2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM. 2-Methylquinazolin-4-ol mammalian aspartate transcarbamylase (ATCase) inhibitor, with 0.20 mM[1][2].
Dulaglutide (LY2189265) is a glucagon-like peptide-1 (GLP-1) receptor agonist. Sequence: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Glu-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-Gly-Gly-Gly;HGEGTFTSDVSSYLEEQAAKEFIAWLVKGGG.
Carbidopa is an inhibitor of DOPA decarboxylase, which is used in parkinson disease.Target: DOPA decarboxylaseCarbidopa (CD), a competitive inhibitor of aromatic l-amino acid decarboxylase that does not cross the blood-brain barrier, is routinely administered with levodopa (LD) to patients with Parkinson disease (PD) to reduce the peripheral decarboxylation of LD to dopamine [1]. CD premedication improves 11C-5-HTP PET image quality and facilitates detection of NET lesions. Because of the similarity of metabolic pathways, this method could probably be applied to improve PET imaging using other tracers like 18F-DOPA and 11C-DOPA [2]. Carbidopa (100 microM) decreased growth of (but did not kill) SK-N-SH neuroblastoma and A204 rhabdomyosarcoma cells and did not affect proliferation of DU 145 prostate, MCF7 breast, or NCI-H460 large cell lung carcinoma lines. sublethal doses of carbidopa produced additive cytotoxic effects in carcinoid cells in combination with etoposide and cytotoxic synergy in SCLC cells when coincubated with topotecan [3].
Pseudoprotodioscin, a furostanoside, inhibits SREBP1/2 and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides[1].
GS-493 is a novel potent, selective SHP2 inhibitor with IC50 of 71±15 nM in enzyme assay; displays 29- and 45-fold selectivity against related SHP1 and PTP1B; blocks HGF-stimulated epithelial-mesenchymal transition of human pancreatic adenocarcinoma (HPAF) cells, and inhibits cell colony formation in the NSCLC cell line LXFA 526L in soft agar; inhibits tumor growth in murine xenograft model.
MOPSO sodium can be used for the preparation of buffer solution. MOPSO sodium is used as a biochemical reagent[1].
TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon)[1].
8-Bromo-2'-deoxyadenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
CYP3A4 enzyme-IN-1 (compound 59) is a potent antibacterial agent, with a MIC of 1 μg/mL for MRSA. CYP3A4 enzyme-IN-1 exhibits low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6, and CYP3A4 enzymes[1].
2-Amino-6-chloropurine -9-beta-D-(2’-deoxy-3’,5’-di-O-benzoyl-2’-fluoro)arabinoriboside is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
2',3'-cGAMP-C2-SH is a ADC cytotoxin that is extracted from patent US20210015941, example 24[1].
Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
Bis-PEG4-acid is a PEG PROTAC linker.
Resolvin D3 (RvD3) is a docosahexaenoic acid (DHA) derived mediator. Resolvin D3 is dysregulated in arthritis and reduces arthritic inflammation[1][2].
VXc-486 is a gyrase B inhibitor, with bactericidal activity. VXc-486 potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively[1].
PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC50 value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase[1].
Tilmicosin is a macrolide antibiotic, is used in veterinary medicine for the treatment of bovine respiratory disease and ovine respiratory disease associated with Mannheimia (Pasteurella) haemolytica.
Atractylenolide III is a major component of Atractylodes rhizome can induce apoptosis of the lung carcinoma cells.IC50 value:Target: Anticancer natural compoundin vitro: ATL-III inhibited cell growth, increased lactate dehydrogenase release and modulated cell cycle on human lung carcinoma A549 cells. ALT-III induced the activation of caspase-3 and caspase-9 and cleavage of poly-(ADP)-ribose polymerase. ATL-III induced the release of cytochrome c, upregulation of bax expression, and translocation of apoptosis-inducing factor [1]. Atractylenolide II did not show cytoprotective effects, but oral administration of atractylenolide III dose-dependently prevented ethanol-induced PRGM cell death and cell membrane damage. The EC50 values were 0.27 and 0.34 mm, respectively [2]. Against adult D. pteronyssinus, atractylenolide III (LD50, 73.8 mg/m2) and atractylon (72.1 mg/m2) were eight times more active than Deet and 2.5-fold more toxic than dibutyl phthalate [3].in vivo: In the in-vivo assay, atractylenolide III 10 mg/kg significantly reduced 70% ethanol-induced Wistar rat gastric ulcer. Atractylenolide III could inhibit matrix metalloproteinase (MMP)-2 and MMP-9 expression through upregulation of tissue inhibitors of metalloproteinase from the gastric ulcerated tissues [2].
Cefetamet pivoxyl is a cephalosporin antibiotic. Cefetamet pivoxyl inhibits 355 enteropathogens Keime, Gram-negative bacteria (ausgenommen Pseudomonas aeruginosa) and Legionella pneumophila[1].
Fmoc-D-Phe(4-F)-OH is a phenylalanine derivative[1].
Ceftizoxime sodium (SKF-88373) is third generation cephalosporin effective against Gram-negative and Gram-positive bacteria. It binds penicillin-binding proteins (PBPs) and inhibits the bacterial cell wall synthesis.
3,4,6-Tri-O-acetyl-D-glucal-13C-1 is the 13C labeled 3,4,6-Tri-O-acetyl-D-glucal[1].
AMPK activator 2 (compound 7a), a fluorine-containing proguanil derivative, up-regulates AMPK signal pathway and downregulates mTOR/4EBP1/p70S6K. AMPK activator 2 inhibits proliferation and migration of human cancer cell lines (UMUC3, T24, A549)[1].
Scopolin is a coumarin isolated from Arabidopsis thaliana (Arabidopsis) roots[1]. Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades[2].
Adenosine 3′-monophosphate (3′-AMP), a nucleotide, is a cyclic AMP production agonist[1].
TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine[1].
Nudiposide is a aromatic glucoside that can be isolated from Berchemia racemosa[1].
BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity[1].
GNE-6776 is a selective USP7 inhibitor.