Search Result
Results for "
time-dependent inhibitor
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-139664
-
|
|
DNA Methyltransferase
|
Cancer
|
|
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
-
- HY-108341A
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
|
-
-
- HY-108341
-
PF-06424439
Maximum Cited Publications
25 Publications Verification
|
Acyltransferase
|
Metabolic Disease
|
|
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
|
-
-
- HY-N0220
-
-
-
- HY-B0363
-
|
R805
|
COX
|
Inflammation/Immunology
Cancer
|
|
Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
|
-
-
- HY-135334
-
|
|
Drug Metabolite
Btk
Cytochrome P450
|
Cancer
|
|
ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM .
|
-
-
- HY-18642
-
|
PF-4981517
|
Cytochrome P450
|
Others
|
|
CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on agent metabolism .
|
-
-
- HY-19832
-
SC66
5 Publications Verification
|
MOFs
Akt
Apoptosis
|
Cancer
|
|
SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
|
-
-
- HY-W704574
-
|
|
Carboxypeptidase
Bradykinin Receptor
Interleukin Related
|
Cardiovascular Disease
Metabolic Disease
|
|
Mergetpa is a reversible Arg-carboxypeptidase inhibitor with high affinity. Mergetpa reduces B1R. Mergetpa blocks the overexpression of IL-1β protein and mRNA in glucose-fed rats. Mergetpa significantly increases the expression of IL-1β protein in the renal cortex. Mergetpa is used to block the conversion of kinins and B2 receptor antagonists into metabolites lacking the C-terminal arginine. Mergetpa inhibits the time-dependent enhancement of the response of isolated rabbit aorta to bradykinin. Mergetpa preserves the chemotactic activity of full-length SDF-1α on cells. Mergetpa reverses hyperglycemia, excessive weight gain, elevated levels of oxidative stress markers and overexpression of inflammatory markers in glucose-fed rats .
|
-
-
- HY-160924
-
|
|
PROTACs
BMI1
E1/E2/E3 Enzyme
Histone Methyltransferase
|
Cancer
|
|
MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H2A Lys119 mono-ubiquitination without altering histone H3 Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma . (Pink: BMI1/RING1B ligand (HY-183634); Blue: VHL ligand (HY-125845); Black: linker)
|
-
-
- HY-P3579
-
|
GIP (1-42), porcine
|
Insulin Receptor
|
Metabolic Disease
|
|
Gastric Inhibitory Peptide (GIP (1-42)), porcine is a porcine glucose-dependent insulinotropic polypeptide and inhibitor of pentagastrin-stimulated gastric acid secretion. Gastric Inhibitory Peptide, porcine stimulates endogenous somatostatin release. Gastric Inhibitory Peptide, porcine acts in a dose- and time-dependent manner in conscious, chronic gastric fistula-equipped rats .
|
-
-
- HY-N6744
-
|
|
Apoptosis
Endogenous Metabolite
Fungal
Parasite
Arp2/3 Complex
|
Infection
Cancer
|
|
Chaetoglobosin A is a secondary metabolite and nematicide. Chaetoglobosin A is produced by Penicillium aquamarinium. Chaetoglobosin A targets Filamentous actin in cells, thereby inducing cell cycle arrest, and inhibiting membrane ruffle formation and cell migration. Chaetoglobosin A preferentially induces Apoptosis in chronic lymphocytic leukemia cells. Chaetoglobosin A induces dose- and time-dependent death in J2 larvae of the southern root-knot nematode (Meloidogyne incognita). Chaetoglobosin A can be used in studies related to root-knot nematode disease and chronic lymphocytic leukemia .
|
-
-
- HY-15648C
-
GSK-J5
1 Publications Verification
|
Histone Demethylase
Parasite
|
Cancer
|
|
GSK-J5 is a potent inhibitor of Schistosome and worm. GSK-J5 increases schistosomula mortality and adult worm motility and mortality, as well as egg oviposition, in a dose- and time-dependent manner .
|
-
-
- HY-16718
-
|
PF-00251802
|
Glucocorticoid Receptor
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
|
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
|
-
-
- HY-110023
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .
|
-
-
- HY-N2382
-
|
|
Cytochrome P450
P-glycoprotein
|
Metabolic Disease
Cancer
|
|
Polyphyllin H is a steroidal saponin. Polyphyllin H is isolated from Paris polyphylla. Polyphyllin H potently inhibits the activities of CYP1A2 (IC50 = 6.44 μM, competitive), CYP2D6 (IC50 = 13.88 μM, competitive) and CYP3A4 (IC50 = 4.52 μM, non-competitive, time-dependent). Polyphyllin H downregulates the expression of ABCB1 and ABCC3. Polyphyllin H binds to membrane cholesterol and disrupts lipid raft structures. Polyphyllin H restores the sensitivity of paclitaxel-resistant breast cancer cells to paclitaxel .
|
-
-
- HY-N8146
-
|
|
STAT
Bcl-2 Family
Ser/Thr Kinase
Survivin
c-Myc
Apoptosis
Necroptosis
CDK
|
Infection
Cancer
|
|
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
|
-
-
- HY-139664A
-
|
|
DNA Methyltransferase
|
Cancer
|
|
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
-
- HY-133862
-
-
-
- HY-155811
-
|
|
iGluR
|
Neurological Disease
|
|
DQP-997-74 (compound 2i) is a selective negative allosteric modulator of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC50: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases .
|
-
-
- HY-110012
-
|
|
Adenosine Receptor
|
Infection
|
|
SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 μM .
|
-
-
- HY-111560
-
|
|
Potassium Channel
|
Neurological Disease
|
|
IQM-266 is a Downstream Regulatory Element Antagonist Modulator (DREAM) ligand with a KD of 4.63 μM. IQM-266 inhibits the KV4.3/DREAM current in a concentration-, voltage-, and time-dependent-manner. IQM-266 also modulates A-type outward potassium currents (IA) from rat dorsal root ganglia (DRG) neurons. IQM-266 can be used for neurological disease research, such as Alzheimer’s disease and Huntington's disease (HD) .
|
-
-
- HY-151285
-
|
|
Apoptosis
JAK
|
Inflammation/Immunology
Cancer
|
|
JAK-2-/3-IN-3 (compound ST4j) is a potent JAK2/3 inhibitor with IC50s of 13.00 and 14.86 nM for JAK2 and JAK3, respectively. JAK-2-/3-IN-3 inhibits autophosphorylation of JAK2 and induces apoptosis in a dose- and time-dependent manner. JAK-2-/3-IN-3 can be used in studies of lymph derived diseases and leukemia .
|
-
-
- HY-U00197
-
|
JTE522; JTP19605; RWJ57504
|
COX
|
Inflammation/Immunology
|
|
Tilmacoxib (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC50 of 85 nM in an enzyme assay.
|
-
-
- HY-172091
-
|
|
EGFR
|
Cancer
|
|
CZY43 is a HER3 degrader. CZY43 can effectively induce HER3 degradation in a dose- and time-dependent manner in breast cancer SKBR3 cells. CZY43 potently inhibits HER3-dependent signaling and cancer cell growth and outperforms Bosutinib (HY-10158) .
|
-
-
- HY-16718A
-
|
PF-00251802 hydrochloride
|
Glucocorticoid Receptor
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
|
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
|
-
-
- HY-118835
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance .
|
-
-
- HY-W012896
-
|
|
Biochemical Assay Reagents
|
Others
|
|
2-Thiohydantoin acts as an inhibitor for the corrosion of mild steel in 0.1 M HCl and its inhibition efficiency is both concentration and immersion time dependent .
|
-
-
- HY-162464
-
|
|
PROTACs
SARS-CoV
|
Infection
|
|
MPD2 is a Cereblon-binding ligand-based PROTAC that degrades MPro, the main protease of SARS-CoV-2. MPD2 effectively reduced MPro protein levels in 293T cells in a time-dependent manner (DC50=296 nM). MPD2 exhibited potent antiviral activity against multiple SARS-CoV-2 strains and had enhanced potency against Nirmatrelvir (HY-138687) resistant strains. MPD2 provides a new direction for antiviral drug development against SARS-CoV-2 and other emerging coronavirus pathogens (Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker (HY-W275882);Red: SARS-CoV-2 MPro Inhibitor MP18 (HY-158763)) .
|
-
-
- HY-N6842
-
|
|
Others
|
Infection
Cancer
|
|
ArnicolideC is a sesquiterpene lactone isolated Centipeda minima . ArnicolideC exertes a cytotoxic effect on the panel of Nasopharyngeal carcinoma (NPC) cells, significantly inhibiting cell growth in a dose- and time- dependent manner. ArnicolideC also exhibits inhibitory effects on NPC proliferation .
|
-
-
- HY-139664B
-
|
|
DNA Methyltransferase
|
Cancer
|
|
(S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
-
- HY-158309
-
|
|
Aminotransferases (Transaminases)
|
Cancer
|
|
hOAT-IN-1 (compound 5) is a mechanical inhibitor of human ornithine aminotransferase (hOAT). hOAT-IN-1 as a time-dependent inhibitor can form tightly bound PLP inhibitor adduct with hOAT. hOAT-IN-1 can result IN tight occupation of the active site of hOAT. hOAT-IN-1 can be used in the study of lung cell carcinoma .
|
-
-
- HY-144689
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-3 (compound 45a) is a potent, selective, time-dependent and pseudoirreversible BChE inhibitor, with an IC50 of 56.9 nM. BChE-IN-3 also shows marginal and reversible (not time-dependent) inhibition of AChE .
|
-
-
- HY-106855
-
|
H 234/09
|
Potassium Channel
|
Cardiovascular Disease
|
|
Almokalant is a class III antiarrhythmic agent, acts as a potassium channel blocker, and inhibits a specific component (Ikr) of the time-dependent delayed rectifier K + current.
|
-
-
- HY-143468
-
|
|
Apoptosis
MEK
|
Cancer
|
|
MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
|
-
-
- HY-P4302
-
|
Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone
|
Cathepsin
|
Cardiovascular Disease
|
|
Z-FK-ck (Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone) is a potent and selective gingipain-K-specific inhibitor. Z-FK-ck prolongs plasma thrombin time (TT) in a dose- and time-dependent manner .
|
-
-
- HY-170962
-
|
|
Neprilysin
Aminopeptidase
|
Neurological Disease
|
|
SDUY817 is a dual APN/NEP inhibitor, with IC50 values of 0.29 μM for APN and 7.4 μM for NEP. SDUY817 exerts analgesic effects in a concentration- and time-dependent manner, and can be used for research in the field of neuropathic pain disorders .
|
-
-
- HY-18642A
-
|
(R)-PF-4981517
|
Cytochrome P450
|
Others
|
|
(R)-CYP3cide ((R)-PF-4981517) is the R-isomer of CYP3cide (HY-18642). CYP3cide is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4) .
|
-
-
- HY-N0220R
-
-
-
- HY-115750
-
|
|
NO Synthase
|
Neurological Disease
|
|
Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O .
|
-
-
- HY-B0363S
-
|
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
|
|
Nimesulide-d5 is a deuterium labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties .
|
-
-
- HY-B0363R
-
|
R805 (Standard)
|
Reference Standards
COX
|
Inflammation/Immunology
Cancer
|
|
Nimesulide (Standard) is the analytical standard of Nimesulide. This product is intended for research and analytical applications. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
|
-
-
- HY-B0363S1
-
|
R805-13C6
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
Cancer
|
|
Nimesulide- 13C6 (R805- 13C6) is 13C labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
|
-
-
- HY-108704
-
|
|
Bcr-Abl
|
Cancer
|
|
CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities . CT-721 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-100740A
-
|
AZD-3293 hydrochloride; LY3314814 hydrochloride
|
Beta-secretase
|
Neurological Disease
|
|
Lanabecestat (AZD3293; LY3314814) hydrochloride is a potent BACE1 inhibitor that has been investigated for its potential as a modifying treatment for Alzheimer's disease. Lanabecestat (hydrochloride) demonstrated significant dose- and time-dependent reductions in concentrations of amyloid beta peptides in plasma, cerebrospinal fluid, and brain. Lanabecestat (hydrochloride) was also shown to produce reductions in Aβ neuritic plaque burden without demonstrating clinical benefits or slowing the progression of Alzheimer's disease pathophysiology.
|
-
-
- HY-N13739
-
|
|
Tyrosinase
|
Cancer
|
|
Taraxinic acid can be found in the roots of Taraxacum flavostylum and Taraxacum lucidum. It is a Tyrosinase inhibitor that dose-dependently inhibits Tyrosinase activity, showing approximately 54.5% inhibition at a concentration of 50 μg/mL. Taraxinic acid has an IC50 of 83.2 μM against melanoma cells A375 and HTB140, and an IC50 of 60.4 μM against melanoma cells WM793, with activity being both dose- and time-dependent. Taraxinic acid holds promise for research in the field of anticancer therapy .
|
-
-
- HY-117540
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
|
-
-
- HY-N7854
-
|
Anacardic acid 15:2
|
Bacterial
|
Infection
|
|
Anacardic acid diene is a polyunsaturated form of anacardic acid (HY-N2020) that has been found in cashew nut shell liquid. It has antibacterial activity against methicillin resistant S. aureus (MRSA) and S. mutans (MICs=12.5 and 6.25 μg/mL, respectively). Anacardic acid diene has schistosomicidal activity against adult S. mansoni worms when used at a concentration of 100 μM. It also inhibits soybean lipoxygenase-1 in a time-dependent manner.
|
-
-
- HY-135334S
-
|
|
Isotope-Labeled Compounds
Drug Metabolite
Btk
Cytochrome P450
|
Cancer
|
|
ACP-5862-d4 is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM .
|
-
-
- HY-168072
-
|
|
Interleukin Related
Apoptosis
Autophagy
|
Cancer
|
|
GP130-IN-1 (compound 49) is a potent GP130 inhibitor with significant in vitro antitumor activity and higher selectivity than Bazedoxifene (HY-A0031). GP130-IN-1 induces ultrastructural changes in cells, causing cell cycle arrest in the G0/G1 phase in a time-dependent manner and triggering apoptosis and autophagy. GP130-IN-1 can be used in the study of triple-negative breast cancer .
|
-
- HY-178149
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-A/B-IN-5 is an orally active MAO-A (IC50 = 73.88 μM) and MAO-B (IC50 = 91.08 μM) inhibitor. MAO-A/B-IN-5 reverses Sodium nitroprusside (SNP) (HY-B0564)-induced cerebral lipid peroxidation (IC50 = 130.2 μM) and protein carbonylation (IC50 = 229.8 μM). MAO-A/B-IN-5 shows dose-dependent and time-dependent antidepressant-like efficacy in mice. MAO-A/B-IN-5 can be used for the study of depressive disorder .
|
-
- HY-110023R
-
|
|
Reference Standards
Serotonin Transporter
|
Neurological Disease
|
|
Zimelidine dihydrochloride (Standard) is the analytical standard of Zimelidine dihydrochloride (HY-110023). This product is intended for research and analytical applications. Zimelidine dihydrochloride is an orally active selective serotonin reuptake inhibitor. Zimelidine dihydrochloride competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine dihydrochloride time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine dihydrochloride strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine dihydrochloride exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine dihydrochloride is used for the study of depressive disorders and analgesic tolerance .
|
-
- HY-118835S
-
|
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Neurological Disease
|
|
Zimeldine-d6 is the deuterium labeled Zimeldine (HY-118835) . Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance .
|
-
- HY-146314
-
|
|
Monoamine Oxidase
Amyloid-β
|
Neurological Disease
|
|
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-150576
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-13 is a potent c-Met inhibitor with an IC50 value of 2.43 nM. c-Met-IN-13 shows excellent cytotoxicity for cancer cells. c-Met-IN-13 shows antiproliferative activity in a concentration- and time- dependent manner. c-Met-IN-13 has the potential for the research of cancer .
|
-
- HY-146312
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BChE/MAO-B-IN-1 is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity .
|
-
- HY-W587743
-
|
AMK hydrochloride
|
Prostaglandin Receptor
PGE synthase
COX
Reactive Oxygen Species (ROS)
|
Neurological Disease
Metabolic Disease
|
|
N1-Acetyl-5-methoxykynuramine (AMK) hydrochloride is an active metabolite of the neurohormone melatonin (HY-B0075). N1-Acetyl-5-methoxykynuramine hydrochloride (200 µM) effectively scavenges singlet oxygen (ROS).1 It also inhibits the production of prostaglandin E2 (PGE2) and prostaglandin D2 (PGD2) induced by epinephrine and arachidonic acid in a concentration- and time-dependent manner, and suppresses the increase in COX-2 levels induced by LPS (HY-D1056) in RAW 264.7 macrophages at a concentration of 500 µM. In a mouse model of Parkinson's disease induced by MPTP (HY-15608), N1-Acetyl-5-methoxykynuramine hydrochloride (20 mg/kg) reduces the increase in lipid peroxidation in the cytosol and mitochondria of the substantia nigra and striatum. N1-Acetyl-5-methoxykynuramine hydrochloride can be used in research on metabolic and neurological diseases
|
-
- HY-W800105
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Geranyl isovalerate is a chemical component that can be extracted from Argyreia Nervosa. Geranyl isovalerate inhibits cancer cell proliferation in a dose-dependent and time-dependent manner. Geranyl isovalerate activates the apoptotic pathway by inducing mitochondrial membrane potential loss and ROS accumulation. Geranyl isovalerate can be used for cancer research .
|
-
- HY-180609
-
|
|
MHC
Interleukin Related
CD3
IFNAR
|
Inflammation/Immunology
|
|
TCR-IN-2 (Compound A-68) is a TCR inhibitor. TCR-IN-2 inhibits the release of IFNγ and IL-2. TCR-IN-2 inhibits the time-dependent phosphorylation of CD3ζ. TCR-IN-2 inhibits TCR-mediated T cell activation, both in response to anti-CD3 antibodies and in response to human cells with unmatched HLA .
|
-
- HY-108341R
-
|
|
Reference Standards
Acyltransferase
|
Metabolic Disease
|
|
PF-06424439 (Standard) is the analytical standard of PF-06424439 (HY-108341). This product is intended for research and analytical applications. PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
|
-
- HY-123965
-
|
|
MAP4K
TNF Receptor
|
Metabolic Disease
Cancer
|
|
PF-06745013 (Compound 37) is a MAP4K4 inhibitor without time-dependent inhibition (TDI) risk of CYP3A4 (IC50 of 0.4 nM for MAP4K4). PF-06745013 has no accumulation CNS-impaired and non-ATP competitive activities in mouse models. PF-06745013 can be used for inflammatory diseases like diabetes and cancers research .
|
-
- HY-108341AR
-
|
|
Reference Standards
Acyltransferase
|
Metabolic Disease
|
|
PF-06424439 methanesulfonate (Standard) is the analytical standard of PF-06424439 (methanesulfonate) (HY-108341A). This product is intended for research and analytical applications. PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
|
-
- HY-182612
-
|
|
TGF-β Receptor
|
Cancer
|
|
SRI-35241 is a thrombospondin TSP-1 inhibitor with a pIC50 of 8.12 nM against human targets. SRI-35241 inhibits the binding of TSP-1 to latent transforming growth factor-β-associated peptide (LAP) and blocks the activation of TGF-β. SRI-35241 shows a certain time-dependent property, with a plasma half-life of 1.8 h after intravenous administration. SRI-35241 can be used for the research of multiple myeloma and fibrotic diseases .
|
-
- HY-180969
-
|
|
PROTACs
Bcr-Abl
|
Cancer
|
|
SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research .
|
-
- HY-179383
-
|
|
Bacterial
|
Infection
|
|
DprE1-IN-14 (Compound 77) is a DprE1 inhibitor, with an IC50 value of 2.5 nM for M. tb. DprE1-IN-14 exhibits anti-tuberculosis activity, with an MIC₉₀ of 0.3 μM for the M. tb mc26230 strain. DprE1-IN-14 mainly shows bacteriostatic activity, demonstrating a time-dependent bactericidal effect at 10-fold MIC concentrations. DprE1-IN-14 can be used in anti-tuberculosis research .
|
-
- HY-P992379
-
|
BAG3-H2L4
|
Bcl-2 Family
|
Cancer
|
|
IB001 is a humanized anti-BAG3 antibody that inhibits BAG3, with a KD value of 14.4 nM for human BAG3. IB001 blocks BAG3-dependent monocyte/macrophage activation, interferes with the interaction between BAG3 and IFITM-2, and disrupts tumor microenvironment signaling pathways. IB001 inhibits tumor growth, reduces α-SMA-positive fibroblasts, and blocks BAG3-dependent IL-6 release. IB001 accumulates in a time-dependent manner in pancreatic ductal adenocarcinoma tumors. IB001 can be used for research related to pancreatic ductal adenocarcinoma .
|
-
- HY-W012896R
-
-
- HY-182382
-
|
|
Apoptosis
MDM-2/p53
Caspase
|
Cancer
|
|
Anticancer agent 311 is an apoptosis inducer and p53 modulator. Anticancer agent 311 increases p53 levels, activates cleaved caspase-3, reduces p-Cdc25C levels, and disrupts p-p44/42 MAPK phosphorylation. Anticancer agent 311 induces G2/M phase arrest, inhibits cancer cell viability in a concentration- and time-dependent manner, and exhibits low toxicity to non-cancer cells. Anticancer agent 311 prevents tumor growth and angiogenesis in mouse xenograft models without detectable toxicity. Anticancer agent 311 can be used for the research of lung cancer .
|
-
- HY-N10188
-
|
|
Others
|
Cancer
|
|
Nidurufin is a potent cell cycle inhibitor with antitumor activity.Nidurufin induces in vitro cell cycle arrest at G2/M transition in the K562 cell line in a concentration and time dependent manner(IC50=12.6 μM) .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3579
-
|
GIP (1-42), porcine
|
Insulin Receptor
|
Metabolic Disease
|
|
Gastric Inhibitory Peptide (GIP (1-42)), porcine is a porcine glucose-dependent insulinotropic polypeptide and inhibitor of pentagastrin-stimulated gastric acid secretion. Gastric Inhibitory Peptide, porcine stimulates endogenous somatostatin release. Gastric Inhibitory Peptide, porcine acts in a dose- and time-dependent manner in conscious, chronic gastric fistula-equipped rats .
|
-
- HY-P4302
-
|
Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone
|
Cathepsin
|
Cardiovascular Disease
|
|
Z-FK-ck (Z-Phe-Lys-2,4,6-Trimethylbenzoyloxy-methylketone) is a potent and selective gingipain-K-specific inhibitor. Z-FK-ck prolongs plasma thrombin time (TT) in a dose- and time-dependent manner .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P992379
-
|
BAG3-H2L4
|
Bcl-2 Family
|
Cancer
|
|
IB001 is a humanized anti-BAG3 antibody that inhibits BAG3, with a KD value of 14.4 nM for human BAG3. IB001 blocks BAG3-dependent monocyte/macrophage activation, interferes with the interaction between BAG3 and IFITM-2, and disrupts tumor microenvironment signaling pathways. IB001 inhibits tumor growth, reduces α-SMA-positive fibroblasts, and blocks BAG3-dependent IL-6 release. IB001 accumulates in a time-dependent manner in pancreatic ductal adenocarcinoma tumors. IB001 can be used for research related to pancreatic ductal adenocarcinoma .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0363S
-
|
|
|
Nimesulide-d5 is a deuterium labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties .
|
-
-
- HY-B0363S1
-
|
|
|
Nimesulide- 13C6 (R805- 13C6) is 13C labeled Nimesulide. Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
|
-
-
- HY-135334S
-
|
|
|
ACP-5862-d4 is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM .
|
-
-
- HY-118835S
-
|
|
|
Zimeldine-d6 is the deuterium labeled Zimeldine (HY-118835) . Zimelidine is an orally active selective serotonin reuptake inhibitor. Zimelidine competitively inhibits central 5-HT uptake and desensitizes 5-HT autoreceptors in dorsal raphe nucleus. Zimelidine time-dependently modulates 5-HT neuronal firing and hippocampal CA3 responses. Zimelidine strengthens central serotonergic neurotransmission and produces related behavioral changes. Zimelidine exerts anxiolytic, analgesic, feeding-suppressive and tolerance-attenuating effects. Zimelidine is used for the study of depressive disorders and analgesic tolerance .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-146314
-
|
|
|
Alkynes
|
|
MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: