Search Result
Results for "
mouse microsomes
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-100432
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LOC14
4 Publications Verification
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PDI
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Neurological Disease
Inflammation/Immunology
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LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
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- HY-150508
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MK-0159
1 Publications Verification
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CD38
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .
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- HY-157421
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NAMPT
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Metabolic Disease
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Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD +, thereby enhancing enzymatic activity and significantly increasing intracellular NAD + levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders .
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- HY-40351
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Drug Intermediate
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Others
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4-Chloro-7H-pyrrolo[2,3-d]pyrimidine is a nitrogen-containing heterocyclic organic synthesis intermediate that can be used for the synthesis of JAK and PKB/Akt inhibitors .
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-
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- HY-15163
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TG02; SB1317
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JAK
CDK
FLT3
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Cancer
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Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
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- HY-167856
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GPR88
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Neurological Disease
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RTI-122 is a selective, blood-brain barrier-permeable GPR88 agonist (cAMP EC50=11 nM), with EC50 values of 11.5 nM and 155 nM for human and mouse GPR88, respectively ([ 35S]GTPγS assay). By activating the GPR88 receptor to regulate the cAMP signaling pathway and G protein activity, RTI-122 significantly attenuates Binge-like drinking, reduces alcohol intake, and decreases alcohol-seeking motivation. RTI-122 blocks the reinstatement of alcohol-seeking behavior without affecting water or sucrose intake. RTI-122 exhibits metabolic stability in mice (T1/2=5.8 h) and can be used to investigate alcohol use disorder .
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- HY-162455
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EAAT
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Neurological Disease
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NA-014 is an excitatory amino acid transporter 2 (EAAT2)-selective positive allosteric modulator. NA-014 increases EAAT2-mediated glutamate uptake. NA-014 can be used for the research of epilepsy, neuropathic pain, stroke, drugs of abuse disorders .
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- HY-107460
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Ephrin Receptor
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Cancer
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LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC .
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- HY-153508
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Chloride Channel
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Others
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ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC50 of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
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- HY-W015782
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Tyrosinase
PKA
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Metabolic Disease
Inflammation/Immunology
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4-Ethylresorcinol is a derivative of resorcinol and can serve as a substrate for tyrosinase. 4-Ethylresorcinol has anti-hyperpigmentation and antioxidant effects and can inhibit melanin synthesis. 4-Ethylresorcinol has potential whitening value .
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- HY-128268
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Parasite
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Infection
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PFK-IN-1 (compound 1) is a phosphofructokinase (PFK) inhibitor, with IC50 values of 0.41 and 0.23 μM against T.brucei and T.cruzi PFK, respectively, and an ED50 of 15.18 μg/mL for T.brucei. The half-lives of PFK-IN-1 in rat and mouse liver microsomes are 9.7 and 408 minutes, respectively .
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- HY-163032
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FABP
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Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
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FABP4-IN-3 (compound C3) is a highly selective FABP4 inhibitor (FABP4 Ki = 25 ± 3 a nM, FABP3 Ki = 15.03 μM) which exhibits a 601-fold selectivity over FABP3. FABP4-IN-3 also shows metabolic stability and potent cellular anti-inflammatory activity, making it promising to get involved in the research of metabolic disease, cardiac dysfunction and inflammation-related disease .
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- HY-168328
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NF-κB
Interleukin Related
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Inflammation/Immunology
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FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
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- HY-175533
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Toll-like Receptor (TLR)
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Neurological Disease
Inflammation/Immunology
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TLR2 antagonist-1 is a selective Toll-like receptor 2 (TLR2) antagonist. TLR2 antagonist-1 can effectively inhibit excessive TLR2 activation (IC50 = 11.41 μM) and the production of inflammatory factors. TLR2 antagonist-1 has metabolic stability with a half-life (T1/2) of 16.67 min in mouse liver microsomes. TLR2 antagonist-1 can be used for the researches of inflammation, immunology, and neurological disease .
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- HY-151229
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DETC-Me; DDTC-Me; Diethyldithiocarbamic acid methyl ester
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Aldehyde Dehydrogenase (ALDH)
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Metabolic Disease
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S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) is the active metabolite of the aldehyde dehydrogenase inhibitor disulfiram (HY-B0240). It is produced by the methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes. S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) inhibits rat liver low Km aldehyde dehydrogenase (ALDH) (ID50=15.5 mg/kg). When administered at a dose of 20.6 mg/kg, it decreases mean arterial pressure (MAP) and increases heart rate in rats during ethanol stimulation.
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- HY-B1341
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Enidrel; SC-4642; NSC 15432
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Endogenous Metabolite
Progesterone Receptor
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Cancer
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Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
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- HY-143255
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Phosphodiesterase (PDE)
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Cancer
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Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouse plasma. Enpp-1-IN-11 can be used for researching anticancer .
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- HY-118717
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mTOR
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Cancer
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mTOR inhibitor WYE-28 (compound 28) is a selective inhibitor of mTOR>/b< (IC50)=0.08 nM. mTOR inhibitor WYE-28 inhibits PI3Kα with an IC50 value of 6 nM. mTOR inhibitor WYE-28 shows a metabolic time (T1/2) in nude mouse microsomes of 13 min .
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- HY-156672
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FGFR
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Cancer
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S6K2-IN-1 (Compound 2) is a S6K2 inhibitor (IC50: 22 nM). S6K2-IN-1 also inhibits FGFR4 (IC50: 216 nM). S6K2-IN-1 has acceptable stability in mouse liver microsomes .
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- HY-170546
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Haspin Kinase
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Cancer
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MU1920 is an ATP-competitive, selective inhibitor for haspin with an IC50 of 6 nM. MU1920 exhibits good pharmacokinetic properties and metabolic stability in mouse plasma and microsomes without obvious anticancer effects, which can be used for development of chemical probes .
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- HY-149920
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Microtubule/Tubulin
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Cancer
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Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min .
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- HY-173235
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Galectin
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Galectin-3-IN-6 (Compound 12) is a human and murine galectin-3 (Gal-3) inhibitor, with an IC50 of 12 nM against human galectin-3, an IC50 of 12.6 nM against mutant murine galectin-3 (V160A), and a Kd of 13 nM for human galectin-3, as well as oral bioavailability. Galectin-3-IN-6 reduces the levels of liver fibrosis markers type I collagen and α-smooth muscle actin in mouse models of acute liver injury and fibrosis. Galectin-3-IN-6 can be used for the research of acute liver injury and fibrosis .
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- HY-P10331
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SDCBP
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Cancer
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KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
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- HY-153822
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Tau Protein
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Neurological Disease
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JG-23 is a 4-chloro modified analog with ability to promote t-tau degradation. JG-23 exhibits good metabolic stability with a long T1/2 value (36 min) in mouse liver microsome assays .
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- HY-136358
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Ephrin Receptor
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Cancer
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LDN-211904 is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 shows good metabolic stability in mouse liver microsomes. LDN-211904 with cetuximab could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab (HY-P9905) resistance in CRC .
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- HY-146410
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Angiotensin Receptor
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Others
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AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
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- HY-117428
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11β-HSD
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Metabolic Disease
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INU-101 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase (11β-HSD) type 1 inhibitor. INU-101 has highly potent inhibitory activity in mouse, monkey and human 11β-HSD1, derived from liver microsomes. INU-101 can enhance insulin sensitivity and lower the fasting blood glucose level. INU-101 can be used for the research of metabolic disease, such as diabetes .
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- HY-170491
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GSK-3
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Infection
Neurological Disease
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GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability) .
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- HY-124084A
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Stearoyl-CoA Desaturase (SCD)
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Cancer
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SW203668 TFA is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 TFA covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 TFA requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 TFA exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 TFA inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 TFA can be used for the research of non-small cell lung cancer .
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- HY-163291
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Bacterial
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Infection
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AM4085 is an orally active Antagonist for FmlH with an IC50 of 0.19 μM. AM4085 reveals metabolic stability in mouse liver microsomes and blood plasma .
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- HY-169194
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Parasite
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Infection
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Antimalarial agent 44 (Compound 3) is an antimalarial agent against parasite. Antimalarial agent 44 has a good permeability across MDCK-MDR1 cell monolayers and a high clearance by mouse liver microsomes .
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- HY-174150
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Filovirus
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Infection
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EBOV entry-IN-2 (compound 16) is an EBOV entry inhibitor with an EC50 of 4.42 μM. EBOV entry-IN-2 shows metabolic stability .
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- HY-169927
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Ferroptosis
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Inflammation/Immunology
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Ferroptosis-IN-16 (Compound 13l) is a specific inhibitor for ferroptosis with an EC50 of 0.7 nM and 0.9 nM in ES-2 cell and LX-2 cell. Ferroptosis-IN-16 ameliorates Acetaminophen (HY-66005)-induced acute liver injury in mouse model, and exhibits good metabolic stability in mouse liver microsomes .
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- HY-N14038
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Fungal
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Infection
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Crocacin A has anti-yeast and filamentous fungal activity. Crocacin A can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin A can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
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- HY-170571
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Mitochondrial Metabolism
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Metabolic Disease
Inflammation/Immunology
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BE2647 is a selective inhibitor for mitochondrial pyruvate carrier (MPC) with an EC50 of 70 nM. BE2647 exhibits good metabolic stability in mouse liver microsomes. BE2647 can be used in research of metabolic diseases, non-alcoholic fatty liver disease (MASLD), or non-alcoholic steatohepatitis (MASH) .
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- HY-N14040
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Fungal
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Infection
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Crocacin B has anti-yeast and filamentous fungal activity. Crocacin B can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin B can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
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- HY-170486
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Mixed Lineage Kinase
FAK
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Cancer
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MLK3-IN-1 (Compound 37) is a selective inhibitor for mixed-lineage protein kinase 3 (MLK3) with an IC50 <1 nM. MLK3-IN-1 inhibits FAK with an IC50 of 15.5 μM. MLK3-IN-1 exhibits good metabolic stability in mouse and human liver microsomes .
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- HY-159088
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Opioid Receptor
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Neurological Disease
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KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
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- HY-151578
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Dipeptidyl Peptidase
Carbonic Anhydrase
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Metabolic Disease
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DPP IV/hCA II-IN-1 is a potent and selective dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA) inhibitor with an IC50 value of 0.049 μM for DPP IV and with Ki values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively .
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- HY-162121
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Others
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Cancer
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Antitumor agent-129 (Compound 68) is a thiazolidin-4-one sulfone derivative and an Osteosarcoma (OS) inhibitor with an IC50 value of 0.217 μM, a half-life of 73.8 min (mouse liver microsome) and an excellent pharmacokinetic profile (in vivo bioavailability F = 115%, intraperitoneal administration). Antitumor agent-129 is a potential candidate for OS research .
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- HY-161663
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Phosphodiesterase (PDE)
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Cardiovascular Disease
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Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
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- HY-149395
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Bacterial
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Infection
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MmpL3-IN-3 (Compound 12) is a MmpL3 inhibitor. MmpL3-IN-3 shows a MIC of 0.1 μM against H37Rv. MmpL3-IN-3 shows good stability in mouse liver microsomes. MmpL3-IN-3 can be used for anti-tubercular research .
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- HY-174402
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SARS-CoV
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Infection
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PLpro-IN-9 (Compound 14e) is a SARS-CoV-2 PLpro inhibitor with an IC50 of 12.0 μM and a KD of 1.86 μM. PLpro-IN-9 has low cytotoxicity but poor metabolic stability. PLpro-IN-9 can be used in the research of SARS-CoV-2 .
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- HY-168562
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Sigma Receptor
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Neurological Disease
Cancer
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σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
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- HY-168998
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Fungal
Casein Kinase
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Infection
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Yck2-IN-1 (Compound 2a) is an inhibitor of the fungal Candida albicans Yck2 kinase. It exhibits an IC50 of approximately 80 nM against Yck2 and a MIC80 of 12.5 µM against C. albicans, with good metabolic stability (66% remaining in mouse liver microsomes). In a mouse model of drug-resistant candidiasis, Yck2-IN-1 significantly reduced fungal burden in the kidneys. Yck2-IN-1 holds promise for research in the field of antifungal infection .
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- HY-173024
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TRP Channel
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Neurological Disease
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TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
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- HY-168956
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Bacterial
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Infection
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Pks13-IN-2 (Compound 43) is an orally active inhibitor of Pks13. Pks13-IN-2 exhibits inhibitory activity against Mycobacterium tuberculosis H37Rv, with a MIC of 0.8-1.8 μM. Pks13-IN-2 shows good metabolic stability in mouse liver microsomes and hepatocytes. Pks13-IN-2 can be used for tuberculosis research .
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- HY-123639
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N-(2-Phenylethyl)-indomethacin amide
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COX
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Inflammation/Immunology
Cancer
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LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC50 of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively .
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- HY-162620
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Adrenergic Receptor
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Cancer
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α2A-AR agonist 1 (Compound B9) is a selective agonist for α2-adrenergic receptor (α2A-AR) with EC50 of 0.23 nM. α2A-AR agonist 1 exhibits a hypnotic effect, with ED50 of 0.138 mg/kg in the loss of righting reflex (LORR) experiment. α2A-AR agonist 1 exhibits metabolic stability in mouse liver microsomes .
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- HY-159941
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α-synuclein
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Neurological Disease
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tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces Aβ plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice .
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- HY-182255
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Endogenous Metabolite
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Others
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ED-594 is the glucuronide form of NB-506. ED-594 is one of the major metabolites of NB-506 in rat bile, mouse liver microsomes, rat liver microsomes and human liver microsomes .
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- HY-117806
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Akt
Drug Isomer
NADPH Oxidase
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Cancer
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TSR-011-isomer is an isomer of Belizatinib (HY-17603), a ALK inhibitor with an IC50 of 6 nM. TSR-011-isomer acts as a substrate for metabolic hydrolysis and NADPH-dependent metabolism. TSR-011-isomer undergoes enzymatic hydrolysis in mouse plasma and NADPH-dependent metabolism in mouse liver microsomes, thereby supporting clearance processes. TSR-011-isomer can be used in studies related to ALK-driven cancers .
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- HY-181917
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PANK
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Metabolic Disease
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Pantothenate kinase-IN-3 is an orally active PANK3-selective binder and CoA biosynthesis activator with a human PANK3 Ki of 9.1 nM, human PANK3 Ka of 1.8 nM, human PANK1β Ki of 113 nM, human PANK1β Ka of 23.4 nM, and oral effectiveness.Pantothenate kinase-IN-3 binds PANK3 via a water-mediated interaction between its sulfonamide NH and Gly193, elevates cellular, hepatic, and forebrain CoA levels, and shows improved metabolic stability in mouse and human microsomes.Pantothenate kinase-IN-3 has solubility properties favorable at pH 7.Pantothenate kinase-IN-3 can be used for the research of hepatic metabolic CoA deficiencies (acidemias) .
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- HY-181107
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Bacterial
DNA/RNA Synthesis
Cytochrome P450
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Infection
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DNA Gyrase/ribosomes-IN-1 is a bacterial ribosome and DNA gyrase inhibitor, with IC50 values of 1.11 μM and 3.31 μM, respectively. DNA Gyrase/ribosomes-IN-1 also inhibits CYP3A4, with an IC50 of 18.5 μM, and exhibits stability in mouse plasma and liver microsomes. DNA Gyrase/ribosomes-IN-1 inhibits bacterial protein synthesis by interacting with ribosomal RNA and associated sites. DNA Gyrase/ribosomes-IN-1 suppresses bacterial DNA replication by interacting with the gyrase complex. DNA Gyrase/ribosomes-IN-1 restores activity against macrolide-resistant, erm-mediated Gram-positive pathogens and enhances activity against Gram-negative bacteria such as Haemophilus influenzae and Moraxella catarrhalis. DNA Gyrase/ribosomes-IN-1 can be used in research on community-acquired bacterial pneumonia .
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- HY-W015782R
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Tyrosinase
PKA
Reference Standards
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Metabolic Disease
Inflammation/Immunology
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4-Ethylresorcinol (Standard) is the analytical standard of 4-Ethylresorcinol (HY-W015782). This product is intended for research and analytical applications. 4-Ethylresorcinol is a derivative of resorcinol and can serve as a substrate for tyrosinase. 4-Ethylresorcinol has anti-hyperpigmentation and antioxidant effects and can inhibit melanin synthesis. 4-Ethylresorcinol has potential whitening value .
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- HY-100432R
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PDI
Reference Standards
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Neurological Disease
Inflammation/Immunology
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|
LOC14 (Standard) is the analytical standard of LOC14 (HY-100432). This product is intended for research and analytical applications. LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
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-
- HY-N14043
-
|
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Fungal
|
Infection
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|
Crocacin C has anti-yeast and filamentous fungal activity. Crocacin C can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin C can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
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-
- HY-N14044
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Fungal
|
Infection
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|
Crocacin D has anti-yeast and filamentous fungal activity. Crocacin D can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin D can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
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-
- HY-181792
-
|
|
STAT
|
Inflammation/Immunology
|
|
ZDZ-553 is an orally active STAT1 inhibitor with an IC50 value of 0.87 μM. ZDZ-553 modulates STAT1 signaling to affect downstream lipid metabolism and inflammatory pathways. ZDZ-553 attenuates hepatic steatosis in NASH mouse models. ZDZ-553 reduces inflammatory responses in NASH mouse models. ZDZ-553 can be used for the research of nonalcoholic steatohepatitis .
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-
- HY-183339
-
-
- HY-182021
-
|
|
Amine N-methyltransferase
|
Endocrinology
|
|
NNMT-IN-8 is a non-SAM-mimicking bisubstrate inhibitor and a selective methyltransferase NNMT inhibitor, with IC50 values of 0.0084 μM and 0.0085 μM against human NNMT, and an IC50 of 0.0072 μM against mouse NNMT. NNMT-IN-8 exhibits prominent renal distribution characteristics and moderate bioavailability in rodents. NNMT-IN-8 dose-dependently inhibits renal NNMT in renal fibrosis models, thereby exerting antifibrotic effects. NNMT-IN-8 can be used to investigate the mechanisms of renal fibrosis .
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-
- HY-W413619
-
|
NITD609 enantiomer; KAE609 enantiomer
|
Parasite
|
Infection
|
|
Cipargamin enantiomer (NITD609 enantiomer) is a Plasmodium falciparum inhibitor that can be characterized as a spirotetrahydro β-carboline (1S,3R stereoisomer). Cipargamin enantiomer exerts antiplasmodial activity against Plasmodium falciparum strains NF54 (IC50 of 77 nM) and K1. Cipargamin enantiomer displays low liver microsomal intrinsic clearance in mouse and human systems. Cipargamin enantiomer does not inhibit CYP2C9. Cipargamin enantiomer can be used for the research of malaria .
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-
- HY-181884
-
|
|
|
Inflammation/Immunology
|
|
TLR9-IN-3 is a TLR9 antagonist with an IC50 of 0.4 μM. TLR9-IN-3 shows selectivity for TLR4 and TLR8, and inhibits CD69 activation in human whole blood with a corresponding IC50 of 1.1 μM. TLR9-IN-3 can be used in research related to pulmonary fibrosis .
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-
- HY-114943
-
|
|
PARP
Wnt
β-catenin
|
Cancer
|
|
TNKS-IN-1 is a selective and potent tankyrase (TNKS1/TNKS2) inhibitor with IC50 values of 7.9 nM and 8.7 nM. TNKS-IN-1 induces axin2 accumulation with an EC50 of 1500 nM. TNKS-IN-1 can antagonize the Wnt signal transduction pathway by stabilizing axin proteins and promoting β-catenin degradation. TNKS-IN-1 can be used for the research of colorectal cancer .
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-
- HY-183717
-
|
|
|
Cancer
|
|
M4K3233 is a selective ALK2 PROTAC degrader with a pDC50 of 7.3 and a pIC50 of 6.6. M4K3233 recruits CRBN to form a ternary complex with ALK2, mediating ALK2 degradation via the proteasomal and lysosomal pathways. M4K3233 induces moderate downregulation of RIPK2 and significant downregulation of SIK3 in mammalian cells. M4K3233 is applicable to research related to glioblastoma .
|
-
- HY-182454
-
|
|
GPR119
|
Metabolic Disease
|
|
GPR119 agonist 4 is a GPR119 agonist and oral glucose-lowering agent with a human GPR119 EC50 of 42 nM.GPR119 agonist 4 activates GPR119.GPR119 agonist 4 reduces blood glucose area under the curve in an oral glucose tolerance test.GPR119 agonist 4 exhibits improved clearance in liver microsomes.GPR119 agonist 4 can be used for the research of type 2 diabetes mellitus .
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-
- HY-181983
-
|
|
SARS-CoV
|
Infection
|
|
VPC285785 is an orally active SARS-CoV-2 main protease inhibitor with an IC50 of 0.8 μM and a Kd of 2.7 μM. VPC285785 functionally inhibits the viral main protease-mediated processing of viral polyprotein precursors required for viral replication. VPC285785 reduces viral loads in the liver, brain and spleen tissues of MHV-infected mice. VPC285785 is applicable to the research of coronavirus infections .
|
-
- HY-183763
-
|
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
RORγt inverse agonist 37 is an orally active RORγt inverse agonist with an IC50 of 10.8 nM against human targets. RORγt inverse agonist 37 destabilizes helix 12 of RORγt in the agonist-bound conformation, thereby inhibiting transcriptional activity. RORγt inverse agonist 37 inhibits the secretion of IL-17 in cells and in LPS-induced systemic inflammation mouse models. RORγt inverse agonist 37 improves disease-related symptoms in mouse models of psoriasiform dermatitis. RORγt inverse agonist 37 can be used in research related to psoriasiform dermatitis and systemic inflammation .
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-
- HY-182267
-
|
|
Bacterial
Interleukin Related
TNF Receptor
|
Infection
Inflammation/Immunology
|
|
Antibiofilm agent-20 is an orally active Escherichia coli biofilm inhibitor (IC50 = 5.5 μg/mL) and show low antibacterial activity (MIC >128 μg/mL). Antibiofilm agent-20 exhibits high lipophilicity and low solubility, resulting in low colon delivery rate. Antibiofilm agent-20 demonstrates anti-inflammatory and reduces IL-17 and TNF-α levels. Antibiofilm agent-20 can be used for the research of inflammatory bowel disease .
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-
- HY-182358
-
|
|
Apoptosis
|
Cancer
|
|
TMLZ-G46 is an orally active ZNF207 inhibitor with blood-brain barrier penetration ability, with a Kd value of 68 nM. TMLZ-G46 inhibits cancer cell proliferation, stemness, migration and invasion, induces G0/G1 cell cycle arrest and apoptosis, and suppresses colony formation. TMLZ-G46 can be used in glioma research .
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-
- HY-182025
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
NAD+ potentiator-1 (Compound R-4b) is a NAD potentiator. NAD+ potentiator-1 increases NAD levels in primary cortical neurons. NAD+ potentiator-1 is used for the research of neurodegenerative diseases .
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-
- HY-107460R
-
|
|
Reference Standards
Ephrin Receptor
|
Cancer
|
|
LDN-211904 oxalate (Standard) is the analytical standard of LDN-211904 (oxalate) (HY-107460). This product is intended for research and analytical applications. LDN-211904 oxalate is a potent and reversible EphB3 inhibitor with an IC50 of 79 nM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with Cetuximab (HY-P9905) could be effective in inhibiting STAT3-activated colorectal cancer (CRC) stemness and Cetuximab resistance in CRC .
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-
- HY-182533
-
|
|
CXCR
|
Cardiovascular Disease
|
|
LN5972 is a selective ACKR3 agonist with an EC50 of 3.40 μM, showing higher selectivity for ACKR3 over CXCR4. LN5972 induces β-arrestin recruitment to ACKR3/CXCR7. LN5972 reduces the surface expression of P-selectin. LN5972 is applicable to studies related to platelet-mediated thrombosis .
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-
- HY-183557
-
|
|
OGA
|
Neurological Disease
|
|
O-GlcNAcase-IN-6 is an orally active, blood-brain barrier-permeable O-GlcNAcase (OGA) inhibitor with an IC50 of 5.4 nM. O-GlcNAcase-IN-6 inhibits OGA activity, thereby increasing the level of O-GlcNAc glycosylation in brain tissues. O-GlcNAcase-IN-6 can be used for the research of Alzheimer's disease .
|
-
- HY-182921
-
|
|
GPR84
Enterovirus
|
Inflammation/Immunology
|
|
GPR84 antagonist 11 is a highly selective GPR84 antagonist, with a human pA2 of 8.41 and a pKi of 8.16. GPR84 antagonist 11 competitively inhibits the binding of agonists to the orthosteric site of GPR84 and has improved druglike properties, though its metabolic stability still requires optimization. GPR84 antagonist 11 can be used in the research of autoimmune diseases and fibrotic diseases .
|
-
- HY-182912
-
|
|
Molecular Glues
Epigenetic Reader Domain
|
Cancer
|
|
PLX-4104 is an orally active BRD4 molecular glue degrader with a DC50 of 2 nM. PLX-4104 selectively promotes BRD4 degradation via DCAF11 recruitment, triggering ubiquitination and proteasomal breakdown. PLX-4104 inhibits cancer cell proliferation. PLX-4104 induces complete regression of AML xenograft tumors. PLX-4104 can be used for the research of acute myeloid leukemia .
|
-
- HY-182356
-
|
|
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
|
Cancer
|
|
MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models .
|
-
- HY-181666
-
|
|
Insulin Receptor
|
Cancer
|
|
Z971169476 is a sulfonamide-based protein-RNA interaction inhibitor targeting the KH34 region of insulin-like growth factor 2 mRNA binding protein 2 (IGF2BP2/IMP2) .
|
-
- HY-172247
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-31 is a selective ATR kinase inhibitor with an IC50 of 7 nM. ATR-IN-31 does not significantly inhibit ATM kinase activity. ATR-IN-31 inhibits viability of prostate cancer cells.ATR-IN-31 can be used for the research of prostate cancer .
|
-
- HY-182585
-
-
- HY-183718
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Neurological Disease
Cancer
|
|
M4K3250 is a selective ALK2 PROTAC degrader with a pDC50 of 7.9. M4K3250 induces the formation of a ternary complex between ALK2 and the E3 ubiquitin ligase CRBN, thereby causing ALK2 degradation and inhibiting ALK2 activity. M4K3250 exhibits cytotoxicity in glioblastoma cells. M4K3250 can be used in studies related to glioblastoma .
|
-
- HY-206259
-
|
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
CCG-203586 is a brain-penetrant glucosylceramide synthase (GCS) inhibitor. CCG-203586 reduces GCS production and brain levels, blocks the first committed step in ganglioside biosynthesis, and lowers downstream ganglioside levels. CCG-203586 can be used for the research of Tay-Sachs, Sandhoff disease, and types 2 and 3 Gaucher disease .
|
-
- HY-183542
-
|
|
Bacterial
|
Infection
|
|
DprE1-IN-15 is a covalent Mycobacterium tuberculosis essential cell wall enzyme DprE1 inhibitor with an IC50 of 0.073 μM. DprE1-IN-15 forms an irreversible covalent adduct with its target enzyme. DprE1-IN-15 shows inhibitory effects against multiple Mycobacterium tuberculosis .
|
-
- HY-182308
-
|
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
LC-PDA-01 is a selective peroxiredoxin 1 (PRDX1) activator with an EC50 of 111.8 nM and a human KD of 123.2 nM. LC-PDA-01 inhibits the expression of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α. LC-PDA-01 can be used in antioxidant/anti-inflammatory research .
|
-
- HY-182905
-
|
|
Somatostatin Receptor
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus .
|
-
- HY-181553
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-44 (compound 2a) is a PROTAC degrader targeting BRD4 with passive membrane permeability. PROTAC BRD4 Degrader-44 maintains stability within 6 hours in medium supplemented with 10% FBS. PROTAC BRD4 Degrader-44 shows a trend of increasing intracellular accumulation within 6 hours, indicating reduced efflux .
|
-
- HY-183673
-
|
|
COX
|
Neurological Disease
Inflammation/Immunology
|
|
COX-1/2-IN-12 is an orally active dual inhibitor of COX-1 and COX-2, with an IC50 of 41.6 nM against human COX-1 and an IC50 of 31.1 nM against human COX-2. COX-1/2-IN-12 induces antinociceptive activity and inhibits edema in in vivo experiments. COX-1/2-IN-12 can be used in research related to inflammation and pain .
|
-
- HY-182268
-
|
|
Bacterial
Interleukin Related
TNF Receptor
|
Infection
Inflammation/Immunology
|
|
Antibiofilm agent-21 is an orally active prodrug of Antibiofilm agent-20 (HY-182268) with glucuronidation. Antibiofilm agent-21 avoids absorption in the small intestine via reduced membrane permeability, improving colon delivery rate, and converts to its active form in the colon. Antibiofilm agent-21 increases colon length and reduces IL-17 and TNF-α levels in a murine DSS (HY-116282C)-induced colitis model. Antibiofilm agent-21 can be used for the research of inflammatory bowel disease .
|
-
- HY-183723
-
|
|
Dihydroceramide Desaturase 1 (DES1)
|
Metabolic Disease
|
|
GAA-4OH is a potent and irreversible dihydroceramide desaturase-1 (DES1) inhibitor with an IC50 of 0.6 μM and a Ki of 139.5 nM. GAA-4OH undergoes oxidation to form a reactive iminoquinone that covalently blocks DES1’s catalytic cavity, causing permanent enzyme inactivation. GAA-4OH modulates sphingolipid balance by reducing ceramide-to-dihydroceramide ratios in liver tissue. GAA-4OH improves liver steatosis, inflammation, fibrosis, and reduces pro-inflammatory and pro-fibrogenic gene expression. GAA-4OH can be used for the research of metabolic dysfunction-associated steatotic liver disease (MASLD) .
|
-
- HY-181882
-
-
- HY-182893
-
|
|
α-synuclein
Reactive Oxygen Species (ROS)
Tyrosine Hydroxylase
|
Neurological Disease
|
|
SK-129 is a blood-brain barrier-permeable inhibitor of α-synuclein (αS) oligomers with a Kd of 221 nM. SK-129 preferentially binds to neurotoxic αS oligomers over physiological αS monomers, inhibits αS aggregation, blocks the interaction and co-aggregation of αS with tau protein, and prevents the maturation of αS-tau condensates into amyloid aggregates. SK-129 reduces ROS production, rescues dopaminergic neuron degeneration, improves motor function, restores endogenous dopamine synthesis, increases the number of Tyrosine Hydroxylase-positive neurons, prevents brain histopathological changes, alleviates neuroinflammation, and improves survival rates in relevant models. SK-129 can be used in research related to Parkinson's disease (PD) and Lewy body dementia (LBD) .
|
-
- HY-181553A
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-45 (Compound 2b) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-45 exhibits enhanced passive membrane permeability, stability in cell culture medium supplemented with 10% FBS, and higher intracellular concentrations in cancer cells .
|
-
- HY-181662
-
|
|
MAP3K
|
Neurological Disease
|
|
DLK-IN-2 is a selective inhibitor of DLK and neuroprotective agent. DLK-IN-2 shows no significant inhibition against CYPs 3A4, 2D6 and 2C9. DLK-IN-2 inhibits acute axonal palmitoylation of DLK, blocks DLK-dependent pro-degenerative axon-to-soma retrograde signaling and suppresses c-Jun phosphorylation. DLK-IN-2 can be used for the mechanistic study of neurodegenerative diseases .
|
-
- HY-183756
-
|
|
Cytochrome P450
Apoptosis
|
Cancer
|
|
CYP4Z1-IN-3 is a selective CYP4Z1 inhibitor with a human IC50 of 55.3 nM. CYP4Z1-IN-3 inhibits breast cancer cell migration and induces apoptosis. CYP4Z1-IN-3 can be used for the research of breast cancer .
|
-
- HY-181932
-
|
|
MAP4K
|
Cancer
|
|
HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer .
|
-
- HY-182050
-
|
|
AP-1
DNA Alkylator/Crosslinker
|
Neurological Disease
|
|
YL0441 is an inhibitor of ΔFOSB/JUND heterodimers and ΔFOSB homomultimers, with IC50 values of 13.7 μM and 12.3 μM, respectively. YL0441 blocks the binding of ΔFOSB to DNA. YL0441 reduces ΔFOSB bound to genomic DNA in the hippocampal tissues of APP mice. YL0441 is applicable to the research of Alzheimer's disease .
|
-
- HY-181779
-
|
|
Bacterial
|
Infection
|
|
Pyridomycin-4-F, Pyridomycin (HY-111402) derivative, is an antimycobacterial agent targeting fatty acid synthesis enzyme InhA (enoyl ACP reductase). Pyridomycin-4-F binds to the pyridomycin binding pocket of InhA, forms hydrogen bond interactions with Lys-165. Pyridomycin-4-F can be used for the research of tuberculosis .
|
-
- HY-182884
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
TNF-α-IN-29 is an orally active and selective TNF-α inhibitor, with IC50 values of 123.0 nM against human targets, and a human Kd of 45.9 nM. TNF-α-IN-29 blocks TNF-α-TNFR1 protein-protein interactions and inhibits TNF-α-mediated inflammatory signaling pathways. TNF-α-IN-29 exhibits anti-inflammatory effects in a mouse model of collagen-induced arthritis and promotes articular cartilage repair. TNF-α-IN-29 can be used for the research of rheumatoid arthritis .
|
-
- HY-181764
-
|
|
Ser/Thr Protease
|
Cancer
|
|
LZL50 is an orally effective human caseinolytic protease P (hClpP) activator with an EC50 of 0.29 μM. LZL50 activates hClpP, a serine protease that mediates mitochondrial quality control by degrading damaged or misfolded mitochondrial proteins. LZL50 exhibits antitumor activity in a breast cancer xenograft mouse model. LZL50 can be used in research related to breast cancer .
|
-
- HY-181449
-
-
- HY-W743094
-
|
|
Drug Derivative
|
Inflammation/Immunology
Cancer
|
|
Methylstenbolone is a steroid and an anti-inflammatory agent. Methylstenbolone inhibits nitric oxide production in macrophages and exhibits cytotoxicity against breast cancer cells and normal fibroblasts. Methylstenbolone can be used for the research of inflammation and breast cancer .
|
-
- HY-59132
-
|
|
Drug Intermediate
|
Others
|
|
2-Amino-1-phenylethanol is a pharmaceutical intermediate that can be used for the synthesis of antimalarial agents and β2-adrenergic receptor agonists .
|
-
- HY-N4267
-
|
|
Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
|
-
- HY-117503
-
|
|
Influenza Virus
|
Infection
|
|
M2WJ332 is an inhibitor of the M2 proton channel of the influenza A virus M2 S31N mutant M2. M2WJ332 potently inhibits the influenza A virus A/M2-S31N proton channel in Xenopus laevis oocytes, with an IC50 of 16 μM. M2WJ332 completely inhibits plaque formation by the influenza A virus carrying the M2 S31N mutant. M2WJ332 is applicable to research related to influenza A virus infection .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-40351
-
|
|
Biochemical Assay Reagents
|
|
4-Chloro-7H-pyrrolo[2,3-d]pyrimidine is a nitrogen-containing heterocyclic organic synthesis intermediate that can be used for the synthesis of JAK and PKB/Akt inhibitors .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10331
-
|
|
SDCBP
|
Cancer
|
|
KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-59132
-
-
-
- HY-W015782
-
-
-
- HY-B1341
-
|
Enidrel; SC-4642; NSC 15432
|
Structural Classification
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Endocrinology
Steroids
Source Classification
|
Endogenous Metabolite
Progesterone Receptor
|
|
Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
|
-
-
- HY-N4267
-
|
|
Cardiovascular Disease
Structural Classification
other families
Classification of Application Fields
Lignans
Phenylpropanoids
Plants
Disease Research Fields
Source Classification
|
Calcium Channel
Platelet-activating Factor Receptor (PAFR)
UGT
Leukotriene Receptor
TNF Receptor
PGE synthase
Interleukin Related
|
|
Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
|
-
-
- HY-N14038
-
|
|
Natural Products
Microorganisms
Source Classification
|
Fungal
|
|
Crocacin A has anti-yeast and filamentous fungal activity. Crocacin A can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin A can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
|
-
-
- HY-N14040
-
|
|
Natural Products
Microorganisms
Source Classification
|
Fungal
|
|
Crocacin B has anti-yeast and filamentous fungal activity. Crocacin B can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin B can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
|
-
-
- HY-W015782R
-
-
-
- HY-N14043
-
|
|
Natural Products
Microorganisms
Source Classification
|
Fungal
|
|
Crocacin C has anti-yeast and filamentous fungal activity. Crocacin C can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin C can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
|
-
-
- HY-N14044
-
|
|
Natural Products
Microorganisms
Source Classification
|
Fungal
|
|
Crocacin D has anti-yeast and filamentous fungal activity. Crocacin D can inhibit mouse fibroblasts L929. In the microsomes of the calf's heart, Crocacin D can interrupt the bc1 segment of electronic transmission, causes redshift of 569 nm peak in cytochrome B reduction spectrum .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-168328
-
|
|
|
Alkynes
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FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
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- HY-B1341
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Enidrel; SC-4642; NSC 15432
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Alkynes
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Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
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