PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity[1].
Cidofovir diphosphate is an active intracellular metabolite of Cidofovir. Cidofovir diphosphate is a selective inhibitor of viral DNA polymerases with Ki values of 6.6, 0.86 and 1.4 μM for HCMV, HSV-1 and HSV-2 DNA polymerase, respectively[1][2].
11-Hydroxyrankinidine is an alkaloid compound isolated from the whole plant of Gelsemium elegans[1].
Mca-Arg-Pro-Lys-Pro-Tyr-Ala-Nva-Trp-Met-Lys(Dnp)-NH2 is a biological active peptide. (MMP substrate)
RG-101 is a hepatocyte targeted N-acetylgalactosamine conjugated oligonucleotide that antagonises miR-122. miR-122 is an important host factor for hepatitis C virus (HCV) replication[1].
Hexamethylphosphoramide-d18 is the deuterium labeled Hexamethylphosphoramide[1].
Fmoc-Trp(Boc)-Ser(psi(Me,Me)pro)-OH is a dipeptide.
Bunazosin hydrochloride is a potent and selective α1-adrenoceptor antagonist. Bunazosin hydrochloride can be used for antihypertensive and ocular hypotensive research[1].
Gentisuric acid, a metabolite of Aspirin (HY-14654), is a substrate of α-amidating monooxygenase (PAM). Gentisuric acid prevents DNA-damage by Mitomycin C (HY-13316)[1][2].
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries. IC50 value: 3.4 nM [1]Target: HT2B receptorin vitro: PRX-08066 inhibits 5-HT-induced mitogen-activated protein kinase activation with IC50 of 12 nM and markedly reduces thymidine incorporation with IC50 of 3 nM in Chinese hamster ovary cells expressing the human 5-HT2BR, which suggests that PRX-08066 can potentially inhibit the pathologic 5-HT-induced vascular muscularization associated with PAH [1]. PRX-08066 inhibits cell proliferation with IC50 of 0.46 nM and with a maximum inhibition of 20% and 5-HT secretion with IC50 of 6.9 nM with a maximum inhibition of 30% in the 5-HT(2B) expressing SI-NET cell line, KRJ-I. PRX-08066 inhibits isoproterenol-stimulated 5-HT release with IC50 of 1.25 nM and a maximum inhibition of 60% in NCI-H720 cells. PRX-08066 (0.5 nM) significantly inhibits ERK phosphorylation in KRJ-I cells. PRX-08066 inhibits TGFβ1, CTGF and FGF2 transcription and secretion in KRJ-I cells. PRX-08066 decreases level of transcripts for Ki67 (84%) as well as Ki67 protein (36.8%) associated with an increase in caspase 3 transcript levels in KRJ-I cells. PRX-08066 decreases level of transcripts of TGFβ1, FGF2 and TPH1 in KRJ-I cells. PRX-08066 significantly increases the number of dead cells (34%) compared with untreated controls in KRJ-I cells. PRX-08066 causes a significant increase in dead/caspase 3 positive cells (76%) and caspase 3 activity (52%) in HEK293 cells [2].in vivo: PRX-08066 (100 mg/kg) treated groups demonstrates less right ventricular hypertrophy and septal flattening than the monocrotaline control group in rats. PRX-08066 significantly reduces peak pulmonary artery pressure at 50 mg/kg and 100 mg/kg compared with monocrotaline control rats. PRX-08066 also significantly reduces right ventricle (RV)/body weight and RV/left ventricle + septum, compared with MCT-treated rats. PRX-08066 significantly attenuates the elevation in pulmonary artery pressure and RV hypertrophy and maintains cardiac function. PRX-08066 significantly reduces the hypoxia-dependent increase in right ventricular systolic pressure in both rats and mice without affecting the systemic mean arterial pressure in the animals [1]. PRX-08066 (100 mg/kg) significantly inhibits both right ventricular systolic pressure and right ventricular/left ventricular +septum weight elevations in rats. PRX-08066 (30 mg/kg) inhibits right ventricular systolic pressure and monocrotaline-induced ERK phosphorylation in whole lung homogenates in rats [3].
CDK7-IN-5 is a CDK7 inhibitor with an IC50 value <100 nM. CDK7-IN-5 has anticancer effects. (WO2015154022A1 (Compound 104))[1].
2’,3’-Bis(O-t-butyldimethylsilyl)-2-thiouridine 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].
Febuxostat sec-butoxy acid is an impurity of Febuxostat. Febuxostat is selective xanthine oxidase inhibitor with a Ki of 0.6 nM[1].
Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.
Methyl 5-hydroxypyridine-2-carboxylate is a phenolic acid that can found in the stems of Mahonia fortune. Methyl 5-hydroxypyridine-2-carboxylate exhibits NO inhibitory effects in vitro[1].
Hexahydrocurcumin is a natural compound which posesses anticancer and anti-inflammatory activities; selective COX-2 inhibitor.IC50 value:Target: in vitro: The relative antioxidant potencies of ginger compounds decreased in similar order of 1-dehydro-[6]-gingerdione, hexahydrocurcumin>6-shogaol>6-dehydroshogaol in both 1,1-diphenyl-2-picyrlhydrazyl (DPPH) radical-scavenging and trolox equivalent antioxidant capacity (TEAC) assays [1]. HHC alone markedly decreased the viability of HT-29 human colon cancer cells compared to control. HHC significantly down-regulates COX-2 mRNA expression compared to the control (control: 100.05% ± 0.03% vs HHC: 61.01% ± 0.35%, P < 0.05) but does not alter COX-1 mRNA. In combined treatment, addition of HHC to a low dose of 5-FU exerts a synergistic effect against the growth of HT-29 cells by markedly reducing cell viability to a greater degree than monotherapy [2].in vivo: The combined effects of HHC with 5-FU exhibit a synergistic inhibition by decreasing ACF formation mediated by down-regulation of COX-2 expression in rats [3].
Ac-AAVALLPAVLLALLAP-YVAD-CHO is a cell-permeable caspase-1 inhibitor that has antitumor activity[1].
sRANKL-IN-1 (compound S3) is a sRANKL (soluble RANKL) inhibitor. sRANKL-IN-1 shows a potent osteoclast inhibition effect with an IC50 value of 0.096 μM and a KD value of 34.80 μM. sRANKL-IN-1 can be used for the research of osteoporosis[1].
BKM1644 is an effective inhibition of the proliferation of metastatic, castration-resistant PCa (mCRPC) cells.
(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research[1].
Lodoxamide is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
(2S)-Isoxanthohumol is a microbial biotransformed metabolite of the hop prenylflavanone Isoxanthohumol[1].
Justin C (compound 14) is a nature product that could be isolated from Justicia procumbens. Justin C can be used in research of cancer[1].
DMAC-PDB is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Porcn-IN-2 (Example 107) is a Wnt inhibitor, with an IC50 value of 0.05 nM. Porcn-IN-2 can be used for research of cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia, etc[1].
Monensin methyl ester, a neutral analog of monensin, is an ion active component for Na+ selective disk electrodes[1].
BMP2-derived peptide is a functional motif from positions 73 to 92 of the amino acid sequence of BMP-2. BMP2-derived peptide promotes osteogenic differentiation of bone marrow stromal cells (BMSCs) and enhances bone regeneration[1].
BODIPY 505/515, a lipophilic bright green fluorescent dye was tested for lipid detection in the microalga Tetraselmis subcordiformis. BODIPY 505/515 displays excitation/emission maxima of 505/515 nm, respectively, and has been used for live and fixed cell applications[1].
Olmesartan methyl ester is an intermediate in the synthesis of Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor antagonist with IC50 of 66.2 μM[1][2].
Suc-Ala-Phe-Lys-AMC is a highly sensitive fluorogenic substrate for plasmin. Suc-Ala-Phe-Lys-AMC is also used for assaying gingipain K[1][2].