Glycine, N-[(1,1-dimethylethoxy)carbonyl]thio-L-phenylalanyl-, methyl ester (compound 3b) is a polypeptide compound containing sulfamide, can be used to synthesis peptide-drug coupling compounds[1].
(+)-SJ733 is a clinical candidate for malaria which can also inhibit Na+-ATPase PfATP4.
Palmitoyl pentapeptide 4 (Matrixyl; Palmitoyl pentapeptide 3; Matrixyl (Palmitoyl Pentapeptide) is a bioactive peptide with anti-ageing effect and has been reported used as a cosmetic ingredient[1]
PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC BRD4 degrader[1].
Imgatuzumab (RG 7160) is a humanized monoclonal antibody against the EGFR. Imgatuzumab acts as an immunomodulator. Imgatuzumab can be used in research of cancer[1].
m-PEG8-CH2CH2-NHS ester is a PEG--based PROTAC linker can be used in the synthesis of PROTACs.
GLP-1R modulator C5 is an allosteric modulator enhancing GLP-1 binding to GLP-1R via a transmembrane site (EC50 1.59 ± 0.53 μM).
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
Nicotinoyl azide is capable of forming high energy intermediates known to form C-8 adducts with adenosine and guanosine[1].
FGFR2-IN-3 is an orally active selective inhibitor of FGFR2[1].
C16-Ceramide is a natural small molecule activating p53 through the direct and selective binding[1].
Secretin (28-54), human is a 27-amino acid residue C-terminally amidated peptide, which acts on secretin receptors.
Ganoapplanoid F, a highly oxygenated lanostane triterpenoid from Ganoderma applanatum, inhibits lipid accumulation in adipocytes. Ganoapplanoid F can be used for the research of obesity[1].
LyP-2 is a peptide that homes to tumor lymphatics. LyP2 homes to lymphatics of C8161 melanomas and cervical carcinomas and K14-HPV16 skin, but not to MDA-MB435 tumors, showing heterogeneity in the molecular markers of tumor cells and lymphatics[1].
N-Formyl-L-leucine is a leucine derivative[1].
KJ Pyr 9 is an inhibitor of MYC with a Kd of 6.5 nM in in vitro assay.
9-Deazaguanine is a nucleoside analog with potent inhibitory activity against purine nucleoside phosphorylase (PNP)[1].
Hydroxytyrosol acetate is found in the olive oil with an antioxidant activity. Hydroxytyrosol acetate had a weaker DPPH radical scavenging activity than hydroxytyrosol[1].
N-Boc-N-bis(PEG2-OH) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
MK-3697 is an isonicotinamide small molecule, acting as a potent and selective Orexin 2 receptor antagonist with Ki = 0.95 nM.IC50 value: 0.95 nM(Ki)Target: Orexin 2 receptor antagonistMK-3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists (2-SORAs) that possess acceptable profiles for clinical development. Herein we report additional SAR studies within the “triaryl” amide 2-SORA series focused on improvements in compound stability in acidic media and time-dependent inhibition of CYP3A4. MK-3697 has improved stability and TDI profiles as well as excellent sleep efficacy across species.
MMPI-1154 is a small molecule MMP-2 inhibitor with IC50 of 10/6.6/13/1.8 uM for MMP1/2/9/13, respectively; shows significant cardio-cytoprotecion, significantly decreases infarct size when applied at 1 μM in an ex vivo model for acute myocardial infarction.
Maohuoside A, a single compound isolated from the E. koreanum that potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways[1][2].
Picropodophyllol is a triol[1].
Cleroindicin F ((-)-Rengyolone), a cleroindicin, is an antimicrobial agent. Cleroindicin F shows relatively high anticandidal activity against Candida strains with a MIC value down to 12.5 µg/mL[1].
p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models[1].
INF4E is a potent NLRP3 inflammasome inhibitor. INF4E inhibits caspase-1 and NLRP3 ATPase activities. INF4E shows protection against the IR-induced myocardial injury and dysfunction[1][2].
LL-37 RKS is an active fragment of LL-37[1].
(6R)-FR054 is an active isomer of FR054. FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect. FR054induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptosis[1].
2’,3’,5’-Tri-O-benzoyl-2-thiouridine 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].
PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR[1]. Antitumor activity[1].