(25R)-Ruscogenin-3-yl α-L-rhamnopyranosyl-(1→2)-[β-D-xylopyranosyl-(1→4)]-β-D-glucopyranoside (compound 1) is a steroidal saponin , can be isolated from the roots of Ophiopogon japonicus[1].
Boc-N-PEG5-C2-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
A small molecule inhibitor of HECT-type ubiquitin ligase with IC50 of 6.8/6.3/6.9 uM for Smurf2/Nedd4/WWP1, respectively; does not block E2 binding but causes a conformational change that results in oxidation of the active site Cys; is active against a range of HECT ligases but does not perturb the ubiquitin system more generally.
H-Thr-Arg-OH is a biologically active peptide.
INH154 is a highly potent inhibitor for Nek2 and Hec1 binding (INH), with IC50s of 200 nM and 120 nM for INH in Hela and MB468 cells.
A1AR antagonist 5 (compound 20) is a potent and selective A1AR (A1 adenosine receptor) antagonist, with a pIC50 of 5.83 and a pKi of 6.11[1].
Veratraldehyde is an important chemical used in perfumery, agrochemical, and pharmaceutical industries.
Pyridoxine is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
Epirosmanol is a nature diterpene lactone from S. officinalis. Epirosmanol shows anti-cancer activity and inhibits melanin biosynthesis against melanoma cells. Epirosmanol also exhibits DPPH radical scavenging activity[1][2].
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range[1][2][3].
4-Methoxybenzimidamide is a reagent used for the determination of reducing carbohydrates and glycoproteins.
Boc-D-Ala(3,3-diphenyl)-OH is a phenylalanine derivative[1].
Bis-(N,N'-PEG4-NHS ester)-Cy5 is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
N2-iso-Butyroyl-2’-fluoro-2’-deoxyarabinoguanosine 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].
JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders[1][2].
MBP146-78 is a potent and selective inhibitor of cGMP dependent protein kinases.
Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor[1][2][3].
EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259)[1].
TMV-IN-5 (compound 1a) is an anti-plant virus/fungal agent. TMV-IN-5 inhibits viral assembly by binding to tobacco mosaic virus (TMV) CP. TMV-IN-5 can be used in the development of pesticides[1].
VP-4556 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. VP-4556 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 8 µg/mL. VP-4556 inhibits the growth of methicillin‐resistant Staphylococcus aureus with growth inhibition >95%[1].
SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM.IC50 value: 31 nMTarget: PRMT3in vitro: SGC707 is the first PRMT3 chemical probe. SGC707 is a potent PRMT3 inhibitor (IC50=31±2 nM, KD=53±2 nM) with outstanding selectivity (selective against 31 other methyltransferases and more than 250 non-epigenetic targets). SGC707 can engage PRMT3 and effectively inhibit its catalytic activity in cells and that overexpressed PRMT3 can methylate histone H4 in cells. SGC707 stabilizes PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM in PRMT3 InCELL Hunter Assays.in vivo: SGC707 is bioavailable and suitable for animal studies. This well characterized chemical probe is an excellent tool to further study the role of PRMT3 in health and disease. We assessed in vivo pharmacokinetic (PK) properties of SGC707. Intraperitoneal injection of SGC707 at 30 mg/kg gave good plasma exposure in CD-1 male mice over 6 h with the peak plasma level of 38000 nM. The plasma level of SGC707 at 6 h post injection was 208 nM, more than 2-fold higher than its IC50 value in the cellular assay and the half-life of SGC707 was about 1 h. This mdose was well tolerated by the test animals. These results suggest that SGC707 is suitable for animal studies in addition to cell-based studies.
(-)-Sesamin isolated from Asarum forbesii Maxim, is an isomer of Sesamin. Sesamin is a potent and selective delta 5 desaturase inhibitor in polyunsaturated fatty acid biosynthesis[1][2].
Artemisinic acid (Qing Hao acid), an amorphane sesquiterpene isolated from Artemisia annua L., possesses a variety of pharmacological activity, such as antimalarial activity, anti-tumor activity, antipyretic effect, antibacterial activity, allelopathy effect and anti-adipogenesis effect[1].
Ala-Ala-Ala-Tyr-Gly-Gly-Phe-Met
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively[1].
Verrucosin (Compound 3) is a compound isolated from Myristica fragrans[1].
RORγt/DHODH-IN-2 (compound 1) is a potent dual RORγt/DHODH inhibitor. RORγt/DHODH-IN-2 can be used for inflammatory bowel disease (IBD) research[1].
cis-Nerolidol is a sesquiterpene alcohol that can be found in various plants. cis-Nerolidol exhibits antioxidant and antibacterial activities. cis-Nerolidol can also potentiate the action of antibiotics[1].
eIF4A3-IN-16 (compound 60) is a silvestrol (HY-13251) analogue. eIF4A3-IN-16 interferes the assembling of eIF4F translation complex with EC50s of 1, 30 and 1 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-16 can be used for the research of human cancer pathogenesis[1].
Clothiapine, an atypical antipsychotic agent, shares with clozapine its strong antiserotonergic properties[1].