T-5224 is a selective inhibitor of c-Fos/activator protein (AP)-1. It also inhibits MMP3/13 with IC50s of 10 nM.
Resorufin acetate is a fluorescent dye that selectively detects hydrazine[1].
L-778123 is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.IC50 value: 2 nM [1]Target: FPTasein vitro: L-778123 can completely inhibit Ki-Ras prenylation. [1] L-778123 as a farnesyltransferase inhibitor can have a good cytotoxic activity as a classic anti-cancer agent. [2]in vivo: In the dog model, L-778123 inhibits HDJ2 prenylation and produces measurable, albeit slight (5%), levels of unprenylatedRap1A in PBMCs. [1]
PD 132002 is an orally active, potent renin inhibitor. PD 132002 weakly inhibits pepsin. PD 132002 produces substantial reductions in blood pressure[1].
ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
BLXA-4 is used potentially to treat gingival diseases.
6-Deoxyisojacareubin is a PKC inhibitor that inhibits the proliferation of QGY-7703 cells in a concentration-dependent manner. 6-Deoxyisojacareubin is also a natural product that can be obtained from Garcinia nervosa. 6-Deoxyisojacareubin can be used in cancer research[1].
Bentiromide is a peptide that is broken down in the pancreas by chymotrypsin. The bentiromide test is an excellent means of confirming the diagnosis of pancreatic exocrine insufficiency by outpatient test of chymotrypsin function[1].
Ki-20227 is a highly selective c-Fms tyrosine kinase(CSF1R) inhibitor with IC50 value of 2 nM; 6 fold and > 100 fold selectivity over VEGFR2(IC50=12 nM) and c-Kit/PDGFRβ(IC50=451/217 nM), respectively.IC50 value: Target: CSF1Rin vitro: Ki20227 did not inhibit other kinases tested, such as fms-like tyrosine kinase-3, epidermal growth factor receptor, or c-Src (c-src proto-oncogene product). Ki20227 was also found to inhibit the M-CSF-dependent growth of M-NFS-60 cells but not the M-CSF-independent growth of A375 human melanoma cells in vitro [1]. Ki20227 inhibited M-CSF-dependent reactions, such as lipopolysaccharide-induced tumor necrosis factor-alpha production, which were enhanced by M-CSF in vitro [2]. in vivo: Ki20227 decreased the number of tartrate-resistant acid phosphatase-positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats [1]. In addition, the number of CD11b(+), Gr-1(+), and Ly-6G(+) cells in the spleen decreased in the Ki20227-treated mice, and the CII-induced cytokine production in splenocytes isolated from the Ki20227-treated arthritic mice was also reduced [2]. Ki20227 treatments inhibited the turn-over/expansion of myeloid cells provoked by the immunization and subsequent MOG-specific T cell responses in our EAE animal model [3].
Atrial Natriuretic Peptide (7-28), human, canine is a peptide fragment of atrial natriuretic peptide, can be used as a peptide tag[1].
Cimicifugoside H-1, a cyclolanostanol xyloside, is a major constituent of C. foetida L. extract. Cimicifugoside H-1 inhibits bone resorption and ovariectomy-induced bone loss[1][2][3].
Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min)， acts as an adrenoceptor antagonist[1].
L-Hyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine.Target: mAChRHyoscyamine is a chemical compound, a tropane alkaloid it is the levo-isomer to atropine. It is a secondary metabolite of some plants, particularly henbane (Hyoscamus niger.)Hyoscyamine is used to provide symptomatic relief to various gastrointestinal disorders including spasms, peptic ulcers, irritable bowel syndrome, pancreatitis, colic and cystitis. It has also been used to relieve some heart problems, control some of the symptoms of Parkinson's disease, as well as for control of respiratory secretions in end of life care [1].
Microsomal aminopeptidase (microsomal aminoptidase) was first reported from C. elegans. The Microsomal aminopeptidase is beneficial for the development of molecular vaccines against parasitic nematodes[1].
2-Benzimidazolethiol-d4 is the deuterium labeled 2-Benzimidazolethiol[1].
L-Gulose, the putative furanose form of L-sorbosone, is an L-hexose sugar and an intermediate in the biosynthesis of L-Ascorbate (vitamin C)[1].
β-Amyrin palmitate shows HMG-CoA reductase inhibition[1]. And β-Amyrin palmitate has anti-diabetes mellitus activity[2].
Elagolix is a highly potent, selective, orally-active, short-duration, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (KD = 54 pM).Target: GnRHin vitro: Elagolix is a short-acting, nonpeptide, GnRH antagonist, administered orally, that unlike injectable depot GnRH agonists and antagonists, produces a dose-dependent suppression of ovarian estrogen production, that is, from partial suppression at lower doses to full suppression at higher doses. Elagolix is regarded as the frontrunner of a new class of GnRH inhibitors that have been denoted as second-generation, due to their non-peptide nature and oral bioavailability.
HDAC8-IN-3 (compound P19) is a potent HDAC8 inhibitor with IC50 value of 9.3 μM and produces thermal stabilization. HDAC8-IN-3 has cytotoxicity and induces apoptosis in leukemic cell lines[1].
Gefitinib D8 (ZD1839 D8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells[1][2].
11β-HSD1-IN-9 (compound c4a) is a potent 11β-HSD1 inhibitor with IC50 values of 0.48 and 1.3 µM for human and murine 11β-HSD1, respectively. 11β-HSD1-IN-9 competitively interacts with rat 11β-HSD1. 11β-HSD1-IN-19 can be used in studies of obesity, hyperglycemia and cognitive impairment[1].
XIAP BIR2/BIR2-3 inhibitor-1 (compound 3) is a dual inhibitor of BIR2 and BIR2-3 with IC50s of 1.9 and 0.8 nM, respectively. XIAP BIR2/BIR2-3 inhibitor-1 can used in study cancers[1].
Mal-PEG2-VCP-Eribulin consists the ADCs linker (Mal-PEG2-VCP) and Eribulin[1]. Eribulin is a mechanistically unique microtubule inhibitor for cancer[2]. Mal-PEG2-VCP-Eribulin is an Eribulin-based drug for antibody conjugates[1].
N2-[(1,1-Dimethylethoxy)carbonyl]-N6-[(2-propynyloxy)carbonyl]-L-lysine is a lysine derivative[1].
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, high affinity histamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research[1][2][3][4].
Sonrotoclax is a potent, orally active Bcl2 inhibitor. Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines[1].
MIV-150 is a nonnucleoside reverse transcriptase (NNRT) inhibitor, blocking HIV-1 and HIV-2 infections, with an EC50<1 nM against HIV-1/HIV-2MN.
Dabcyl-RGVVNASSRLA-Edans (Dabcyl-CMV-Edans) is a fluorogenic substrate for human cytomegalovirus (HCMV) protease[1].
Propargyl-PEG9-bromide is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
L 741742 hydrochloride is an orally active and selective antagonist of hD4 receptors. L 741742 hydrochloride has a good brain penetration. L 741742 hydrochloride can be used in study nervous system disorders, particularly schizophrenia[1].