Search Result
Results for "
blocker ATP
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
11
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N6782
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-
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- HY-15206
-
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Glyburide
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Potassium Channel
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
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Metabolic Disease
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Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
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- HY-W040118
-
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Lactate Dehydrogenase
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Cancer
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Galloflavin is a potent lactate dehydrogenase (LDH) inhibitor. The calculated Kis for pyruvate are 5.46 μM (LDH-A) and 15.06 μM (LDH-B). Galloflavin hinders the proliferation of cancer cells by blocking glycolysis and ATP production .
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- HY-11005
-
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PDK-1
Apoptosis
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Cancer
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BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis .
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- HY-16929
-
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LAT-A
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Arp2/3 Complex
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Cancer
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Latrunculin A (LAT-A), found in the red sea sponge Latrunculia magnifica, is a G-actin polymerization inhibitor. Latrunculin A binds to actin monomers and inhibits polymerization of actin with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively. Latrunculin A has effective anti-metastatic properties for cancer research. Latrunculin A blocks cell migration .
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- HY-12283
-
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PST 2238
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Na+/K+ ATPase
RSV
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Cardiovascular Disease
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Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na +,K +-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity .
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- HY-12054
-
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Aurora Kinase
Autophagy
Influenza Virus
Parasite
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Cancer
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Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral .
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- HY-D1297
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Fluorescent Dye
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Others
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ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation .
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- HY-103259
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-
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- HY-B0753
-
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S1702; SE1702
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Potassium Channel
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Cardiovascular Disease
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Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic .
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- HY-108652
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P2X Receptor
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Inflammation/Immunology
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α,β-Methylene-ATP trisodium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP trisodium can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP trisodium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP trisodium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
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- HY-D1431
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Fluorescent Dye
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Cancer
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ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation. Ex/Em=587/615 nm .
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- HY-11079
-
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Sodium Channel
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Neurological Disease
Inflammation/Immunology
Cancer
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A-803467 is a potent and selective tetrodotoxin-resistant Nav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter .
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- HY-127111
-
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ATP Citrate Lyase
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Cancer
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NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate .
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- HY-B0860
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Diuron
2 Publications Verification
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Environmental Pollutants
Reactive Oxygen Species (ROS)
Herbicide
MDM-2/p53
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Cancer
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Diuron is an orally active phenylurea herbicide. Diuron inhibits photosynthesis in plants by blocking the formation of ATP and NADH. Diuron increases the production of ROS. Diuron increases expression of p53 in certain cell lines. Diuron has herbicidal activity against annual and perennial broadleaf weeds and grass weeds. Diuron promotes DMBA/BBN-induced bladder cancer. Diuron can be used in breast cancer research .
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- HY-44170
-
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PANK
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Neurological Disease
Metabolic Disease
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Pantothenate kinase-IN-2 is a pantothenate kinase inhibitor with IC50 values of 92 nM for PanK2, 70 nM for PanK1β, and 25 nM for PanK3. Pantothenate kinase-IN-2 can bind specifically to the ATP-PanK3 complex and block CoA biosynthesis. Pantothenate kinase-IN-2 can be used for the research of pank-associated neurodegeneration and type 2 diabetes .
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- HY-10261B
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(E/Z)-BIBW 2992
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EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
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Others
Cancer
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(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells .
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- HY-136615
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Potassium Channel
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Neurological Disease
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5-Hydroxydecanoate sodium is a selective ATP-sensitive K + (KATP) channel blocker (IC50 of ~30 μM). 5-Hydroxydecanoate sodium is a substrate for mitochondrial outer membrane acyl-CoA synthetase and has antioxidant activity .
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- HY-B0254
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CP 28720; K 4024
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Potassium Channel
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Metabolic Disease
Cancer
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Glipizide (CP 2872; K 4024)?a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2?diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium?(KATP) channels among β cells of pancreatic islets of Langerhans .
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- HY-101511
-
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P-glycoprotein
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Cancer
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TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
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- HY-125209
-
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DNA/RNA Synthesis
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Cancer
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TH5427 is a promising, targeted inhibitor that can be used to further study NUDT5 activity and ADP-ribose metabolism. TH5427, blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells. NUDT5 is recently identified as a rheostat of hormone-dependent gene regulation and proliferation in breast cancer cells .
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- HY-B0347
-
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Calcium Channel
Reactive Oxygen Species (ROS)
Caspase
Apoptosis
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Cardiovascular Disease
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Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
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- HY-D1429
-
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Fluorescent Dye
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Others
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ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining fixed cells. Staining followed by fixation is possible, but cells fixed with aldehydes will only retain partial fluorescence (Ex/Em = 374/ 430-640 nm) .
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- HY-N0165
-
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HIV
Reverse Transcriptase
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Cardiovascular Disease
Infection
Inflammation/Immunology
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Methyl-Hesperidin is a glycoside compound. Methyl-Hesperidin has hypotensive, coronary dilating, smooth muscle relaxing, capillary stabilizing, choleretic, and anti-ulcer activities. Methyl-Hesperidin act as a competitive substrate to inhibit HIV-1 reverse transcriptase activity. Methyl-Hesperidin potentiates coronary dilating actions of adenine nucleotides and 3'-AMP, enhances depressant action on isolated atria, and prolongs adenosine- and ATP-induced heart block in guinea pigs .
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- HY-145939
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BRD5846
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Casein Kinase
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Cancer
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BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways .
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- HY-148105
-
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MNK
Eukaryotic Initiation Factor (eIF)
Apoptosis
FLT3
DYRK
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Cancer
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DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC50 value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia .
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- HY-114869
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DPQ
3 Publications Verification
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PARP
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Neurological Disease
Cancer
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DPQ is a selective PARP-1 inhibitor that blocks PARP-1-mediated DNA damage repair and NAD +/ATP consumption, thereby inhibiting excessive inflammatory responses. DPQ inhibits NF-κB pathway activation, reduces the expression of pro-inflammatory factors (such as TNF-α, IL-6) and oxidative stress. DPQ can be used in inflammation-related studies of acute lung injury, myocardial infarction, and neurodegenerative diseases .
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- HY-160215
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TGF-β Receptor
p38 MAPK
TGF-beta/Smad
Interleukin Related
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Cancer
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GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma .
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- HY-P10856
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P-glycoprotein
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Cancer
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CPI1 is a multidrug resistance protein 1 (MRP1) inhibitor with a Ki value of 100 nM. CPI1 binds to the same substrate-binding site as leukotriene C4, stabilizes MRP1 in an apo-like inward-facing conformation, blocks the conformational changes required for ATP hydrolysis and substrate transport, and inhibits the ATPase activity of human and bovine MRP1. CPI1 serves as a tool for investigating the substrate transport mechanism of MRP1. CPI1 is applicable to research related to cancer multidrug resistance .
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- HY-108667
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P2X Receptor
Interleukin Related
Fluorescent Dye
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Neurological Disease
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TNP-ATP triethylammonium is a P2X receptor antagonist with an IC50 of 0.010 μM for P2X3 and an IC50 of 0.062 μM for P2X2/3. TNP-ATP triethylammonium acts as an inhibitor of CheA autophosphorylation, with a Ki of 0.7 µM. TNP-ATP triethylammonium blocks the functional activation of P2X1-7 receptors. TNP-ATP triethylammonium attenuates hypoxia-induced IL-1β expression and release. TNP-ATP triethylammonium alleviates visceral pain, and improves hypoxia-induced cognitive impairment, insufficient myelination and neuroinflammation. Binding of TNP-ATP triethylammonium to CheA enhances the fluorescence of the TNP group. TNP-ATP triethylammonium can be used in studies related to visceral pain. NP-ATP triethylammonium can be used in studies related to hypoxia-induced insufficient myelination and cognitive decline .
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- HY-15272
-
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mTOR
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Inflammation/Immunology
Cancer
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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.
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- HY-13072
-
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AS-703569; R-763
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Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
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Cancer
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Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
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- HY-171616
-
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HSP
β-catenin
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Cancer
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DCEM1 binds to heat shock protein 60 (HSP60) and inhibits the interaction of HSP60 with ClpP, thereby blocking the mitochondrial unfolded protein response. DCEM1 inhibits β-catenin expression and ATP production in PC-3 and TKO cells. DCEM1 can be used in prostate cancer research .
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- HY-142686A
-
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SGK
CDK
P-glycoprotein
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Inflammation/Immunology
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SGK1-IN-3 hydrochloride (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 hydrochloride blocks the activity of CDK family members. SGK1-IN-3 hydrochloride serves as a P-glycoprotein substrate. SGK1-IN-3 can be used for the research of osteoarthritis .
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- HY-DY1074
-
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Fluorescent Dye
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Others
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ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206) , highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining fixed cells. Staining followed by fixation is possible, but cells fixed with aldehydes will only retain partial fluorescence .
Solvent and concentration: DMSO: 1 mM
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- HY-144310
-
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Oxidative Phosphorylation
Mitochondrial Metabolism
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Cancer
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DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor (IC50=3.6 nM). DX3-213B impairs ATP generation (IC50=11 nM), and blocks MIA PaCa-2 cell growth (GI50=11 nM). DX3-213B is used for the research of the pancreatic cancer .
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- HY-12700
-
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Trace Amine-associated Receptor (TAAR)
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Neurological Disease
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RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages .
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- HY-12964
-
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TAM Receptor
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Cancer
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SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy)[1][2][3].
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- HY-15206S1
-
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Glyburide-d3
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Potassium Channel
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
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Metabolic Disease
|
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Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
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- HY-108589
-
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PNU 37883A
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Potassium Channel
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Neurological Disease
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PNU 37883 hydrochloride (PNU 37883A) is a selective vascular ATP-sensitive potassium (Kir6, KATP) channels blocker. PNU 37883 hydrochloride has diuretic effects with specific binding in kidney and vascular smooth muscle rather than in brain or pancreatic beta cells .
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- HY-134440A
-
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P2X Receptor
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Inflammation/Immunology
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α,β-Methylene-ATP is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
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- HY-125221
-
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ROCK
Cdc42-binding kinase
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Cancer
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DJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC50 values:5 and 50 nM) and MRCKα/β (IC50 values:10 and 100 nM). DJ4 blocks stress fiber formation and inhibits migration and invasion of cancer cells. DJ4 can be used for study of lung cancer, breast cancer, and pancreatic (PANC-1) cancer .
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- HY-136650A
-
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F-ara-ATP trisodium
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Nucleoside Antimetabolite/Analog
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
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Cancer
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Fludarabine triphosphate (F-ara-ATP) trisodium, the active metabolite of Fludarabine (HY-B0069), is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC50 of 2.3 μM and a Ki of 6.1 μM. Fludarabine triphosphate trisodium inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate trisodium inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis .
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- HY-115570
-
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GW108X
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Kinesin
ULK
Autophagy
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Cancer
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GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK .
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- HY-15206S
-
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Isotope-Labeled Compounds
Potassium Channel
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
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Metabolic Disease
|
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Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
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- HY-15208
-
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HMR 1098
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Potassium Channel
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Neurological Disease
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Clamikalant sodium (HMR 1098) is an ATP-sensitive potassium (KATP) channel blocker. Clamikalant sodium can be used for the research of arrhythmia .
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- HY-103442
-
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DAPH
|
EGFR
Amyloid-β
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Neurological Disease
Cancer
|
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CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease .
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- HY-DY1043
-
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Fluorescent Dye
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Others
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206) , highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation .
Solvent and concentration: DMSO: 1 mM
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- HY-B0254S
-
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Isotope-Labeled Compounds
Potassium Channel
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Metabolic Disease
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Glipizide-d11 is the deuterium labeled Glipizide. Glipizide (CP 2872; K 4024)?a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2?diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium?(KATP) channels among β cells of pancreatic islets of Langerhans .
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- HY-B0254R
-
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CP 28720 (Standard); K 4024 (Standard)
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Reference Standards
Potassium Channel
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Metabolic Disease
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Glipizide (Standard) is the analytical standard of Glipizide. This product is intended for research and analytical applications. Glipizide (CP 2872; K 4024) a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2 diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium (KATP) channels among β cells of pancreatic islets of Langerhans .
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- HY-124857
-
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7-Desacetoxy-6,7-dehydrogedunin
|
PERK
Prokineticin Receptor
P2X Receptor
Caspase
NOD-like Receptor (NLR)
Pyroptosis
Tyrosinase
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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7DG (7-Desacetoxy-6,7-dehydrogedunin) is a PKR inhibitor, P2X7 purinergic receptor inhibitor, and skin-lightening agent. 7DG binds outside the ATP-catalytic domain of PKR, blocks the kinase activity-independent protein-protein interactions of PKR, inhibits the phosphorylation and activity of PKR, disrupts ASC assembly and caspase-1 activation, and suppresses the activation of the NLRP1 inflammasome. 7DG inhibits pyroptosis, suppresses the ATP-P2X7 signaling pathway, and abolishes ATP-induced increases in the expression levels of MITF, tyrosinase, PMEL/gp100, and melanin content. 7DG exerts skin-lightening effects in cultured skin in vitro. 7DG can be used in research related to chronic obstructive pulmonary disease, gout, type 2 diabetes, Alzheimer's disease, and hyperpigmentary skin disorders .
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- HY-A0176
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-
- HY-B0753R
-
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S1702 (Standard); SE1702 (Standard)
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Reference Standards
Potassium Channel
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Cardiovascular Disease
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Gliclazide (Standard) is the analytical standard of Gliclazide. This product is intended for research and analytical applications. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic .
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-
- HY-110335
-
|
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ROCK
|
Cancer
|
|
OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis .
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-
- HY-155941
-
|
|
Potassium Channel
|
Neurological Disease
|
|
5-Hydroxydecanoic acid (5-HD） is a KATP channel antagonist，which has the effect of blocking the K KATP channel only during ischaemia by competing with the ATP binding site and does not affect pancreatic KATP channels .
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-
- HY-142686
-
|
|
SGK
P-glycoprotein
CDK
|
Inflammation/Immunology
|
|
SGK1-IN-3 (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC50 of <1 nM against hSGK1. SGK1-IN-3 blocks the activity of CDK family members. SGK1-IN-3 is a P-glycoprotein substrate. SGK1-IN-3 can be used for research on osteoarthritis .
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-
- HY-DY1026
-
|
|
Fluorescent Dye
|
Cancer
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206) , highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation. Ex/Em=587/615 nm .
Solvent and concentration: DMSO: 1 mM
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-
- HY-17451
-
-
- HY-B0753S
-
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|
Potassium Channel
|
Cardiovascular Disease
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|
Gliclazide-d4 (S1702 D4) is the deuterium labeled Gliclazide. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic .
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-
- HY-13072R
-
|
AS-703569 (Standard); R-763 (Standard)
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
Reference Standards
|
Cancer
|
|
Cenisertib (Standard) is the analytical standard of Cenisertib. This product is intended for research and analytical applications. Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
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-
- HY-125927
-
|
8-NH2-Ado
|
DNA/RNA Synthesis
Akt
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity .
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-
- HY-136650
-
|
F-ara-ATP
|
Nucleoside Antimetabolite/Analog
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Fludarabine triphosphate (F-ara-ATP), the active metabolite of Fludarabine (HY-B0069), is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC50 of 2.3 μM and a Ki of 6.1 μM. Fludarabine triphosphate inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis .
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-
- HY-W107722
-
|
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LRRK2
|
Endocrinology
|
|
IN04 is a inhibitor of leucine-rich repeat kinase 1 (LRRK1). IN04 can completely block the binding of ATP to the human LRRK1 kinase domain, thereby inhibiting the kinase activity of LRRK1. IN04 can significantly impair the bone resorption ability of osteoclasts, with an IC50 value of 5.72 μM. IN04 can be used for the study of osteoporosis .
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-
- HY-177936
-
|
|
NEDD8-activating Enzyme
|
Cancer
|
|
NAE-IN-3 (compound 1) is a potent, selective and non-covalent competitive NEDD8-activating enzyme (NAE) inhibitor (IC50 = 0.8 μM). NAE-IN-3 inhibits NAE by blocking the ATP-binding domain. NAE-IN-3 exhibits selectivity over analogous E1 enzymes UAE and SAE. NAE-IN-3 can be used for cancer research .
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-
- HY-19382
-
|
|
SOD
ERK
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
EUK-189 is a synthetic superoxide dismutase (SOD) and catalase mimetic. EUK-189 can block oxygen/glucose deprivation (OGD)-induced ERK1/2 dephosphorylation, ATP depletion and eliminate ROS production. EUK-189 exhibits neuroprotective effect and can inhibit delayed radiation injury. EUK-189 can be used for the research of neurological disease, such as ischemic stroke .
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-
- HY-B0347S1
-
|
|
Apoptosis
Caspase
Calcium Channel
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
|
|
Lacidipine- 13C8 is the deuterium labeled Lacidipine . Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
|
-
- HY-124764
-
|
|
PAK
|
Cancer
|
|
KY-04031 is a potent PAK4 inhibitor with IC50 of 0.79 μM. KY-04031 binds to the ATP-binding pocket of PAK4. KY-04031 blocks tumor cell growth and invasion .
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-
- HY-178450
-
|
|
P2X Receptor
|
Neurological Disease
|
|
HW091077 is a highly selective P2X3 receptor antagonist with an IC50 of 17 nM. HW091077 blocks ATP-induced calcium influx and cell depolarization to inhibit cough reflex pathways. HW091077 is promising for research of chronic cough .
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-
- HY-172959
-
|
|
Mitochondrial Metabolism
|
Cardiovascular Disease
|
|
mPTP-IN-1 (Compound 14e) is a mitochondrial permeability transition pore (mPTP) inhibitor. mPTP-IN-1 blocks calcium-induced mPTP opening by targeting the C subunit of ATP synthase. mPTP-IN-1 can be used to study myocardial ischemia/reperfusion injury (IRI) .
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-
- HY-145422
-
|
|
IRE1
Apoptosis
|
Others
|
|
KIRA9 is a potent IRE1 inhibitor (IC50=4.8 μM in INS-1 cells). KIRA9 is able to fully engage the ATP-binding site of IRE1α. KIRA9 can block ER-localized mRNA decay and apoptosis .
|
-
- HY-108671
-
|
|
P2X Receptor
|
Neurological Disease
|
|
NF110 is a P2X3 receptor antagonist (Ki = 36 nM) and inactive toward P2Y receptors stably expressed (IC50s > 10 M). NF110 blocks alphabeta-methylene-ATP-induced currents (IC50 = 527 nM) in rat dorsal root ganglia neurons .
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-
- HY-134440
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
α,β-Methylene-ATP dilithium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP dilithium can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP dilithium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP dilithium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
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-
- HY-160215A
-
|
|
TGF-β Receptor
p38 MAPK
TGF-beta/Smad
Interleukin Related
|
Cancer
|
|
GFH018 is an orally active, selective and ATP-competitive TGF-βR1 inhibitor with an IC50 of 40 nM. GFH018 reactivates the immune system by blocking the immunosuppression mediated by regulatory T cells and M2 macrophages. GFH018 inhibits tumor angiogenesis. GFH018 suppresses tumor growth in mouse tumor models. GFH018 can be used for the research of solid tumors, hepatocellular carcinoma, colorectal cancer, breast cancer, and relapsed/metastatic nasopharyngeal carcinoma .
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-
- HY-117622
-
|
|
IRAK
|
Inflammation/Immunology
Cancer
|
|
ND-2110 is a selective IRAK4 inhibitor (Ki: 7.5 nM). ND-2110 binds to the ATP pocket of IRAK4. ND-2110 targets
the subset of activated B cell-like (ABC) subtype of diffuse large B cell lymphoma (DLBCL) cell lines with MYD88 L265P mutations,. ND-2110 inhibits LPS-induced TNF production, alleviates collagen-induced arthritis, and blocks gout formation in mouse models .
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-
- HY-17451R
-
|
|
Reference Standards
Potassium Channel
|
Metabolic Disease
|
|
Glibornuride (Standard) is the analytical standard of Glibornuride. This product is intended for research and analytical applications. Glibornuride is a blocker of ATP-sensitive K+ channels (KATP channel) with a pKi of 5.75 . Antidiabetic agent .
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-
- HY-155754
-
|
|
ATP Synthase
|
Others
|
|
3’-Acetate-ATP, an ATP analogue, is ATP acetylation product with an maxima uv absorption at 259 nm in water at neutral pH. 3’-Acetate-ATP exerts a blocking effect on nucleic acid polymerization .
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-
- HY-135337
-
|
|
Potassium Channel
|
Metabolic Disease
|
|
Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877) . Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM .
|
-
- HY-119306
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
MCC-134, a blocker of mitochondrial and opener of surface ATP-sensitive K+ (KATP) channels, abrogates cardioprotective effects of chronic hypoxia. MCC-134 is a vasorelaxing agent .
|
-
- HY-12283R
-
|
PST 2238 (Standard)
|
Na+/K+ ATPase
RSV
Reference Standards
|
Cardiovascular Disease
|
|
Rostafuroxin (Standard) is the analytical standard of Rostafuroxin. This product is intended for research and analytical applications. Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na+,K+-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity .
|
-
- HY-W723322
-
|
|
Isotope-Labeled Compounds
Potassium Channel
|
Metabolic Disease
|
|
Ethyl tosylcarbamate-d7 is the deuterium labeled Ethyl tosylcarbamate (HY-135337). Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877) . Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM .
|
-
- HY-13072B
-
|
AS-703569 benzoate; R-763 benzoate
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-168474
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
P2X4 antagonist-4 (compound 64) is a potent P2X4R antagonist with an IC50 value of 8 µM. P2X4 antagonist-4 blocks the ATP-induced NLRP3 inflammasome activation and release of IL-1β .
|
-
- HY-176246
-
|
|
Bacterial
|
Infection
|
|
Antitubercular agent-52 (Compound 7k) is an antitubercular agent targeting Mycobacterium tuberculosis (Mtb). Antitubercular agent-52 selectively inhibits the cytochrome bcc (cyt-bcc) electron transport chain of Mtb and also acts on cytochrome bd (cyt-bd). Antitubercular agent-52 blocks electron transfer and ATP production by interfering with the key energy metabolism pathway of Mtb. Antitubercular agent-52 is promising for research of tuberculosis .
|
-
- HY-W424851
-
|
6,7-Dimethoxy-2-(1-piperazinyl)-4-quinazolinamine hydrochloride
|
PARP
|
Infection
Inflammation/Immunology
|
|
DPQ hydrochloride is a blood-brain barrier permeable and selective PARP-1 inhibitor that blocks PARP-1-mediated DNA damage repair and NAD +/ATP consumption, thereby inhibiting excessive inflammatory responses. DPQ hydrochloride inhibits NF-κB pathway activation, reduces the expression of pro-inflammatory factors (such as TNF-α, IL-6) and oxidative stress. DPQ hydrochloride can be used in inflammation-related studies of acute lung injury, myocardial infarction, and neurodegenerative diseases .
|
-
- HY-10261BR
-
|
(E/Z)-BIBW 2992 (Standard)
|
EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
Reference Standards
|
Others
|
|
(E/Z)-Afatinib (Standard) is the analytical standard of (E/Z)-Afatinib. This product is intended for research and analytical applications. (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells .
|
-
- HY-159074
-
|
|
MAP3K
|
Inflammation/Immunology
Cancer
|
|
Cot-IN-5 (compound 1) is a potent ATP-competitive inhibitor of cancer osaka thyroid (COT). Cot-IN-5 can block COT kinase autophosphorylation .
|
-
- HY-P992446
-
|
|
NTPDase
|
Cancer
|
|
PUR001 is a monoclonal antibody targeting NTPDase 1 (CD39). PUR001 blocks the hydrolysis of extracellular ATP and ADP into AMP by inhibiting CD39, reduces the production of immunosuppressive adenosine, and increases extracellular ATP concentration to activate anti-tumor immune responses. PUR001 can be used in studies related to solid tumors .
|
-
- HY-19174
-
|
|
Potassium Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
BTS-67582 is an orally active nonsulfonylurea insulinotropic agent and potassium channel blocker. BTS-67582 affects the K + ATP channel in the islet cell but at a different binding site than the sulfonylureas. BTS-67582 is an antidiabetic agent .
|
-
- HY-108652R
-
|
|
Reference Standards
P2X Receptor
|
Inflammation/Immunology
|
|
α,β-Methylene-ATP trisodium (Standard) is the analytical standard of α,β-Methylene-ATP (trisodium) (HY-108652). This product is intended for research and analytical applications. α,β-Methylene-ATP trisodium is an agonist of P2X1 and P2X3 receptors and can cross the blood-brain barrier. α,β-Methylene-ATP trisodium can trigger a reflex pressor response by activating P2X receptors in peripheral muscles and the central locus coeruleus (LC); this effect can be blocked by the P2X antagonist PPADS (HY-108960). α,β-Methylene-ATP trisodium also activates noradrenergic neurons in the central locus coeruleus, mediating antinociceptive effects; this effect can be attenuated by the locus coeruleus damaging agent DSP-4 (HY-103210/HY-121602). α,β-Methylene-ATP trisodium can be used to study the pathological mechanisms of neuropathic pain, cardiovascular reflex regulation, and antinociceptive effects of the central nervous system .
|
-
- HY-147127
-
|
|
Bacterial
ATP Synthase
|
Infection
|
|
WEN05-03 is a EscN ATPase inhibitor. WEN05-03 blocks the active site of EscN ATPase and competitively inhibits its ATP hydrolysis activity. WEN05-03 completely blocks actin cluster formation, reduces actin pedestal formation, and decreases the toxicity of infected mammalian cells. WEN05-03 can be used in studies related to enteropathogenic E. coli (EPEC) infection .
|
-
- HY-182430
-
|
|
JAK
STAT
Apoptosis
|
Cancer
|
|
NVP-BVB808 is a selective and ATP-competitive JAK2 inhibitor with an IC50 of 0.35 nM. NVP-BVB808 binds to JAK2’s ATP-binding site, stabilizes JAK2’s active conformation, increases JAK2 activation loop phosphorylation, and blocks downstream kinase function. NVP-BVB808 exhibits antiproliferative and pro-apoptosis effects, suppresses constitutive STAT5a phosphorylation. NVP-BVB808 can be used for the research of cancer, such as leukemia .
|
-
- HY-181478
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-45 is a Hsp90 inhibitor. Hsp90-IN-45 competitively binds to the ATP-binding site of purified Hsp90α with a Kd of 70 nM, blocks ATP hydrolysis, and disrupts Hsp90 client signaling. Hsp90-IN-45 inhibits ATPase activity of purified Hsp90α. Hsp90-IN-45 will be radiolabeled with 76/ 77Br for use as a radiotheragnostic agent for PET imaging and Meitner-Auger electron therapy. Hsp90-IN-45 can be used for the research of cancer .
|
-
- HY-176894
-
|
|
Carnitine Palmitoyltransferase (CPT)
Others
|
Metabolic Disease
|
|
Hemiacetylcarnitinium chloride is a inhibitor of fatty acid metabolism, specifically targeting carnitine palmitoyltransferase I (CPT I). Hemiacetylcarnitinium chloride disrupts the conversion of fatty acyl-CoA to fatty acyl carnitine, thereby blocking the subsequent oxidation of long-chain fatty acids and reducing the production of ATP required for energy-dependent cellular processes. Hemiacetylcarnitinium chloride can be used for the study of fatty acid metabolism .
|
-
- HY-137744
-
|
|
Adenylate Cyclase
Nucleoside Antimetabolite/Analog
|
Infection
|
|
MANT-GppNHp is a competitive adenyl cyclase (AC) inhibitor. MANT-GppNHp is a fluorescently labeled GTP (HY-113225) analogue. MANT-GppNHp interacts with the hydrophobic pocket near the AC catalytic site through its MANT group, thereby directly blocking the binding of the substrate ATP. MANT-GppNHp can be used to study diseases related to the increased activity of AC (such as cholera) .
|
-
- HY-182721
-
|
|
PI4K
Hedgehog
|
Cancer
|
|
Pipinib is an ATP-competitive and selective phosphatidylinositol 4-kinase IIIb (PI4KB) inhibitor with an IC50 of 2.2 μM. Pipinib reduces intracellular PI4P levels. Pipinib inhibits GLI-mediated transcription, the expression of Hedgehog target genes, and blocks the trafficking of Smoothened to cilia. Pipinib can be used in the research of basal cell carcinoma and medulloblastoma .
|
-
- HY-183920
-
|
|
CMV
p97
|
Infection
|
|
LC-1310 is an antiviral agent that targets and inhibits p97, and it suppresses the in vitro replication of human cytomegalovirus (HCMV) with an EC50 value of 0.3 μM. LC-1310 targets the D2 ATP-binding site of p97, downregulates the expression of early viral proteins, thereby blocking the transcription and proliferation of early viral genes. LC-1310 can be used for research on human cytomegalovirus infection .
|
-
- HY-165486
-
|
|
Potassium Channel
Calcium Channel
|
Cardiovascular Disease
|
|
AWD 122-60 is a potassium channel blocker and calcium sensitizer, with IC50 values of 11 μM and 29 μM, respectively, against mouse skeletal muscle ATP-sensitive potassium (KATP) channels. AWD 122-60 exerts potent positive inotropic activity. AWD 122-60 exhibits antiarrhythmic activity in vivo and prolongs myocardial refractory period in vitro. AWD 122-60 can be used for research related to arrhythmias .
|
-
- HY-183627
-
|
|
PI5P4K
|
Cancer
|
|
066ATZ is a PIP4K2A/2B inhibitor with human PIP4K2A Ki 100 nM and PIP4K2B Ki 800 nM. 066ATZ binds to ATP-binding sites of PIP4K2A and PIP4K2B to block lipid kinase activity. 066ATZ can be used for the research of non-small cell lung cancer .
|
-
- HY-103442R
-
|
DAPH (Standard)
|
Reference Standards
EGFR
Amyloid-β
|
Neurological Disease
Cancer
|
|
CGP52411 (Standard) is the analytical standard of CGP52411 (HY-103442). This product is intended for research and analytical applications. CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease .
|
-
- HY-182303
-
|
CATR
|
Methionine Adenosyltransferase (MAT)
|
Neurological Disease
|
|
Carboxyatractyloside (CATR) is a tight-binding inhibitor of adenine nucleotide translocase, and represents the major toxic component of Xanthium sibiricum. Carboxyatractyloside competes with ADP for binding to the translocase, blocks the translocation of ADP/ATP across the inner mitochondrial membrane, and thereby inhibits ADP-stimulated respiration. In the presence of Cyclosporin A (HY-B0579), Carboxyatractyloside still induces permeability transition in liver mitochondria of aged rats, exhibiting significant hepatotoxicity and nephrotoxicity. Carboxyatractyloside is widely used in studies related to hepatotoxicity, nephrotoxicity and Alzheimer's disease .
|
-
- HY-101511R
-
|
|
P-glycoprotein
Reference Standards
|
Cancer
|
|
TTT-28 (Standard) is the analytical standard of TTT-28 (HY-101511). This product is intended for research and analytical applications. TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1 .
|
-
- HY-15206R
-
|
Glyburide (Standard)
|
Mitochondrial Metabolism
Autophagy
CFTR
P-glycoprotein
Potassium Channel
Reference Standards
|
Metabolic Disease
|
|
Glibenclamide (Standard) is the analytical standard of Glibenclamide. This product is intended for research and analytical applications. Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
|
-
- HY-N17788
-
|
|
Tie
|
Cancer
|
|
6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether is a selective inhibitor of Tie2 kinase, with an IC50 value of 2.1 μM. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether interacts with the ATP binding site of Tie2 kinase, inhibiting kinase activity and subsequently blocking tumor angiogenesis. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether can be isolated from sponges of the genus Dysidea .
|
-
- HY-B0347S3
-
|
|
Calcium Channel
Caspase
Reactive Oxygen Species (ROS)
Apoptosis
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
|
-
- HY-123393
-
|
|
Topoisomerase
|
Others
|
|
PNU-142586 is the major metabolite of Linezolid (HY-10394). PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis, ultimately leading to antiproliferative and cytotoxic effects, including mitochondrial dysfunction. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism .
|
-
- HY-B0347R
-
|
|
Reference Standards
Calcium Channel
Reactive Oxygen Species (ROS)
Caspase
Apoptosis
|
Cardiovascular Disease
|
|
Lacidipine (Standard) is the analytical standard of Lacidipine. This product is intended for research and analytical applications. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
|
-
- HY-B0860S
-
|
|
Isotope-Labeled Compounds
Herbicide
Reactive Oxygen Species (ROS)
MDM-2/p53
|
Cancer
|
|
Diuron-d6 is the deuterium labeled Diuron (HY-B0860). Diuron is an orally active phenylurea herbicide. Diuron inhibits photosynthesis in plants by blocking the formation of ATP and NADH. Diuron increases the production of ROS. Diuron increases expression of p53 in certain cell lines. Diuron has herbicidal activity against annual and perennial broadleaf weeds and grass weeds. Diuron promotes DMBA/BBN-induced bladder cancer. Diuron can be used in breast cancer research .
|
-
- HY-121197
-
|
Ophiocordin; Azepinostatin
|
MARCKS
PKA
PKC
|
Others
|
|
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
|
-
- HY-156685
-
|
|
PI4K
Parasite
|
Infection
Metabolic Disease
Cancer
|
EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children .
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-
- HY-W540972
-
|
Primuline
|
Fluorescent Dye
HCV
Dengue Virus
|
Infection
|
|
Primulin is a versatile fluorescent dye and bioactive compound widely used in analytical, biological, botanical and virological studies. Primulin acts as a versatile stain that labels plant cell walls and differentiates live and dead spermatozoa via distinct fluorescence patterns. Primulin exhibits strong albumin‑binding capacity. Primulin acts as a retrograde axonal tracer in neurobiological investigations. Primulin and its derivatives inhibit HCV NS3, block dengue virus NS3-mediated ATP hydrolysis, and disrupt HCV replicase assembly .
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-
- HY-180244
-
|
|
Protease Activated Receptor (PAR)
p38 MAPK
|
Cancer
|
|
P2L-003 is a selective PAR2 antagonist with an IC50 of 0.62 μM in HT-29 cells. P2L-003 blocks PAR2-mediated Ca 2+ mobilization without affecting PAR1, PAR4, or ATP-mediated signaling and dose-dependently suppresses the downstream MAPK signaling cascades, including ERK1/2 and p38 phosphorylation. P2L-003 can be used for colon cancer research .
|
-
- HY-W654323
-
|
|
Topoisomerase
Drug Metabolite
|
Others
|
|
PNU-142586 sodiu) is the major metabolite of Linezolid (HY-10394). PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis, ultimately leading to antiproliferative and cytotoxic effects, including mitochondrial dysfunction. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism .
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-
- HY-15206S2
-
|
Glyburide-13C6
|
Isotope-Labeled Compounds
Autophagy
Mitochondrial Metabolism
Potassium Channel
CFTR
P-glycoprotein
|
Metabolic Disease
|
|
Glibenclamide- 13C6 (Glyburide- 13C6) is 13C labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
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-
- HY-173275
-
|
|
PDGFR
|
Cancer
|
|
PDGFRα kinase inhibitor 3 (Compound L7) is a highly potent inhibitor targeting the PDGFRα D842V kinase with IC50s values of 23.8 nM and 2.1 nM in biochemical and cellular assays, respectively. PDGFRα kinase inhibitor 3 binds to the ATP-binding pocket of PDGFRα D842V to block its downstream signaling pathways and inhibit kinase activity. PDGFRα kinase inhibitor 3 can be used for gastrointestinal stromal tumors (GISTs) study .
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-
- HY-158618
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia .
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-
- HY-B0860R
-
|
|
Herbicide
Reference Standards
Reactive Oxygen Species (ROS)
MDM-2/p53
|
Cancer
|
|
Diuron (Standard) is the analytical standard of Diuron (HY-B0860). This product is intended for research and analytical applications. Diuron is an orally active phenylurea herbicide. Diuron inhibits photosynthesis in plants by blocking the formation of ATP and NADH. Diuron increases the production of ROS. Diuron increases expression of p53 in certain cell lines. Diuron has herbicidal activity against annual and perennial broadleaf weeds and grass weeds. Diuron promotes DMBA/BBN-induced bladder cancer. Diuron can be used in breast cancer research .
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-
- HY-157941
-
|
|
ATM/ATR
Checkpoint Kinase (Chk)
DNA/RNA Synthesis
|
Cancer
|
|
ART0380 is a potent, selective and orally active ATR kinase inhibitor. ART0380 potently inhibits human ATR-ATRIP complex with an IC50 of 51.7 nM. ART0380 binds the ATP pocket of the ATR-ATRIP complex, blocks ATR-dependent Chk1 serine 345 phosphorylation, and induces cell cycle disorder and DNA damage. ART0380 demonstrates potent and selective antitumor activity in preclinical models with varying types of ataxia-telangiectasia mutated (ATM) gene aberrancy. ART0380 can be used for the research of cancer, such as colorectal cancer and prostate cancer .
|
-
- HY-153066
-
|
KIF18A-IN-7
|
Kinesin
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
VLS-1272 (Compound 22) is an orally active KIF18A inhibitor that binds to the KIF18A-microtubule complex in an ATP-noncompetitive manner (IC50 = 41 nM), blocking its ATPase activity and inhibiting microtubule translocation. This leads to abnormal accumulation of KIF18A at spindle poles, disrupting chromosome alignment and inducing mitotic arrest and apoptosis in CIN High tumor cells (e.g., ovarian cancer OVCAR-3, breast cancer JIMT-1). VLS-1272 is a promising candidate for anti-tumor research .
|
-
- HY-P1137
-
10Panx
1 Publications Verification
|
Gap Junction Protein
|
Others
|
|
10Panx is a competitive inhibitor of selective Pannexin 1 (PANX1) channels. 10Panx blocks the opening of PANX1 channels, inhibits ATP release and downstream P2X7 receptor-mediated signaling pathways, thereby reducing cell death and inflammatory responses. 10Panx can be used in the study of diseases such as neuropathic pain, inflammatory bowel disease, and Clostridioides difficile infection. 10Panx can effectively reduce mechanical hyperalgesia and enhanced C-reflexes, and inhibit the expression of pro-inflammatory factors such as IL-6[1][2][3].
|
-
- HY-135474
-
KM91104
2 Publications Verification
|
ATP Synthase
Toll-like Receptor (TLR)
|
Others
|
|
KM91104 is a cell-permeable V-ATPase a3-b2 inhibitor (IC50 = 2.3 µM). KM91104 reduces the metabolic activity, cell proliferation capacity and V-ATPase subunit protein expression levels of primary human hepatic stellate cells, increases intracellular ATP levels and decreases cytoplasmic pH. KM91104 reduces TLR4 expression on the surface of oligodendrocyte precursor cells, blocks the ENV-TLR4 interaction, and reverses oligodendrocyte myelination defects induced by ENV protein .
|
-
- HY-122658
-
|
MB-1
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
MitoBloCK-1 (MB-1) is an inhibitor that blocks the import of substrates that use the TIM22 import pathway. MitoBloCK-1 inhibits import by preventing binding of substrate to tim9/10 complex to the substrate, thus the substrate failed to be reach the TIM22 translocon. MitoBloCK-1 inhibits protein import of TIM22 substrates into mitochondria. MitoBloCK-1 attenuates the import of the carrier proteins including the ADP/ATP and phosphate carriers. MitoBloCK-1 also inhibits the import of an additional carrier protein, PiC, and the outer membrane protein Tom40 .
|
-
- HY-16461
-
|
(-)-Solenopsin A
|
Akt
Ribosomal S6 Kinase (RSK)
PI3K
PDK-1
FOXO
Mitophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
|
Cardiovascular Disease
|
|
Solenopsin ((-)-Solenopsin A) is an ATP-competitive and selective Akt-1 inhibitor with an IC50 of 5-10 μM, and also acts as an RSK1 inhibitor. Solenopsin inhibits the activities of PDK1 in lipid rafts, downregulates PI3K, blocks PI3K-dependent generation of 3-phosphoinositides, and suppresses the phosphorylation of FOXO1a. Solenopsin induces Mitophagy and ROS production, reduces mitochondrial oxygen consumption, and exhibits antiproliferative and antiangiogenic activities. Solenopsin can be used in research related to hyperproliferative skin diseases and malignant diseases .
|
-
- HY-124253
-
|
|
p97
|
Cancer
|
|
SMDC818909 is an indole amide-derived uncompetitive inhibitor targeting p97 AAA+ ATPase, with an IC50 of 3.5 μM and a Ka of 9.1 μM. SMDC818909 binds to the D2 ATPase domain of p97, preferentially associates with the ADP-bound conformation of p97, allosterically blocks the ATP hydrolysis cycle of p97, and inhibits its mediated intracellular protein homeostasis regulatory function. SMDC818909 is applied to the research and development of p97-targeted antitumor drugs, as well as studies on cancer-related proteotoxic stress mechanisms .
|
-
- HY-N0165R
-
|
|
Reference Standards
HIV
Reverse Transcriptase
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Methyl-Hesperidin (Standard) is the analytical standard of Methyl-Hesperidin (HY-N0165). This product is intended for research and analytical applications. Methyl-Hesperidin is a glycoside compound. Methyl-Hesperidin has hypotensive, coronary dilating, smooth muscle relaxing, capillary stabilizing, choleretic, and anti-ulcer activities. Methyl-Hesperidin act as a competitive substrate to inhibit HIV-1 reverse transcriptase activity. Methyl-Hesperidin potentiates coronary dilating actions of adenine nucleotides and 3'-AMP, enhances depressant action on isolated atria, and prolongs adenosine- and ATP-induced heart block in guinea pigs .
|
-
- HY-121628
-
|
|
Fungal
|
Infection
|
|
Flusulfamide is a sulfonanilide Fungicide that effectively inhibits the germination of resting spores of Plasmodiophora brassicae, the pathogen causing clubroot in cruciferous crops. Flusulfamide blocks the developmental process of resting spores from stage 1 to stage 2. By downregulating germination-related genes and upregulating immunophilin genes (such as PbCyp3), it induces abnormal accumulation of the PbCYP3 protein, thereby causing the spores to deplete energy in a state of continuous energy consumption without germination, and reducing their infectivity. Flusulfamide reduces soil ATP content in the early stage of application, but soil microbial biomass gradually recovers 3 days later. Flusulfamide is widely used in research on clubroot control .
|
-
- HY-182314
-
|
|
JAK
STAT
Apoptosis
|
Cancer
|
|
JAK3-IN-20 is a selective and orally active JAK3 inhibitor with an IC50 of 0.7473 nM. JAK3-IN-20 forms a covalent bond with JAK3 Cys909, outcompetes ATP for catalytic site binding, and blocks JAK-STAT pathway activation. JAK3-IN-20 inhibits migration, proliferation, and tumor growth of Bortezomib (HY-10227)-resistant cancer cells. JAK3-IN-20 induces dose-dependent apoptosis. JAK3-IN-20 can be used for the research of Bortezomib-resistant multiple myeloma .
|
-
- HY-181966
-
|
|
Bacterial
DNA/RNA Synthesis
Potassium Channel
|
Infection
|
|
Sideromycin 7 is an antibacterial agent. Sideromycin 7 forms a 7-Bi 3+ coordination complex with bismuth citrate, exerting a three-pronged antibacterial mode of action: direct DNA binding to induce damage and arrest replication, suppression of KdpC synthesis to block KdpFABC-mediated potas-sium transport, and inhibition of ATP production. Sideromycin 7 exhibits potent antibacterial activity against Ciprofloxacin (HY-B0356)-resistant Pseudomonas aeruginosa strains. Sideromycin 7 exerts antibiofilm activity against Pseudomonas aeruginosa. Sideromycin 7 can be used for the research of ciprofloxacin-resistant Pseudomonas aeruginosa infection .
|
-
- HY-P991444
-
|
|
NTPDase
ATP Synthase
|
Inflammation/Immunology
Cancer
|
|
IPH5201 is a selective CD39 inhibitor and a humanized IgG1 monoclonal antibody. IPH5201 selectively binds to and inhibits the enzymatic activity of both membrane-bound and soluble CD39, blocking ATP hydrolysis. IPH5201 enhances the phenotypic maturation and activation of dendritic cells and macrophages. IPH5201 potentiates the anti-tumor effect of Oxaliplatin (HY-17371). IPH5201 shows preliminary evidence of disease stabilization in advanced solid tumor models when used as a single agent or in combination with Durvalumab (HY-P9919). IPH5201 can be used for the research of advanced solid tumors .
|
-
- HY-137191
-
|
|
EGFR
|
Cancer
|
|
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
|
-
- HY-110333
-
|
|
EGFR
|
Cancer
|
|
BMS-599626 dihydrochloride is a small molecule pan-HER (human epidermal growth factor receptor) kinase inhibitor. BMS-599626 dihydrochloride primarily targets HER1 (IC50=20 nmol/L) and HER2 (IC50=30 nmol/L) kinase activity in the HER family. BMS-599626 inhibits the kinase activity of HER1 and HER2 by competing with their ATP-binding sites, and can inhibit the downstream signaling pathway by blocking the heterodimer formation of HER1 and HER2. BMS-599626 dihydrochloride can be used to study the antitumor effects of multiple HER1 or HER2 overexpressed tumor models .
|
-
- HY-118447
-
|
|
CDK
Survivin
|
Cancer
|
|
RO0505124 is a selective CDK4 inhibitor with an IC50 of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitotic entry, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer .
|
-
- HY-150270A
-
|
|
P2X Receptor
Prostaglandin Receptor
NOD-like Receptor (NLR)
Caspase
Interleukin Related
|
Inflammation/Immunology
|
|
NP-1815-PX sodium is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis) .
|
-
- HY-150270
-
|
|
Prostaglandin Receptor
P2X Receptor
NOD-like Receptor (NLR)
Caspase
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
NP-1815-PX is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX is used in studies related to asthma and inflammatory bowel disease (colitis) .
|
-
- HY-125209A
-
|
|
Apoptosis
PARP
DNA/RNA Synthesis
|
Cancer
|
|
TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
|
-
- HY-17355A
-
|
(R)-Pramipexole dihydrochloride; R-(+)-Pramipexole dihydrochloride; KNS-760704 dihydrochloride
|
ATP Synthase
Sodium Channel
Glutathione Peroxidase
NOD-like Receptor (NLR)
Mitophagy
Ferroptosis
PINK1/Parkin
Autophagy
Apoptosis
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Dexpramipexole ((R)-Pramipexole) dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole dihydrochloride induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more .
|
-
- HY-17355B
-
|
(R)-Pramipexole; R-(+)-Pramipexole; KNS-760704
|
PINK1/Parkin
Glutathione Peroxidase
Sodium Channel
ATP Synthase
NOD-like Receptor (NLR)
Mitophagy
Ferroptosis
Autophagy
Apoptosis
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Dexpramipexole ((R)-Pramipexole) is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more .
|
-
- HY-119976
-
|
|
Environmental Pollutants
Apoptosis
Fungal
Mitochondrial Metabolism
Succinate Dehydrogenase
|
Infection
|
|
Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis .
|
-
- HY-D0976
-
NF279
1 Publications Verification
|
P2X Receptor
HIV
NTPDase
CXCR
|
Infection
|
|
NF279 is a selective P2X1 receptor antagonist and NTPDase inhibitor, with a P2X1 IC50 value of 19 nM. NF279 suppresses GABA-evoked currents, reduces ATP-excited respiratory activity, alters hypoglossal nerve burst parameters, and blocks CXCR4, CCR5, CXCR3, and CXCR7-mediated calcium responses. NF279 arrests HIV-1 fusion downstream of CD4 binding, inhibits R5- and X4-tropic HIV-1 strains. NF279 can be used for the research of HIV-1 infection .
|
-
- HY-183206
-
|
|
Potassium Channel
Calcium Channel
|
Cardiovascular Disease
Inflammation/Immunology
|
|
UR 8225 is an orally active ATP-sensitive K + channel activator with vasodilator, smooth muscle relaxant, antihypertensive, and bronchodilator activities. UR 8225 induces membrane hyperpolarization by increasing outward K + conductance and reduces Ca 2+ influx through voltage-gated L-type Ca 2+ channels. UR 8225 reduces total peripheral vascular resistance, shortens cardiac action potential duration, inhibits agonist-induced Ca 2+ influx, and stimulates renin release. UR 8225 induces reflex tachycardia but lacks β-adrenergic receptor blocking activity. UR 8225 is widely applicable to research in fields related to hypertension, myocardial ischemia, ventricular fibrillation, and other conditions .
|
-
- HY-N1939
-
-
- HY-185215
-
|
|
DNA/RNA Synthesis
RSV
|
Infection
|
|
GS-646089 is a broad-spectrum antiviral nucleoside analog that exhibits significant inhibitory activity against respiratory syncytial virus (RSV), human metapneumovirus (hMPV), rhinovirus (enterovirus) and enteroviruses. The IC50 of GS-646089 targeting RNA-dependent RNA polymerase (RdRp) ranges from 43 to 46 nM. GS-646089 blocks viral replication by being converted into a triphosphate metabolite intracellularly, which competes with ATP for incorporation into nascent RNA strands and acts as an immediate chain terminator. GS-646089 is the parent compound of the double prodrug GS-7682 (HY-161877), and is used in studies of acute respiratory viral infections and infections caused by related pathogens .
|
-
- HY-15322
-
|
P505-15; PRT-2607; BIIB-057
|
Syk
Apoptosis
Caspase
|
Inflammation/Immunology
Cancer
|
|
PRT062607 (P505-15; PRT-2607) is an orally active ATP-competitive Syk inhibitor with an IC50 value of 1 nM, and exhibits at least 80-fold selectivity over other kinases. PRT062607 blocks B cell antigen receptor-mediated activation, Fcε receptor 1-mediated basophil degranulation and microglial phagocytosis, and induces caspase-dependent apoptosis and microglial death. PRT062607 inhibits tumor growth and peripheral nerve injury-induced mechanical allodynia, and prevents neuronal loss. PRT062607 can be used in research related to rheumatoid arthritis, chronic lymphocytic leukemia, non-Hodgkin's lymphoma, neurodegenerative diseases and neuropathic pain .
|
-
- HY-17355AR
-
|
(R)-Pramipexole dihydrochloride (Standard); R-(+)-Pramipexole dihydrochloride (Standard); KNS-760704 dihydrochloride (Standard)
|
Reference Standards
ATP Synthase
Sodium Channel
Glutathione Peroxidase
NOD-like Receptor (NLR)
Mitophagy
Ferroptosis
PINK1/Parkin
Autophagy
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Dexpramipexole ((R)-Pramipexole) dihydrochloride (Standard) is the analytical standard of Dexpramipexole (dihydrochloride). This product is intended for research and analytical applications. Dexpramipexole dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole dihydrochloride induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.
|
-
- HY-17355BS
-
|
(R)-Pramipexole-d3 dihydrochloride; R-(+)-Pramipexole-d3 dihydrochloride; KNS-760704-d3 dihydrochloride
|
Isotope-Labeled Compounds
ATP Synthase
Sodium Channel
Glutathione Peroxidase
NOD-like Receptor (NLR)
Mitophagy
Ferroptosis
PINK1/Parkin
Autophagy
Apoptosis
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Dexpramipexole-d3 ((R)-Pramipexole-d3) dihydrochloride is the deuterium labeled Dexpramipexole. Dexpramipexole ((R)-Pramipexole) dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole dihydrochloride induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.
|
-
- HY-119976S
-
|
|
Isotope-Labeled Compounds
Apoptosis
Fungal
Mitochondrial Metabolism
Succinate Dehydrogenase
|
Others
|
|
Boscalid-d4 is the deuterium labeled Boscalid. Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis .
|
-
- HY-181954
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer .
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-
- HY-108960
-
|
|
P2X Receptor
Interleukin Related
|
Neurological Disease
|
|
PPADS is a P2X receptor (P2X Receptor) antagonist and a reversible competitive antagonist of NAADP receptors, with IC50 values of 68 nM (P2X1) and 214 nM (P2X3), respectively. PPADS alleviates pain-related behaviors in the central and peripheral nervous systems of mice after peripheral neuropathy, inhibits the overproduction of IL-1β, IL-6, iNOS and nNOS, and suppresses the hydrolytic activity of extracellular ATPase. PPADS blocks ATP-mediated inward currents on recombinant rat P2X1 and P2X3 receptors, and inhibits purinergic nerve stimulation-induced contraction of rabbit bladder detrusor muscle. PPADS is applicable to research related to neuropathic pain .
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-
- HY-186072
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
Cytochrome P450
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .
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-
- HY-13817
-
|
|
Deubiquitinase
Autophagy
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Endocrinology
Cancer
|
|
IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
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-
- HY-108659
-
|
|
P2Y Receptor
|
Inflammation/Immunology
|
|
NF340 is a P2Y11 receptor inhibitor with a pIC50 of 7.3-7.7 against human P2Y11 receptor, and it exhibits high selectivity over other P2Y family receptors. NF340 binds to the ATP-binding amino acid residues of the P2Y11 receptor to inhibit its activity, block nociceptive activity, and reduce spinal dorsal horn P2Y11 receptor upregulation induced by spinal cord injury. NF340 attenuates the NFκB signaling pathway activated by IL-1β by decreasing IκBα phosphorylation, nuclear p65 accumulation and NFκB promoter activity. NF340 inhibits IL-1β-induced pro-inflammatory cytokine expression, reduces intracellular ROS and 4-HNE levels, and suppresses IL-1β-induced matrix metalloproteinase expression in primary fibroblast-like synoviocytes. NF340 inhibits ATP-induced elevation of intracellular calcium 2+ concentration and cell migration in human hepatocellular carcinoma cells. NF340 is applicable to the research of neuropathic pain, myocardial ischemia/reperfusion injury, inflammatory pain, rheumatoid arthritis and hepatocellular carcinoma .
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-
- HY-182037
-
|
|
DNA/RNA Synthesis
Pyruvate Kinase
|
Cancer
|
|
Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research .
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-
- HY-182243
-
|
|
Hexokinase
VDAC
Apoptosis
AMPK
Bcl-2 Family
|
Cancer
|
|
HK2-IN-4 is a selective hexokinase 2 (HK2) inhibitor with an IC50 value of 0.79 μM and a Kd value of 0.41 μM. HK2-IN-4 blocks the interaction between HK2 and voltage-dependent anion channel 1 (VDAC1). HK2-IN-4 reduces lactate and ATP levels in cancer cells. HK2-IN-4 induces the production of apoptosis (apoptosis) markers in cancer cells, including increased p-AMPK/AMPK ratio and Bax levels, as well as decreased Bcl2 levels. HK2-IN-4 inhibits the proliferation of cancer cells with high HK2 expression. HK2-IN-4 can be used in research related to colorectal cancer and non-small cell lung cancer .
|
-
- HY-164445
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
|
-
- HY-N1939R
-
|
Icarisid I (Standard)
|
Reference Standards
Apoptosis
Reactive Oxygen Species (ROS)
NOD-like Receptor (NLR)
STAT
CDK
Bcl-2 Family
Aryl Hydrocarbon Receptor
JAK
Caspase
IFNAR
PD-1/PD-L1
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
Icariside I (Standard) is the analytical standard of Icariside I (HY-N1939). This product is intended for research and analytical applications. Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape .
|
-
- HY-119976R
-
|
|
Reference Standards
Apoptosis
Fungal
Mitochondrial Metabolism
Succinate Dehydrogenase
|
Infection
|
|
Boscalid (Standard) is the analytical standard of Boscalid. This product is intended for research and analytical applications. Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis .
|
-
- HY-182383
-
|
|
CDK
Apoptosis
|
Cancer
|
|
VMY-1-101 is a fluorescent cyclin-dependent kinase (CDK) inhibitor, with an excitation of 410 nm and emission of 512 nm. VMY-1-101 competitively inhibits ATP binding to CDKs. VMY-1-101 induces G2/M cell cycle arrest in human breast cancer cells. VMY-1-101 induces modest apoptosis in human breast cancer cells. VMY-1-101 blocks proliferation of human breast cancer cells, including multidrug resistance-positive cells, and is not a substrate for p-glycoprotein. VMY-1-101 localizes to the cytoplasm of human breast cancer cells. VMY-1-101 shows increased binding to human breast cancer tissue compared to fluorophore alone. VMY-1-101 can be used for the research of breast cancer .
|
-
- HY-123859
-
|
|
Casein Kinase
FLT3
CDK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease .
|
-
- HY-181587
-
|
|
PDGFR
Carbonic Anhydrase
STAT
Akt
ERK
Apoptosis
Caspase
|
Cancer
|
|
PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia .
|
-
- HY-159520
-
|
Ofirnoflast; HT-6184
|
NEKs
NOD-like Receptor (NLR)
Caspase
Apoptosis
Pyroptosis
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia .
|
-
- HY-14668
-
|
AEGR-733 mesylate; BMS-201038 mesylate
|
Microsomal Triglyceride Transfer Protein (MTP)
mTOR
LDLR
Autophagy
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
Lomitapide (AEGR-733; BMS-201038) mesylate is an orally active microsomal triglyceride transfer protein (MTP) inhibitor and a selective mTORC1 inhibitor with lipid-lowering activity and BBB permeability. Lomitapide mesylate significantly reduces plasma LDL levels by blocking the assembly and secretion of very-low-density lipoprotein (VLDL). Lomitapide mesylate inhibits mTORC1 in an ATP-dependent manner, thereby inducing AMPK-independent autophagic cell death and suppressing cancer cell growth and apoptosis. Lomitapide mesylate also enhances tumor infiltration of CD8 + T cells. In addition, Lomitapide mesylate inhibits HDAC, improves endothelial function, effectively alleviates vascular inflammation and oxidative stress, and exerts neuroprotective effects in a cerebral ischemia/reperfusion injury model. Lomitapide mesylate can be used in research on related diseases such as colorectal cancer, breast cancer, melanoma, ischemic stroke, and familial hypercholesterolemia .
|
-
- HY-116470
-
|
|
Mps1
|
Cancer
|
|
Mps1/TTK-IN-1 (Compound cpd-5), a derivative of NMS-P715 (HY-12382), is a Mps1 kinase inhibitor with an IC50 of 9.2 nM and a Kd of 1.6 nM. Mps1/TTK-IN-1 specifically targets the ATP-binding pocket of the Mps1 kinase. Mps1/TTK-IN-1 maintains inhibitory activity against Mps1 drug-resistant mutants (C604Y, C604W) with IC50 values of 170 and 19 nM and Kd values of 471 and 349 nM. Mps1/TTK-IN-1 can block the phosphorylation of kinetochore protein KNL1 mediated by Mps1, interfere with the spindle assembly checkpoint function, prevent the correct separation of chromosomes, and thereby inhibit the mitosis and proliferation of tumor cells .
|
-
- HY-173447
-
|
|
NTPDase
CD73
|
Cancer
|
|
8-BuS-AMP is a NTPDase1 inhibitor and a CD73/CD39 inhibitor, with an IC50 of 35 μM and a Ki value of 0.292 μM against human NTPDase1; its Ki values against human CD73 and CD39 are 1.19 μM and 0.847 μM, respectively. 8-BuS-AMP binds to the substrate-binding pockets of NTPDase1 and CD73 to effectively block the conversion of ATP and AMP to adenosine, thereby enhancing the activation and proliferation of human peripheral T lymphocytes. 8-BuS-AMP possesses excellent enzymatic hydrolysis resistance and metabolic stability, resists hydrolysis by multiple NTPDase subtypes, and shows no activity against P2Y1 and P2Y12 receptors. 8-BuS-AMP can be used in purinergic signaling pathway and cancer-related studies .
|
-
- HY-145425
-
|
|
IRE1
Apoptosis
FGFR
|
Inflammation/Immunology
|
|
PAIR2 is a highly selective inhibitor targeting the kinase domain of human IRE1α, with a Ki value of 8.8 nM against human IRE1α. PAIR2 fully occupies the ATP-binding site of the IRE1α kinase domain, partially antagonizes the ribonuclease activity of IRE1α, specifically inhibits regulated IRE1α-dependent decay (RIDD) and its mediated substrate cleavage, while preserving the splicing function of Xbp1 mRNA. PAIR2 also promotes the differentiation of B cells into plasma cells, blocks IRE1α-induced cell apoptosis, and restores the expression of Fgfr2 mRNA in AT2 cells. PAIR2 effectively reaches a steady-state concentration in the lung tissues of Mus musculus, and serves as an important tool for investigating the function of the IRE1α signaling pathway in diseases such as pulmonary fibrosis .
|
-
- HY-142035
-
|
|
Mitochondrial Metabolism
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
N-Propargylglycine is a brain-penetrant and orally active PRODH inhibitor. N-Propargylglycine covalently modifies enzyme-bound FAD and active site lysine, causing enzyme structural distortion, protein decay, and irreversible inhibition of proline and 4-hydroxyproline catabolism. N-Propargylglycine induces UPRmt, upregulates mitochondrial chaperones and YME1L1, enhances mitochondrial proteostasis, blocks astrocytic L-proline consumption, and abolishes L-proline’s ATP-maintaining and viability-protective effects. N-Propargylglycine stimulates neural processes, increases brain proline, hydroxyproline, and sarcosine levels, partially normalizes Huntington’s disease whole brain transcriptomes. N-Propargylglycine reduces hyperoxaluria, prevents calcium oxalate stone formation, reduces kidney tubular damage, and restores weight and survival in Grhpr knockout mice. N-Propargylglycine can be used for the research of breast cancer, neurodegenerative disorders, Huntington’s disease, and primary hyperoxaluria type 2 .
|
-
- HY-W017087
-
|
|
NOD-like Receptor (NLR)
Caspase
Interleukin Related
|
Infection
Metabolic Disease
|
|
1,2,4-Trimethoxybenzene is an orally active NLRP3 selective inhibitor. 1,2,4-Trimethoxybenzene can markedly suppress Nigericin (HY-127019) or ATP (HY-B2176)-induced NLRP3 inflammasome activation, thus decreasing caspase-1 activation and IL-1β secretion. 1,2,4-Trimethoxybenzene specifically inhibits the activation of NLRP3 inflammasome without affecting absent in melanoma 2 (AIM2) inflammasome activation. 1,2,4-Trimethoxybenzene inhibits oligomerization of the apoptosis-associated speck-like protein containing a CARD (ASC) and protein-protein interaction between NLRP3 and ASC, thus blocking NLRP3 inflammasome assembly. 1,2,4-Trimethoxybenzene can be used for the study of experimental autoimmune encephalomyelitis (EAE), multiple sclerosis, and type 2 diabetes .
|
-
- HY-182354
-
|
|
VEGFR
FGFR
FLT3
PDGFR
RET
Akt
ERK
c-Kit
|
Cancer
|
|
VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors .
|
-
- HY-N5112A
-
|
Arnebin 1
|
FGFR
Necroptosis
Apoptosis
CDK
JNK
|
Inflammation/Immunology
|
|
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
|
-
- HY-128586
-
|
|
Apoptosis
Carbonic Anhydrase
NEDD8-activating Enzyme
|
Cancer
|
|
TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
|
-
- HY-128586A
-
|
|
NEDD8-activating Enzyme
Carbonic Anhydrase
Apoptosis
|
Cancer
|
|
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
|
-
-
-
HY-L907
-
|
|
12,412 compounds
|
|
The most prominent mechanism of action of kinase inhibitors is their competition with ATP by binding to the hinge region of the kinase protein. Once the kinase is blocked by an inhibitor, it loses the ability to transfer phosphate groups from ATP to other molecules, resulting in the loss of kinase activity.
The hinge-binding region of kinase inhibitors mimics the interaction pattern between the ATP nucleobase and the kinase. MCE extracted thousands of kinase inhibitors from the ChEMBL database and isolated their molecular fragments. In certain cases, the amino and amide groups on the molecular fragments are crucial for binding in the hinge region. Therefore, we enhanced the diversity of the collected results by adding these two groups to unoccupied positions on the ring system. Subsequently, the fragments were assessed for their hinge region binding ability via docking at distinct kinases, we also applied pharmacophore constraints to ensure interactions with key amino acids in the kinase hinge region, ultimately obtaining kinase-related molecular fragments.
MCE provides over 12,412 kinase fragment molecules that meet the above requirements and are available off the shelf, serving as an effective tool for screening and developing drugs targeting kinases.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D1297
-
|
|
Fluorescent Dye
|
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation .
|
-
- HY-D1431
-
|
|
Fluorescent Dye
|
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation. Ex/Em=587/615 nm .
|
-
- HY-D1429
-
|
|
Fluorescent Dye
|
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206), highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining fixed cells. Staining followed by fixation is possible, but cells fixed with aldehydes will only retain partial fluorescence (Ex/Em = 374/ 430-640 nm) .
|
-
- HY-DY1074
-
|
|
Fluorescent Dye
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206) , highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining fixed cells. Staining followed by fixation is possible, but cells fixed with aldehydes will only retain partial fluorescence .
Solvent and concentration: DMSO: 1 mM
|
-
- HY-DY1043
-
|
|
Fluorescent Dye
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206) , highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation .
Solvent and concentration: DMSO: 1 mM
|
-
- HY-DY1026
-
|
|
Fluorescent Dye
|
ER-Tracker dye is a derivative of BODIPY series dyes coupled with Glibenclamide (HY-15206) , highly selective binding to the endoplasmic reticulum, non-toxic to cells at low concentrations, this type of dye is an environmentally sensitive probe, and formaldehyde treatment can still retain part of the fluorescence, with high fluorescence life, good extinction coefficient and other characteristics. Glibenclamide is an atp-dependent K + channel blocker (Kir6, KATP) and CFTR Cl-channel blocker that binds in the endoplasmic reticulum. ER-Tracker is not suitable for staining cells after fixation. Ex/Em=587/615 nm .
Solvent and concentration: DMSO: 1 mM
|
| Cat. No. |
Product Name |
Type |
-
- HY-119976
-
|
|
Biochemical Assay Reagents
|
|
Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis .
|
-
- HY-W540972
-
|
Primuline
|
Biochemical Assay Reagents
|
|
Primulin is a versatile fluorescent dye and bioactive compound widely used in analytical, biological, botanical and virological studies. Primulin acts as a versatile stain that labels plant cell walls and differentiates live and dead spermatozoa via distinct fluorescence patterns. Primulin exhibits strong albumin‑binding capacity. Primulin acts as a retrograde axonal tracer in neurobiological investigations. Primulin and its derivatives inhibit HCV NS3, block dengue virus NS3-mediated ATP hydrolysis, and disrupt HCV replicase assembly .
|
-
- HY-119976R
-
|
|
Biochemical Assay Reagents
|
|
Boscalid (Standard) is the analytical standard of Boscalid. This product is intended for research and analytical applications. Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1137
-
10Panx
1 Publications Verification
|
Gap Junction Protein
|
Others
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10Panx is a competitive inhibitor of selective Pannexin 1 (PANX1) channels. 10Panx blocks the opening of PANX1 channels, inhibits ATP release and downstream P2X7 receptor-mediated signaling pathways, thereby reducing cell death and inflammatory responses. 10Panx can be used in the study of diseases such as neuropathic pain, inflammatory bowel disease, and Clostridioides difficile infection. 10Panx can effectively reduce mechanical hyperalgesia and enhanced C-reflexes, and inhibit the expression of pro-inflammatory factors such as IL-6[1][2][3].
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- HY-P10856
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P-glycoprotein
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Cancer
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CPI1 is a multidrug resistance protein 1 (MRP1) inhibitor with a Ki value of 100 nM. CPI1 binds to the same substrate-binding site as leukotriene C4, stabilizes MRP1 in an apo-like inward-facing conformation, blocks the conformational changes required for ATP hydrolysis and substrate transport, and inhibits the ATPase activity of human and bovine MRP1. CPI1 serves as a tool for investigating the substrate transport mechanism of MRP1. CPI1 is applicable to research related to cancer multidrug resistance .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P991444
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NTPDase
ATP Synthase
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Inflammation/Immunology
Cancer
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IPH5201 is a selective CD39 inhibitor and a humanized IgG1 monoclonal antibody. IPH5201 selectively binds to and inhibits the enzymatic activity of both membrane-bound and soluble CD39, blocking ATP hydrolysis. IPH5201 enhances the phenotypic maturation and activation of dendritic cells and macrophages. IPH5201 potentiates the anti-tumor effect of Oxaliplatin (HY-17371). IPH5201 shows preliminary evidence of disease stabilization in advanced solid tumor models when used as a single agent or in combination with Durvalumab (HY-P9919). IPH5201 can be used for the research of advanced solid tumors .
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(5)
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- HY-P992446
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NTPDase
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Cancer
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PUR001 is a monoclonal antibody targeting NTPDase 1 (CD39). PUR001 blocks the hydrolysis of extracellular ATP and ADP into AMP by inhibiting CD39, reduces the production of immunosuppressive adenosine, and increases extracellular ATP concentration to activate anti-tumor immune responses. PUR001 can be used in studies related to solid tumors .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N6782
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- HY-16929
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- HY-N0165
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- HY-N1939
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- HY-N5112A
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Arnebin 1
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Quinones
Structural Classification
other families
Classification of Application Fields
Other Diseases
Plants
Naphthalene Quinones
Pteris livida Mett.
Disease Research Fields
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FGFR
Necroptosis
Apoptosis
CDK
JNK
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β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
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- HY-121197
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Ophiocordin; Azepinostatin
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Structural Classification
Natural Products
Microorganisms
Source Classification
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MARCKS
PKA
PKC
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Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
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- HY-125927
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- HY-N1939R
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- HY-N17788
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Structural Classification
Monophenols
Animals
Phenols
Source Classification
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Tie
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6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether is a selective inhibitor of Tie2 kinase, with an IC50 value of 2.1 μM. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether interacts with the ATP binding site of Tie2 kinase, inhibiting kinase activity and subsequently blocking tumor angiogenesis. 6-Hydroxy-2,2′,4,4′-tetrabromodiphenyl ether can be isolated from sponges of the genus Dysidea .
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- HY-N0165R
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Structural Classification
Flavonoids
other families
Flavonones
Phenols
Polyphenols
Plants
Source Classification
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Reference Standards
HIV
Reverse Transcriptase
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Methyl-Hesperidin (Standard) is the analytical standard of Methyl-Hesperidin (HY-N0165). This product is intended for research and analytical applications. Methyl-Hesperidin is a glycoside compound. Methyl-Hesperidin has hypotensive, coronary dilating, smooth muscle relaxing, capillary stabilizing, choleretic, and anti-ulcer activities. Methyl-Hesperidin act as a competitive substrate to inhibit HIV-1 reverse transcriptase activity. Methyl-Hesperidin potentiates coronary dilating actions of adenine nucleotides and 3'-AMP, enhances depressant action on isolated atria, and prolongs adenosine- and ATP-induced heart block in guinea pigs .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-15206S1
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Glyburide-d3 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
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- HY-15206S
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Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
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- HY-B0254S
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Glipizide-d11 is the deuterium labeled Glipizide. Glipizide (CP 2872; K 4024)?a potent, orally active and sulfonylurea class anti-diabetic agent and can be used for type 2?diabetes mellitus research but not type 1. Glipizide acts by partially blocking ATP-sensitive potassium?(KATP) channels among β cells of pancreatic islets of Langerhans .
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- HY-B0860S
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Diuron-d6 is the deuterium labeled Diuron (HY-B0860). Diuron is an orally active phenylurea herbicide. Diuron inhibits photosynthesis in plants by blocking the formation of ATP and NADH. Diuron increases the production of ROS. Diuron increases expression of p53 in certain cell lines. Diuron has herbicidal activity against annual and perennial broadleaf weeds and grass weeds. Diuron promotes DMBA/BBN-induced bladder cancer. Diuron can be used in breast cancer research .
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- HY-B0753S
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Gliclazide-d4 (S1702 D4) is the deuterium labeled Gliclazide. Gliclazide (S1702) is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM. Gliclazide is used as an antidiabetic .
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- HY-B0347S1
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Lacidipine- 13C8 is the deuterium labeled Lacidipine . Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
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- HY-17355BS
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Dexpramipexole-d3 ((R)-Pramipexole-d3) dihydrochloride is the deuterium labeled Dexpramipexole. Dexpramipexole ((R)-Pramipexole) dihydrochloride is an orally active, blood-brain barrier permeable mitochondrial protective agent. Dexpramipexole dihydrochloride upregulates the expression of Parkin, PINK1, GPX4 and FSP1; binds to mitochondrial F1/Fo-ATP synthase; blocks the Nav1.8 sodium channel; and inhibits the activation of the NLRP3 inflammasome. Dexpramipexole dihydrochloride induces mitophagy, inhibits ferroptosis, pyroptosis, apoptosis, neuroinflammation and eosinophilopoiesis; maintains mitochondrial function and redox homeostasis; reduces reactive oxygen species production; and decreases myocardial infarct size. Dexpramipexole dihydrochloride is applicable to studies on eosinophilic asthma, myocardial ischemia/reperfusion injury, sepsis-associated encephalopathy, analgesia, and more.
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- HY-W723322
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Ethyl tosylcarbamate-d7 is the deuterium labeled Ethyl tosylcarbamate (HY-135337). Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877) . Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM .
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- HY-B0347S3
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Lacidipine- 13C4 is 13C labeled Lacidipine (HY-B0347). Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI) .
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- HY-15206S2
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Glibenclamide- 13C6 (Glyburide- 13C6) is 13C labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K + channel (KATP) inhibitor and can be used for the research of diabetes and obesity . Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR) . Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability . Glibenclamide can induce autophagy .
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- HY-119976S
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Boscalid-d4 is the deuterium labeled Boscalid. Boscalid is a succinate dehydrogenase (SDHI) inhibitor with antifungal activity. Boscalid binds to the ubiquinone-binding site of fungal mitochondrial complex II, blocks ATP production and aerobic respiration, exhibits good control efficacy against a variety of plant fungal diseases including gray mold, sclerotinia rot and powdery mildew, and is widely used for disease control in agriculture. Boscalid induces apoptosis, altered lipid metabolism, mitochondrial dysfunction, respiratory impairment, oxidative stress, ROS accumulation and neurodevelopmental disorders in zebrafish. Boscalid reduces foraging ability, shortens median death time and causes chronic toxicity in exposed honeybees. Boscalid also possesses genotoxicity, cytotoxicity, elevated mitochondrial superoxide levels and early-stage apoptosis .
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| Cat. No. |
Product Name |
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Classification |
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- HY-142035
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Alkynes
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N-Propargylglycine is a brain-penetrant and orally active PRODH inhibitor. N-Propargylglycine covalently modifies enzyme-bound FAD and active site lysine, causing enzyme structural distortion, protein decay, and irreversible inhibition of proline and 4-hydroxyproline catabolism. N-Propargylglycine induces UPRmt, upregulates mitochondrial chaperones and YME1L1, enhances mitochondrial proteostasis, blocks astrocytic L-proline consumption, and abolishes L-proline’s ATP-maintaining and viability-protective effects. N-Propargylglycine stimulates neural processes, increases brain proline, hydroxyproline, and sarcosine levels, partially normalizes Huntington’s disease whole brain transcriptomes. N-Propargylglycine reduces hyperoxaluria, prevents calcium oxalate stone formation, reduces kidney tubular damage, and restores weight and survival in Grhpr knockout mice. N-Propargylglycine can be used for the research of breast cancer, neurodegenerative disorders, Huntington’s disease, and primary hyperoxaluria type 2 .
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