NPB is a specific and potent inhibitor of BAD phosphorylation at Ser99, with an IC50 of 0.41 μM[1].
UK-383367 (UK 383367) is a potent and selective inhibitor of BMP-1 (procollagen C-proteinase) with IC50 of 44 nM; Selective for BMP-1 over MMPs 1, 2, 3, 9 and 14 (IC50 values are >10,000 nM for listed MMPs).IC50 value: 44 nMTarget: procollagen C-proteinaseUK-383367 (UK 383367) is useful for anti-scarring agent
Ruxolitinib is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3.
2-(2,6-Dioxopiperidin-3-yl)phthalimidine (EM-12), a teratogenic Thalidomide analogue, is more active than Thalidomide and is much more stable for hydrolysis. 2-(2,6-Dioxopiperidin-3-yl)phthalimidine enhances 1,2-dimethylhydrazine-induction of rat colon adenocarcinomas[1][2].
Nuvenzepine is an mAChR antagonist previously in phase I clinical trials for the treatment of gastrospasm.
Dibenzoyl Thiamine (Bentiamine), a derivative of thiamine, is rapidly absorbed into the body and converted to thiamine.
PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of B-RafV600E with an IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf[1][2].
HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity[1].
Bentracimab (PB 2452) is a neutralizing monoclonal antibody that binds Ticagrelor (HY-1006) and its major active circulating metabolite with high affinity. Bentracimab can rapidly reverse the antiplatelet effect of Ticagrelor[1].
Ald-Ph-PEG5-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ormutivimab (rhRIG) is a recombinant human monoclonal antibody, targeting rabies virus. Ormutivimab neutralizes a variety of rabies virus strains. Ormutivimab exhibits potent potency against rabies post-exposure prophylaxis (PEP) model[1][2].
2'-Deoxyadenosine-5'-triphosphate-d14 (dATP-d14) dilithium is deuterium labeled 2'-Deoxyadenosine-5'-triphosphate (HY-136648). 2'-Deoxyadenosine-5'-triphosphate (dATP) is a nucleotide used in cells for DNA synthesis (or replication), as a substrate of DNA polymerase.
Dihydrotanshinone I is a natural compound extracted from Salvia miltiorrhiza Bunge which has been widely used for treating cardiovascular diseases.
N1,N11-Diethylnorspermine tetrahydrochloride (DENSPM tetrahydrochloride) potently induces SSAT (spermidine/spermine N1-acetyltransferase) mRNA and effectively stabilizes SSAT enzyme activity[1].
IX 207-887 is a novel antiarthritic agent which inhibits the release of interleukin-1 (IL-1).
M1/M2/M4 muscarinic agonist 3 (compound 45) is a muscarinic mAChR M1/M2/M4 agonist with EC50s of 3.2 nM, 32 nM and 1.7 nM, respectively[1].
1-Bromotridecane-d4 is the deuterium labeled 1-Bromotridecane[1].
Sulbactam pivoxil is a prodrug of sulbactam. Sulbactam is a β-lactamase inhibitor which poorly adsorbed from gastrointestinal tract. Sulbactam pivoxil has a better absorption than the parent drug and provides high serum levels after oral administration[1].
Rubrofusarin gentiobioside is isolated from the seeds of Cassia tora L. Rubrofusarin gentiobioside has a radical scavenging effect[1].
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase (Top1) inhibitor with antitumor activity[1].
Rivularin (Skullcapflavone) is a flavonoid that can be found in Radix scutellariae[1].
S-(N-Methylcarbamoyl)glutathione-d3 is the deuterium labeled S-(N-Methylcarbamoyl)glutathione[1].
5'-O-DMT-ibu-dC can be used in the synthesis of oligodeoxyribonucleotides[1].
Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.Target: PDE5Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). In contrast, the IC50 of vardenafil for PDE1 was 180 nM; for PDE6, 11 nM; for PDE2, PDE3 and PDE4, more than 1000 nM. Relative to PDE5, the ratios of the IC50 for PDE1 were 257 (60), for PDE6 16 (7.4). Vardenafil significantly enhanced the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiated both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle [1]. Both vardenafil doses(10 mg or 20 mg) significantly enhanced the rates of successful penetration (P < 0.0001) and successful intercourse (P < 0.0001) compared with placebo. Vardenafil treatment was effective in increasing intercourse success rates at all levels of baseline ED severity, at each level of plasma HbA1c, and for type 1 and 2 diabetes [2].
Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the peptide Val-Cit-PAB.
4-(Aminomethyl)benzoic acid is an unnatural amino acid derivative, is an antifibrinolytic.
Cetirizine Impurity C dihydrochloride is an impurity of Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist[1][2].
4,5,6,7-Tetrabromobenzimidazole is a selective and ATP competitive CK2 (casein kinase 2) inhibitor[1].
6-Aminocaproic acid hydrochloride, a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders[1][2].
Coumarin153 is a coumarin. Coumarin153 can used as a fluorescence probe of Na dodecyl sulfate and cetyltrimethylammonium bromide[1].