Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity[1].
3’-Deoxy-3’-azido-isocytidine 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].
3'-beta-Azido-2',3'-dideoxyuridine 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].
QR-6401 is an orally active and selective macrocyclic CDK2 inhibitor with IC50 values of 0.37, 10, 22, 34 and 45 nM for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3 and CDK4/D1, respectively. QR-6401 has potent antitumor activity in an OVCAR3 ovarian cancer xenograft model. QR-6401 has the potential to be used in the study of cancer[1].
Guttiferone G inhibits recombinant human SIRT1 and SIRT2 (IC50: 9 and 22 μM, respectively). Guttiferone G is weakly cytotoxic in A2780 human ovarian cell line (IC50: 8.0 μg/mL). Guttiferone G can be isolated from Garcinia macrophylla[1][2].
Triazavirin (Riamilovir sodium dihydrate) is a broad-spectrum antiviral agent targeting influenza viruses, lassa virus, TBEV and Ebola virus; suppresses the replication of influenza virus in cell culture and in chicken chorioallantoic membranes, and protects mice from death caused by type A and B influenza viruses.
5-Iodo-2’-O-methylcytidine is a cytidine nucleoside analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
EIF2α activator 2 (Compound 1) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 2 exhibits high potency in SRB cell proliferation assays (IC50=0.46 μM). EIF2α activator 2 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.79 and 10.52 μM, respectively[1].
Palmitic acid-13C2 is the 13C-labeled Palmitic acid. Palmitic acid is a long-chain saturated fatty acid commonly found in both animals and plants. Palmitic acid can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
3’-Deoxy-3’-fluoro-5-methoxyluridine 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].
5’-O-Triphenylmethyl-2’-deoxyuridine 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].
eIF4A3-IN-14 (compound 51) is a silvestrol (HY-13251) analogue. eIF4A3-IN-14 interferes the assembling of eIF4F translation complex with EC50s of 40 and 50 nM for myc-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-14 can be used for the research of human cancer pathogenesis[1].
2′-Bromo-2′-deoxyuridine 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].
NSC 295642 is a phosphatase inhibitor. NSC 295642 can significantly increase phospho-Erk cytonuclear differences in intact cells. NSC 295642 can be used for the research of cancer[1].
(S)-PERK-IN-5 is the S-enantiomer of PERK-IN-5. (S)-PERK-IN-5 (example 39) is a PERK inhibitor, with an IC50 of 0.101-0.250 μM[1][2].
D8-MMAE is a deuterated labeled MMAE, a potent mitotic inhibitor.
BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC50 of 2 nM.
2'-Deoxypseudoisocytidine is a nucleoside analogue.
T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death[1].
1-(3’-O-[4,4’-dimethoxytrityl]-alpha-L-threofuranosyl)uridine 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].
Dihydrocoumarin is a compound found in Melilotus officinalis. Dihydrocoumarin is a yeast Sir2p inhibitor. Dihydrocoumarin also inhibits human SIRT1 and SIRT2 with IC50s of 208 μM and 295 μM, respectively[1].
2-Iodoacetamide-d4 is the deuterium labeled 2-Iodoacetamide[1]. 2-Iodoacetamide (Iodoacetamide), an alkylating agent, is a commonly used agent for alkylation of cysteine during sample preparation for proteomics[2][3].
2'-OMe-A(Bz) Phosphoramidite is a modified phosphoramidite monomer, which can be used for the oligonucleotide synthesis.
S-MGB-234 is a minor groove binder of Animal African Trypanosomiasis (AAT). S-MGB-234 displays excellent in vitro activities against the principal causative organisms of AAT; Trypanosoma congolense, and Trypanosoma vivax. S-MGB-234 does not show cross-resistance with the current diamidine drugs and are not internalized via the transporters used by diamidines[1].
5’-O-DMTr-5-iodo-2’-dU-3’-CED phosphoramidite 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].
Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response[2]. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner[3]. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells[4].
ETP-46464 is an effective mTOR and ATR inhibitor with IC50s of 0.6 and 14 nM, respectively.
8-Hydroxy-xyloguanosine 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].
2'-Deoxy-5'-O-DMT-5-methylcytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].
Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].