Labetuzumab is a humanised anti-carcinoembryonic antigen (CEA) monoclonal antibody that inhibits tumour growth and sensitises human medullary thyroid cancer xenografts to Dacarbazine chemotherapy[1].
Vanillin-13C6 is the 13C labeled Vanillin[1]. Vanillin (p-Vanillin) is a single molecule extracted from vanilla beans and also a popular odor used widely in perfume, food and medicine[2][3].
Succinate/succinate receptor antagonist 1 (compound 7a) is a succinate/succinate receptor antagonist. Succinate/succinate receptor antagonist 1 blocks succinate signaling in gingival tissue. Succinate/succinate receptor antagonist 1 inhibits the activation of succinate receptor 1 (SucnRl) with an IC50 value of 20 μΜ. Succinate/succinate receptor antagonist 1 can be used for the research of periodontal disease[1].
KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na+ channels. KB130015 opens large-conductance Ca2+-activated K+ channels and relaxes vascular smooth muscle[1][2][3].
Erlotinib mesylate inhibits purified EGFR kinase with an IC50 of 2 nM.
Tacrine is a potent acetylcholinesterse (AChE) inhibitor (IC50=109 nM), also acting as a CYP1A2 substrate drug. Tacrine exhibits certain hepatotoxicity in some individuals. Tacrine can be used for researching Alzheimer's disease (AD)[1][2][3].
Lathyrol is a natural product, and is used for cancer treatment.
Cefditoren pivoxil is a new-third generation cephalosporin antibiotic that has a broad spectrum of activity against Gram-positive and Gram-negative bacteria, including common respiratory and skin pathogens.Target: AntibacterialCefditoren pivoxil, a new-third generation cephalosporin antibiotic that has recently been granted approval in Spain, shows important activity over a large part of the pathogens causing skin, soft tissue and respiratory tract infections, including Gram-negative and Gram-positive bacteria. Cefditoren is also marketed under the name Meiact. Cefditoren has a broad spectrum of activity and has been used to treat bacterial infections of the skin and respiratory tract including bronchitis, pneumonia, and tonsillitis. The following represents MIC susceptibility data for a few medically significant microorganisms.Cefditoren has shown excellent in vitro activity against the Gram-positive pathogens penicillin-susceptible and -intermediate Streptococcus pneumoniae, S. pyogenes and methicillin-susceptible Staphylococcus aureus. Cefditoren was inactive against methicillin-resistant S. aureus. Of the important Gram-negative pathogens, cefditoren had potent antibacterial effects against beta-lactamase-positive and -negative Haemophilus influenzae, H. parainfluenzae and beta-lactamase-positive and -negative Moraxella catarrhalis.
VU0080241 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 4 (mGluR4), with an EC50 of 4.6 μM[1].
BI-1950 is a potent, selective LFA-1 antagonist that inhibits the binding of LFA-1 to ICAM-1 with Kd value of 9 nM; displays >1,000 fold selectivity against the most closely related b2-integrin Mac-1 and b1-integrin function; inhibits the production of IL-2 in human PBMC and whole blood with IC50 value of 3 nM and 120 nM, respectively; exhibits an attractive DMPK profile, BI-1950 is a excellent molecule for testing pharmacological hypotheses in vitro and in vivo.
alpha-Man-TEG-N3 is a click chemistry reagent containing an azide group[1].
Gumokimab (AK 111) is a monoclonal antibody targeting IL-17A, which can be used in the study of psoriasis, ankylosing spondylitis. Gumokimab competitively blocks the binding of human IL-17A to IL-17R.
Boc-D-Pen(Mob)-OH is a phenylalanine derivative[1].
Thymosin β10Arg is a thymosin β4-like peptide that contains an additional amino acid, arginine, inserted following lysine-38[1].
ICMT-IN-54 (compound 7c) is an adamantyl analogue and an ICMT inhibitor (IC50=12.4 μM), which can inhibit ICMT Methylation. ICMT-in-54 inhibits BFC (N-biotinyl-(6-aminohexanoic)-S-farnesyl-L-cysteine) methylation in saccharomyces cerevisiae expressing ICMT, which is an indirect effect of inhibiting ICMT methylation[1].
Eleutheroside E, a principal component of Eleutherococcus enticosus, has anti-inflammatory and protective effects in ischemia heart. IC50 value:Target:In vitro: Treatment of 10 μM Eleutheroside E (EE) for 24 h increased basal glucose uptake as well as improved TNF-α-mediated suppression of glucose uptake. [2]In vivo: To investigate the effect of Eleutheroside E (EE) on arthritis, the CIA model in DBA/1 mice was used. Compared to vehicle-treated CIA mice, 15 mg/kg TG treatment and 30 and 60 mg/kg EE treatment obviously decreased the arthritis scores and body weight loss in CIA mice (P<0.01) [1].
[Tyr12] Somatostatin 28 (1-14) is an analogue of Somatostatin-28 (1-14) (HY-P1499). Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28[1].
ARQ 531 is a reversible non-covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively[1].
DENV-IN-9 (Compound 5f) is a DENV2 inhibitor with an EC50 of 0.88 μM[1].
5,6-Didehydroginsenoside Rd is a dammarane-type saponin isolated from the dried roots of Panax notoginseng[1].
Mordant Blue 13 is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Raloxifene N-Oxide is a Raloxifene oxidative degradation product[1].
L-Methionine hydrochloride is a Methionine (HY-13694) derivative[1].
D-Ribose-13C-1 is the 13C labeled D-Ribose. D-Ribose is an energy enhancer, and acts as a sugar moiety of ATP, and widely used as a metabolic therapy supplement for chronic fatigue syndrome or cardiac energy metabolism. D-Ribose is active in protein glyca
PI3Kγ inhibitor 1 is a PI3Kδ and PI3Kγ inhibitor extracted from patent WO2014004470A1, Compound 168 in Table 4, has IC50s of <100 nM.
Bevemipretide is a biodegradable silica hydrogel composite. Bevemipretide can be used for ocular indication[1].
1-Methyladenine is a product of alkylation damage in DNA which can be repaired by damage reversal by oxidative demethylation.
DHODH-IN-18 is a human DHODH inhibitor (IC50 = 0.2 nM).
MMV390048 is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent[1].