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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
213 Results for "
ETC inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (213)
213 Results for "ETC inhibitor" in MCE Product Catalog:
42
42 Publications Verification
BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
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25 Cited Publications
Synonyms: ETC-1002; ESP-55016
Target:
Research Areas:
Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor . Bempedoic acid (ETC-1002) activates AMPK .
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24 Cited Publications
Cat. No.: HY-164388
CAS No.: 162852-62-2
Target:
Research Areas:
24
Category:
Cardiovascular Disease other families Leguminosae Plants Endogenous metabolite Disease Research Fields Glycyrrhiza uralensis Fisch. Inflammation/Immunology Steroids
Target:
24
24 Cited Publications
Synonyms: β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
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17
Category:
Infection Natural Products Liliaceae Plants Disease Research Fields A．Sativam L. var．Viviparum Regel
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11
11 Cited Publications
Synonyms: PEG-PPG-PEG, 12600 (Average Mn)
10
10 Cited Publications
Research Areas:
TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
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10 Cited Publications
Research Areas:
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
9
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
9
Target:
Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis
Research Areas:
Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
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7
Research Areas:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Zorifertinib (AZD3759) is a potent, orally active, BBB-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .
5
5 Cited Publications
Cat. No.: HY-N2389
CAS No.: 50773-42-7
Category:
Paris polyphylla Smith var. chinensis (Franch.) Hara Liliaceae Plants Disease Research Fields Saccharides Cancer
Target:
4
4 Cited Publications
Synonyms: DHEA sulfate; Prasterone sulfate
Category:
Human Gut Microbiota Metabolites Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Steroids
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4
4 Cited Publications
Synonyms: DHEA sulfate sodium; Prasterone sulfate sodium
Target:
3
3 Cited Publications
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) .
3
3 Cited Publications
Cat. No.: HY-N0385
CAS No.: 66280-25-9
Category:
Cardiovascular Disease Monophenols Lignans Phenols Phenylpropanoids Plants Schisandraceae Disease Research Fields Schisandra chinensis (Turcz.) Baill.
Target:
2
2 Cited Publications
Target:
Research Areas:
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
