| DC75686 |
Quipazine dimaleate |
Quipazine dimaleate is a selective 5-HT3 receptor agonist that also displays antagonist activity at peripheral 5-HT3 receptors. [3H]-Quipazine labels 5-HT3 sites in the cortical membranes. |
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| DC75687 |
Lenacapavir |
Lenacapavir, also known as GS-6207, is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs). Lenacapavir demonstrated picomolar potency in vitro with no cross resistance to existing antiretroviral classes and potent antiviral activity in persons with HIV-1. In persons with HIV-1, there was no preexisting resistance to lenacapavir regardless of treatment history. |
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| DC75688 |
Pardoprunox HCl |
Pardoprunox, also known as SLV-308; DU-126891; SME-308, is dopamine D2/5-HT1A receptor agonist potentially for the treatment of Parkinson's disease. It was also being investigated for the treatment of depression and anxiety but these indications appear to have been abandoned. Pardoprunox acts as a D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist (IA = 50% and 67%, respectively) and 5-HT1A receptor (pKi = 8.5) full agonist (IA = 100%). It also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity. |
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| DC75689 |
Remodelin HBr |
Remodelin is a cell-permeable, potent, and stable analog of CPTH2. Remodelin inhibits acetyl-transferase NAT10, a nucleolar N-acetyltransferase involved in stabilization of microtubules. Remodelin is a cell-permeable, potent, and stable analog of CPTH2. Remodelin was found to correct cell defects associated with progeria, restoring and improving nuclear shape and reducing the DNA damage believed to be associated with mutations in the gene for laminin A. |
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| DC75690 |
Obeticholic Acid |
Obeticholic Acid (INT747; 6-ECDCA) is a novel derivative of cholic acid which acts as a potent and selective FXR agonist displaying anticholeretic activity in an in vivo rat model of cholestasis. It inhibits vascular smooth muscle cell inflammation and migration as well as promotes adipocyte differentiation and regulates adipose cell function in vivo. |
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| DC75691 |
Mitoglitazone |
Mitoglitazone, also known as CAY10415, is a novel peroxisome proliferator-activated receptor (PPAR)γ ligand. CAY10415 induced cell death and ROS generation in a PPARγ-independent manner. CAY10415 enhanced γ-radiation-induced apoptosis and caspase-3-mediated poly (ADP-ribose) polymerase (PARP) cleavage in vitro. The combined CAY10415 / γ-radiation treatment triggered caspase-8 activation, and this initiator caspase played an important role in the combination-induced apoptosis. The combined treatment of CAY10415 and γ-radiation synergistically induced DNA damage and apoptosis, which was regulated by ROS. |
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| DC75692 |
PYR-5084 |
PYR-5084, CAS#59435-08-4, is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs. |
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| DC75693 |
Mycophenolate mofetil free acid |
Mycophenolate mofetil, also known as MMF or CellCept, is a prodrug of mycophenolic acid, and classified as a reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH). It is an immunosuppressant combined with drugs such as Cyclosporine and corticosteroids to prevent organ rejection after hepatic, renal, and cardiac transplants. |
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| DC75694 |
NB-598 free base |
NB-598 is a potent competitive inhibitor of squalene epoxidase (SE). NB-598 suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 suppresses the secretion of cholesterol and triacylglycerol and simultaneously reduces apolipoprotein B in HepG2 cells. NB-598 reduced basolaterally secreted radioactivity in cholesterol, cholesterol ester, PL and TG. Furthermore, NB-598 suppressed the basolateral secretion of apolipoprotein (apo) B. When microsomes prepared from control Caco-2 cells were incubated with 10 microM NB-598, acyl CoA:cholesterol acyltransferase (ACAT) activity was inhibited slightly. |
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| DC75695 |
MC-Val-Cit-PAB-PNP |
MC-Val-Cit-PAB-PNP, also known as Mc-Val-Cit-PABC-PNP, is a cathepsin cleavable ADC peptide linker. The Val-Cit will specifically be cleaved by catepsin B. Because this enzyme is only present in the lysosome, the ADC payload will only be released in the cell. The Azido group will react with DBCO, BCN or other Alkyne groups through click chemistry. The hydrophilic PEG spacer increases solubility in aqueous media.||* * * * * *|Please also see similar products: #610235: MC-Val-Cit-PAB (ADC peptide linker) and #610234: MC-Val-Cit-PAB-PNP (ADC peptide linker); #620108 Val-cit-PAB-OH (ADC peptide linker). |
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| DC75696 |
Mupirocin Lithium |
Mupirocin is an antibiotic and bacterial metabolite that has been found in P. fluorescens. It is bacteriostatic against S. aureus (MIC = 0.05 µg/ml) and active against skin wound clinical isolates of methicillin-resistant S. aureus (MRSA; MICs = 1-4 µg/ml). Mupirocin inhibits MRSA and P. aeruginosa biofilm formation in vitro.4 It inhibits bacterial cell wall isoleucyl-tRNA synthetase, slowing bacterial growth. Topical administration of Mupirocin (2% v/v) reduces the number of wound colony forming units (CFUs) in a mouse model of MRSA skin infection. Lithium mupirocin as been used to study mupirocin resistance in staphylococcus aureus and in mycoplasma susceptibility studies. |
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| DC75697 |
GNF2133 HCl |
GNF2133 is a potent and selective DYRK1A inhibitor (IC50 = 6 nM). In vitro, GNF2133 is able to proliferate both rodent and human β-cells. In vivo, GNF2133 demonstrated significant dose-dependent glucose disposal capacity and insulin secretion in response to glucose-potentiated arginine-induced insulin secretion (GPAIS) challenge in rat insulin promoter and diphtheria toxin A (RIP-DTA) mice. |
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| DC75698 |
Asenapine free base |
Asenapine, also known as Org 5222, shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors. Asenapine behaves as an antagonist at all receptors. It exhibits potent activity in animal models predictive of antipsychotic efficacy. Note this product we supply is a racemic mixture. |
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| DC75699 |
SR-59230A oxalate |
SR-59230A is a potent and selective β3 adrenoceptor antagonist (IC50 values are 40, 408 and 648 nM for β3, β1 and β2 receptors respectively). SR-59230A was subsequently shown to also act at α1 adrenoceptors at high doses. It has been shown to block the hyperthermia produced by MDMA in animal studies. SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism. |
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| DC75700 |
Fenebrutinib free base |
Fenebrutinib, also known as GDC-0853, is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, GDC-0853 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways, which leads to the inhibition of the growth of malignant B-cells that overexpress BTK. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B-lymphocyte development, activation, signaling, proliferation and survival. |
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| DC75701 |
Azide-PEG4-Amine free base |
Azido-PEG4-amine is a PEG derivative containing an amino group with an azide group. The amino group is reactive with carboxylic acids, activated NHS esters, carbonyls (ketone, aldehyde) etc. The azide group can react with alkyne, BCN, DBCO via Click Chemistry to yield a stable triazole linkage. PEG Linkers may be useful in the development of antibody drug conjugates and drug delivery methods. |
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| DC75702 |
AG-045572 |
AG-045572 is a selective gonadotropin-releasing hormone (GnRH) receptor antagonist that suppresses testosterone and luteinising hormone (LH) levels in vivo. |
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| DC75703 |
Minocycline HCl |
Minocycline (INN) is a broad-spectrum tetracycline antibiotic, and has a broader spectrum than the other members of the group. It is a bacteriostatic antibiotic, classified as a long-acting type. As a result of its long half-life it generally has serum levels 2–4 times that of the simple water-soluble tetracyclines (150 mg giving 16 times the activity levels compared with 1 g of tetracycline at 24–48 hours). Minocycline is the most lipid-soluble of the tetracycline-class antibiotics, giving it the greatest penetration into the prostate and brain. Minocycline is not a naturally-occurring antibiotic, but was synthesized semi-synthetically from natural tetracycline antibiotics by Lederle Laboratories in 1966. (https://en.wikipedia.org/wiki/Minocycline) ) |
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| DC75704 |
P7C3A20-analog |
P7C3A20-analog, as known as defluoro-P7C3-A20, is a structural analogue of P7C3-A20. Compared to P7C3-A20 structure, P7C3-A20 analog has no fluorine atom in the 1,3-diaminopropane-bridge. P7C3-A20 analog was synthesized by mistake during a process to make P7C3-A20. The bioactivity of P7C3-A20 analog is unknown. P7C3-A20 analog may be used for research to compare with P7C3-A20. P7C3-A20 is a proneurogenic, neuroprotective agent. P7C3-A20 displayed increased activity and an improved toxicity profile compared to P7C3. P7C3-A20 demonstrated greater proneurogenic efficacy than a wide spectrum of currently marketed antidepressant drugs. P7C3-A20 showed neuroprotective properties in rodent models of Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury and age-related cognitive decline. |
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| DC75705 |
ANR-94 |
ANR-94 is an adenosine A2A receptor (AA2AR) antagonist that displays activity in the treatment of Parkinson's disease in vivo, improves parkinsonian motor deficits and tremors, and exhibits neuroprotective and anti-inflammatory effects. |
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| DC75706 |
CCRP2 |
CCRP2, also known as TLX agonist 1 and SUN23314, is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity. CCRP2 was reported in PLoS One . 2014 Jun 17;9(6):e99440. |
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| DC75707 |
(±)-AC 7954 hydrochloride |
(±)-AC 7954 hydrochloride is a selective nonpeptidic druglike urotensin-II receptor agonist. |
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| DC75708 |
NG-25 HCl |
NG-25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner. It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12D mouse orthotopic model of colorectal cancer. |
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| DC75709 |
IKK-16 (free base) |
IKK-16 is a potent and slective inhibitor of IκB kinase (IKK) (IC50 values are 40, 70 and 200 nM for IKKβ, IKK complex and IKKα respectively). KK-16 inhibits TNFα-stimulated expression of the adhesion molecules E-selectin, ICAM-1, and VCAM-1 in HUVEC cells. |
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| DC75710 |
TWS-119 |
TWS-119 is a potent and selective inhibitor of glycogen synthase kinase-3β (IC50 = 30 nM). TWS119 could activate Wnt/β-catenin pathway and up-regulate the expression of CD62L in a dose-dependent manner, but it decreased the expression of CD107a. Glycogen synthase kinase (GSK)-3, a constitutively active serine-threonine kinase, acts as a key regulator of major signaling pathways, including the Wnt, Hedgehog, and Notch pathways. |
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| DC75711 |
RA371 |
RA371, a derivative of PTP1B-IN-8 (CAS#919091-61-5), is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor |
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| DC75712 |
UAMC-3203 |
UAMC-3203 is an inhibitor of ferroptosis for inhibition of erastin-induced ferroptosis in IMR-32 neuroblastoma cells. It decreases iron-induced plasma lactate dehydrogenase (LDH) levels in a mouse model of acute iron poisoning when administered at a dose of 20 µmol/kg. It is not toxic to mice following chronic administration of a 20 µmol/kg dose for four weeks. UAMC-3203 has increased solubility and a longer half-life in mouse, rat, and human microsomes and isolated plasma than the ferroptosis inhibitor ferrostatin-1. In an in silico membrane dynamics study, UAMC-3203 was incorporated into a phospholipid bilayer. |
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| DC75713 |
HKI-357 |
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation. |
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| DC75714 |
JAB-3068 free base |
JAB-3068, also known as HMN23485, SHP2-IN-6, is a potent SHP2 inhibitor. JAB-3068 targets, binds to and inhibits the activity of SHP2. This prevents SHP2-mediated signaling, inhibits MAPK signaling and prevents growth of SHP2-expressing tumor cells. SHP2, an oncoprotein overexpressed in a variety of cancer cell types, regulates cell survival, differentiation and proliferation through activation of the Ras-Raf-MEK-ERK signaling pathway. The Ras-MAPK pathway is often hyperactivated in cancer cells due to specific mutations and rearrangements and are dependent on SHP2 for their oncogenic signaling. SHP2 also regulates programmed cell death 1 (PD-1)-mediated signal transduction and is involved in immune checkpoint modulation. |
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| DC75715 |
ASP4132 tosylate |
ASP4132 is an AMPK activator with potential antineoplastic activity. Upon oral administration, ASP4132 affects oxidative phosphorylation in mitochondria of metabolically-active tumor cells, which reduces both energy production and tumor cell proliferation. Mitochondrial oxidative phosphorylation is hyperactivated in tumor cells and plays a key role in the promotion of tumor cell proliferation. |
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