ASPER-29 is Asperphenamate HY-129578 analog. ASPER-29 also is a dual cathepsin L and S inhibitor with IC50 value of 6.03 μM and 5.02 μM, respectively. ASPER-29 can be used for the research of the migration and invasion of cancer[1].
CCG-232601 is a potent (IC50=0.55 uM), orally bioavailable Rho/MKL1/SRF transcriptional pathway that target transcriptional factor MRTF; inhibits the development of bleomycin-induced dermal fibrosis in mice when administered at 50mg/kg.
Ibandronate Sodium is a highly potent nitrogen-containing bisphosphonate used for the treatment of osteoporosis.Target: OthersIbandronate (1.25-2 μM) significantly reduces endothelial cell growth, while ibandronate (2 μM) also significantly reduces capillary-like tube formation and increases apoptosis of endothelial cells. Ibandronate (< 100 μM) dose-dependently increases VEGF expression in endothelial cells [1]. Ibandronate (< 100 μM) inhibits growth of both prostate cancer cell lines (LNCaP and PC-3) in a dose dependent manner [2].Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly reduces the risk of new morphometric vertebral fractures by 62% and 50% (p = 0.0006), respectively, in osteoporotic women after 3 years' treatment. Ibandronate administered either daily (2.5 mg) or intermittently (20 mg every other day for 12 doses every 3 months) significantly and progressively increases BMD of lumbar spine by 6.5% and 5.7%, respectively, in osteoporotic women after 3 years' treatment [3]. Ibandronate (< 125 mg/kg s.c.) results in a dose dependent increase in bone mineral density (BMD), trabecular bone volume and trabecular number, load to failure (Fmax), and yield load in long bones and vertebrae in ovariectomized rats, and increased trabecular separation in ovariectomized rats is fully prevented by all doses [4].
Xylohexaose is a hexasaccharide consisting of six xylose residues.
Pravastatin-d3 (CS-514-d3) sodium salt is the deuterium labeled Pravastatin sodium salt. Pravastatin (CS-514) sodium salt is a competitive HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM[1][2].
MK-8245 is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.IC50 value: 1 nM (hSCD1) [1]Target: SCD1in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay [1].in vivo: Administration of MK-8245 at 10 mg/kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg/kg.
Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity[1].
Neoline, the active ingredient of processed aconite root (PA), alleviated oxaliplatin-induced peripheral neuropathy in mice. Neoline can be used as a marker compound to determine the quality of the PA products for the treatment of neuropathic pain[1].
Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC50 of 197 nM[1].
Kdo2-Lipid A ammonium is a chemically defined lipopolysaccharide (LPS) with endotoxin activity equal to LPS. Kdo2-Lipid A ammonium is highly selective for TLR4. Kdo2-Lipid A ammonium stimulates the release of both TNF and PGE2[1].
Atevirdine is a potent non-nucleoside HIV-1 reverse transcriptase inhibitor. Atevirdine inhibits non-nucleoside reverse transcriptase that leads to viral multiplication[1].
Tribromoacetonitrile is a nitrogen-containing disinfection byproduct[1].
HD5 is a biological active peptide. (a natural lectin-like human defensins-5 (HD5) peptide secreted by the Paneth cells in the crypts of Lieberkuhn, could interact with glycosylated proteins and lipid components)
NUN82647 inhibits cell cycle at G2 phase and induces apoptosis[1].
Temozolomide (NSC 362856; CCRG 81045) is an oral DNA alkylating agent used to treat some brain cancers.
(d(CH2)51,Tyr(Me)2,Thr4,Orn8,Tyr-NH29)-Vasotocin is an oxytocin antagonist and can be used for the research of sexual behavior[1].
NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
Quercetin-3-O-sambubioside is a monomeric compound found in Eucommia ulmoides male flowers. Quercetin-3-O-sambubioside promotes the stimulation of the nerve center. Antioxidant and anticancer activities[1][2].
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP+-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as Cisplatin, in killing cancer cells[1][2][3][4].
Thevetin A is a thevetia cardiac glycoside. Thevetin A can be isolated from the methanol extract of the seeds of Cascabela thevetioides[1].
[Asn23] β-Amyloid (1-40), Iowa mutation is a biological active peptide. (Several mutations in the beta amyloid precursor gene cause autosomal dominant Alzheimer's Disease in a number of kindreds. The Iowa mutation, where Asp 23 is replaced with Asn, is associated with severe cerebral amyloid beta-protein angiopathy (CAA). The affected individuals share a missense mutation in APP at position 694. The mutated beta-amyloid peptide aggregates more rapidly and forms toxic fibrils.)
7-Hydroxymethotrexate-d3 is the deuterium labeled 7-Hydroxymethotrexate. 7-Hydroxymethotrexate is a major metabolite of Methotrexate (MTX; HY-14519). Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis[1][2].
Carvedilol(BM14190) is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation.IC50 Value: 3.8 μM ( inhibition of LDL oxidation)Target: beta Adrenergic ReceptorCarvedilol is a nonselective-blocking agent and is used in the treatment of hypertension and angina pectoris. As a third-generation β-adrenergic blocker (β-blocker), Carvedilol is able to reverse cardiac structural remodeling. Recentresults demonstrated that the effect caused by Carvedilol on cardiac remodeling is largely dependent on endogenous NO.
Sotalol Hydrochloride is an adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias.Target: Adrenergic ReceptorSotalol is a non-selective competitive β-adrenergic receptor blocker that also exhibits Class III antiarrhythmic properties by its inhibition of potassium channels. Sotalol is a competitive beta adrenoceptor antagonist devoid of membrane-stabilizing activity and intrinsic sympathomimetic activity that has no preferential actions on beta 1 or beta 2 responses. Sotalol causes concentration-dependent increases in the contractility of isolated ventricular tissue that is not blocked by previous beta or alpha blockade or catecholamine depletion. Sotalol consistently reduces the heart rate to a greater degree than propranolol and causes significantly less cardiac suppression than propranolol at a given heart rate [1]. Sotalol is not only a beta blocker but a class III antiarrhythmic drug. Its possible antifibrillatory activity was therefore investigated in both the ventricles and atria of dog heart in situ, since vulnerability to fibrillation is not the same in both these parts of the myocardium [2].
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC)[1][2][3][4].
PHGDH-inactive has no activity against PHGDH and serves as a negative control of NCT-502 and NCT-503[1].
PNU288034 is a potent oxazolidinone antibiotic.
3-Furaldehyde is a member of furans and an aldehyde, and can be used to synthesize the neoclerodane diterpene Salvinorin A[1][2].
Methimazole(Tapazole, Northyx) is an antithyroid medicine.Target: OthersMethimazole is an antithyroid drug, and part of the thioamide group. Like its counterpart propylthiouracil, a major side effect of treatment is agranulocytosis. Methimazole is a drug used to treat hyperthyroidism, a condition that occurs when the thyroid gland begins to produce an excess of thyroid hormone. The drug may also be taken before thyroid surgery to lower thyroid hormone levels and minimize the effects of thyroid manipulation. Additionally, Methimazole is used in the veterinary setting to treat hyperthyroidism in cats.Methimazole inhibits the enzyme thyroperoxidase, which normally acts in thyroid hormone synthesis by oxidizing the anion iodide (I-) to iodine (I0), facilitating iodine's addition to tyrosine residues on the hormone precursor thyroglobulin, a necessary step in the synthesis of triiodothyronine (T3) and thyroxine. It does not inhibit the action of the sodium-dependent iodide transporter located on follicular cells' basolateral membranes. Inhibition of this step requires competitive inhibitors such as perchlorate and thiocyanate.It acts at CXCL10.
Pivalopril is a new orally active angiotensin converting enzyme (ACE) inhibitor.