1
|
Cardiovascular Disease
|
|
BT-114143 is a plasminogen activation inhibitor, with an IC50 of 8.42 μM. BT-114143 can be used in the research of hemorrhagic diseases caused by hyperfibrinolysis, such as traumatic bleeding, severe menstrual bleeding, postpartum hemorrhage, and complications of hemophilia .
|
-
- HY-19700S
-
|
|
MEK
ERK
Endogenous Metabolite
|
Others
|
|
trans-Zeatin-d5 is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
|
-
- HY-118086
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Cancer
|
|
MRS 1067 is a competitive antagonist of the adenosine A3 receptor that inhibits the suppression of adenylate cyclase by adenosine A3 receptor agonists and affects the activation of G proteins. MRS 1067 can be used in research related to inflammation and cancer .
|
-
- HY-125522
-
|
|
ERK
Apoptosis
|
Inflammation/Immunology
|
|
Methyl helicterate is a triterpenoid, that can be isolated from Helicteres angustifolia (Sterculiaceae). Methyl helicterate inhibits hepatic stellate cell activation and promotes cell apoptosis through downregulating the ERK1/2 signaling pathway .
|
-
- HY-N0499
-
|
IdB 1027
|
RANKL/RANK
|
Cancer
|
|
Cyanidin Chloride (IdB 1027), a subclass of anthocyanin, displays antioxidant and anti-carcinogenesis properties. Cyanidin Chloride (IdB 1027) inhibits osteoclast formation, hydroxyapatite resorption, and receptor activator of NF-κB ligand (RANKL)-induced osteoclast marker gene expression .
|
-
- HY-N0840
-
|
(-)-Bruceantin; NCI165563; NSC165563
|
c-Myc
Caspase
Mitochondrial Metabolism
Apoptosis
Parasite
|
Infection
Cancer
|
|
Bruceantin ((-)-Bruceantin) is a quassinoid found in B. javanica. Bruceantin activates caspase signaling pathway, causes the mitochondrial dysfunction, inhibits cell proliferation, induces cell differentiation and apoptosis. Bruceantin exhibits anti-leukemia and antiprotozoal activities .
|
-
- HY-N11058
-
|
|
Lipoxygenase
NO Synthase
|
Inflammation/Immunology
|
|
Damnacanthol is a natural product that can be isolated from Damnacanthus major . Damnacanthol has anti-15-lipoxygenase activity and can inhibit nitric oxide production in LPS-activated macrophages RAW 264.7 cells .
|
-
- HY-116704
-
-
- HY-N0826R
-
-
- HY-105940
-
|
|
Amino Acid Derivatives
|
Cardiovascular Disease
|
|
IQB-782 is a cysteine derivative. IQB-782 has inhibition for thrombin activatable fibrinolysis inhibitor (TAFI), with an Ki(app) of 0.14 μM. IQB-782 shows a potent mucolytic-expectorant activity .
|
-
- HY-13757AS1
-
|
ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
Apoptosis
Autophagy
HSP
|
Cancer
|
|
Tamoxifen-d3 is the deuterium labeled Tamoxifen . 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-164501
-
|
|
Apoptosis
Mps1
Mitosis
|
Cancer
|
|
Mps-BAY1 is an MPS1 inhibitor with anticancer activity. Mps-BAY1 inhibits cell proliferation and induces apoptosis by activating mitotic catastrophe in cancer cells, generating global aneuploidy and polyploidy. Mps-BAY1 can be used in the study of colorectal cancer and cervical cancer .
|
-
- HY-N13191
-
|
Ingenol 3-benzoate
|
PKC
|
Others
|
|
Ingenol 3-monobenzoate (Ingenol 3-benzoate) is a disgust inducing agent. Ingenol 3-monobenzoate can bind to and activate PKC (Ki=0.14 nM), inhibit the gene expression of phosphoenolpyruvate carboxykinase, thereby inhibiting gluconeogenesis, and increasing blood cortisol levels, producing food aversion .
|
-
- HY-N0722
-
|
trans-5-O-Caffeoylquinic acid
|
NF-κB
Interleukin Related
TNF Receptor
COX
|
Inflammation/Immunology
Cancer
|
|
Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and IL-1β. Neochlorogenic acid suppresses iNOS and COX-2 protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.
|
-
- HY-101084
-
|
|
EGFR
Histone Acetyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR . NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM .
|
-
- HY-16677A
-
|
MDL72974A
|
Monoamine Oxidase
|
Neurological Disease
|
|
Mofegiline hydrochloride (MDL72974A) is an orally active and selective enzyme-activated irreversible inhibitor of MAO-B, with marked selectivity on the MAO-B over MAO-A with IC50s of 3.6 nM (MAO-B) and 680 nM (MAO-A), respectively. Mofegiline hydrochloride is also an inhibitor of semicarbazide-sensitive amine oxidase (SSAO) .
|
-
- HY-162333
-
-
- HY-W010270A
-
-
- HY-N2892
-
|
Aristololactam A IIIa; Sch 546909
|
DYRK
|
Cardiovascular Disease
Cancer
|
|
Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid that can be isolated from Glycosmis chlorosperma. Aristolactam A IIIa is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells .
|
-
- HY-159605
-
|
|
Autophagy
JNK
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Autophagy inducer 5 (compound 21o) is a potent MCF-7 inhibitor (IC50: 2 μM), and a potential breast cancer inhibitor. Autophagy inducer 5 induces cellular autophagy by activating the ROS/JNK signaling pathway, which increases ROS generation and JNK phosphorylation, exerting cytotoxic effects .
|
-
- HY-161062
-
|
|
EAAT
|
Neurological Disease
|
|
TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death .
|
-
- HY-P5182
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity .
|
-
- HY-114277A
-
|
AMG-510 racemate
|
Ras
p38 MAPK
|
Cancer
|
|
Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research .
|
-
- HY-10999S2
-
|
GSK1120212-13C,d3; JTP-74057-13C,d3
|
Isotope-Labeled Compounds
MEK
Autophagy
Apoptosis
|
Cancer
|
|
Trametinib- 13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis .
|
-
- HY-N3005
-
|
|
Apoptosis
Autophagy
NOD-like Receptor (NLR)
Pyroptosis
|
Inflammation/Immunology
Cancer
|
|
Britannin is an NLRP3 inhibitor with an IC50 of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics .
|
-
- HY-143235
-
|
|
Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
|
Cancer
|
|
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
|
-
- HY-160876
-
|
|
Keap1-Nrf2
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
BC-1901S is a proteasome-independent NRF2 activator and stabilizer. BC-1901S binds to DCAF1 (E3 ligase subunit) and disrupts NRF2/DCAF1 interaction, and activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner. BC-1901S shows anti-inflammatory effect in a murine model of LPS-induced acute lung injury .
|
-
- HY-107818R
-
|
|
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
4-Hydroxychalcone (Standard) is the analytical standard of 4-Hydroxychalcone. This product is intended for research and analytical applications. 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-P990025
-
|
ARGX-117
|
Complement System
|
Inflammation/Immunology
|
|
Empasiprubar (ARGX-117) is a humanized inhibitory monoclonal antibody targeting complement C2. Empasiprubar binds to the Sushi-2 domain of C2, preventing the formation of C3 pre convertase and inhibiting the activation of classical and lectin pathways upstream of C3 activation. Empasiprubar can prevent complement mediated autoimmune hemolytic anemia and antibody mediated organ transplant rejection. Empasiprubar can prevent neuroglial lymphoconjunctival injury in GM1 antibody mediated mouse models .
|
-
- HY-W040055
-
|
D-(+)-Neopterin; D-erythro-Neopterin
|
NF-κB
PPAR
ERK
Raf
Src
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Neopterin is an immune system activator metabolized by GTP and can be produced by activated macrophages. Neopterin has the potential to resist vascular inflammation and atherosclerosis. Neopterin inhibits the phosphorylation of NF-κB and promotes the expression of PPAR-γ, thereby suppressing the inflammatory response of vascular endothelial cells, reducing the formation of macrophage foam cells, and regulating the migration and proliferation of vascular smooth muscle cells. Neopterin can be used in research fields such as cardiovascular diseases (such as atherosclerosis), inflammation-related diseases and tumor immunomonitoring .
|
-
- HY-126675A
-
|
|
CDK
STAT
|
Inflammation/Immunology
|
|
AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene .
|
-
- HY-133095
-
|
|
STAT
PPAR
|
Inflammation/Immunology
|
|
BML-260 is a potent inhibitor of dual-specific phosphatases JSP-1 and DUSP22. BML-260 can activate UCP1 and thermogenesis in adipocytes in a JSP-1-independent manner. The effect of BML-260 on adipocytes is partially achieved through the activation of CREB, STAT3, and PPAR signaling pathways. BML-260 can be used in the research of inflammatory and proliferative disorders associated with JNK signaling dysfunction as well as obesity .
|
-
- HY-101287
-
|
|
Microtubule/Tubulin
JNK
Apoptosis
Caspase
|
Cancer
|
|
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line .
|
-
- HY-B0722
-
|
|
Endogenous Metabolite
Reactive Oxygen Species (ROS)
|
Metabolic Disease
Cancer
|
|
Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .
|
-
- HY-147082
-
GA-017
2 Publications Verification
|
YAP
|
Cancer
|
|
GA-017 is a potent and selective LATS1 and LATS2 (large tumor suppressor kinase 1/2) inhibitor, with IC50 values of 4.10 and 3.92 nM, respectively. GA-017 is an activator of cell proliferation. GA-017 promotes YAP/TAZ activation and nuclear translocation. GA-017 promotes cell growth under 3D culture conditions. GA-017 enhances the ex vivo formation of mouse intestinal organoids .
|
-
- HY-119013
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
VPC32183 is a competitive antagonist of LPA1 and LPA3 receptors. The activity of VPC32183 can inhibit lipid phosphatase 1 (LPP1), thereby preventing the activation of ERK(1/2) by dioctanoic acid diglyceride (DGPP 8:0). By reducing the expression of LPP1, VPC32183 can further reduce DGPP 8:0-induced ERK(1/2) activation. The effects of VPC32183 suggest that it may have a positive regulatory function in cell signaling processes .
|
-
- HY-P3641
-
|
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
|
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
|
-
- HY-10255R
-
|
SU 11248 Malate (Standard)
|
Reference Standards
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (Malate) (Standard) is the analytical standard of Sunitinib (Malate). This product is intended for research and analytical applications. 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-10219R
-
|
Sirolimus (Standard); AY-22989 (Standard)
|
Reference Standards
mTOR
FKBP
Fungal
Autophagy
Endogenous Metabolite
Antibiotic
Bacterial
|
Cancer
|
|
Rapamycin (Standard) is the analytical standard of Rapamycin. This product is intended for research and analytical applications. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .
|
-
- HY-117656
-
ESI-05
3 Publications Verification
NSC 116966
|
Acyltransferase
|
Neurological Disease
Metabolic 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-112700
-
|
|
Phosphatase
|
Neurological Disease
|
|
SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 μM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease .
|
-
- HY-102073
-
|
|
Glutaminase
Integrin
FAK
Src
|
Cancer
|
|
TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research .
|
-
- HY-122727
-
|
|
DNA-PK
Apoptosis
|
Cancer
|
|
STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor with an IC50 of 3.5 μM. STL127705 interferes the binding of Ku70/80 to DNA and by inhibits the activation of the DNA-PKCS kinase. STL127705 shows antiproliferative and anticancer activity. STL127705 induces apoptosis .
|
-
- HY-18259
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
103D5R (Compound 15) is an inhibitor for the activation of hypoxia-inducible factor-1 (HIF-1) with an IC50 of 35 µM, through reduction of the HIF-1α protein synthesis. 103D5R inhibits the proliferation of LN229 with IC50 of 26 µM .
|
-
- HY-101997
-
|
|
Apoptosis
Caspase
|
Infection
Cancer
|
|
BEPP hydrochloride is a double-stranded RNA-dependent protein kinase (PKR) inducer and antiviral agent. BEPP hydrochloride effectively inhibits the growth of human lung cancer cell lines overexpressing PKR and induces apoptosis and activates caspase-3 in sensitive cells. In addition, BEPP hydrochloride can also significantly inhibit vaccinia virus replication .
|
-
- HY-149652
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
IRF5-IN-1 (Compound C5) is a conformationally locked inhibitor for SLC15A4. IRF5-IN-1 blocks the downstream IRF5 activation, inhibits the TLR7/8 signaling pathway. IRF5-IN-1 exhibits anti-inflammatory responses .
|
-
- HY-155864
-
-
- HY-116626
-
|
|
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-122936
-
|
|
Histone Methyltransferase
Keap1-Nrf2
Sirtuin
|
Cardiovascular Disease
Cancer
|
|
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .
|
-
- HY-152949
-
|
|
Myosin
|
Neurological Disease
|
|
Myosin V-IN-1 (compound 8) is a potent and selective Myosin V inhibitor, with a Ki of 6 μM. Myosin V-IN-1 shows acute inhibition of myosin V. Myosin V-IN-1 slows the actin-activated myosin V ATPase by specifically inhibiting ADP release from the actomyosin complex .
|
-
- HY-113592
-
|
|
ERK
|
Cancer
|
|
ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2 .
|
-
- HY-123669A
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Trans-R-138727 is the trans isomer of R-138727 (HY-123669). R-138727 is the active metabolite of the antiplatelet agent Prasugrel (HY-15284). R-138727 is an irreversible inhibitor for the platelet receptor P2Y12, and inhibits ADP-induced platelet activation and aggregation .
|
-
- HY-116664
-
|
|
Apoptosis
Ras
Raf
Caspase
|
Cancer
|
|
DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer .
|
-
- HY-129239
-
|
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice .
|
-
- HY-118482
-
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Saurolactam
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Others
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Neurological Disease
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Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells . Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation .
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- HY-131649
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DNA/RNA Synthesis
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Cancer
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Compound C108 is a G3BP2 inhibitor. Compound C108 also targeted stress granule-associated proteins and Gtpase-activating protein (SH3 domain) binding protein 2. Compound C108 potently inhibits esophageal squamous cell carcinoma (ESCC) cell metastasis .
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- HY-A0042R
-
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CGP 33101 (Standard); E 2080 (Standard); RUF 331 (Standard)
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Sodium Channel
Reference Standards
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Neurological Disease
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Rufinamide (Standard) is the analytical standard of Rufinamide (HY-A0042). This product is intended for research and analytical applications. Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
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- HY-135231
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NL-1
3 Publications Verification
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Mitochondrial Metabolism
Autophagy
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Cancer
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NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 μM and 56.26 μM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway .
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- HY-151629
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Others
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Cancer
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MRV03-069 (Compound 3) is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-069 can be used in colorectal cancer research .
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- HY-N5018
-
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Musizin
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Parasite
AMPK
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Infection
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Nepodin (Musizin) is a quinone oxidoreductase (PfNDH2) inhibitor isolate from Rumex crispus .Nepodin (Musizin) stimulates the translocation of GLUT4 to the plasma membrane by activation of AMPK .Nepodin (Musizin) has antidiabetic and antimalarial activities.
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- HY-135702
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NF-κB
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Others
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UBS109, as a curcumin analogue, can promote the differentiation and mineralization of osteoblasts. UBS109 shows to regulate bone cell function by activating Smad and inhibiting NF-kB. UBS109 can be used in bone tissue engineering and osteoporosis research .
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- HY-118618
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Hiyodorilactone A; Schkuhrin I
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STAT
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Cancer
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Eucannabinolide is a STAT3 inhibitor. Eucannabinolide suppresses STAT3 activation at tyrosine 705, inhibiteds its translocation to nucleus, and decreases its DNA binding capacity. Eucannabinolide can be used for triple negative breast cancer (TNBC) diseases research .
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- HY-108163A
-
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Calcium Channel
Potassium Channel
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Neurological Disease
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SB-237376 is a blocker of potassium and calcium channels. SB-237376 inhibits the rapidly activating delayed rectifier potassium current I(Kr) (IC50: 0.42 μM) and blocks the L-type calcium current I(Ca,L) at high concentrations .
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- HY-111036
-
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TRP Channel
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Others
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AMG0347 is a transient receptor potential type V1 receptor antagonist. AMG0347 inhibits activation of the rat TRPV1 channel by heat (IC50 = 0.2 nm), protons (IC50= 0.8 nm), or capsaicin (IC50 = 0.7 nm) .
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- HY-18330
-
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MDM-2/p53
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Cancer
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MI 63 is an activator for p53, by targeting the MDM2 (Ki is 3 nM). MI 63 inhibits the proliferation of embryonic and alveolar rhabdomyosarcoma (ERMS and ARMS) cells (IC50 is 0.58 μM in RH36 cells), and induces apoptosis in ERMS and ARMS .
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- HY-19820
-
|
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Akt
Ser/Thr Protease
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Neurological Disease
Cancer
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NSC45586 is an inhibitor of pleckstrin homology domain and leucine-rich repeat protein phosphatase (PHLPP). NSC45586 targets the PP2C phosphatase domain in PHLPP1 and PHLPP2. NSC45586 can activate AKT in neurons .
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- HY-B0649R
-
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2,6-Diisopropylphenol (Standard)
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Reference Standards
GABA Receptor
Endogenous Metabolite
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Neurological Disease
Cancer
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Propofol (Standard) is the analytical standard of Propofol. This product is intended for research and analytical applications. Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic .
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- HY-149055
-
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CXCR
|
Inflammation/Immunology
|
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ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11 .
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- HY-B0289S
-
-
- HY-N13138
-
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NO Synthase
|
Inflammation/Immunology
|
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Angulasaponin B, a natural product, can be obtained from Vigna angularis. Angulasaponin B inhibits nitric oxide production in LPS-activated RAW264.7 macrophages with IC50 values ranging from 13 μM to 24 μM .
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-
- HY-P3204A
-
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AL-78898A TFA
|
Complement System
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Metabolic Disease
|
|
POT-4 TFA (AL-78898A TFA), a Compstatin derivative, is a potent inhibitor of complement factor C3 activation. POT-4 TFA can be used for age-related macular degeneration research .
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-
- HY-135042
-
|
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Toll-like Receptor (TLR)
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Neurological Disease
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CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model .
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- HY-N6679A
-
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HSP
TGF-beta/Smad
|
Infection
Cancer
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10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity .
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-
- HY-W011102
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NSC 83265; S-Tritylcysteine; 3-Tritylthio-L-alanine
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Kinesin
Apoptosis
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Cancer
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S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities .
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-
- HY-119339
-
|
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CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity .
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-
- HY-19820A
-
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Akt
Ser/Thr Protease
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Neurological Disease
Cancer
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NSC45586 sodium is an inhibitor of pleckstrin homology domain and leucine-rich repeat protein phosphatase (PHLPP). NSC45586 sodium targets the PP2C phosphatase domain in PHLPP1 and PHLPP2. NSC45586 sodium can activate AKT in neurons .
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-
- HY-B0285B
-
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MK-870 hydrochloride dihydrate
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Sodium Channel
Apoptosis
TRP Channel
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Cardiovascular Disease
Metabolic Disease
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Amiloride hydrochloride dihydrate (MK-870 hydrochloride dihydrate) is an inhibitor of both epithelial sodium channel (ENaC ) and urokinase-type plasminogen activator receptor (uTPA ). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2 ) channel.
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-
- HY-151628
-
|
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Others
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Cancer
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MRV03-068 (Compound 2) is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-068 can be used in colorectal cancer research .
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- HY-W725955
-
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BMS-663068 sodium
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HIV
|
Infection
|
|
Fostemsavir sodium (BMS-663068 sodium) is an HIV-1 attachment inhibitor with antiviral activity against multidrug-resistant HIV-1. Co-inhibition with fostemsavir sodium also showed a trend toward reduction in markers of monocyte activation and coagulation abnormalities .
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-
- HY-155487
-
|
|
ROR
|
Neurological Disease
Inflammation/Immunology
|
|
JTE-151 is a RORγ inhibitor, which can suppress overactive immune response through inhibition of RORγ related to the activation of Th17 cells, making JTE-151 possible to be used in autoimmune disease research .
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-
- HY-N0629R
-
|
Crategolic acid (Standard); 2α-Hydroxyoleanolic acid (Standard)
|
Reference Standards
NF-κB
Bacterial
HIV
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Maslinic acid (Standard) is the analytical standard of Maslinic acid. This product is intended for research and analytical applications. Maslinic acid can inhibit the DNA-binding activity of NF-κB p65 and abolish the phosphorylation of IκB-α, which is required for p65 activation.
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- HY-N2078
-
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Neodiosgenin
|
LXR
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Metabolic Disease
|
|
Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes .
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-
- HY-158312
-
-
- HY-N0112S
-
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Ampelopsin-d4; Ampeloptin-d4
|
Isotope-Labeled Compounds
Autophagy
Influenza Virus
mTOR
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Dihydromyricetin-d4 (Ampelopsin-d4) is deuterium labeled Dihydromyricetin. Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
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-
- HY-12810
-
|
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Ras
|
Cancer
|
|
EHop-016 is a potent and selective Rac GTPase Rac1 and Rac3 inhibitor. EHop-016 inhibits Rac1 activity with an IC50 of 1.1 μM in MDA-MB-435 cells. EHop-016 inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration .
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-
- HY-114511
-
|
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Factor VIIa
|
Cardiovascular Disease
|
|
BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT) .
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- HY-172816
-
|
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Carbonic Anhydrase
mTOR
NKCC
|
Neurological Disease
|
|
Carbonic anhydrase inhibitor 32 (compound 5B) is an orally active and selective hCA (Carbonic anhydrase ) II/VII inhibitor with the Ki values of 6.3 nM, 10.1 nM and 681 nM for hCA II, hCA VII and hCA I,respectively. Carbonic anhydrase inhibitor 32 shows neuroprotective and anticonvulsant potential by reducing mTOR activation, and raising hippocampus KCC2 levels .
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-
- HY-Y0586
-
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Asaronic acid
|
NF-κB
STAT
|
Metabolic Disease
Inflammation/Immunology
|
|
2,4,5-Trimethoxybenzoic acid (Asaronic acid) is a compound identified in purple perilla extracts. 2,4,5-Trimethoxybenzoic acid inhibits LPS (HY-D1056)-induced inflammatory responses, inhibits the activation of NF-κB and STAT signaling pathways. 2,4,5-Trimethoxybenzoic acid inhibits M1 macrophage phenotype-mediated inflammation in diabetes .
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- HY-151252
-
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Proteasome
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β .
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-
- HY-155978A
-
|
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Tyrosinase
|
Inflammation/Immunology
|
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RDN2150 (Compound 25) TFA is a ZAP-70 inhibitor (IC50: 14.6 nM). RDN2150 TFA covalently binds to the C346 residue of ZAP-70. RDN2150 TFA inhibits the expression of CD25 and CD69, and inhibits CD4 + T cell activation. RDN2150 TFA can be used for research of psoriasis .
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-
- HY-N2006R
-
|
|
EBV
Reference Standards
HIV Protease
|
Infection
Inflammation/Immunology
|
|
Ganoderic acid B (Standard) is the analytical standard of Ganoderic acid B. This product is intended for research and analytical applications. Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease (IC50: 170 μM) .
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- HY-N0112R
-
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Ampelopsin (Standard); Ampeloptin (Standard)
|
Reference Standards
mTOR
Influenza Virus
DNA/RNA Synthesis
Autophagy
|
Infection
Cancer
|
|
Dihydromyricetin (Standard) is the analytical standard of Dihydromyricetin. This product is intended for research and analytical applications. Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
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-
- HY-12495A
-
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|
Biochemical Assay Reagents
Eukaryotic Initiation Factor (eIF)
|
Neurological Disease
|
|
ISRIB is a brain-penetrant inhibitor of integrated stress response (ISR). Persistent activation of the ISR has been linked to the development of several neurological disorders as ISR represses translation through inhibiting eIF2B. ISRIB inhibits the ISR by promoting the nucleotide exchange activity of eIF2B and recovering the translation, and thus can be used for neurological disorders research .
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-
- HY-B0167AR
-
|
Salicylic acid sodium salt (Standard); 2-Hydroxybenzoic acid sodium salt (Standard)
|
Reference Standards
COX
NF-κB
Ribosomal S6 Kinase (RSK)
Autophagy
Apoptosis
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Sodium Salicylate (Standard) is the analytical standard of Sodium Salicylate. This product is intended for research and analytical applications. Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation . Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle .
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-
- HY-14654
-
-
- HY-101761
-
|
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PAI-1
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-148510
-
|
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Phosphatase
Apoptosis
Akt
ERK
Reactive Oxygen Species (ROS)
|
Cancer
|
|
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 induces apoptosis. HKB99 inhibits the formation of invasive pseudopodia and inhibits migration. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC) .
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-
- HY-111766
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
YD-3 is a platelet activation inhibitor. YD-3 inhibits Thrombine-induced rabbit platelets aggregation (IC50: 28.3 μM) and phosphoinositol production. In addition, YD-3 also inhibits Trypsin-induced platelet aggregation in human and rabbit with the IC50 of 38.1 μM and 5.7 μM, respectively, but does not affect the proteolytic activity of trypsin .
|
-
- HY-110189S1
-
|
3β-Hydroxy-5-pregnen-20-one monosulfate-d4 sodium
|
Isotope-Labeled Compounds
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate-d4 (sodium) is the deuterium labeled Pregnenolone monosulfate. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
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-
- HY-N11009
-
|
|
EBV
|
Infection
|
|
11-Oxomogroside II A1 (compound 7) is an oxidized cucurbitin. It can be isolated from the ethanol extract of Rohanberry fruit. 11-Oxomogroside II A1 inhibits the activation of Epstein-Barr virus (EBV) early antigen (EBV-EA) induced by 12-O-tetradecanoylphorbol-13-acetate (TPA). 11-Oxomogroside II A1 also weakly inhibits the activation of (±)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor .
|
-
- HY-109041
-
|
AKB-9778
|
Phosphatase
Tie
|
Inflammation/Immunology
|
|
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
|
-
- HY-W778408
-
|
ICI 47699-13C6; (Z)-Tamoxifen-13C6; trans-Tamoxifen-13C6
|
Isotope-Labeled Compounds
Apoptosis
Autophagy
HSP
Estrogen Receptor/ERR
|
Endocrinology
|
|
Tamoxifen- 13C6 (ICI 47699- 13C6) is the 13C-labeled Tamoxifen (HY-13757A). 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 transgenic mouse .
|
-
- HY-141645
-
|
WS070117
|
AMPK
TGF-β Receptor
NF-κB
JNK
AP-1
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
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-113469B
-
|
|
STING
Endogenous Metabolite
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
Cyclic GMP TBAOH is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP TBAOH can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP TBAOH may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP TBAOH, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP TBAOH can be used in the study of antiviral immunity and cardiovascular diseases .
|
-
- HY-113469R
-
|
|
STING
Endogenous Metabolite
Reference Standards
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
Cyclic GMP (Standard) is the analytical standard of Cyclic GMP. This product is intended for research and analytical applications. Cyclic GMP is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP can be used in the study of antiviral immunity and cardiovascular diseases.
|
-
- HY-113469A
-
|
|
STING
Endogenous Metabolite
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
Cyclic GMP (cGAMP) sodium is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP sodium can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP sodium may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP sodium, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP sodium can be used in the study of antiviral immunity and cardiovascular diseases .
|
-
- HY-113469
-
|
|
STING
Endogenous Metabolite
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
Cyclic GMP (cGAMP) is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. cGMP may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of cyclic GMP (cGMP), 8-Br-cGMP, has antiplatelet activity, and cyclic GMP can be used in the study of antiviral immunity and cardiovascular diseases .
|
-
- HY-13757AR
-
|
ICI 47699(Standard); (Z)-Tamoxifen(Standard); trans-Tamoxifen (Standard)
|
Reference Standards
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Endocrinology
Cancer
|
|
Tamoxifen (Standard) is the analytical standard of Tamoxifen (HY-13757A). This product is intended for research and analytical applications. 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-168650
-
|
|
ROCK
HDAC
|
Inflammation/Immunology
Cancer
|
|
ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity .
|
-
- HY-N4205
-
|
|
Cytochrome P450
|
Cancer
|
|
Tetrahydropiperine is an orally effective, selective inhibitor of NF-κB and MAPKs<、b>, and an activator of the PI3K/Akt/mTOR<、b> pathway. Tetrahydropiperine reduces the production of pro-inflammatory cytokines such as TNF-α, IL-6, and nitric oxide (NO) by inhibiting the nuclear translocation of NF-κB and the phosphorylation of MAPKs such as ERK, JNK, and p38. At the same time, Tetrahydropiperine inhibits excessive autophagy by activating the PI3K/Akt/mTOR pathway, protecting neurons from oxidative damage. Tetrahydropiperine has anti-inflammatory, anti-apoptotic, and neuroprotective effects, and is mainly used in the study of inflammatory diseases (such as endotoxemia, arthritis) and neurological diseases such as ischemic stroke .
|
-
- HY-13559
-
|
Azaspirane
|
Apoptosis
|
Cancer
|
|
Atiprimod (Azaspirane) is an orally bioavailable small molecule with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) by inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3). Atiprimod also downregulates the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB transcription factors .
|
-
- HY-N6953
-
|
|
STAT
Keap1-Nrf2
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC50 for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer .
|
-
- HY-50937
-
|
|
MyD88
|
Inflammation/Immunology
|
|
ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity .
|
-
- HY-N8218
-
-
- HY-118979
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
L-691678 can bind to FLAP by recognizing the amino acid residues of 5-lipoxygenase-activating protein (FLAP), thereby inhibiting leukotriene biosynthesis. L-691678 can be used in the study of leukotriene-related diseases such as allergies, asthma, and inflammation .
|
-
- HY-101255R
-
|
|
Reference Standards
Guanylate Cyclase
Apoptosis
|
Cancer
|
|
ODQ (Standard) is the analytical standard of ODQ. This product is intended for research and analytical applications. 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-N3711
-
|
|
JNK
ERK
Apoptosis
|
Neurological Disease
|
|
Dehydrocrenatidine, a β-carboline alkaloid that can be isolated from Picrasma quassioides. Dehydrocrenatidine induces cell apoptosis by activates ERK and JNK. Dehydrocrenatidine inhibits invasion and migration of cancer cells, it also suppresses neuronal excitability to exert analgesic effects .
|
-
- HY-13030
-
-
- HY-13772R
-
|
AD-32 (Standard)
|
Reference Standards
PKC
Antibiotic
|
Inflammation/Immunology
Cancer
|
|
Valrubicin (Standard) is the analytical standard of Valrubicin. This product is intended for research and analytical applications. Valrubicin is a chemotherapy agent, inhibits TPA-and PDBu-induced PKC activation with IC50s of 0.85 and 1.25 μM, respectively, and has antitumor and antiinflammatory activity.
|
-
- HY-N0168AS
-
-
- HY-141550
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP .
|
-
- HY-124156A
-
|
|
Wnt
|
Metabolic Disease
|
|
KY-02327 acetate, a metabolically stabilized KY-02061 analog, is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 acetate shows an activating effect on the Wnt/β-catenin pathway, resulting in promotion of osteoblast differentiation .
|
-
- HY-158145
-
|
|
Phospholipase
|
Cancer
|
|
DS55980254 is the orally active inhibitor for phosphatidylserine synthase 1 (PTDSS1) that blocks the synthesis of intracellular phosphatidylserine. PTDSS1 deficiency affects the balance of cell membrane phospholipid components, and activates B cell receptor (BCR) signaling pathway .
|
-
- HY-N0436R
-
|
|
Reference Standards
NF-κB
|
Infection
Inflammation/Immunology
|
|
Engeletin (Standard) is the analytical standard of Engeletin. This product is intended for research and analytical applications. 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-77293
-
|
|
Apoptosis
Keap1-Nrf2
|
Cancer
|
|
(E)-[6]-Dehydroparadol, an oxidative metabolite of [6]-Shogaol (HY-14616), is a potent Nrf2 activator. (E)-[6]-Dehydroparadol can inhibit the growth and induce the apoptosis of human cancer cells .
|
-
![(E)-[6]-Dehydroparadol](//file.medchemexpress.com/product_pic/hy-77293.gif)
- HY-N1469R
-
|
|
Reference Standards
Potassium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Kaurenoic acid (Standard) is the analytical standard of Kaurenoic acid. This product is intended for research and analytical applications. Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway .
|
-
- HY-139361
-
|
PIN1-3
|
PIN1
|
Cancer
|
|
Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors .
|
-
- HY-120294
-
|
|
CGRP Receptor
TRP Channel
|
Neurological Disease
|
|
Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research .
|
-
- HY-120560
-
|
|
MAGL
|
Neurological Disease
|
|
OMDM169 is a potent and selective monoacylglycerol lipase (MAGL) inhibitor with activity to increase 2-AG levels. OMDM169 exerts analgesic activity through indirect activation of cannabinoid receptors. The effective concentration of OMDM169 is 0.13 μM .
|
-
- HY-129087
-
|
|
Apoptosis
|
Cancer
|
|
BC-1258，an F-box/LRR-repeat protein 2 (FBXL2) activator，can stabilize and upregulate FBXL2 levels. BC-1258 induces apoptosis of tumorigenic cells，and profoundly inhibits tumor formation in mice .
|
-
- HY-161840
-
|
|
FGFR
|
Cancer
|
|
Antitumor agent-176 (Compound 22), an antitumor agent, can effectively bind to FGF2 and inhibit the activation of fibroblast growth factor receptor (FGFR) in multiple myeloma (MM) cells, exhibiting significant antitumor activity both in vivo and in vitro against MM .
|
-
- HY-N0708R
-
|
|
Reference Standards
NF-κB
Bacterial
Endogenous Metabolite
|
Infection
Inflammation/Immunology
|
|
Vanillic acid (Standard) is the analytical standard of Vanillic acid. This product is intended for research and analytical applications. Vanillic acid is a flavoring agent found in edible plants and fruits, also found in Angelica sinensis. Vanillic acid inhibits NF-κB activation. Anti-inflammatory, antibacterial, and chemopreventive effects .
|
-
- HY-127002
-
|
|
Src
|
Cancer
|
|
Squarunkin A is a potent and selective UNC119-cargo interaction inhibitor, interrupting the UNC119A-myristoylated Src N-terminal peptide interaction (IC50=10 nM). Squarunkin A interferes with the activation of Src kinase in cells .
|
-
- HY-B0464
-
|
|
Bcl-2 Family
Caspase
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Hydralazine hydrochloride is an antihypertensive agent. Hydralazine hydrochloride can inhibit mitochondrial fission and human peritoneal mesothelial cell proliferation. Hydralazine hydrochloride has immunomodulation and anti-migratory effect. Hydralazine hydrochloride activates the intrinsic pathway of apoptosis and causes DNA damage .
|
-
- HY-P99904
-
|
MEDI-507
|
CD2
|
Inflammation/Immunology
Cancer
|
|
Siplizumab (MEDI-507) is a humanized IgG1 monoclonal antibody against CD2. Siplizumab depletes T cells, decreases T cell activation, inhibites T cell proliferation and enriches naïve and bona fide regulatory T cells .
|
-
- HY-124156
-
|
|
Wnt
|
Metabolic Disease
|
|
KY-02327, a metabolically stabilized KY-02061 analog, is a potent Dishevelled (Dvl)-CXXC5 interaction inhibitor. KY-02327 shows an activating effect on the Wnt/β-catenin pathway, resulting in promotion of osteoblast differentiation .
|
-
- HY-32735S
-
|
PG490-d3
|
Isotope-Labeled Compounds
NF-κB
Apoptosis
|
Cancer
|
|
Triptolide-d3 is the deuterium labeled Triptolide. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor .
|
-
- HY-114335
-
|
|
NF-κB
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Triphala, an Ayurvedic polyherbal formulation comprising of equiproportional fruit parts of Terminalia chebula, Terminalia bellerica, and Phyllanthus emblica . Triphala inhibits NF-κB activation. Triphala exerts antifungal action . Anti-adipogenic, anti-inflammatory, and anti-neoplastic activities.
|
-
- HY-141867
-
|
Z-Phe-Phe-FMK
|
Cathepsin
|
Neurological Disease
|
|
Z-FF-FMK is a selective cathepsin-L inhibitor. Z-FF-FMK can prevent β-amyloid to induce apoptotic changes such as activation of caspase-3, cleavage of the DNA repair enzyme, poly-ADP ribose polymerase, and DNA fragmentation .
|
-
- HY-169162
-
|
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Neurological Disease
|
|
hBChE-IN-3 (compound 30) is a combination of carbonic anhydrase (CA) activator and cholinesterase (ChE) inhibitor with IC50 values of 7.4 and 1.9 nM for AchE and BchE, respectively. hBChE-IN-3 can be used in the study of neurodegeneration and psychiatric disorders .
|
-
- HY-34431
-
|
7H-Imidazo(4,5-d)pyrimidine
|
Endogenous Metabolite
PARP
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Purine is an endogenous metabolite. Purine bases are the building blocks of the nucleic acids. Purine inhibits the activation of PARP. Purine protects against oxidant-induced cell injury. Purine can be used in the research of cancer and nervous system diseases .
|
-
- HY-17592R
-
|
|
Reference Standards
Parasite
Bacterial
|
Infection
Cancer
|
|
Bithionol (Standard) is the analytical standard of Bithionol. This product is intended for research and analytical applications. 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-152089
-
-
- HY-B0289R
-
-
- HY-116050
-
-
- HY-P991127
-
|
|
Complement System
|
Inflammation/Immunology
|
|
Claseprubart is a monoclonal antibody targeting human complement C1s. Claseprubart specifically binds to complement C1s to inhibit the activation of the complement system, exerting immunosuppressive activity. Claseprubart is promising for research of autoimmune diseases and inflammation-related diseases .
|
-
- HY-N0822
-
|
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-N2553
-
|
|
LPL Receptor
|
Metabolic Disease
|
|
4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase .
|
-
- HY-124958
-
|
|
NF-κB
Dipeptidyl Peptidase
|
Metabolic Disease
Inflammation/Immunology
|
|
NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene expression. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al .
|
-
- HY-N8884
-
|
|
PTEN
Akt
NF-κB
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein .
|
-
- HY-107613A
-
|
DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride
|
PKC
5-HT Receptor
|
Infection
Inflammation/Immunology
Cancer
|
|
R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
|
-
- HY-101664
-
|
IY-81149
|
Proton Pump
TOPK
|
Inflammation/Immunology
Cancer
|
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
|
-
- HY-107613
-
|
DKGI-I; Diacylglycerol kinase inhibitor I
|
PKC
5-HT Receptor
|
Inflammation/Immunology
|
|
R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
|
-
- HY-14654C
-
-
- HY-149257
-
|
|
JAK
STAT
|
Cancer
|
|
HAT-SIL-TG-1&AT is a Janus tyrosine kinase (JAK) inhibitor with antitumor effects. HAT-SIL-TG-1&AT is the hypoxia-activated prodrug, witch inhibits JAK-STAT signaling in tumor tissue. And HAT-SIL-TG-1&AT inhibits HEL cells proliferation and downregulated phosphorylated STAT3/5 under hypoxic conditions .
|
-
- HY-134901
-
WM-3835
4 Publications Verification
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice .
|
-
- HY-N6771
-
|
|
Calcium Channel
5-HT Receptor
MDM-2/p53
Apoptosis
RSV
|
Infection
|
|
Cyclopiazonic acid is an endoplasmic reticulum calcium ATPase (ECAs) inhibitor and human respiratory syncytial virus (RSV) inhibitor (EC50 value of 4.13 μ M), which can reduce the antagonistic effect of 5-HT receptors in rat thoracic aorta, induce p53 dependent cell apoptosis and reproductive toxicity in mouse testes, and inhibit the biological activation of aflatoxin B [1][4][5].
|
-
- HY-101761A
-
|
|
PAI-1
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-B0689B
-
|
MK-639 ethanolate; L735524 ethanolate
|
Apoptosis
MMP
HIV
HIV Protease
SARS-CoV
|
Infection
Cancer
|
|
Indinavir sulfate ethanolate (MK-639 ethanolate) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir sulfate ethanolate exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir sulfate ethanolate is also a SARS-CoV 3CL pro inhibitor .
|
-
- HY-116683
-
|
MAL2-11B
|
HSP
DNA/RNA Synthesis
|
Infection
Cancer
|
|
116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70 .
|
-
- HY-119234
-
|
|
CXCR
|
Inflammation/Immunology
|
|
CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis .
|
-
- HY-114038
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
SB-747651A is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A can be used for inflammation research .
|
-
- HY-14654B
-
|
Acetylsalicylic acid DL-lysine; ASA DL-lysine
|
COX
NF-κB
p38 MAPK
|
Cardiovascular Disease
Others
Inflammation/Immunology
|
|
Aspirin DL-lysine (ASA DL-lysine) is a lysine-containing aspirin derivative. Aspirin DL-lysine inhibits cyclooxygenase (COX) in platelets, blocks the synthesis of thromboxane A2 (TXA2), and thus inhibits platelet aggregation and activation. Aspirin DL-lysine can be used to study thrombin generation in patients with unstable angina pectoris .
|
-
- HY-149391
-
|
|
PROTACs
Btk
|
Inflammation/Immunology
|
|
PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6) .
|
-
- HY-N6009
-
|
|
Parasite
NF-κB
|
Infection
|
|
8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE) . 8-Deoxygartanin exhibits antiplasmodial activity with an IC50 of 11.8 μM for the W2 strain of Plasmodium falciparum . 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC50 of 11.3 μM .
|
-
- HY-162901
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
NLRP3-IN-48 is an NLRP3 inhibitor. NLRP3-IN-48 targets the NLRP3 protein, affecting the assembly of the NLRP3 inflammasome and thereby inhibiting its activation. NLRP3-IN-48 has anti-inflammatory activity in a mouse model of acute colitis induced by DSS .
|
-
- HY-P5182A
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity .
|
-
- HY-14644B
-
|
STA 5326 hydrochloride; LAM-002A (free base) hydrochloride; AIT-101 hydrochloride
|
NOD-like Receptor (NLR)
|
Infection
Inflammation/Immunology
|
|
Apilimod (STA 5326) hydrochloride is a PIKFYVE kinase inhibitor that promotes NLRP3 inflammatory vesicle activation and IL-1β secretion. Apilimod hydrochloride has been shown to inhibit host cell proteases, which may prevent viral invasion but also block antiviral immune responses, potentially exacerbating immunosuppression in COVID-19.
|
-
- HY-116364
-
|
3'-Azido-3'-deoxythymidine-5'-triphosphate
|
HIV
DNA/RNA Synthesis
HBV
Reactive Oxygen Species (ROS)
Apoptosis
|
Infection
|
|
AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway .
|
-
- HY-118628
-
|
N-(p-Amylcinnamoyl) anthranilic acid; ACA
|
Phospholipase
TRP Channel
|
Cardiovascular Disease
|
|
(E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker . (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia .
|
-
- HY-124514
-
|
|
SOS1
Ras
ERK
|
Cancer
|
|
UC-857993 is a selective SOS1-Ras inhibitor (Kd=14.7 μM, His6-SOS1cat), suppressing catalytic activity. UC-857993 also inhibits ERK and Ras activation, suppresses the growth of mouse embryonic fibroblasts (MEFs) .
|
-
- HY-106428
-
|
ITF1697
|
P-selectin
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Icrocaptide (ITF1697) is a stable Lys-Pro-containing peptide that inhibits the intracellular Ca 2+-dependent fusion of Weibel-Palade bodies with the plasma membrane. Icrocaptide exerts its activity at the early stages of endothelial activation and inhibits P-selectin and von Willebrand factor secretion. Icrocaptide can be used for the study of a variety of microvascular disorders .
|
-
- HY-128588
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research .
|
-
- HY-108355
-
R59949
1 Publications Verification
|
PKC
|
Cancer
|
|
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol .
|
-
- HY-158050
-
|
|
c-Fms
|
Cancer
|
|
PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC .
|
-
- HY-144894
-
|
|
Kinesin
Microtubule/Tubulin
|
Cancer
|
|
AM-5308 is the inhibitor for KIF18A (IC50=47 nM) that inhibits KIF18A-mediated microtubule ATPase activity. AM-5308 activates mitotic checkpoints, regulates cell division processes, including chromosome segregation and spindle assembly. AM-5308 exhibits antitumor activity .
|
-
- HY-138869
-
|
|
Endogenous Metabolite
|
Cancer
|
|
AubipyOMe serves as a potent inhibitor of tartrate-resistant acid phosphatase (TRAP/ACP5), a metalloenzyme found in activated osteoclasts and macrophages, demonstrating IC50 values of 1.3 μM for TRAP5a and 1.8 μM for TRAP5b, while effectively inhibiting TRAP activity in extracts from murine macrophages and human lung tissue.
|
-
- HY-13418A
-
|
Compound C; BML-275
|
Organoid
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599) .
|
-
- HY-163607
-
|
|
Apoptosis
NF-κB
|
Cancer
|
|
SpiD3, a spirocyclic dimer, is an anticancer agent. SpiD3 markedly inhibits malignant B-cell proliferation and suppressed NF-κB activation independent of TME-associated stimuli. SpiD3 induces apoptosis and inhibits protein synthesis in chronic lymphocytic leukemia cells. SpiD3 can be used for study of chronic lymphocytic leukemia (CLL) .
|
-
- HY-17376S3
-
|
SCH 58235-13C6
|
Isotope-Labeled Compounds
Autophagy
Keap1-Nrf2
|
Cancer
|
|
Ezetimibe- 13C6 (SCH 58235- 13C6) is the 13C-labeled Ezetimibe (HY-17376). Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
|
-
- HY-W286906
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Mcl1-IN-15 (Compound 7) is the inhibitor for myeloid cell leukemia 1 (Mcl-1) with an IC50 of 8.73 μM. Mcl1-IN-15 inhibits Mcl1-BH3 peptide interaction, activates the Bak/Bax-mediated apoptosis and exhibits antitumor activity .
|
-
- HY-154960
-
|
|
Akt
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin/AKT1-IN-1 (Compound D1-1) is an inhibitor of tubulin polymerization and AKT pathway activation. Tubulin/AKT1-IN-1 significantly inhibits the proliferation and metastasis of H1975 cells and slightly induced their apoptosis and can be used for non-small-cell lung cancer (NSCLC) research .
|
-
- HY-110313
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
SB-747651A dihydrochloride is an ATP-competitive mitogen- and stress-activated kinase 1 (MSK1) inhibitor with an IC50 of 11 nM. SB-747651A dihydrochloride also inhibits PRK2, RSK1, p70S6K and ROCK-II. SB-747651A dihydrochloride can be used for inflammation research .
|
-
- HY-P1111
-
|
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders .
|
-
- HY-P1045
-
|
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein .
|
-
- HY-168171
-
|
|
ERK
Caspase
Apoptosis
|
Cancer
|
|
ERK1/2 inhibitor 11 (compound L6) is a dual inhibitor of ERK1/2, lending to DSB accumulation and ERK1/2 expression degradation. ERK1/2 inhibitor 11 lowers the levels of BCL-2, and induces DNA damage by inhibiting PARP and ERK1/2. ERK1/2 inhibitor 11 activates caspase 3 to inducing apoptosis. .
|
-
- HY-P1111A
-
|
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders .
|
-
- HY-100738
-
|
NSC144303
|
Apoptosis
|
Cancer
|
|
Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
|
-
- HY-136741
-
BOT-64
1 Publications Verification
|
IKK
|
Inflammation/Immunology
|
|
BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription .
|
-
- HY-121685
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Tipepidine reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine subsequently activates VTA dopamine neuron . Tipepidine, a non-narcotic antitussive, exerts an antidepressant-like effect .
|
-
- HY-N2344
-
|
Proanthocyanidin A1
|
PKC
|
Inflammation/Immunology
|
|
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects .
|
-
- HY-13595R
-
|
Chrysophanic acid (Standard)
|
Reference Standards
EGFR
|
Cancer
|
|
Chrysophanol (Standard) is the analytical standard of Chrysophanol. This product is intended for research and analytical applications. Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
|
-
- HY-155786
-
|
|
TGF-beta/Smad
|
Others
|
|
3,7-DMF is an orally active inhibitor of TGF-β1-induced activation of HSCs. 3,7-DMF induces antioxidant genes and quenches ROS away, which can be used to study liver fibrosis .
|
-
- HY-103639
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
M62812 (free base) is a toll-like receptor 4 (TLR4) signal transduction inhibitor. M62812 can suppress endothelial cell and leukocyte activation and prevents lethal septic shock in mice. M62812 can be used for the research of sepsis .
|
-
- HY-B0764A
-
|
Dibutyryl cAMP calcium salt; DBcAMP calcium salt
|
PKA
Phosphodiesterase (PDE)
Apoptosis
|
Others
|
|
Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
|
-
- HY-P99166
-
|
|
PD-1/PD-L1
CTLA-4
|
Inflammation/Immunology
Cancer
|
|
Vudalimab is a potent dual PD-1 and CTLA-4 inhibitor as a fully humanized bispecific monoclonal antibody. Vudalimab targets immune checkpoint receptors PD-1 and CTLA-4 and promotes tumor-selective T-cell activation .
|
-
- HY-122311
-
|
SMTP-7
|
Reactive Oxygen Species (ROS)
|
Neurological Disease
Inflammation/Immunology
|
|
Orniplabin (SMTP-7) is a low-molecular-weight compound that enhances plasminogen–fibrin binding, urokinase-catalyzed activation of plasminogen, and urokinase and plasminogen-mediated fibrin degradation. Orniplabin shows potential thrombolytic and anti-inflammatory effects. Orniplabin inhibits ROS .
|
-
- HY-N0014R
-
-
- HY-124176
-
|
|
Phosphodiesterase (PDE)
Calmodulin
|
Cardiovascular Disease
|
|
L-6355 is an Amiodarone (HY-14187) related compound, which inhibits Ca 2+/calmodulin activated cyclic nucleotide phosphodiesterase with an IC50 value of 0.65 μM. L-6355 is promising for research of antiarrhythmic and antianginal agent .
|
-
- HY-137934
-
|
7-Deacetylforskolin
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Deacetylforskolin is a deacetylated derivative of forskolin (HY-15371) that can be extracted from C. forskohlii. Deacetylforskolin activates rat adipocyte adenylyl cyclase (IC50 = 20 µM), inhibits glucose transport in rat adipocyte plasma membranes and exhibits antihypertensive activity .
|
-
- HY-N8812
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
19-[(β-D-Glucopyranosyl)oxy]-19-oxo-ent-labda-8(17),13-dien-16,15-olide, the metabolite of Neoandrographolide, inhibits nitric oxide (NO) production in lipopolysaccharide-activated macrophages .
|
-
![19-[(β-D-Glucopyranosyl)oxy]-19-oxo-ent-labda-8(17),13-dien-16,15-olide](//file.medchemexpress.com/product_pic/hy-n8812.gif)
- HY-121685A
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Tipepidine hydrochloride reversibly inhibits dopamine (DA) D2 receptor-mediated GIRK currents (IDA(GIRK)) with an IC50 of 7.0 μM. Tipepidine hydrochloride subsequently activates VTA dopamine neuron . Tipepidine hydrochloride, a non-narcotic antitussive, exerts an antidepressant-like effect .
|
-
- HY-B1104R
-
|
(±)-Indoprofe (Standard)
|
Akt
AMPK
Reference Standards
NF-κB
p38 MAPK
|
Inflammation/Immunology
|
|
Indoprofen (Standard) is the analytical standard of Indoprofen. This product is intended for research and analytical applications. Indoprofen activates AKT-AMPK signaling pathway, inhibits NF-κB/MAPK signaling pathway. Indoprofen exhibits anti-inflammatory and immunomodulatory activities. Indoprofen is orally active .
|
-
- HY-162762
-
|
|
Protease Activated Receptor (PAR)
|
Cancer
|
|
PAR-2 antagonist 1 (Compound 9a) is a protease-activated receptor 2 (PAR2) antagonist with an IC50 value of 0.9 μM. PAR-2 antagonist 1 can effectively inhibit the proliferation and migration of breast cancer cells .
|
-
- HY-114174
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursor protein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing .
|
-
- HY-153343A
-
|
|
DGK
ERK
|
Cancer
|
|
(S)-BAY 2965501 is the left-handed isomer of BAY 2965501 (HY-153343). 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-110249
-
CINPA1
1 Publications Verification
|
Constitutive Androstane Receptor
|
Metabolic Disease
|
|
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function .
|
-
- HY-19700R
-
|
|
Reference Standards
MEK
ERK
Endogenous Metabolite
|
Others
|
|
trans-Zeatin (Standard) is the analytical standard of trans-Zeatin. This product is intended for research and analytical applications. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
|
-
- HY-101837
-
|
|
PDGFR
|
Inflammation/Immunology
|
|
CGP 53716 is a potent protein tyrosine kinase inhibitor. CGP 53716 has selective activity of platelet-derived growth factor (PDGF) receptor. CGP 53716 can be used in the study of disease induced by abnormal cell proliferation induced by PDGF receptor activation .
|
-
- HY-145996
-
|
|
Bacterial
|
Infection
|
|
STC314 is a small polyanion that interact electrostatically with histones. STC314 blocks disruption of lipid-bilayers by histones that inhibits the cytotoxic, platelet-activating and erythrocyte-damaging effects of histones. STC314 has anti-infective effects and can be uesd for sepsis research .
|
-
- HY-P991123
-
|
|
Adenylate Cyclase
|
Inflammation/Immunology
|
|
Bocunebart is a humanized monoclonal antibody targeting human adenylate cyclase-activating polypeptide (ADCYAP1). Bocunebart exerts anti-inflammatory activity by specifically binding to ADCYAP1 and inhibiting related inflammatory signaling pathways. Bocunebart is promising for research of inflammation-related diseases .
|
-
- HY-P6183
-
|
|
MMP
|
Cancer
|
|
LXJ-02 is a potent inhibitor of EDPs/EBP peptide–protein interaction, with the KD of 117 μM for EDPs. LXJ-02 activates the macrophage-MMP-12 axis to increase MMP-12 expression and degrade ECM components like elastin .
|
-
- HY-162334
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
HYOU1-IN-1 (Compound 33) is an inhibitor of hypoxia-upregulated protein 1 (HYOU1) with anti-inflammatory activity. HYOU1-IN-1 can be used in research on the regulation of fibroblast activation, chronic inflammation, and fibrotic diseases .
|
-
- HY-147769
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 23 (Compound 4m) is an anti-inflammatory agent. Anti-inflammatory agent 23 inhibits the production of NO activated by LPS with an IC50 of 0.449 μM. Anti-inflammatory agent 23 has a good affinity for p65 protein .
|
-
- HY-103344
-
|
|
Aminopeptidase
mGluR
|
Neurological Disease
Inflammation/Immunology
|
|
ZJ43 is a potent NAAG peptidase inhibitor, with an IC50 of 2.4 nM and a Ki of 0.8 nM. ZJ43 sufficiently activates group II mGluR and reduces some of the behavioral effects of PCP. ZJ43 shows an analgesic effect in neuropathic and inflammatory and pain models .
|
-
- HY-135487
-
|
AR-C68397AA free base; AR-C68397XX
|
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Sibenadet (AR-C68397AA free base) is a dual dopamine D2/β2-adrenoceptor agonist with selective β2-adrenoceptor agonism. Sibenadet inhibits capsaicin-induced plasma protein extravasation in rat trachea. Sibenadet suppresses edema from sensory nerve fiber activation by activating β2-adrenoceptor. Sibenadet is promising for research of chronic obstructive pulmonary disease (COPD) .
|
-
- HY-150751
-
|
ODN A151
|
Toll-like Receptor (TLR)
AIM2
|
Inflammation/Immunology
|
|
ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3' .
|
-
- HY-124152
-
|
Methyl-3,4-dephostatin
|
MAP3K
MAP4K
Phosphatase
|
Neurological Disease
|
|
3,4-Dephostatin (Methyl-3,4-dephostatin) is an inhibitor of protein-tyrosine phosphatase (PTPase). 3,4-Dephostatin accelerates nerve growth factor (NGF)-induced neurite formation in PC12h cells. 3,4-Dephostatin sustains the NGF-induced tyrosine phosphorylation of proteins, most prominently that of mitogen-activated protein (MAP) kinase. 3,4-Dephostatin also prolongs epidermal growth factor (EGF)-induced tyrosine phosphorylation and activation of MAP kinase .
|
-
- HY-77278
-
|
|
VD/VDR
Aryl Hydrocarbon Receptor
LXR
PPAR
|
Others
|
|
25-Hydroxytachysterol3 is the metabolite of Vitamin D3 (HY-15398). 25-Hydroxytachysterol3 inhibits the proliferation of epidermal keratinocytes and dermal fibroblasts, stimulates the expression of differentiation- and antioxidant-related genes in keratinocytes. 25-Hydroxytachysterol3 activates vitamin D receptor (VDR) and aryl hydrocarbon receptor (AhR), liver X receptor α/β (LXR α/β) and peroxisome proliferator-activated receptor γ (PPARγ), stimulates the expression of CYP24A1 .
|
-
- HY-161643
-
|
|
Cholinesterase (ChE)
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
|
S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
|
-
- HY-120158
-
|
|
Potassium Channel
|
Neurological Disease
|
|
ZD0947 is an ATP-sensitive potassium channel activator with relatively effective activation of smooth muscle KATP channels (SUR2B/Kir6.1 and SUR2B/Kir6.2). ZD0947 partially antagonizes pancreatic KATP channels (SUR1/Kir6.2) and cardiac KATP channels (SUR2A/Kir6.2). ZD0947 is potentially used to inhibit overactive bladder (OAB) .
|
-
- HY-126675
-
|
|
CDK
STAT
|
Inflammation/Immunology
|
|
AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene .
|
-
- HY-150751C
-
|
ODN A151 sodium
|
AIM2
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
ODN TTAGGG sodium, inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG sodium is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG sodium can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3' .
|
-
- HY-N1472
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
PPAR
GSK-3
Tau Protein
Ras
TGF-β Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Levistolide A is an apoptosis inducer and a PEDV virus inhibitor. Levistolide A can induce apoptosis in colon cancer cells and suppress the replication of porcine epidemic diarrhea virus (PEDV) by promoting ROS generation. Levistolide A activates peroxisome proliferator-activated receptor γ (PPARγ) in N2a/APP695swe cells and reduces excessive phosphorylation of tau through the GSK3α/β pathway, improving symptoms in Alzheimer’s mice. Levistolide A improves kidney damage in 5/6 nephrectomy (Nx) mice by inhibiting the RAS,TGF-β1/Smad, and MAPK pathways .
|
-
- HY-110189R
-
|
|
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate (sodium) (Standard) is the analytical standard of Pregnenolone monosulfate (sodium). This product is intended for research and analytical applications. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
|
-
- HY-137497
-
|
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
|
-
- HY-146765
-
|
|
NOD-like Receptor (NLR)
|
Neurological Disease
Inflammation/Immunology
|
|
AMS-17 is a potent NLRP3 inhibitor, inhibiting microglia activation in vitro and in vivo. AMS-17 also inhibits cytokines such as caspase-1, TNF-α, IL-1β and inducible nitric oxide synthase (iNOS) in N9 cells. AMS-17 can be used for researching inflammation-associated neurological disorders, such as vascular dementia (VaD) .
|
-
- HY-125542
-
|
|
Apoptosis
PI3K
Akt
|
Cancer
|
|
DCZ3301 is a potent aryl-guanidino inhibitor. DCZ3301 inhibits cell proliferation, induces G2/M cell cycle arrest and apoptosis. DCZ3301 inhibits the activation of the PI3K/AKT pathway by downregulating the protein expression of PI3K and phosphorylation of AKT. DCZ3301 can be used in research of cancer .
|
-
- HY-160698
-
|
|
MALT1
|
Inflammation/Immunology
Cancer
|
|
SGR-1505 is an orally active MALT1 allosteric inhibitor. SGR-1505 inhibits MALT1 enzymatic activity and shows anti-proliferative activity in BTK inhibitor (BTKi)-sensitive and BTKi-resistant activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines. SGR-1505 can be used for research of B-cell lymphomas .
|
-
- HY-107427
-
|
|
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
|
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect .
|
-
- HY-14654A
-
-
- HY-N12960
-
|
|
Apoptosis
Bcl-2 Family
Caspase
COX
MMP
STAT
|
Cancer
|
|
Artobiloxanthone (Compound AA3) exhibits antitumor activity, particularly against oral squamous cell carcinoma (OSCC). Artobiloxanthone inhibits Akt/mTOR pathway and STAT3 pathway, inhibits proliferation of SAS and T.Tn (with IC50 of 11 and 22 μM), and inhibits the cancer cell migration. Artobiloxanthone arrests cell cycle at S phase, and induces apoptosis in OSCC cells through activation of caspase 3/9 .
|
-
- HY-10585AS1
-
|
Sodium Valproate-d14 sodium
|
Isotope-Labeled Compounds
HDAC
Autophagy
Mitophagy
HIV
Notch
Endogenous Metabolite
|
Cancer
|
|
Valproic acid-d14 (sodium) is deuterium labeled Valproic acid (sodium). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
|
-
- HY-P10438
-
|
|
Raf
|
Cancer
|
|
TAT-Braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by TAT-Braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers .
|
-
- HY-156247
-
|
|
SDCBP
NF-κB
MMP
|
Cancer
|
|
IVMT-Rx-3 is a inhibitor of SDCBP targeting of the PDZ1 and PDZ2 Domains of MDA-9/Syntenin. IVMT-Rx-3 blocks MDA-9/Syntenin interaction with Src, reduces NF-κB activation, and inhibits MMP-2/MMP-9 expression. IVMT-Rx-3 inhibits Melanoma Metastasis [1]
|
-
- HY-170484
-
|
|
MAP3K
p38 MAPK
|
Neurological Disease
|
|
KAI-11101 is the inhibitor for dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 0.7 nM. KAI-11101 inhibits Paclitaxel (HY-B0015)-induced cJun phosphorylation (IC50=95 nM) and thus inhibits the activation of MAPK pathway. KAI-11101 is blood brain barrier penetrable and can be further investigated for its neuroprotective property .
|
-
- HY-12034
-
|
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro .
|
-
- HY-112288
-
|
TTI-101
|
STAT
Apoptosis
|
Cancer
|
|
C188-9 (TTI-101) is a STAT3 inhibitor, with a Kd of 4.7 nM. C188-9 inhibits G-CSF-induced STAT3 activation and STAT3-dependent gene expression. C188-9 induces apoptosis in AML cell lines and primary samples and inhibits colony formation by primary AML blasts .
|
-
- HY-N11262
-
|
|
p38 MAPK
ERK
|
Inflammation/Immunology
|
|
Sudachitin, a polymethoxyflavone that can be isolated from Citrus sudachi, suppresses lipopolysaccharide-induced inflammatory responses in mouse macrophage-like RAW264 cells. Sudachitin can activate the p38MAPK pathway and inhibit the ERK1/2 pathway in HaCaT cells .
|
-
- HY-160818
-
MC3138
1 Publications Verification
|
Sirtuin
|
Cancer
|
|
MC3138 is a selective SIRT5 activator. MC3138 has antitumor activity on human PDAC cells, with IC50 values of 25.4-236.9 μM. MC3138 combined with Gemcitabine (HY-17026) significantly inhibits tumor growth in mice .
|
-
- HY-148174
-
|
|
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-P10234
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Poneratoxin is the modulator for voltage-gated sodium channel (NaV, EC50 for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals .
|
-
- HY-13626
-
|
ES-285
|
PKC
Apoptosis
|
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. Spisulosine induces apoptosis in PC-3 and LNCaP cells .
|
-
- HY-100112
-
|
|
RIP kinase
|
Others
|
|
WEHI-345 analog is the analog of WEHI-345. WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation .
|
-
- HY-N7459
-
|
|
AMPK
Autophagy
Fungal
|
Cancer
|
|
Sakurasosaponin is a saponin with potential anticancer activity that can be extracted from the root of Primula sieboldii. Sakurasosaponin can activate the AMPK pathway to induce cell autophagy and exert anti-NSCLC cell proliferation activity. Sakurasosaponin also has antifungal activity and significantly inhibits the growth of anthrax.
|
-
- HY-118375
-
|
ISC-4
|
Apoptosis
|
Cancer
|
|
Phenylbutyl isoselenocyanate (ISC-4) is a selective apoptosis inducer that increases reactive oxygen species levels to inhibit androgen receptor (AR) and activate p53 pathway. Phenylbutyl isoselenocyanate induces apoptosis in LNCaP prostate cancer cells and has anti-prostate cancer properties.
|
-
- HY-P5117
-
|
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
TAT-CIRP is a a small peptide, refers to Trans-trans-activating (Tat)-cold-inducible RNA binding protein. TAT-CIRP is an inhibitor of myeloid differentiation protein 2 (MD2). TAT-CIRP exhibits robust neuroprotection against ischemic and hemorrhagic stroke in mice .
|
-
- HY-P9947
-
|
|
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-P5133
-
|
SSTN92-119
|
Integrin
|
Cancer
|
|
Synstatin (92-119) is an anti-tumor agent that inhibits angiogenesis and cancer cell invasion. Synstatin (92-119) down-regulates integrin α?β3 and reduces the activation of angiogenic growth factors VEGF and FGF-2 .
|
-
- HY-164502
-
|
|
Akt
|
Cancer
|
|
NAP1051 is a biomimetic analog of lipin A4 that achieves anti-tumor effects by targeting the inflammatory tumor microenvironment. NAP1051 inhibits neutrophil chemotaxis to fMLP and stimulates macrophage efferocytosis by activating AKT. NAP1051 can be used in colorectal cancer research .
|
-
- HY-P0024
-
|
DG3173; PTR-3173
|
Somatostatin Receptor
|
Endocrinology
Cancer
|
|
Veldoreotide (DG3173) a somatostatin analogue, binds to and activate the somatostatin receptors (SSTR) 2, 4, and 5. Veldoreotide inhibits growth hormone (GH) secretion in adenomas compared with Octreotide (HY-P0036). Veldoreotide has the potential to be used as pain modulating agent
|
-
- HY-160696
-
|
|
CD73
|
Cancer
|
|
ORIC-533 is an orally active, selective CD73 inhibitor with AMP-competition. ORIC-533 restores immunosuppressed CD8+ T cell proliferation and activation, triggers significant lysis and cell death of multiple myeloma cells in the bone marrow microenvironment .
|
-
- HY-122481
-
|
|
Topoisomerase
Apoptosis
Bcl-2 Family
Cytochrome P450
|
Cancer
|
|
Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri .
|
-
- HY-163859
-
|
|
Histone Demethylase
|
Cardiovascular Disease
|
|
LSD1-IN-33 (7d), an orally active LSD1 inhibitor with an IC50 of 4.51 nM, alleviates Ang II-induced NRCFs activation in vitro and reducing pathological myocardial remodeling in TAC-induced cardiac remodeling and heart failure in vivo .
|
-
- HY-101942
-
|
CM-4620
|
CRAC Channel
|
Neurological Disease
|
|
Zegocractin (CM-4620) is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM and 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively .
|
-
- HY-142972
-
|
|
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-W012980
-
|
|
Endogenous Metabolite
AMPK
PKA
|
Metabolic Disease
|
|
Isovaleric acid is an oral active short-chain fatty acid that inhibits osteoclast differentiation by stimulating AMPK phosphorylation and promotes colonic smooth muscle relaxation by activating the cAMP/PKA pathway. Isovaleric acid can be used in research on skeletal diseases (such as osteoporosis) and intestinal disorders .
|
-
- HY-19137
-
|
KW 2189 free base
|
Antibiotic
|
Infection
Cancer
|
|
Pibrozelesin (KW 2189 free base) is the derivative of antibiotic Duocarmycin B2. Pibrozelesin exhibits antitumor activity, inhibits proliferation of cell H69 with an IC50 of 1.9 μM. Pibrozelesin induces the DNA strand breaks upon activation via carboxyl esterase .
|
-
- HY-B1505A
-
-
- HY-114568
-
-
- HY-N0253
-
|
Kalopanaxsaponin B
|
Bacterial
p38 MAPK
NF-κB
Apoptosis
|
Infection
Inflammation/Immunology
|
|
Hederacoside C (Kalopanaxsaponin B) is an ingredient that can be obtained mainly from ivy leaves. Hederacoside C mediates inflammation by inhibiting activation of MAPK/NF-κB and its downstream signaling pathway. Hederacoside C has anti-inflammatory and antibacterial activity .
|
-
- HY-160769
-
|
|
YAP
|
Others
|
|
NIBR-LTSi is an orally active and selective LATS kinase inhibitor. NIBR-LTSi can activate YAP signaling. NIBR-LTSi promotes stem cell proliferation, maintains stemness and blocks differentiation. NIBR-LTSi accelerates liver regeneration following extended hepatectomy in mice .
|
-
- HY-113492
-
-
- HY-124887
-
-
- HY-157538
-
|
|
PDHK
|
Cardiovascular Disease
|
|
PDK4-IN-2 (compound 8) is a pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 of 46 µM. PDK4-IN-2 improves ejection fraction of failing hearts by regulating bioenergetics via activation of the tricarboxylic acid cycle .
|
-
- HY-159928
-
-
- HY-10619B
-
|
MK-4827 tosylate
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-P990552A
-
|
MNPR-101
|
Integrin
|
Cancer
|
|
huATN-658 (MNPR-101) is a humanized monoclonal antibody inhibitor targeting urokinase-type plasminogen activator receptor (uPAR). huATN-658 blocks the interaction between uPAR and integrins, inhibiting the proliferation, invasion and migration of tumor cells. huATN-658 is promising for research of breast cancer (especially triple-negative breast cancer) .
|
-
- HY-146419
-
|
|
NF-κB
COX
TNF Receptor
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 20 (compound 5a) is a potent inhibitor of NO activity. Anti-inflammatory agent 20 shows anti-inflammatory activity. Anti-inflammatory agent 20 suppresses LPS-induced inflammation via inhibiting the activation of NF-κB and MAPK signaling and thereby reducing IL-6, TNF-α, iNOS, and COX-2 upregulation .
|
-
- HY-B0130AR
-
|
Perindopril tert-butylamine salt (Standard); S-9490 erbumine (Standard)
|
Reference Standards
Sirtuin
NF-κB
STAT
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Cancer
|
|
Perindopril (erbumine) (Standard) is the analytical standard of Perindopril (erbumine). This product is intended for research and analytical applications. Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure .
|
-
- HY-156618
-
|
ABSK011
|
FGFR
|
Cancer
|
|
Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model .
|
-
- HY-163695
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-41 (compd S-9) is an orally active and brain-penetrant NLRP3 inhibitor with anti-inflammatory activities, anti-neuroinflammatory effect and without obvious cytotoxicity. NLRP3-IN-41 inhibits the priming and activation stages of the NLRP3 inflammasome and can be used for inflammasome-related diseases research .
|
-
- HY-A0042S
-
|
CGP 33101-d2; E 2080-d2; RUF 331-d2
|
Isotope-Labeled Compounds
Sodium Channel
|
Neurological Disease
|
|
Rufinamide-d2 (CGP 33101-d2) is the deuterium labeled Rufinamide (HY-A0042). Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na + current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome .
|
-
- HY-P99161
-
|
BGB149
|
TAM Receptor
|
Cancer
|
|
Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas .
|
-
- HY-B0116
-
-
- HY-B0116A
-
-
- HY-172198
-
|
|
GSK-3
β-catenin
DYRK
JNK
CDK
CDKL
|
Neurological Disease
|
|
GSK3-IN-10 (Compound 4) is a multi-target inhibitor, that mainly targets GSK3α and GSK3β with IC50 of 1.0 nM and 2.0 nM. GSK3-IN-10 inhibits the activation of β-catenin, promotes the neuronal survival, and exhibits a protective effect against endoplasmic reticulum stress .
|
-
- HY-120417
-
|
|
Src
FAK
|
Cardiovascular Disease
|
|
JP-153 is the Src-FAK-Paxillin signaling inhibitor. JP-153 inhibits Src-dependent phosphorylation of paxillin (Y118) and downstream activation of Akt (S473). JP-153 reduces VEGF-induced migration and proliferation in retinal endothelial cells. JP-153 can be uesd for the study of neovascular eye disease .
|
-
- HY-N12604
-
|
|
NF-κB
|
Others
|
|
Penicisteck acid F (Compound 2) is a Marine derived tanzanic acid derivative that is a NF-κB inhibitor. Penicisteck acid F inhibits osteoclast expression by decreasing RANKL-induced IκBα degradation, NF-κB p65 nuclear translocation, NFATc1 activation and nuclear translocation, and related mRNA expression. Penicisteck acid F can be used in osteoporosis research .
|
-
- HY-N15380
-
|
|
PARP
Reactive Oxygen Species (ROS)
Caspase
Apoptosis
Pyroptosis
|
Cancer
|
|
4,4′-Secalonic acid D (Compound 12) is a PARP1 inhibitor. 4,4′-Secalonic acid D induces the accumulation of ROS and DNA damage, activates the caspase-3/GSDME pathway, and triggers apoptosis and pyroptosis of tumor cells by inhibiting PARP1. 4,4′-Secalonic acid D has anti-tumor activity .
|
-
- HY-170936
-
|
|
FAK
Hippo (MST)
YAP
|
Cancer
|
|
MY-1576 is a FAK inhibitor with an IC50 of 8 nM. MY-1576 can activate the Hippo pathway, thereby blocking the regulation of YAP/TAZ. MY-1576 also effectively inhibits tumor growth in the KYSE30 xenograft mouse model, demonstrating good safety, and effectively downregulates the autophosphorylation of FAK and the levels of YAP/TAZ in vivo .
|
-
- HY-B0004
-
-
- HY-174801
-
|
|
Cyclic GMP-AMP Synthase
|
Inflammation/Immunology
|
|
XL-3156 is a potent, selective, and cross-species cGAS inhibitor. XL-3156 can simultaneously occupy both allosteric and orthosteric sites, and inhibit the interaction and phase separation between cGAS and DNA by stabilizing the closed conformation of the activation loop. XL-3156 can be used in the research of autoimmune diseases, inflammatory conditions and other diseases .
|
-
- HY-N0039R
-
|
Gypenoside III (Standard)
|
Reference Standards
Na+/K+ ATPase
IRAK
NF-κB
Autophagy
Mitophagy
HSV
|
Inflammation/Immunology
Cancer
|
|
Ginsenoside Rb1 (Standard) is the analytical standard of Ginsenoside Rb1. This product is intended for research and analytical applications. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na +, K +-ATPase activity with an IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65 .
|
-
- HY-114569
-
|
|
Ras
Cyclin G-associated Kinase (GAK)
Autophagy
|
Cancer
|
|
6-CEPN is a RAS inhibitor. 6-CEPN can inhibit RAS activation by binding to Icmt binding sites. 6-CEPN has anticancer activity. 6-CEPN can block cancer cells in the G1 phase. 6-CEPN can induce autophagy and necrosis of Cancer cells (Icmt: isovalerylcysteine carboxymethyltransferase) .
|
-
- HY-N0177R
-
|
|
Reference Standards
STAT
MicroRNA
|
Metabolic Disease
|
|
Diosgenin (Standard) is the analytical standard of Diosgenin. This product is intended for research and analytical applications. Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway . Diosgenin is an exogenous activator of Pdia3/ERp57 . Diosgenin inhibits aortic atherosclerosis progression by suppressing macrophage miR-19b expression .
|
-
- HY-101318
-
|
β-FNA hydrochloride
|
Opioid Receptor
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
β-Funaltrexamine (β-FNA) hydrochloride is a selective μ opioid receptor antagonist. β-Funaltrexamine hydrochloride also inhibits cytokine-induced iNOS activation. β-Funaltrexamine hydrochloride inhibits neuroinflammation and ameliorated neuronal degeneration. β-Funaltrexamine hydrochloride has anti-inflammatory and neuroprotective effects and can be used for research of neurodegenerative diseases (eg: stroke) [1] [2]
|
-
- HY-135815R
-
|
|
EGFR
|
Cancer
|
|
Mobocertinib (Standard) is the analytical standard of Mobocertinib. This product is intended for research and analytical applications. Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research .
|
-
- HY-146666
-
|
|
Apoptosis
STAT
|
Cancer
|
|
STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-18938A
-
|
GS-4997 hydrochloride
|
Apoptosis
MAP3K
|
Cancer
|
|
Selonsertib hydrochloride (GS-4997 hydrochloride) is an orally bioavailable enzyme inhibitor with potential anti-inflammatory, anti-tumor and anti-fibrotic activities. Selonsertib hydrochloride blocks ASK1 phosphorylation and activation by binding to the catalytic kinase domain. Selonsertib hydrochloride prevents the production of inflammatory cytokines and reduces the expression of genes associated with fibrosis. Selonsertib hydrochloride inhibits excessive apoptosis and limits cell proliferation .
|
-
- HY-108361
-
|
|
Ras
|
Inflammation/Immunology
Cancer
|
|
CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. Potential anti-metastasis Agent .
|
-
- HY-B0466BR
-
|
|
Beta-lactamase
Reference Standards
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Cloxacillin (sodium) (Standard) is the analytical standard of Cloxacillin (sodium). This product is intended for research and analytical applications. Cloxacillin sodium is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 μM. Cloxacillin sodium can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins .
|
-
- HY-B0466R
-
|
|
Beta-lactamase
Reference Standards
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Cloxacillin (sodium monohydrate) (Standard) is the analytical standard of Cloxacillin (sodium monohydrate). This product is intended for research and analytical applications. Cloxacillin sodium monohydrate is an orally active antibacterial agent and β-lactamase inhibitor with an IC50 of 0.04 μM. Cloxacillin sodium monohydrate can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins .
|
-
- HY-W748591
-
|
|
Apoptosis
Amyloid-β
|
Cancer
|
|
Cannflavin A can be isolated from Cannabis sativa L. Cannflavin A has anti-cancer, neuroprotective and anti-inflammatory activity. Cannflavin A inhibits Aβ1-42 aggregation. Cannflavin A also inhibits kynurenine-3-monooxygenase (KMO). Cannflavin A activates apoptosis via caspase-3 cleavage .
|
-
- HY-171047
-
|
|
Apoptosis
Autophagy
DNA/RNA Synthesis
Akt
mTOR
|
Cancer
|
|
Autophagy inducer 7 (Compound SSA) is an Autophagy and Apoptosis inducer. Autophagy inducer 7 activates autophagy by inhibiting Akt/mTOR signaling and the expression of downstream proteins. Autophagy inducer 7 suppresses DNA synthesis and causes a G0-G1 cell-cycle arrest. Autophagy inducer 7 inhibits tumor cell growth .
|
-
- HY-N0447R
-
|
|
Reference Standards
TRP Channel
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
|
8-Gingerol (Standard) is the analytical standard of 8-Gingerol. This product is intended for research and analytical applications. 8-Gingerol, found in the rhizomes of ginger (Z. officinale) with oral bioavailability, activates TRPV1, with an EC50 of 5.0 μM. 8-Gingerol inhibits COX-2, and inhibits the growth of H. pylori in vitro .
|
-
- HY-15959
-
|
Volitinib; HMPL-504; AZD-6094
|
c-Met/HGFR
|
Cancer
|
|
Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity .
|
-
- HY-P3369
-
|
AXT-107
|
VEGFR
Tie
Akt
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Gersizangitide (AXT107) is an anti-angiogenic peptide consisting of 20 amino acids, derived from collagen IV. Gersizangitide is an inhibitor of VEGF-A and VEGF-C and an activator of Tie2. Gersizangitide can block VEGF receptor signaling, inhibit vascular leakage, neovascularization and inflammation. Gersizangitide can be used in the research of diseases related to ocular neovascularization and angiogenesis .
|
-
- HY-18982R
-
|
Flagecidin (Standard); Wuningmeisu C (Standard)
|
Reference Standards
DNA/RNA Synthesis
JNK
Bacterial
Apoptosis
Antibiotic
Parasite
|
Infection
Cancer
|
|
Anisomycin (Standard) is the analytical standard of Anisomycin. This product is intended for research and analytical applications. Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system[1]. Anisomycin is a JNK activator, which increases phospho-JNK[2][3]. Anisomycin is a bacterial antibiotic[4].
|
-
- HY-164455
-
|
|
STAT
JAK
Aurora Kinase
Mitosis
|
Inflammation/Immunology
|
|
AJI-214 is a dual-target inhibitor of Aurora kinase A and JAK2. AJI-214 directly blocks Aurora kinase A to inhibit T cell mitotic progression and cell polarity, and inhibits JAK2 activation to inhibit STAT3 phosphorylation, thereby reducing the differentiation of TH1 and TH17 cells. AJI-214 can be used in studies on regulating immune responses and preventing graft-versus-host disease (GVHD) .
|
-
- HY-161155
-
|
|
HDAC
|
Inflammation/Immunology
|
|
HDAC6-IN-31 (compound 8m) is a selective HDAC6 inhibitor, with the IC50 value of 0.026 μM, that significantly inhibits the production and release of pro-inflammatory cytokines. While HDAC6 is critically involved in the activation of inflammasomes, HDAC6-IN-31 has the potential to inhibit NLRP3 inflammasome-driven inflammatory diseases. HDAC6-IN-31 also inhibits glioblastoma cell migration .
|
-
- HY-W371165
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C1s-IN-1 trihydrochloride (Compound A1) is the selective inhibitor for C1s protease with the Ki of 5.8 μM. C1s-IN-1 trihydrochloride inhibits cleavage of C2 by C1s with an IC50 of 85 μM, inhibits the activation of classic pathway with an IC50 of 22 μM. C1s-IN-1 trihydrochloride is the competitive inhibitor for thrombin with the Ki of 51.2 μM .
|
-
- HY-156119
-
|
|
Mixed Lineage Kinase
Necroptosis
|
Metabolic Disease
Cancer
|
|
MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor targeting Mixed Lineage Kinase domain-like (MLKL). MLKL-IN-6 inhibits cell necrosis. MLKL-IN-6 inhibits MLKL phosphorylation and oligomerization during cell necrosis, inhibits immune cell death, and reduces the expression of adhesion factors. MLKL-IN-6 has low cytotoxicity, and it inhibits hepatic stellate cell activation, reduces liver fibrosis marker levels, and has anti-fibrotic effects .
|
-
- HY-P1045A
-
|
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein .
|
-
- HY-176066A
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
c-Myc inhibitor 16 iodide (Compound W11) is a selective c-Myc G-quadruplex (c-Myc G4) inhibitor. c-Myc inhibitor 16 iodide inhibits the transcription and translation of the c-Myc gene, disrupts the tumor cell cycle, arrests cell growth in the G0/G1 phase and activates the mitochondrial apoptosis pathway to induce early apoptosis of cancer cells. c-Myc inhibitor 16 iodide is promising for research of breast cancer .
|
-
- HY-13649
-
|
ZIO 301; D 24851
|
Microtubule/Tubulin
Apoptosis
|
Neurological Disease
Cancer
|
|
Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis .
|
-
- HY-N3426
-
|
|
NO Synthase
Akt
AMPK
|
Metabolic Disease
|
|
Kazinol B, a prenylated flavan with a dimethyl pyrane ring, is an inhibitor of nitric oxide (NO) production. Kazinol B improves insulin sensitivity by enhancing glucose uptake via the insulin-Akt signaling pathway and AMPK activation. Kazinol B has the potential for diabetes mellitus research .
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-
- HY-155773
-
|
|
FAAH
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
VU534 is a NAPE-PLD activator, with an EC50 of 0.30 μM. VU534 is dual inhibitors of FAAH and sEH (IC50 of 1.2 μM). VU534 increases efferocytosis in a NAPE-PLD dependent manner. VU534 has the potential for cardiometabolic diseases study [1] .
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-
- HY-105627A
-
|
CI-572 hydrochloride
|
GABA Receptor
iGluR
|
Cardiovascular Disease
|
|
Profadol (CI-572) hydrochloride is a potent analgesic agent. Profadol is a µ-opioid receptor (MOR) agonist. Profadol hydrochloride activates the γ-aminobutyric acid (GABA) receptors and inhibits the N-methyl-D-aspartate (NMDA) receptor. Profadol increases the mRNA and protein expression of MOR .
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-
- HY-14590
-
-
- HY-137640A
-
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|
PKA
|
Inflammation/Immunology
|
|
Sp-8-Br-cAMPS sodium is a cAMP analog, which performs a protein kinase A (PKA) activating activity with EC50 of 360 nM. Sp-8-Br-cAMPS sodium inhibits proliferation of T cells and the haemocyte non-self response in Lepidoptera larve .
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-
- HY-P1402
-
|
|
PKC
|
Others
|
|
[Glu27]-PKC (19-36) is an inactive control for protein kinase C (PKC) (19-36). PKC (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C, it may be responsible for maintaining the enzyme in the inactive form in the absence of allosteric activators such as phospholipids .
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-
![[Glu27]-PKC (19-36)](//file.medchemexpress.com/product_pic/hy-p1402.gif)
- HY-128586A
-
|
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NEDD8-activating Enzyme
|
Cancer
|
|
TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM . TAS4464 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-108565
-
|
|
Adenylate Cyclase
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
BMY 45778 is a non-prostanoid prostacyclin mimetic. BMY 45778 inhibits human (IC50 = 35 nM), rabbit (IC50: 136 nM) and rat (IC50 : 1.3 μM) platelet aggregation. BMY 45778 also activates adenylyl cyclase. BMY 45778 is a partial agonist at the prostacyclin receptor .
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-
- HY-17386B
-
-
- HY-162510
-
|
|
NF-κB
|
Cancer
|
|
SPDZi1 is a potent and selective syntenin inhibitor that binds to PDZ1 and PDZ2 domains of syntenin. SPDZi1 binds to the syntenin PDZ tandem (STNPDZ) with a Kd of 3.6 μM. SPDZi1 suppresses glioblastoma and reduces the activation of NF-κB, a downstream effector of syntenin .
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-
- HY-N14932
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
Aggreceride A is a platelet aggregation inhibitor. Aggreceride A shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen .
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-
- HY-16059
-
|
(+)-Arglabin
|
NOD-like Receptor (NLR)
Farnesyl Transferase
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Arglabin ((+)-Arglabin), a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor. Arglabin shows anti-inflammatory and antitumor activities . The antitumor activity of Arglabin proceeds through its inhibition of farnesyl transferase which leads to the activation of RAS proto-oncogene .
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-
- HY-P99794
-
|
BAY 1213790
|
Factor Xa
|
Cardiovascular Disease
|
|
Osocimab (BAY 1213790), an anti-FXIa antibody (Ki=2.4 nM; EC50=0.2 nM). FXI inhibition may reduce the risk of thrombosis. Osocimab inhibits thrombin generation, and prolongs activated partial thromboplastin time. Osocimab exhibits anticoagulant effects .
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-
- HY-145686
-
|
|
Wnt
Nuclear Factor of activated T Cells (NFAT)
|
Inflammation/Immunology
|
|
AV023 is a potent inhibitor of ANKRD22. AV023 promotes the expansion of gastrointestinal mucosal epithelial stem cells and indirectly activates the Wnt classical pathway, which helps the recovery of damaged gastrointestinal mucosal tissues in the body (extracted from patent CN111205231B) .
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- HY-W762011
-
-
- HY-125827
-
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13-Methylberberinium chloride
|
Interleukin Related
|
Metabolic Disease
Cancer
|
|
13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS .
|
-
- HY-17386
-
-
- HY-B0764
-
|
Dibutyryl cAMP sodium salt; DBcAMP sodium salt
|
PKA
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing .
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-
- HY-14460
-
|
|
FLAP
|
Inflammation/Immunology
|
|
AM679 is a potent, selective 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 2 nM in a human FLAP membrane binding assay. AM679 markedly reduces the respiratory syncytial virus-driven ocular pathology as well as the synthesis of cysteinyl leukotrienes (CysLTs) in the eye .
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-
- HY-139664
-
|
|
DNA Methyltransferase
|
Cancer
|
|
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-107212
-
|
|
Parasite
Chloride Channel
P-glycoprotein
Bacterial
|
Infection
|
|
Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM .
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-
- HY-W015300R
-
|
Octanedioic acid (Standard)
|
Reference Standards
Endogenous Metabolite
|
Metabolic Disease
|
|
Suberic acid (Standard) is the analytical standard of Suberic acid. This product is intended for research and analytical applications. Suberic acid is an orally active crystalline dibasic acid. Suberic acid activates the Akt signaling pathway and regulates the expression of molecules related to the TGF-β and MAPK signaling pathways. Suberic acid inhibits skin dryness .
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-
- HY-111926
-
|
|
Phosphorylase
|
Metabolic Disease
|
|
N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM . N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor .
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-
- HY-32735R
-
|
PG490 (Standard)
|
Reference Standards
NF-κB
Apoptosis
|
Cancer
|
|
Triptolide (Standard) is the analytical standard of Triptolide. This product is intended for research and analytical applications. Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor .
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-
- HY-120035
-
|
|
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 .
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-
- HY-NP019
-
|
|
Sirtuin
Caspase
Apoptosis
|
Neurological Disease
|
|
Agkistrodon halys batroxobin is a thrombin-like serine protease. Agkistrodon halys batroxobin reduces the expression of Sirt1 and extracellular signal-regulated kinase activation in brain tissue. Agkistrodon halys batroxobin reduces cleaved caspase-3 expression and inhibits neuronal apoptosis in rat .
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-
- HY-17386A
-
-
- HY-111053
-
|
|
Phospholipase
|
Cancer
|
|
P11 is a selective inhibitor of platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3 that impairs cancer cell survival. P11 exhibits IC50 values of ~40 and 900 nM for PAFAH1b2 and 1b3, respectively .
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-
- HY-103254
-
|
|
Arrestin
Apelin Receptor (APJ)
|
Neurological Disease
|
|
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
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-
- HY-162170
-
|
|
NF-κB
Keap1-Nrf2
p38 MAPK
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 72 (compound 5) is a novel resveratrol derivative hybrid with benzoylhydrazine. Anti-inflammatory agent 72 shows anti-inflammatory and antioxidant activities by activating Nrf2 and inhibiting NF-κB p65/iNOS and MAPKs signaling pathways .
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-
- HY-75247R
-
-
- HY-P10399
-
|
Mouse KGYY15; KGYY15 peptide
|
TNF Receptor
|
Metabolic Disease
|
|
KGYY15 (Mouse KGYY15) is a CD40 targeting peptide, which weakly inhibits the CD40-CD40L interaction with IC50 of more than 1mM. KGYY15 activates 33% NF-κB pathway at 100 μM .
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-
- HY-113469AR
-
|
|
STING
Endogenous Metabolite
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
Cyclic GMP (sodium) (Standard) is the analytical standard of Cyclic GMP (sodium). This product is intended for research and analytical applications. Cyclic GMP (cGAMP) sodium is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP sodium can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP sodium may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP sodium, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP sodium can be used in the study of antiviral immunity and cardiovascular diseases .
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-
- HY-W767865
-
|
|
Isotope-Labeled Compounds
STING
Endogenous Metabolite
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
Cyclic GMP sodium- 13C5 is the 13C-labeled Cyclic GMP sodium (HY-113469A). Cyclic GMP (cGAMP) sodium is an endogenous second messenger that triggers interferon production in response to cytoplasmic DNA. Cyclic GMP sodium can activate the stimulator of interferon genes (STING), activating the signaling cascade that leads to the production of type I interferons and other immune mediators. Cyclic-GMP-AMP, a conjugate of cyclic GMP and AMP, can induce IRF3 phosphorylation and nuclear translocation, enhancing antiviral immune responses. Cyclic GMP sodium may also activate PDE to degrade cAMP, inhibit myocardial calcium current ICa, and regulate myocardial contractility. The derivative of Cyclic GMP sodium, 8-Br-cGMP, has antiplatelet activity, and Cyclic GMP sodium can be used in the study of antiviral immunity and cardiovascular diseases .
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-
- HY-13757S
-
|
ICI 46474-d3 hydrochloride; (Z)-Tamoxifen-d3 hydrochloride; trans-Tamoxifen-d3 hydrochloride
|
Apoptosis
Estrogen Receptor/ERR
Autophagy
HSP
Isotope-Labeled Compounds
|
Cancer
|
|
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). 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 .
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-
- HY-13757R
-
|
ICI 46474 (Standard); (Z)-Tamoxifen Citrate (Standard); trans-Tamoxifen Citrate (Standard)
|
Reference Standards
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen (Citrate) (Standard) is the analytical standard of Tamoxifen (Citrate). This product is intended for research and analytical applications. 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 .
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-
- HY-170929
-
|
|
Bcl-2 Family
Cytochrome P450
Apoptosis
Caspase
|
Cancer
|
|
EMT inhibitor-3 (compound 11i) is a epithelial-mesenchymal transition (EMT) inhibitor. EMT inhibitor-3 inhibits neuroblastoma SK-N-SH cells with an IC50 of 2.5 μM. EMT inhibitor-3 inhibits SK-N-SH cell proliferation, migration, and invasion. EMT inhibitor-3 increases the Bax/Bcl-2 protein expression ratio, promotes Cytochrome C ( HY-125857) release from mitochondria, and activates caspases 9 and caspases 3, inducing mitochondria-mediated endogenous tumor cell Apoptosis. EMT inhibitor-3 is potential for cancer research .
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-
- HY-110189S
-
|
3β-Hydroxy-5-pregnen-20-one monosulfate sodium-13C2,d2
|
Isotope-Labeled Compounds
Cannabinoid Receptor
TRP Channel
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate (sodium)- 13C2,d2 is the 13C- and deuterium labeled Pregnenolone monosulfate sodium. Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication . Pregnenolone monosulfate sodium salt is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels .
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-
- HY-13721
-
|
Idronoxil; Dehydroequol; Haginin E
|
Caspase
Apoptosis
Topoisomerase
|
Cancer
|
|
Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner .
|
-
- HY-173360
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
PDE10A-IN-5 (Compound A30) is an inhibitor of phosphodiesterase 10A (PDE10A) with oral activity, and its IC50 value is 3.5 nM. PDE10A-IN-5 exerts the activity of inhibiting pulmonary vascular remodeling by inhibiting PDE10A and activating the cyclic adenosine monophosphate (cAMP)-associated signaling pathway, and can be used for research in the field of pulmonary arterial hypertension .
|
-
- HY-10585AS
-
|
Sodium Valproate-d7(sodium)
|
Isotope-Labeled Compounds
HDAC
Autophagy
Mitophagy
HIV
Notch
Endogenous Metabolite
|
Cancer
|
|
Valproic acid-d7 (sodium) is the deuterium labeled Valproic acid (sodium salt). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches .
|
-
- HY-G0017
-
|
Norimatinib; Imatinib metabolite N-Desmethyl imatinib
|
Drug Metabolite
|
Cancer
|
|
N-Desmethyl imatinib (Norimatinib) is a c-Abl tyrosine kinase inhibitor. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways, and inhibits c-Abl-related neurodegenerative activity and neuroinflammation in vitro. N-Desmethyl imatinib can be used to study neurodegenerative diseases (such as Parkinson's disease) .
|
-
- HY-112447
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-5 is a potent STAT3 inhibitor. STAT3-IN-5 inhibits STAT3-Y705 phosphorylation with an EC50 value of 170 nM. STAT3-IN-5 inhibits cytokine induced JAK activation. STAT3-IN-5 induces apoptosis. STAT3-IN-5 can be used in research of cancer .
|
-
- HY-155532
-
|
|
Apoptosis
|
Cancer
|
|
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
|
-
- HY-123888
-
|
|
E1/E2/E3 Enzyme
Bacterial
|
Cancer
|
|
Viomellein is a SUMOylation inhibitor with antibacterial and anticancer activities. Viomellein inhibits biofilm formation of strains produced from the fungus Aspergillus ochraceus from the Mediterranean sponge Agelas oroides. Viomellein exhibits cytotoxicity against A2780 human ovarian cancer cells with an IC50 value of 5.0 μM. Viomellein also inhibits SUMOylation of RanGAP1 (GTPase activating protein) with an IC50 of 10.2 μM .
|
-
- HY-15586
-
L67
1 Publications Verification
DNA Ligase Inhibitor
|
DNA/RNA Synthesis
Caspase
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC50 are 10 μM). L67 can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research .
|
-
- HY-N7046S
-
|
Silibinin B-d3
|
Isotope-Labeled Compounds
Amyloid-β
Apoptosis
JNK
p38 MAPK
|
Neurological Disease
Cancer
|
|
Silybin B-d3 (Silibinin B-d3) is a deuterated Silybin B (HY-N7046). Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator, that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity .
|
-
- HY-N7046R
-
|
Silibinin B (Standard)
|
Reference Standards
JNK
Amyloid-β
p38 MAPK
Apoptosis
|
Neurological Disease
Cancer
|
|
Silybin (Silibinin B) (Standard) is the analytical standard of Silybin B (HY-N7046). This product is intended for research and analytical applications. Silybin B (Silibinin B) is an orally active amyloid-β aggregation inhibitor and ATR pathway activator, that can cross the blood-brain barrier. Silybin B inhibits Aβ fibril formation and promotes amorphous aggregate formation, while activating the ATR-mediated DNA damage repair pathway and inhibiting JNK/p38 MAPK signaling. Silybin B can reduce Cisplatin (HY-17394)-induced neuronal DNA damage and apoptosis. Silybin B has anti-oxidative stress, cell cycle regulation and neuroprotective activities. Silybin B is mainly used in the study of Alzheimer's disease and Cisplatin chemotherapy-related neurotoxicity .
|
-
- HY-N1970R
-
|
|
Reference Standards
Keap1-Nrf2
Arenavirus
Caspase
PARP
|
Neurological Disease
|
|
5,7-Dihydroxychromone (Standard) is the analytical standard of 5,7-Dihydroxychromone. This product is intended for research and analytical applications. 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-144634
-
|
|
Keap1-Nrf2
|
Neurological Disease
Inflammation/Immunology
|
|
DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD) .
|
-
- HY-120920
-
|
|
Dopamine Receptor
|
Inflammation/Immunology
|
|
UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions .
|
-
- HY-N7536
-
|
|
TRP Channel
|
Others
|
|
Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .
|
-
- HY-157793
-
|
|
Toll-like Receptor (TLR)
NF-κB
MAPKAPK2 (MK2)
|
Inflammation/Immunology
Cancer
|
|
SMU-L11 is a specific TLR7 agonist (EC50=0.024 μM), which recruits MyD88 adapter protein and activates downstream NF-κB and MAPK signaling pathways. In murine models, SMU-L11 significantly enhances immune cell activation and promotes the proliferation of CD4 + T and CD8 + T cells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases .
|
-
- HY-172915
-
|
|
MDM-2/p53
Apoptosis
Checkpoint Kinase (Chk)
|
Cancer
|
|
p53 Stabilizer 2 (Compound 17a16) is a p53 stabilizer. p53 Stabilizer 2 induces S-phase arrest and apoptosis in both p53-proficient and p53-deficient cancer cells. p53 Stabilizer 2 induces mitochondrial stress and activates two checkpoint pathways: NA-PKcs-dependent p53 stabilization and ATR-Chk1 axis activation. p53 Stabilizer 2 inhibits tumor growth in p53-deficient xenograft model .
|
-
- HY-N0106R
-
|
(Rac)-Danshensu sodium (Standard); (Rac)-Tanshinol sodium (Standard)
|
Reference Standards
Keap1-Nrf2
NF-κB
Mitochondrial Metabolism
Apoptosis
|
Infection
Cardiovascular Disease
Inflammation/Immunology
|
|
(Rac)-Salvianic acid A (sodium) (Standard) is the analytical standard of (Rac)-Salvianic acid A (sodium). This product is intended for research and analytical applications. (Rac)-Salvianic acid A sodium is the racemic form of Salvianic acid A (HY-N1913). Salvianic acid A is an orally active phenolic compound that induces Nrf2/HO-1 activation and inhibits the NF-κB pathway, and it also activates the mitochondrial antioxidant defense system (Mitochondrial Metabolism). Salvianic acid A exhibits anti-inflammatory, antioxidant, and anti-apoptotic properties (Apoptosis), demonstrating potential for research into inflammation and cardiovascular diseases .
|
-
- HY-B0736A
-
|
FI7056
|
Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
Cancer
|
|
Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
|
-
![(E)-[6]-Dehydroparadol](http://file.medchemexpress.com/product_pic/hy-77293.gif)
![19-[(β-D-Glucopyranosyl)oxy]-19-oxo-ent-labda-8(17),13-dien-16,15-olide](http://file.medchemexpress.com/product_pic/hy-n8812.gif)
![[Glu27]-PKC (19-36)](http://file.medchemexpress.com/product_pic/hy-p1402.gif)
