Ceritinib dihydrochloride (LDK378 dihydrochloride) is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.
RS100329 hydrochloride is a potent and selective α1A-adrenoceptor antagonist with pKi values of 9.6, 7.9 and 7.5 for α1A, α1D, and α1B, respectively. RS100329 hydrochloride inhibits reflex urethral contractions. RS100329 hydrochloride can be used in research of benign prostatic hyperplasia[1][2].
Grossamide is a natural product that can be isolated from fructus cannabis, the dried fruit of Cannabis sativa L.. Grossamide has anti-neuroinflammatory effects[1].
GSK-J5 is a potent inhibitor of Schistosome and worm. GSK-J5 increases schistosomula mortality and adult worm motility and mortality, as well as egg oviposition, in a dose- and time-dependent manner[1].
dTAGV-1 TFA is a potent and selective degrader of mutant FKBP12F36V fusion proteins. dTAGV-1 TFA can induce degradation of FKBP12F36V-Nluc in vivo[1].
XT-1 is an antimicrobial peptide derived from skin secretions of Xenopus tropicalis. XT-1 has strong activity against S.aureus, E.coli and C.albicans, the vaule of MIC are 5, 6, 50 μM , respectively[1].
Macelignan(Anwuligan) is a natural compound isolated from Myristica fragrans Houtt; possesses therapeutic potentials against neurodegenerative diseases with oxidative stress and neuroinflammation.IC50 value:Target: in vitro: Macelignan significantly attenuated the ROS production and neurotoxicity induced by glutamate in HT22 cell [1]. At 24 h of biofilm growth, S. mutans, A. viscosus and S. sanguis biofilms were reduced by up to 30%, 30% and 38%, respectively, after treatment with 10 microg/mL macelignan for 5 min [2]. Cisplatin-induced phosphorylation of c-Jun N-terminal kinase1/2 (JNK1/2) and extracellular signal-regulated kinase1/2 (ERK1/2) was abrogated by pretreatment with macelignan, however, that of p38 was not significantly affected [3].in vivo: Macelignan attenuated the expression of phosphorylated c-Jun in cisplatin-treated mice [3]. Daily administration of macelignan reduced the spatial memory impairments induced by the chronic LPS infusions [4].
9-(2-O-Acetyl-3,5-di-O-benzoyl-β-D-xylofuranosyl)-6-chloro-9H-purine 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].
NMDI14 is a nonsense mediated RNA decay (NMD) inhibitor.
Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
PDP-Pfp is a reducible ADC linker used for the agents that target for the extracellular loop 1 (ECL1) of TM4SF1 (transmembrane 4 L6 family member 1)[1].
D-Galactose-6-O-sulfate sodium salt is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
5-Hydroxytryptophol is a mammalian serotonin metabolite, acting as a marker of acute alcohol consumption.
4’-C-Methyl-4-deoxyuridine 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].
Thiocystine is a relatively stable trisulfide analog of Cystine. Thiocystine functions as a persullide in transferring its sulfane sulfur to thiophilic acceptors[1][2].
Pyridine-2,6-dicarboxylic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Desketoraloxifene is an estrogen receptors alpha (ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer[1].
Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK[1].
AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research[1].
Ceftobiprole medocaril (BAL5788) sodium is the parenteral prodrug of Ceftobiprole (HY-112579). Ceftobiprole is a parenteral pyrrolidinone cephalosporin. Ceftobiprole is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci. Ceftobiprole also inhibits gram-positive and gram-negative pathogens[1][2].
TIM-063 (TIM063) is a potent, selective, ATP-competitive CaMKK inhibitor with Ki of 0.35/0.2 uM for CaMKKα and CaMKKβ, respectively.TIM-063 directly targets the catalytic domain of CaMKK, similar to STO-609.TIM-063 suppressed the ionomycin-induced phosphorylation of exogenously expressed CaMKI, CaMKIV, and endogenous AMPKα in HeLa cells with an IC50 of 0.3 uM.TIM-063 suppressed CaMKK isoform-mediated CaMKIV phosphorylation in transfected COS-7 cells.TIM-063 displayed cell permeability and the ability to inhibit CaMKK activity in cells. TIM-063 is a useful chemical probe for the precise analysis of CaMKK-mediated signaling pathways.
D-(-)-Quinic acid is a cyclohexanecarboxylic acid and is implicated in the perceived acidity of coffee.
Anticancer agent 72 (compound 8c) is a potent inhibitor of K+ channel. Anticancer agent 72 induces apoptosis[1].
Lacutamab (IPH4102) is a humanized monoclonal antibody (mAb) directed against the immune receptor molecule KIR3DL2, produced by recombinant technology in CHO cells. Lacutamab can be used in research of cutaneous T-cell lymphoma[1].
Deoxycalyciphylline B is a hepatotoxic alkaloid that can be isolated from Daphniphyllum calycinum[1].
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 STX-478 shows robust and durable tumor regression and can be used in cancer research[1].
A-69412 is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase (5-LO).
Drupacine is a natural product, that can be isolated from Cephalotaxus harringtonia. Drupacine shows nematotoxicity and anticancer activity[1][2].
Diethylglycine is a Glycine (HY-Y0966) derivative[1].