| DC29239 |
MC3482 (MC 3482) |
MC3482 is a potent, specific SIRT5 inhibitor, increases the ammonia content in cells leading to autophagy and mitophagy, shows selective SIRT5 inhibition vs SIRT1-3. |
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| DC31037 |
IBET151-Az |
IBET151-Az is a IBET151 derivative for PROTAC synthesis.. |
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| DC31039 |
JQ1-Az |
JQ1-Az is a JQ1 derivative.. |
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| DC31040 |
FT-1101 |
FT-1101 is a potent pan-BET bromodomain inhibitor that displays equipotent inhibition for BRD2, BRD3, BRD4, and BRDT with Kd < 20 nM. |
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| DC31042 |
MM-102 trifluoroacetate |
A high-affinity, small-molecule peptidomimetic inhibitor of MLL1/WDR5 protein-protein interaction with Ki of 2.4 nM. |
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| DC31043 |
PF-CBP1 hydrochloride |
A potent, highly selective inhibitor of the CBP and p300 bromodomains with IC50 of 125 nM and 363 nM, respectively. |
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| DC31053 |
GSK525768A |
GSK525768A is an enantiomer, negative control compound of I-BET762 (GSK525762A), shows no activity against BET family proteins BRD2, BRD3 and BRD4.. |
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| DC31058 |
GSK4027 |
GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe of PCAF/GCN5 bromodomain with pKi of 8.9 for both. |
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| DC31060 |
GSK-340 |
GSK-340 is a potent, selective inhibitor of second bromodomains of the BET family (BD2) with pKd of 8.18, 7.49, 7.72 and 7.68 for BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2, respectively. |
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| DC39097 |
NEO2734
Featured
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NEO2734 (EP31670) is a novel, orally active and selective dual inhibitor of p300/CBP and BET bromodomain with IC50 of both <30 nM. |
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| DC39111 |
Tubastatin A TFA |
Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. |
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| DC40117 |
Tucidinostat D4 |
Tucidinostat D4 (Chidamide D4) is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively. |
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| DC40150 |
MT1 |
MT1 is a bivalent chemical probe of BET bromodomains, with an IC50 of 0.789 nM for BRD4(1). |
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| DC40205 |
TP-238 |
TP-238 is a potent and selective dual CECR2/BPTF probe with pIC50 values of 7.5 and 6.5, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases. |
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| DC40312 |
Nicotinamide riboside tartrate |
Nicotinamide riboside tartrate, an orally active NAD+ precursor, increases NAD+ levels and activates SIRT1 and SIRT3. Nicotinamide riboside tartrate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside tartrate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease. |
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| DC40313 |
Nicotinamide riboside malate |
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. Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease. |
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| DC40462 |
Lys-CoA TFA |
Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation. |
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| DC40525 |
DM-01 |
DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors. |
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| DC40724 |
MS117
Featured
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MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM. |
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| DC40750 |
SIRT-IN-3 |
SIRT-IN-3 is a potent SIRT inhibitor, with an IC50 of 17 μM for SIRT1. SIRT-IN-3 shows about 4-fold and 14-fold selectivity for SIRT1 over SIRT2 and SIRT3, respectively (IC50 of 74 μM and 235 μM for SIRT2 and SIRT3, respectively). |
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| DC40782 |
SIRT7 inhibitor 97491
Featured
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SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway.. |
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| DC40845 |
UNC2399 |
UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM. |
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| DC40849 |
SIRT1-IN-1
Featured
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SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC50 of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC50 of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity. |
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| DC40874 |
CPI-1612 |
CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity. |
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| DC40900 |
MI-3454 |
MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis. |
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| DC41019 |
CBP/P300 bromodomain inhibitor-3 |
CBP/P300 bromodomain inhibitor-3 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/P300 bromodomain inhibitor-3 inhibits CBP (IC50=0.01-0.1 μΜ) and BRD4 (IC50=1-1000 μΜ) activity. |
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| DC41049 |
Trotabresib (CC-90010)
Featured
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Trotabresib (CC-90010) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors. |
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| DC41094 |
UNC926 hydrochloride |
UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC50 of 3.9 μM. |
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| DC41114 |
AMI-1 free acid |
AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding. |
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| DC41319 |
Psammaplin A |
Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity. |
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