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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC78377 Heptanoyl thio-PC
Heptanoyl thio-PC is a sn-2 thiol-labeled Phospholipase A2 (PLA2) substrate that can be used to detect the activity of Phospholipase A2.
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DC78376 L-threo-PPMP hydrochloride
L-threo-PPMP hydrochloride is a GlcT (UDP-Glc: Ceramide β1,1glucosyltransferase) inhibitor. L-threo-PPMP hydrochloride inhibits glycosphingolipid biosynthesis and induces apoptosis. L-threo-PPMP hydrochloride has anti-cancer activity.
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DC78375 AB19
AB19 is a potent Vav1 inhibitor. AB19 inhibits Vav1 and reduces its downstream ERK phosphorylation. AB19 shows anti-proliferative activity in pancreatic cancer models. AB19 can be used for pancreatic cancer research.
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DC78374 RC-552
RC-552 is a novel synthetic glycolipid related in chemical structure to MLA. RC-552 induces delayed cardioprotective effects via an iNOS-dependent pathway. RC-552 attenuates myocardial stunning.
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DC78373 TD034
TD034 is a selective, reversible and noncovalent HDAC11 inhibitor with an IC50 of 5.1 nM and a Ki of 1.5 nM. TD034 does not inhibit other HDACs or sirtuins. TD034 inhibits the defatty acylation of SHMT2 (HDAC11 substrate). TD034 decreases the YAP1 level via HDAC11 inhibition. TD034 can be used for the study of lung cancer.
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DC78372 (Z)-Flupenthixol decanoate
(Z)-Flupenthixol decanoate is the cis form of Flupenthixol decanoate. (Z)-Flupenthixol decanoate is a potent dopamine D1/D2 receptor antagonist. (Z)-Flupenthixol decanoate shows antipsychotic effect.
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DC78371 C22:1 1-Deoxyceramide (m18:1/22:1)
C22:1 1-Deoxyceramide (m18:1/22:1) (C22:1(13Z) 1-Deoxyceramide) is a deoxyceramide lipid that lacks the 1-hydroxyl group and is a ceramide variant. C22:1 1-Deoxyceramide (m18:1/22:1) has potential neurotoxicity and is involved in mitochondrial stress and cell death signaling. It can be used to study abnormal sphingolipid metabolism and neurodegenerative diseases.
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DC78370 CH-4630808 sodium
CH-4630808 (sodium) is a serine palmitoyl transferase (SPT) inhibitor. CH-4630808 (sodium) exhibits anti-HCV activity.
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DC78369 1,2-Bis(heptanoylthio)-sn-glycero-3-PG sodium
1,2-Bis(heptanoylthio)-sn-glycero-3-PG (1,2-Bis(heptanoylthio) glycerophosphatidylglycerol) sodium is a fatty acylthioesterified phosphatidylglycerol derivative that can be used to mimic the action of phospholipases or as a probe molecule for membrane fusion studies.
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DC78368 1,2-Bis(heptanoylthio)-sn-glycero-3-PE
1,2-Bis(heptanoylthio)-sn-glycero-3-PE (Diheptanoyl thio-PE) is a sulfur-containing phosphoethanolamine.
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DC78367 BBL454
BBL454 (Compound 43) is a Cholecystokinin 2B (CCK2B) receptor agonist. BBL454 induces hyperactivity and improves memory in rat models while it has weak activity on the peripheral CCK2 receptor and no anxiogenic activity. BBL454 increases gastric acid output in anesthetised rat models. BBL454 can be used for diabetes research.
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DC78366 E-5531
E-5531 is an endotoxin antagonist. E-5531 quickly becomes inactive after binding with HDL. E-5531 can block the Toll like receptor 4 (TLR4) signaling pathway. E-5531 can be used for the study of endotoxemia and septic shock.
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DC78365 U-46619 Glycine methyl ester
U-46619 Glycine methyl ester has a modification at the C-1 position of U-46619, which uniquely alter its binding properties to the TP receptor or any of the PGH2-metabolizing enzymes. U-46619 is a stable analog of the endoperoxide PGH2. U-46619 is also an agonist of TP receptor. U-46619 can change the shape of platelet, aggregation and contraction of vascular smooth muscle. U-46619 Glycine methyl ester can be studied in research to explore the inhibition of various enzymes in the arachidonic acid metabolic pathway. U-46619 Glycine methyl ester can also act as a lipophilic prodrug form of U-46619 that alters its distribution and pharmacokinetic properties.
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DC78364 EXP-7711
EXP-7711 is a non peptide angiotensin II (Ang II) AT1 receptor antagonist. EXP-7711’s affinity for wild-type AT1 receptor (Ki =180 nM) is lower than peptide antagonists, but higher than losartan (Ki = 12 nM). EXP-7711 can be used for research on cardiovascular conditions.
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DC78363 CR 3834
CR 3834 is a angiotensin-AT1 antagonist. CR 3834 can be used for the research of cardiovascular disease.
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DC78362 Carbaprostacyclin-biotin
Carbaprostacyclin-biotin (cPGI-biotin; Carbacyclin-biotin) is a biotin-bound Carbacyclin (Carbaprostacyclin)). Carbacyclin is a PGI2 analogue, acts as a prostacyclin (PGI2) receptor agonist and vasodilator, and potently inhibits platelet aggregation.
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DC78361 Jacaric acid methyl ester
Jacaric acid methyl ester is a methyl ester form of the conjugated PUFA jacaric acid. Jacaric acid can induce apoptosis selectively in human prostate cancer cells. Jacaric acid induces concentration- and time-dependent LNCaP cell death. Jacaric acid methyl ester can be studied in anticancer research.
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DC78360 8(9)-EET
8(9)-EET is a major cytochrome P450 (CYP450) metabolite in the renal cortex[1][2]. It activates PPARα in HEK293 cells when used at a concentration of 1 μM but inhibits NF-κB activity induced by IL-1β in a PPARα-dependent and -independent fashion. It is also a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM .
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DC78359 (±)5(6)-EET Ethanolamide
(±)5(6)-EET Ethanolamide is a metabolite of Anandamide generated via oxidation by cytochrome P450 enzymes. (±)5(6)-EET Ethanolamide is also a selective cannabinoid receptor 2 (CB2) agonist. (±)5(6)-EET Ethanolamide has Ki values of 11.4 μM and 8.9 nM for human CB1 and CB2, respectively . (±)5(6)-EET Ethanolamide can be used in research on immunomodulation and neuroinflammation.
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DC78358 KIT-13
KIT-13 is an orally active plasmalogen derivative to inhibit neuroinflammation and mitochondrial DNA leakage associated with Mecp2 deficiency. KIT-13 significantly reduce neurological symptoms and improves the life span of the Rett Syndrome (RTT) model mice. KIT-13 can be used for the study of RTT and other neuroinflammation-related diseases.
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DC78356 Menin-MLL inhibitor MI-2 dihydrochloride
Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective Menin-MLL interaction inhibitor with an IC50 value of 446 nM and a Ki value of 158 nM. Menin-MLL inhibitor MI-2 dihydrochloride downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL).
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DC78355 KUNB106
KUNB106 is a selective Hsp90β inhibitor with KDs of 91 nM and 38 μM against Hsp90β and Hsp90α. KUNB106 exhibits antiproliferative activity against MDA-MB-231 cells, A549 and SKOV-3 cells. KUNB106 can be used for the study of triple negative breast cancer.
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DC78354 Topobexin
Topobexin (Topobexin 9) is a highly selective inhibitor for TOP2B. Topobexin selectively inhibits TOP2B in vitro and immobilizes TOP2B on DNA. Topobexin demonstrates significant protection of cardiomyocytes against DAU-induced damage. Topobexin prevents anthracycline-induced cardiotoxicity and DAU-induced decrease in LV systolic function in vivo with rabbit model.
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DC78353 BB-3497
BB-3497 is a potent, orally active and selective peptide deformylase (PDF) inhibitor. BB-3497 is highly selective for PDF (IC50 = 7 nM for E. coli PDF.Ni) over the other mammalian metalloenzymes (MMP-1/2/3/7 and enkephalinase). BB-3497 exhibits potent activity against gram-positive bacteria and some gram-negative pathogens. BB-3497 protects mice from infection in systemic models of Staphylococeus aureus. BB-3497 can be used for anti-bacterial infection research.
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DC78352 P2Y12R ligand-1
P2Y12R ligand-1 (Compound 41) is a high-affinity P2Y12R ligand with a Ki value of 17.1 nM. P2Y12R ligand-1 labeled with [18F] can be used in studies of brain PET imaging.
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DC78351 MRS8454
MRS8454 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR). MRS8454 can significantly enhance the maximum effect of the standard agonist Cl-IB-MECA by approximately 286%-300%, and significantly reduce its EC50 value. MRS8454 effectively enhances the ability of A3AR agonists to inhibit the cAMP accumulation induced by Forskolin. MRS8454 can be used for the development of molecular probes.
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DC78350 E-2508 free base
E-2508 free base is an orally active and highly selective corticotropin-releasing factor type 1 receptor (CRF1) antagonist with anxiolytic effects (IC50=11 nM). E-2508 free base blocks CRF-induced cAMP accumulation via CRF1 receptor inhibition. E-2508 free base is promising for research of stress-related psychiatric disorders, such as anxiety and depression.
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DC78349 R-836
R-836 is a phosphodiesterase inhibitor. R-836 is a bronchodilator. R-836 can alleviate bronchial constriction caused by antigens or platelet activating factors.
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DC78348 YM-358 hydrate potassium
YM-358 hydrate (potassium) is an orally active angiotensin II type 1 (AT1)-receptor antagonist. YM-358 hydrate (potassium) can decrease cardiac volume overload. YM-358 hydrate (potassium) can be used for the research of cardiovascular disease, such as hypertension.
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DC78347 HTS05585
HTS05585 (Compound Hit-1) is a selective macrophage migration inhibitory factor (MIF) inhibitor with a Kd value of 0.29 μM measured by microscale thermophoresis (MST) and 0.32±0.01 μM verified by isothermal titration calorimetry (ITC). HTS05585 inhibits the release of pro-inflammatory factors (TNF-α, IL-6, IL-1β) from LPS-induced macrophages. HTS05585 is promising for research of inflammation-related diseases such as sepsis.
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