ginsenoside-Rb1 BDBM50317541 Ginsenoside Rb1 CHEMBL501515
ginsenoside-Rb3 CHEMBL507688 BDBM50317540 ginsenoside Rb3
ginsenoside-Rd CHEMBL473659 Ginsenoside Rd BDBM50317539
CHEBI:77147 BDBM50023457 Ginsenoside Rh2 20(S)-Ginsenoside
BDBM50023447 Ginsenoside Rh1
BDBM50317538 CHEMBL1095007 Ginsenoside F2
CHEMBL1095004 BDBM50317544 Ginsenoside F3
Ginsenoside Rb2 CHEBI:77152 BDBM50450908
20(R)-Ginsenoside Rg2 CHEMBL1095006 BDBM50317542
20(S)-Ginsenoside Rg2 CHEMBL1095005 BDBM50317543
20(S)-ginsenoside Rg3 BDBM50317537 CHEMBL398412
CHEMBL1095008 BDBM50317536 20(R)-Ginsenoside Rg3
CHEMBL1783835 20(R)-Ginsenoside BDBM50023450 CVD-0019899
- Fatmawati, S; Ersam, T; Yu, H; Zhang, C; Jin, F; Shimizu, K 20(S)-Ginsenoside Rh2 as aldose reductase inhibitor from Panax ginseng. Bioorg Med Chem Lett 24: 4407-9 (2014)
- Teng, J; Chen, Y; Xiao, S; Li, T; Su, G; Wang, G; Zhao, Y Novel ginsenoside derivatives induce apoptosis in HepG-2 cells via the MDM2-p53 signaling pathway. Bioorg Med Chem Lett 78: (2022)
- ChEMBL_2276753 Inhibition of RB1 phosphorylation in human OVCAR-3 cells assessed as reduction in phosphorylation at Serine 807/811 residue incubated for 1 hr by ELISA
- CDKi Biochemical Assay Biochemical assays measured the inhibitory effects of compounds in this disclosure on the enzymatic activity of CDK enzyme in complex with Cyclin protein partner by phosphorylation of Ser-780 (S780) on retinoblastoma protein peptide (RB1) in the presence of 1 mM adenosime-5-triphosphate (ATP) and varying concentration of test compound in 20 mM 2-[4-(2-hydroxyethyl)paperazin-1-yl] ethanesulfonic acid (HEPES), pH 7.5, 10 mM MgCl2, 1 mM dithiothreitol (DTT), 0.01% bovine serum albumin (BSA), 0.005% Tween 20. Total Reaction volume of 10 μL proceeded for 60 minutes at room temperature (25° C.) and were quenched with 5 μL of 200 mM 2′,2″,2′″-(Ethane-1,2-diyldinitrilo)tetraacetic acid (EDTA) pH 8.0 before addition of 5 μL detection solution containing 100 nM fluorophore conjugate streptavidin allophycocyanin (SA-APC), 2 nM Europium labelled Anti-p-RB(S780)-K (Perkin Elmer, 64CUSKAY), 50 mM HEPES, pH 7.5, 400 mM potassium fluoride (KF), 0.1% BSA, and 0.01% Tween-20. Phosphorylation of S780 on RB1 peptide (His-MBP-RB1[773-924]-SEQ ID NO. 9) was detected by TR-FRET after 3 hour incubation with detection solution. Percent phosphorylation activity was plotted against log concentration of compound to generate an apparent ICSO. The following CDK enzyme in complex with different cyclin proteins and protein peptide substrate were used in these assays: CDK1/CyclinB1, Avi-tag, 10 pM used in the assay CDK2/CyclinE1, Avi-tag, 100 pM used in the assay CDK4/cyclinD1, Avi-tag, 20 pM used in the assay CDK6/cyclinD3, Avi-tag, 10 pM used in the assay His-MBP-RB1[773-924], Avi-tag, 200 nM used in the assay