Cinerubin B, a glycosylated anthracycline antibiotic, is an anticancer agent from Streptomyces sp. SPB74[1].
Tyr-Somatostatin-28 is a somatostatin that adds a Tyrosine amino acid to Somatostatin-28[1].
Ketorolac D4 (RS37619 D4) is the deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2[1][2].
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice[1].
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma[1].
Tigatuzumab (CS-1008) is a humanized IgG1 monoclonal antibody targets death receptor 5 (DR5). Tigatuzumab induces cell Apoptosis of cancer cells and inhibits tumor growth in vivo. Tigatuzumab can be used for the research of cancer[1].
PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.
15:0 Lyso PG-d5 is deuterium labeled 15:0 Lyso PG.
Risevistinel (NYX-783) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease[1].
H-D-2-Nal-OH is an alanine derivative[1].
Garsorasib is a potent inhibitor of KRAS G12C with an IC50 of 10 nM. Garsorasib has the potential for the research of various cancer such as pancreatic cancer, endometrial cancer, colorectal cancer, or lung cancer (non-small cell lung cancer) (extracted from patent WO2020233592A1, compound 2)[1].
Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM)[1][2].
PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction[1].
KTX-582 intermediate-3 is an intermediate in the synthesis of KTX-582 (HY-148274) and can be used for ADC preparation. KTX-582 is an IRAK4 degrader and inducer of apoptosis with DC50 of 4 nM and 5 nM for IRAK4 and Ikaros, respectively[1].
Curculigoside is the main saponin in C. orchioide, exerts significant antioxidant, anti-osteoporosis, antidepressant and neuroprotection effects. Curculigoside possesses significant anti-arthritic effects in vivo and in vitro via regulation of the JAK/STAT/NF-κB signaling pathway[1].
Azide-PEG5-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Pirimicarb-d6 is the deuterium labeled Diuron. Diuron is a phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (2,500 ppm, dietary) increases the incidence of urinary bladder urothelial carcinomas in male
threo Ifenprodil hemitartrate is a σ receptor agonist, with Kis of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC50=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC 50 of 88 nM, showing antiarrhythmic activity[1][2][3].
S 2101 is a lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.
AA 497 is a bronchodilator[1].
Porphyra 334 is an antioxidative and anti-photoaging agent. Porphyra 334 suppresses ROS production and the expression of MMPs following UVA irradiation[1][2].
AGI-24512 is a methionine adenosyltransferase 2A (MATA2 ) inhibitors useful for treatment of cancer. AGI-24512 blocks growth of MTAP-deleted cancer cells in vitro.
Methyl 2-aminoacetate hydrochloride is a Glycine (HY-Y0966) derivative[1].
TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose[1].
Polyphyllin VI, an active saponin mainly isolated from traditional medicinal plant Paris polyphylla, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis[1][2].
Ac-IHIHIQI-NH2 is a fibril-forming heptapeptide with high catalytic activity to laccase mimics. Ac-IHIHIQI-NH2 exhibits selectivity for hydrophobic p-nitrophenyl (ONp) ester substrates in the process of self-assembly[1][2].
ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM)[1][2].
H-Trp-Trp-Trp-OH is a tripeptide consisting of tryptophan. H-Trp-Trp-Trp-OH has antibacterial activity[1].
3’-Azido-3’-deoxy-5-iodouridine 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].
4-(Methylamino)butanoic acid-d9 hydrochloride is the deuterium labeled 4-(Methylamino)butanoic acid hydrochloride[1].