Ornidazole diol (Ro 11-2616) is a diol produced by ornidazole rapidly hydrolysing in basic solutions[1].
UCM53, a FtsZ inhibitor, is an antibacterial agent. UCM53 can inhibit the growth of clinical isolates of antibiotic-resistant Staphylococcus aureus and Enterococcus faecalis[1]
Crizotinib is a potent inhibitor of c-Met and ALK with an IC50 of 11 nM and 24 nM in cell-based assays, respectively.
Morusinol is a flavonoid isolated from Morus alba root bark. Morusinol has an antiplatelet activity and significantly inhibits arterial thrombosis in vivo[1].
H-Ser-Pro-OH is a dipeptide containing serine and proline, which can serve as a substrate for prolinase I (PD I) and PD II. H-Ser-Pro-OH can also be used for the synthesis of polypeptide[1][2].
Anti-infective agent 3 (compound 3l) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 0.47 and 0.13 μM, respectively. Anti-infective agent 3 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 4 μg/mL[1].
Xanthine oxidoreductase-IN-4 is an orally active xanthine oxidoreductase (XOR) inhibitor. Xanthine oxidoreductase-IN-4 has inhibitory activity against XOR with an IC50 value of 29.3 nM. Xanthine oxidoreductase-IN-4 can be used for the research of hyperuricemia[1].
MOBS is an amphoteric buffer, a butane analogue of the Good buffers MOPS [3-(N-morpholino) propanesulfonic acid] and MES [2-(N-morpholino) ethanesulfonic acid][1].
Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer[1][2][3].
G-Subtide is a G-substrate peptide localized in Purkinje cells of the cerebellum. G-Subtide has little activity distinct from background and is a preferentially phosphorylated peptide substrate of recombinant PfPKG2 protein[1].
7-Deaza-2′-deoxyguanosine 5′-triphosphate (7-Deaza-2'-dGTP), a nucleotide analogue, is a telomerase inhibitor (IC50: 11 μM)[1].
C188-9 is a Stat3 inhibitor, with a Kd of 4.7 nM.
(S)-2-(2-Aminopropanamido)acetic acid is a Glycine (HY-Y0966) derivative[1].
p-Fluoro-L-phenylalanine (4-Fluoro-L-phenylalanine) is a substrate for tyrosine hydroxylase (TH) that can be used to study the regulation of that enzyme. p-Fluoro-L-phenylalanine binds to the L-leucine specific receptor of Escherichia coli (KD=0.26 μM)[1][2].
Trametinib DMSO solvate is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.
PPARγ-IN-2 (Compound 5a) is a PPARγ inhibitor. PPARγ-IN-2 inhibits TG accumulation in 3T3-L1 preadipocytes (EC50: 0.106 μM). PPARγ-IN-2 inhibits high-cholesterol diet (HFC)-induced obesity and related metabolic syndrome, and reduces lipid accumulation in adipose tissue[1].
Dopamine HCl is a catecholamine neurotransmitter present in a wide variety of animals,And a dopamine D1-5 receptors agonist.Target: Dopamine ReceptorDopamine (or 3,4-dihydroxyphenethylamine) is a neuroendocrine transmitter in the catecholamine and phenethylamine families that plays a number of important roles in the brain and bodies of humans. Several important diseases of the nervous system are associated with dysfunctions of the dopamine system. Outside the nervous system, dopamine functions in several parts of the body as a local chemical messenger. In the blood vessels, it inhibits norepinephrine release and acts as a vasodilator; in the kidneys, it increases sodium excretion and urine output; in the pancreas, it reduces insulin production; in the digestive system, it reduces gastrointestinal motility and protects intestinal mucosa; and in the immune system, it reduces the activity of lymphocytes. A variety of important drugs work by altering the way the body makes or uses dopamine. Dopamine itself is available for intravenous injection: although it cannot reach the brain from the bloodstream, its peripheral effects make it useful in the treatment of heart failure or shock, especially in newborn babies. L-DOPA, the metabolic precursor of dopamine, does reach the brain and is the most widely used treatment for Parkinson's disease. From Wikipedia.
C22:1 Ceramide-d7 is deuterium labeled C22:1 Ceramide.
Lith-O-Asp is a sialytransferase (ST) inhibitor, with IC50s of 12-37 μM.
N-Acetyl-2′-deoxycytidine 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].
GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.IC50 value: 3.2 pM [1]Target: PDE4Bin vitro: GSK256066 is a slow and tight binding inhibitor of PDE4B with apparent IC50 of 3.2 pM. GSK256066 is an extremely potent inhibitor of LPS-stimulated TNFα production in PBMCs with pIC50 of 11.0 and IC50 of 10 pM and human whole-blood cultures with pIC50 of 9.90 and IC50 of 126 pM. GSK256066 is highly selective for PDE4 (>3.8 × 105-fold versus PDE1, PDE2, PDE3, PDE5, and PDE6 and >2.5 × 103-fold against PDE7). GSK256066 inhibits PDE4 isoforms A-D with equal affinity [1].in vivo: GSK256066 inhibits the LPS-induced pulmonary neutrophilia with an ED50 of 1.1 μg/kg, achieving maximal inhibition of 72% at 30 μg/kg when given in the aqueous suspension. GSK256066 inhibits the LPS-induced pulmonary neutrophilia with ED50 of 2.9 μg/kg, achieving maximal inhibition of 62% when given in the dry powder formulation. GSK256066 shows a moderate plasma clearance of 39 ml/min/kg, a moderate volume of distribution of 0.8 L/kg, and a relatively short half-life of 1.1 hour in the male CD rat [1]. GSK256066 sustains at a high lung concentration of 2.6 μg/g after intra-tracheal administration as an aqueous suspension at a dose of 30 μg/kg in rats [2]. GSK256066 (10 μg/kg) is administered intratracheally at different times (2, 6, 12, 18, 24, and 36 hours) before LPS administration, inhibiting LPS-Induced Pulmonary Neutrophilia in rat lipopolysaccharide (LPS)-induced models of acute pulmonary inflammation. GSK256066 (0.3–100 μg/kg) inhibits LPS-induced increases in exhaled nitric oxide with ED50 of 35 μg/kg in rat. GSK256066 (10 μg/kg) is administered half a hour before OVA administration in rat, inhibiting OVA-induced pulmonary eosinophilia with ED50 of 0.4 μg/kg. GSK256066 administered intratracheally as a dry powder blended in respiratory-grade lactose at doses of 3 to 100 μg/kg 2 hours before inhaled LPS challenge in ferrets, inhibiting LPS-induced pulmonary neutrophilia with ED50 of 18 μg/kg without inducing emetic episodes [3].
LY2880070 is an orally active CHK1 inhibitor. LY2880070 can be used as an anticancer agent for combination with DNA damaging agents[1].
endo-BCN-PEG2-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect[1][2][3].
Benzyl 4-hydroxybenzoate-d4 is the deuterium labeled Benzyl 4-hydroxybenzoate[1].
Ifosfamide is an alkylating chemotherapeutic agent with activity against a wide range of tumors.
Aminooxy-PEG3-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5-Formylindole-CE phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
CFTR activator 1 is a potent and selective CFTR activator, with an EC50 of 23 nM. CFTR activator 1 can be used to ameliorate dry eye disease[1].
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.