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Epigenetics

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Cat. No. Product Name Field of Application Chemical Structure
DC71317 2,4-PDCA
2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-PDCA is a target chemical in the field of bio-based plastics.
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DC71315 DS17701585
DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.040, 0.15, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. DS17701585 can be used for cancer research.
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DC71314 HC-Toxin
HC-Toxin, a cyclic tetrapeptide, is a potent HDAC inhibitor with an IC50 of 30 nM. HC-Toxin induces tumor cell apoptosis and has anticancer effects.
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DC7562 MM-102 Featured
MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM.
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DC9293 MS023 Featured
MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM.
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DC7682 MS417 Featured
MS417 is a novel BrD inhibitor with high affinity and specificity For the BrDs of BET proteins. pIC50 7.52 (IC50 30 nM).
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DC8823 XY1 Featured
Negative control of SGC 707. Exhibits >3000-fold lower potency (IC50 >100 μM) compared to the active analog.
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DC9758 NI-57 Featured
NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry.
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DC1109 PCI-34051 Featured
PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM.
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DC11256 OTS193320 Featured
OTS193320 (OTS-193320) is a potent inhibitor of protein methyltransferase SUV39H2 with IC50 of 22.2 nM.
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DC8291 PFI-4 Featured
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM).
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DC8661 Pimelic Diphenylamide 106(TC-H 106) Featured
Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs.
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DC10786 PLX51107 Featured
PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation.
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DC71230 SDR-04
SDR-04 is a BET inhibitor and exhibits strong BRD4-BD1 affinity and inhibition activity. SDR-04 potently suppresses MV4;11 cancer cell line proliferation.
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DC71179 GEM144
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts.
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DC71108 RSC133
RSC133 exhibits dual activity by inhibiting histone deacetylase and DNA methyltransferase. RSC133 effectively facilitates reprogramming of human somatic cells to pluripotent stem cells and supports the maintenance of an undifferentiated state of human pluripotent stem cells.
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DC71077 MAK683 hydrochloride
MAK683 hydrochloride is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay.
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DC71069 JPS036
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
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DC71068 JPS035
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
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DC71067 JPS016
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
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DC71066 JPS014
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
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DC71021 Coumarin-SAHA
Coumarin-SAHA is a fluorescent probe for determining the binding affinities (kd) and the dissociation off-rates (koff) of the HDAC8-inhibitor complexes.
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DC70995 2-Hexyl-4-pentynoic acid
2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), valproic acid (VPA) derivative, exhibits potential roles of HDAC inhibition (IC50=13 µM) and HSP70 induction. Potent neuroprotective effects. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons.
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DC70993 2′,3′,5′-Triacetyl-5-azacytidine
2′,3′,5′-Triacetyl-5-azacytidine is an orally active prodrug of 5-Azacytidine. 5-Azacytidine is an inhibitor of DNA methyltransferase.
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DC70972 MI-1
MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM.
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DC70945 [18F]-NT160
[18F]-NT160, a Florbetapir (18F)-radiolabeled NT160, is a diagnostic tool for positron emission tomography (PET). NT160 is a brain-penetrant and selective class-IIa HDAC inhibitor with an IC50 of 46 nM. NT160 exhibits a remarkably high inhibition against HDAC4, HDAC5, HDAC7, and HDAC9 with IC50s of 0.08 nM, 1.2 nM, 1.0 nM, and 0.9 nM, respectively.
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DC8654 PTACH (NCH-51) Featured
PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDAC. PTACH exerts potent growth inhibition against various human cancer cells, with EC50 values ranging from 1 to 10 μM.
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DC7795 RG2833 (RGFP109) Featured
RG2833 is a brain-penetrant inhibitor of HDAC with IC50 values of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.
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DC10002 Salermide Featured
Salermide is an inhibitor of SIRT1 and SIRT2, causing tumor-specific apoptotic cell death. In MOLT4 leukemia cells, salermide causes 90% apoptosis within 72 hours (IC50 ~ 20 μM) by reactivating proapototic genes that are repressed by SIRT1.
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DC10429 SGC2085 Featured
SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM.
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