Niraparib (MK-4827) is a highly potent PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively.
UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.IC50 Value: 120 nM (Kd) [1]Target: L3MBTL3 In vitro: UNC1215 binds L3MBTL3 with a K(d) of 120 nM, competitively displacing mono- or dimethyllysine-containing peptides, and is greater than 50-fold more potent toward L3MBTL3 than other members of the MBT family while also demonstrating selectivity against more than 200 other reader domains examined. X-ray crystallography identified a unique 2:2 polyvalent mode of interaction between UNC1215 and L3MBTL3. In cells, UNC1215 is nontoxic and directly binds L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutants that disrupt the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization [1].
E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent[1][2].
MIR96-IN-1 selectively inhibits biogenesis of microRNA-96, upregulating a protein target (FOXO1) and inducing apoptosis in cancer cells.Target: microRNA-96in vitro: MIR96-IN-1 inhibits biogenesis of its target precursor miRNA to varying extents : MIR96-IN-1 reduces the expression level of miR-96 by 90% at 40 μM. MIR96-IN-1 efficiently and selectively silences production of miR-96 at 40 μM while not affecting miR-182 or -183. Moreover, MIR96-IN-1 inhibits Drosha cleavage of pri-miR-96, as evidenced by an increase in the levels of pri-miR-96 and a reduction in levels of pre- and mature miR-96 in treated cells, as expected if MIR96-IN-1 binds to the Drosha site. [1]
UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.IC50 value: 63 pM(Ki); 9 nM (ECSD assay) [1]Target: G9aIt was found that replacing the 5-carbon chain in compound 13 with an ethoxyethyl chain resulted in compound 29{UNC0321} (IC50 = 6 nM (CLOT) and 9 nM (ECSD)), the most potent G9a inhibitor to date. 29 had a Morrison Ki of 63 pM and was about 40-fold more potent than 10 (Morrison Ki = 2.6 nM) and 250-fold more potent than 3a (Morrison Ki = 16 nM) in this G9a assay. UNC0321 potentially useful small molecule tools for the biomedical research community to investigate the biology of G9a and its role in chromatin remodeling as well as PTMs of other proteins.
TNKS-2-IN-2 is a potent and selective inhibitor of TNKS2 with an IC50 of 22 nM[1].
SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5 > 300 μM), and is more potent than Resveratrol and the closest sirtuin homologues[1].
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo[1][2].
EZH2-IN-15 (SHR2554) is a EZH2 inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors[1].
EN884 is a BRD4 degrader via a SKP1- and proteasome-dependent manner. EN884 can be used in synthetic proteolysis targeting chimeras (PROTACs)[1].
Nicotinamide Hydrochloride is a form of vitamin B3 or niacin that inhibits sirtuin 2 (SIRT2) activity in vitro, with an EC50 of 2 μM. Nicotinamide Hydrochloride inhibits up to 90% melanoma cell number and increases cellular NAD+, ATP, ROS levels. Nicotinamide Hydrochloride inhibts tumor growth in vivo and improves survival of melanoma-bearing mice, which can be used for the research of skin cancers such as melanoma[1].
DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
PF-03814735 is a potent, orally available and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
5-Heptadecylresorcinol (AR-C17), a phenolic lipid component, is also an orally active mitochondrial protector. 5-Heptadecylresorcinol improves mitochondrial function via sirtuin3 signaling pathway, thus alleviates endothelial cell damage and apoptosis. 5-Heptadecylresorcinol induces sirtuin3-mediated autophagy. 5-Heptadecylresorcinol reduces the atherosclerotic plaques in the aortic root region of mice heart. 5-Heptadecylresorcinol can be used for research of atherosclerosis prevention and obesity[1][2].
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].
Venadaparib (IDX-1197) hydrochloride is a potent and selective PARP inhibitor with anticancer activities. Venadaparib hydrochloride can be used for solid tumors research[1][2].
GS-626510 is a potent, and orally bioavailable BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively[1].
SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM[1]. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels[2].
CGP60474 is a potent VEGFR-2 inhibitor, with an IC50 of 84 nM, and also an ATP-competitive PKC inhibitor.
I-BET151 is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
AMPK-α1β1γ1 activator 1 (M1) is an acyl glucuronide metabolite of Indole-3-carboxylic Acid-based AMPK activator. AMPK-α1β1γ1 activator 1 can selectively activated human β1 isoforms with an EC50 value of 38.1nM. AMPK-α1β1γ1 activator 1 can direct binding with human AMPK α1β1γ1 isoform. AMPK-α1β1γ1 activator 1 can be used for the research of diabetic nephropathy[1].
Guadecitabine (SGI-110) is a DNA methyltransferases (DNMT) inhibitor.
AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
Nicotinamide riboside malate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities[1]. Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease[2].
MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].
Platycodin D is a saponin isolated from Platycodi Radix, acts as an activator of AMPKα, with anti-obesity property[1].
2-(3-Hydroxypicolinamido)acetic acid is a 2OG oxygenase inhibitor with an IC50 value of 3.4 μM. 2-(3-Hydroxypicolinamido)acetic acid can be used as a functional probe for potential therapeutic research[1].
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM[1].