c 82

C-82 is a specific CBP/β-catenin antagonist. It inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.

C82 acts as an inhibitor of Mycobacterium tuberculosis (Mtb) cyclic dinucleotide phosphodiesterase (CdnP), with an IC50 value of 17.5 µM. This particular enzyme is responsible for breaking down cyclic di-AMP (c-di-AMP) into adenosine 5'-monophosphate (AMP). Notably, C82 demonstrates selectivity for Mtb CdnP over other bacterial cyclic dinucleotide phosphodiesterases (CDN PDEs) such as Yybt, RocR, and Group B Streptococcus (GBS) CdnP, as well as the mammalian CDN PDE ENPP1, and the viral CDN PDE poxin, showing effectiveness at a concentration of 200 µM.

C-Reactive Protein (CRP) 77-82 is the 77-82 fragment of C-Reactive Protein. CRP, the prototypic marker of inflammation, is a cardiovascular risk marker and may promote atherogenesis. CRP is an annular (ring-shaped), pentameric protein found in blood plasma, whose circulating concentrations rise in response to inflammation. It is an acute-phase protein of hepatic origin that increases following interleukin-6 secretion by macrophages and T cells.

C-Reactive Protein (CRP) 77-82 acetate is the 77-82 fragment of C-Reactive Protein. C-Reactive Protein (CRP), the prototypic marker of inflammation, is a cardiovascular risk marker and may promote atherogenesis.C-reactive protein (CRP) is an annular (ring

NSC 828467 is one of the top five CA-IX inhibitors with significant in vitro anticancer activity (IC50: 27.2 nM).

Vadimezan (DMXAA) is a vascular disrupting agent, a murine STING agonist, and an inducer of cytokines such as type I IFN. Vadimezan has antitumor activity and induces a rapid cessation of blood flow in tumors without affecting blood flow in normal tissues.

Zavondemstat (QC8222 free base) is a histone lysine demethylase 4 (KDM4) inhibitor with anticancer and antitumor activity for the study of triple-negative and breast cancers.

Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.

Vesnarinone HCl (OPC-8212 HCl) is an orally active phosphodiesterase 3 (PDE3) inhibitor.Vesnarinone HCl modulates calcium and potassium ions, increasing calcium flux and decreasing potassium flux.Vesnarinone HCl is a new positive inotropic compound that enhances myocardial contractility and can be be used in heart failure studies.

Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.

Ursolic acid (Prunol) is a natural product, a pentacyclic triterpene carboxylic acid extracted from Rhododendron caprifolium. Ursolic acid has anti-tumor, anti-inflammatory, anti-bacterial and hypoglycemic activities.

Nalidixic acid (NSC-82174) is a synthetic 1, 8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA GYRASE.

Capsaicin is an active natural component found in chili peppers and acts as a TRPV1 agonist (EC50 = 0.29 μM). It possesses multiple activities, including pain relief, antitumor, anti-inflammatory, antioxidant, and neuroprotective effects, as well as some neurotoxicity. Capsaicin can be used to establish itch models.

Gentamicin sulfate (SCH9724) is a broad-spectrum, orally administered aminoglycoside antibiotic that exhibits inhibitory activity against aerobic Gram-negative bacteria by interfering with mRNA translation.

Methotrexate (WR19039) is a folate analog, an inhibitor of the dihydrofolate reductase DHFR. Methotrexate has antimetabolic, antitumor, and immunosuppressive activities, and is commonly used in rheumatoid arthritis and various tumors.

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50:10/39 nM).

PRI-724 is a second-generation, selective small molecule inhibitor of the β-catenin/CBP interaction.

Amphethinile, an anti-tubulin agent, has a Ka with tubulin of 1.3 μM.

Gefitinib hydrochloride (ZD-1839 hydrochloride) is an orally active selective and potent tyrosine kinase (EGFR) inhibitor. Gefitinib hydrochloride exhibits antitumor activity, selectively inhibits EGF-stimulated tumor cell growth, induces cellular autophagy, improves lung dysfunction, and inhibits inflammation. Gefitinib hydrochloride has antitumor activity, selectively inhibits EGF-stimulated tumor cell growth, induces cellular autophagy, ameliorates lung dysfunction, and inhibits the progression of inflammation and fibrosis.

NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM). NTRC-824 is an effective, selective, and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist (IC50: 38 nM and a Ki : 202 nM).

Ethionine (NSC-82393) is an antimetabolite and methionine antagonist. It also produces liver neoplasms.

UNC8212 is a potent TAM kinase inhibitor. It exhibits strong inhibitory activity against MERTK and AXL, with IC50 values of 1.5 nM and 1.3 nM, respectively, and also inhibits TYRO3 with an IC50 of 6.7 nM. By targeting the structurally diverse "back-pocket" region within the TAM kinase family, UNC8212 modulates polypharmacology characteristics. It binds tightly to TAM kinases and effectively inhibits MERTK and AXL phosphorylation. UNC8212 possesses antitumor properties and is applicable in cancer immunotherapy and target studies for tumor cells.

Zavondemstat (L-lysine) (QC8222; TACH 101) is an inhibitor of the histone lysine demethylase 4D (KDM4D) with antitumor properties.