SKF-34288 hydrochloride (3-Mercaptopicolinic acid) is a phosphoenolpyruvate carboxykinase (PEPCK) inhibitor.SKF-34288 hydrochloride is a potent hypoglycemic agent via inhibition of glucose synthesis through the specific inhibition of PEPCK in the gluconeogenesis pathway[1]. SKF-34288 hydrochloride inhibits Asn metabolism and results in an increase in amino acids and amides[2].
Vidarabine monohydrate is an adenine arabinoside. Vidarabine monohydrate an antiviral drug which is active against herpes simplex viruses (HSV) and varicella zoster viruses[1].
CDK4/6-IN-9 (compound 10) is a selective CDK4/6 inhibitor with an IC50 of 905 nM for CDK6/cyclin D1. CDK4/6-IN-9 has the potential for multiple myeloma (MM) research[1].
Ubiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 can be used to treat disease by blocking the degradation of tumor suppressors[1].
SARS-CoV-2-IN-38 (compound 24) is a SARS-CoV-2 inhibitor with good oral bioavailability in mice (F%=39.75%)[1].
Tubulin polymerization-IN-37 is a tubulin polymerization inhibitor (IC50: 2.3 μΜ). Tubulin polymerization-IN-37 binds to the colchicine site of tubulin and inhibits colchicine binding. Tubulin polymerization-IN-37 can be used in the research of cancers, such as lymphomas[1].
3,29-Dibenzoyl rarounitriol is one major bioactive compound of multiflorane triterpene esters Trichosanthes kirilowii, can be chosen as the marker for quantitation of Trichosanthes kirilowii[1].
Phorbol 12,13-dibutyrate (Phorbol dibutyrate) is a PKC activator and a potent skin tumor promoter[1][2].
Isolongifolene ((-)-Isolongifolene) is a tricyclic sesquiterpene isolated from Murraya koenigii. Isolongifolene attenuates Rotenone-induced oxidative stress, mitochondrial dysfunction and apoptosis through the regulation of P13K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties[1].
Tropanserin is a serotoninergic active compound, as well as a 5HT3 receptor antagonist. Tropanserin modulates Cardio-respiratory reflex effects of an exogenous serotonin challenge[1].
ONC206 is an analogue of TRAIL inducer ONC201[1]. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity[2].
Metallo-beta-lactamase ligand 1 is a class B β-lactamase inhibitor with antibacterial activity extracted from patent WO2019221122A1, compound A[1].
5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine (5'-O-DMT-dU) is a competitive inhibitor of E. coli dUTP nucleotidohydrolase (dUTPase), with the Ki higher than 1000 μM. 5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine can be used in machine-assisted DNA synthesis by synthesizing nucleosidic phosphoramidite blocks[1][2].
Bis-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5-(3-Hydroxybenzylidene)-rhodanine, a derivative of rhodanine, can be used as an algicidal agent[1].
2-Methoxy-3,5-dimethylpyrazine-d3 is the deuterium labeled 2-Methoxy-3,5-dimethylpyrazine[1].
Fazpilodemab (BFKB8488A) is a humanized, agonistic, bispecific antibody targeting fibroblast growth factor receptor 1c (FGFR1c) and Klothoβ. Fazpilodemab can be used for the research of type 2 diabetes mellitus (T2DM) or nonalcoholic fatty liver disease (NAFLD)[1].
BDP FL maleimide is a thiol-reactive dye (Ex: 503 nm; Em: 509 nm). BDP FL maleimide can be used for protein labeling, peptide modification, and can replace fluorescein (FAM) for microscopy[1].
RX-3117(TV-1360; Fluorocyclopentenylcytosine) is novel a cytidine analog; shows anticancer activity in several cancer cell lines, including gemcitabine-resistant variants.IC50 value: 0.4- >30 nM (15 cancer cell lines) [1]Target: cytidine analogin vitro: RX-3117 showed a different sensitivity profile compared to cyclopentenyl-cytosine (CPEC) and azacytidine, substrates for uridine-cytidine-kinase (UCK).RX-3117 was a very poor substrate for cytidine deaminase (66,000-fold less than gemcitabine). In sensitive U937 cells 1 μM RX-3117 resulted in 90% inhibition of RNA synthesis but 100 μM RX-3117 was required in A2780 and CCRF-CEM cells. RX-3117 at IC50 values did not affect the integrity of RNA [1].in vivo: Orally-administered RX-3117 was examined in 9 different human tumor xenograft models (colon, non-small cell lung, small cell lung, pancreatic, renal and cervical), grown subcutaneously in athymic nude mice. In the Colo 205, H460, H69 and CaSki models, gemcitabine treatment resulted in 28%, 30%, 25% and 0% tumor growth inhibition (TGI), respectively, whereas oral treatment with RX-3117 induced 100%, 78%, 62% and 66% TGI, respectively [2].
LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
DOTA tert-Butyl ester is a benxyl derivative of the cyclic tosamide; can be nitrated directly; is more convenient to incorporate the nitro group after deprotection lithium aluminum hydride.
Geranyl pyrophosphate triammonium is a key intermediate in the isoprenoid biosynthesis pathway (IBP). Geranyl pyrophosphate triammonium plays key roles in cellular metabolism and is responsible for the production of both sterol and non-sterol isoprenoids[1][2].
Bixin (BX), isolated from the seeds of Bixa orellana, is a carotenoid, possessing anti-inflammatory, anti-tumor and anti-oxidant activities. Bixin treatment ameliorated cardiac dysfunction through inhibiting fibrosis, inflammation and reactive oxygen species (ROS) generation[1].
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP.
DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
VEGFR-2-IN-25 (compound 5d) is a highly potent VEGFR-2 inhibitor with an IC50 value of 12.1 nM. VEGFR-2-IN-25 can be used for researching anticancer[1].
Boc-D-Asp-OBzl is an aspartic acid derivative[1].
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
Bocodepsin hydrochloride (OKI-179) is an orally active and selective HDAC inhibitor, with antitumor activity. Bocodepsin hydrochloride can be used for suppression on solid tumor and hematologic malignancies[1].
Me-Tet-PEG2-COOH is an ADC Linker containing 2 PEG units. Me-Tet-PEG2-COOH can use its own Tetrazine group to undergo a specific inverse electron demand Diels-Alder reaction (iEDDA) with compounds with TCO groups.