I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that targets the CBP/p300 bromodomains.
Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM.Target: HIV proteaseLopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats.
PDS-0330 is a specific and potent Claudin-1 inhibitor. PDS-0330 interferes with claudin-1/Src association and inhibits colorectal cancer (CRC) progression and metastasis[1].
VEGFR-2-IN-37 (compound 12) is an inhibitor of VEGFR-2. The inhibition rate at 200 μM was approximately 56.9 μM. VEGFR-2-IN-37 is a potential inhibitor of human umbilical vein endothelial cell (HUVEC) proliferation[1].
6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C). IC50 value:Target: K-Ras G12C6H05 gives the greatest degree of modification, which allosterically modifies the oncogenic G12C mutant of highly homologous protein H-Ras without affecting wild-type K-Ras [1]. 6H05 can be used as an intermediate for the synthesis of other oncogenic K-Ras(G12C) inhibitors [2].
HL-8 is a PROTAC molecule targeting PI3K kinase. HL-8 has a significant and complete degradation effect on PI3K kinase at a concentration of 10 μM within 8 h. HL-8 has the potential for the research of cancer diseases[1].
LGK974 is a potent and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM.
cis-Clovamide, a natural phenolic compound with antioxidant, anti-inflammatory and antiapoptotic activities[1].
3’-Deoxy-N6-methyladenosine 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].
(16R)-E-Isositsirikine is an indole alkaloid compound from Catharanthus roseus Tissue Cultures IV1[1].
Fmoc-Lys(5'-FAM)-OH is a lysine derivative[1].
Acenaphthylene-d8 is the deuterium labeled Acenaphthylene[1]. Acenaphthylene is a polycyclic aromatic hydrocarbon (PAH). PAHs are derived naturally from coal and tar deposits, and produced by incomplete combustion of organic matter[2].
QH536 (Compound 29) is a potent HMGCR degrader with an EC50 of 0.22 μM. QH536 has no side-effect of inducing cholesterol accumulation in cells. QH536 shows anti-inflammatory and can be used for cardiovascular disease and nonalcoholic steatohepatitis research[1].
Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).
Ganoderic acid T-Q (Ganodermic acid T-Q) (compound 1) is a natural product that can be found in ganoderma lucidum. Ganoderic acid T-Q stimulates tubulin polymerization[1].
2-Bromoadenosine, antimalarial agent is a purine nucleoside analogue. 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].
ODN 20844, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 20844 disrupts TLR7- and TLR9-mediated immune cell immune responses. ODN 20844 sequence: 5'-TCCTGGCGc7GGGAAGT-3'[1].
Netarsudil mesylate is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.
Orenetide is an innovative peptide drug developed in the study to restore sexual desire and concomitant functions in women with HSDD (Hypoactive desire disorder)[1]
Taccalonolides C, isolated from T. plantaginea, is an anti-cancer agent[1].
DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
Lansoprazole(AG 1749) is a proton pump inhibitor which prevents the stomach from producing acid.Target: Proton PumpLansoprazole, a substituted benzimidizole proton pump inhibitor, on pharmacokinetics and metabolism of theophylline has been studied in healthy adults given oral lansoprazole 30 mg once daily for 11 days. On Days 4 and 11 of 300 mg aminophylline was simultaneously administered orally and blood samples for theophylline analysis were taken over 24 h [1]. Patients in the lansoprazole group were significantly less likely to have a recurrence of ulcer complications than patients in the placebo group (P=0.008). There was no significant difference in mortality between the two groups [2]. lansoprazole (AG-1749) and omeprazole, were found to have significant activities against this organism. The activity of lansoprazole was comparable to that of bismuth citrate, with MICs ranging from 3.13 to 12.5 micrograms/ml, and fourfold more potent than that of omeprazole [3]. Clinical indications: Duodenal ulcer; Esophagitis; Gastroesophageal reflux; Gastrointestinal disease; Helicobacter pylori infection; Peptic ulcer; Stomach ulcer; Ulcer; Zollinger-Ellison syndromeFDA Approved Date: May 10, 1995Toxicity: Symptoms of overdose include abdominal pain, nausea and diarrhea.
3-Methylcatechol is a building block in the chemical synthesis produced by Pseudomonas putida MC2[1].
1-Hexanol-d13 is the deuterium labeled 1-Hexanol[1]. 1-Hexanol, a primary alcohol, is a surfactant that can be employed in industrial processes to enhance interfacial properties[2]. 1-Hexanol uncouples mitochondrial respiration by a non-protonophoric mechanism[3].
Trisulfo-Cy5-Alkyne is a click chemistry reagent containing an azide group. Trisulfo-Cy5-Alkyne can participate in copper-catalyzed Click Chemistry reactions. Trisulfo-Cy5-Alkyne is a near infrared (NIR) fluorescent dye[1].
Soyasaponin Af (Acetyl-soyasaponin A2) is a saponin isolated from Black bean (Phaseolus vulgaris L.) seed coats[1].
Edrecolomab (Panorex) is a murine monoclonal antibody to the cell-surface glycoprotein 17-1A, expressed on epithelial tissues and on various carcinomas. Edrecolomab shows anti-tumor activity and can be used in colorectal carcinoma research[1][2].
N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM[1]. N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor[2].
Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase[1].