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KM mice

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Antifolate (1) Apoptosis (2) Aryl Hydrocarbon Receptor (3) Bcl-2 Family (1) Calcium Channel (1) Caspase (1) Cathepsin (1) COX (1) Cytochrome P450 (3) Dopamine Receptor (1) FAAH (1) GABA Receptor (1) Interleukin Related (1) Isotope-Labeled Compounds (1) MDM-2/p53 (1) MEK (1) Mitophagy (1) NAMPT (1) NF-κB (1) NO Synthase (1) p38 MAPK (1) PI3K (1) Potassium Channel (1) Reactive Oxygen Species (ROS) (1) Reference Standards (1) STAT (1) Thymidylate Synthase (1) Thyroid Hormone Receptor (1) TNF Receptor (1) Toll-like Receptor (TLR) (1) TRP Channel (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Endocrinology (1) Infection (1) Inflammation/Immunology (2) Metabolic Disease (5) Neurological Disease (6)
Click Chemistry:	Alkynes (1)

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Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0973

Dibenzothiophene DBT; Diphenylene sulfide	Cytochrome P450 Aryl Hydrocarbon Receptor	Metabolic Disease
Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with a *K_m* of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms .

HY-170621

STAT1/3-IN-1	STAT NO Synthase COX Interleukin Related TNF Receptor	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
STAT1/3-IN-1 is a potent STAT1/3 inhibitor with potent anti-inflammatory effect. STAT1/3-IN-1 inhibits phosphorylation and nuclear translocation of STAT1/3 to modulate microglial inflammation, reduces LPS (HY-D1056)-induced pro-inflammatory cytokines (NO, IL-1β, IL-6, and TNF-α) and inflammatory mediators (iNOS, COX-2). STAT1/3-IN-1 exhibits low toxicity in mice. STAT1/3-IN-1 can be used for the research of neuroinflammation .

HY-N0392

Polygalasaponin F	Toll-like Receptor (TLR) PI3K Akt NF-κB MDM-2/p53 Caspase MEK Bcl-2 Family p38 MAPK Mitophagy Reactive Oxygen Species (ROS) Apoptosis Calcium Channel	Cardiovascular Disease Infection Neurological Disease
Polygalasaponin F is an orally active triterpenoid saponin monomer. Polygalasaponin F downregulates the expression of Bax, p53, caspase-3, NF-κB p65 and MEK1; restores and upregulates the expression of Bcl-2; activates the PI3K/Akt signaling pathway; inhibits the phosphorylation of p38 MAPK, nuclear translocation of NF-κB, TLR4-mediated signaling pathway, mitophagy (Mitophagy) and ROS production; enhances cell viability and suppresses apoptosis (Apoptosis). Polygalasaponin F maintains mitochondrial function, alleviates Ca ²⁺ overload, upregulates pCREB and BDNF, preserves cell viability and inhibits the release of inflammatory cytokines. Polygalasaponin F alleviates lung injury induced by influenza A H1N1 and cerebral ischemia-reperfusion injury. Polygalasaponin F is applicable to researches related to Parkinson's disease, cerebral ischemia, pneumonia induced by influenza A H1N1, stroke and Alzheimer's disease .

HY-144372

TRPV1 antagonist 3	TRP Channel	Neurological Disease
TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC₅₀ of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant .

HY-164495

Sob-AM2	FAAH Thyroid Hormone Receptor	Inflammation/Immunology Endocrinology
Sob-AM2 is a potent substrate (K_m=1.3 μM) targeting fatty acid amide hydrolase (FAAH) expressed in the brain and has blood-brain barrier permeability. Sob-AM2 delivers high concentrations of Sobetirome (HY-14823) to the central nervous system with minimal peripheral systemic dose, thereby stimulating central thyroid hormone receptor β (TRβ). In addition, Sob-AM2 can prevent myelin and axon degeneration in experimental autoimmune encephalomyelitis (EAE) mice .

HY-177099

Lorotomidate	GABA Receptor	Neurological Disease
Lorotomidate (Example 16) is a GABAA receptor agonist. Lorotomidate has anaesthetic effects (ED₅₀: i.v., 2 mg/kg in KM mice; LD₅₀: 46.5 mg/kg in KM mice). Lorotomidate has no inhibitory effect on the secretion of corticosteroids in animals, and thus has good safety .

HY-123189

LY 171859	Dopamine Receptor	Neurological Disease
LY 171859 is a D2 receptor agonist with significant reductase activity. LY 171859 exhibits enzymatic activity in the cytoplasm of liver, lung, and kidney, and also contains significant reductase activity in rat and human blood. LY 171859 has higher hepatic reductase activity in guinea pigs, followed by hamsters, rabbits, rats, and mice. The substrate of LY 171859 shows an apparent Km of 5.6 μM. The reduction reaction of LY 171859 is NADPH-dependent with an apparent Km of 14.8 μM. Only the A-side hydrogen of NADPH is incorporated in the reduction product of LY 171859. The reaction of LY 171859 is inhibited by cyanide and thiol reagents, and phenobarbital does not induce its activity in rats .

HY-B0973S

Dibenzothiophene-d8	Isotope-Labeled Compounds Cytochrome P450 Aryl Hydrocarbon Receptor	Metabolic Disease
Dibenzothiophene-d₈ is the deuterium labeled Dibenzothiophene (HY-B0973). Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with *K_m* of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms .

HY-B0973R

Dibenzothiophene (Standard) DBT (Standard); Diphenylene sulfide (Standard)	Reference Standards Cytochrome P450 Aryl Hydrocarbon Receptor	Metabolic Disease
Dibenzothiophene (Standard) is the analytical standard of Dibenzothiophene (HY-B0973). This product is intended for research and analytical applications. Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with *K_m* of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms .

HY-113798

ICI 198583	Thymidylate Synthase Antifolate	Cancer
ICI 198583 is a thymidylate synthase (TS) inhibitor with a K_i value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a *K_m* of 40 μM. ICI 198583 exerts persistent, dose-dependent inhibition on thymidylate synthase flux in mice. ICI 198583 is applicable to relevant research on leukemia .

HY-181874

E0714	Potassium Channel	Neurological Disease
E0714 is a blood-brain barrier-permeable, selective Kv7.2 potassium channel activator, with EC₅₀ values of 1.90 μM and 0.021 μM for homotetrameric Kv7.2 channels and heterotetrameric Kv7.2/7.3 channels, respectively. E0714 exhibits anticonvulsant activity. E0714 can be used in research related to epilepsy .

HY-181655

Cathepsin D degrader 1	Cathepsin	Metabolic Disease
Anti-hepatic fibrosis agent 3 is an orally active anti-hepatic fibrosis compound targeting Cathepsin D. Anti-hepatic fibrosis agent 3 shows an IC₅₀ of 53.18 μM against COL1A1-promoter and a K_d of 8.86 μM for binding to Cathepsin D. Anti-hepatic fibrosis agent 3 directly binds to and promotes the degradation of Cathepsin D, with no significant effect on Cathepsin B or Cathepsin L. Anti-hepatic fibrosis agent 3 inhibits hepatic stellate cell activation and reduces extracellular matrix deposition and inflammatory cytokine expression. Anti-hepatic fibrosis agent 3 exhibits remarkable anti-fibrotic activity in rat BDL and mouse CDAHFD-induced hepatic fibrosis models. Anti-hepatic fibrosis agent 3 can be used for the study of hepatic fibrosis .

HY-181578

Nampt-IN-17	NAMPT Apoptosis	Cancer
Nampt-IN-17 is an selective orally active NAMPT inhibitor with a human NAMPT IC₅₀ of 17 nM and K_i of 25.9 nM. Nampt-IN-17 depletes intracellular NAD ⁺ and ATP, disrupts mitochondrial membrane potential, suppresses cell proliferation, self-renewal, invasion, and migration, induces cell-cycle arrest and apoptosis. Nampt-IN-17 exhibits selective activity against NAPRT-deficient gastric cancer cells. Nampt-IN-17 can be used for the research of NAPRT-deficient gastric cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0392

Polygalasaponin F	Triterpenes Structural Classification Classification of Application Fields Terpenoids Polygalaceae Polygala japonica Houtt. Plants Inflammation/Immunology Disease Research Fields Source Classification	Toll-like Receptor (TLR) PI3K Akt NF-κB MDM-2/p53 Caspase MEK Bcl-2 Family p38 MAPK Mitophagy Reactive Oxygen Species (ROS) Apoptosis Calcium Channel
Polygalasaponin F is an orally active triterpenoid saponin monomer. Polygalasaponin F downregulates the expression of Bax, p53, caspase-3, NF-κB p65 and MEK1; restores and upregulates the expression of Bcl-2; activates the PI3K/Akt signaling pathway; inhibits the phosphorylation of p38 MAPK, nuclear translocation of NF-κB, TLR4-mediated signaling pathway, mitophagy (Mitophagy) and ROS production; enhances cell viability and suppresses apoptosis (Apoptosis). Polygalasaponin F maintains mitochondrial function, alleviates Ca ²⁺ overload, upregulates pCREB and BDNF, preserves cell viability and inhibits the release of inflammatory cytokines. Polygalasaponin F alleviates lung injury induced by influenza A H1N1 and cerebral ischemia-reperfusion injury. Polygalasaponin F is applicable to researches related to Parkinson's disease, cerebral ischemia, pneumonia induced by influenza A H1N1, stroke and Alzheimer's disease .

Cat. No.	Product Name	Chemical Structure

HY-B0973S

Dibenzothiophene-d8
Dibenzothiophene-d₈ is the deuterium labeled Dibenzothiophene (HY-B0973). Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with *K_m* of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms .

Dibenzothiophene-d8

Dibenzothiophene-d₈ is the deuterium labeled Dibenzothiophene (HY-B0973). Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with K_m of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms .

Cat. No.	Product Name		Classification

HY-113798

ICI 198583		Alkynes
ICI 198583 is a thymidylate synthase (TS) inhibitor with a K_i value of 10 nM for both mouse and human TS. ICI 198583 serves as a substrate for folylpolyglutamate synthetase (FPGS) with a *K_m* of 40 μM. ICI 198583 exerts persistent, dose-dependent inhibition on thymidylate synthase flux in mice. ICI 198583 is applicable to relevant research on leukemia .

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