| DC70865 |
UHRF1 PHD inhibitor MLD4
Featured
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UHRF1 PHD inhibitor MLD4 is a specific compound that selectively inhibits the UHRF1-histone interaction (IC50=12.4 uM), targets the PHD finger of UHRF1, specifically disrupting histone H3 arginine 2 interactions with the PHD finger.UHRF1 PHD inhibitor MLD4 inhibited binding between H3K9me3(FAM) and UHRF1 with IC50 of 24-26 uM, displace UHRF1-histone H3 binding in cells. |
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| DC70866 |
UHRF1 PHD inhibitor MLD5 |
UHRF1 PHD inhibitor MLD5 is a specific compound that selectively inhibits the UHRF1-histone interaction (IC50=7.4 uM), targets the PHD finger of UHRF1, specifically disrupting histone H3 arginine 2 interactions with the PHD finger.UHRF1 PHD inhibitor MLD5 inhibited binding between H3K9me3(FAM) and UHRF1 with IC50 of 24-26 uM, displace UHRF1-histone H3 binding in cells. |
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| DC70868 |
UM-002 |
UM-002 is a highly potent, selective, brain penetrant BRD4 bromodomain inhibitor with IC50 of 8.8 and 2.4 nM for BRD4-1 and BRD4-2, respectively.UM-002 is more potent than JQ1 at inhibiting BRD2-1, BRD4-1, and BRD4-2.UM-002 reduces GBM cell proliferation more than JQ1, or the brain penetrant BET inhibitor MK-8628.UM-002 not affect the enzymatic activity of histone deacetylases, histone acetyltransferases.UM-002 inhibits GBM cell proliferation in vitro with EC50 of 0.13 and 0.24 uM for GBM22 cells and GBM39 cells, repectively.UM-002 reduces proliferation of GBM cells co-cultured with cerebral brain organoids, reduces the expression of cell-cycle related genes in vivo and reduces the expression of invasion related genes within the non-proliferative cells present in tumors. |
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| DC70902 |
WDR5 inhibitor 41 |
WDR5 inhibitor 41 is a potent, selective and orally bioavailable WDR5 WIN-site inhibitor with TR-FRET Ki value of <0.02 nM, inhibits cell proliferation of MV4:11 and MOLM-13 with IC50 of 13 and 27 nM, respectively.WDR5 inhibitor 41 is well tolerated in mice by both iv and po dosing and showed no clinical sign of abnormalities suggesting an enhanced safetyprofile for the series. |
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| DC70911 |
XP-524 |
XP-524 (XL-223, XP524) is a potent, dual-BET/EP300 inhibitor, inhibits BRD4-BD (IC50=5.8 nM) and BRD4-BD2 (IC50=1.5 nM).XP-524 binds strongly to and inhibits EP300 and CBP proteins with IC50 of 28 and 116 nM, respectively.XP-524 (XL-223) showed high potency and selectivity (Kd < 1 nM) across BET family proteins. Selectivity for BRD proteins over all other bromodomain proteins was >400-fold.XP-524 significantly decreased expression of Myc pathway oncogenes such as c-MYC and n-MYC, increased expression of CDKN1B, a tumor suppressor that prevents the activation of the cyclin-D/CDK4 complex, and also reduced expression of cyclin-D (CCND1) itself.XP-524 showed increased potency and superior tumoricidal activity than the benchmark BET inhibitor JQ-1 in vitro, with comparable efficacy to higher-dose JQ-1 combined with the EP300/CBP inhibitor SGC-CBP30.XP-524 prevented KRAS-induced, neoplastic transformation in vivo and extended survival in two transgenic mouse models of aggressive PDAC. |
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| DC70912 |
XY153 |
XY153 is a potent, BD2-selective BET inhibitor with IC50 of 0.79 nM for BRD4 BD2, 354-fold selectivity over BRD4 BD1.XY153 displays 6-fold BRD4 BD2 domain selectivity over other BET BD2 domains.XY153 displayed potent antiproliferative activity against multiple tumor cell lines, especially MV4-11 (IC50=0.55 nM), also demonstrated good metabolic stability in vitro. |
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| DC70913 |
YC8-02 |
YC8-02 is a small molecule mitochondrial-targeting SIRT3 inhibitor with IC50 of 0.53 uM.YC8-02 inhibits SIRT1 and SIRT2 with IC50 of 2.8 and 0.062 uM in in vitro biochemical assays.YC8-02 manifested increased ratio of mitochondria to total cell concentration, as measured by mass spectrometry in purified mitochondria extracts and total cell lysates.YC8-02 increased mitochondrial protein acetylation, inhibited GDH activity and induced autophagy in DLBCL cells.YC8-02 could phenocopy the effects of SIRT3 depletion.YC8-02 (30 mg/kg) caused regression of the tumors in DLBCL xenografts, with no evidence of discomfort or weight loss. |
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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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| DC70972 |
MI-1 |
MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 μM. |
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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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| 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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| 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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| 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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| 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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| 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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| 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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| 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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| 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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| 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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| 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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| 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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| 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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| DC71316 |
MC2652
Featured
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MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells. |
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| 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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| DC71318 |
YM458 |
YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer. |
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| DC71319 |
OXFBD02 |
OXF BD 02 is a selective inhibitor of BRD4(1) (the first bromodomain of BRD4) with IC50
value of 382 nM. |
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| DC71320 |
(2S,3R)-LP99 |
(2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion. |
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| DC71321 |
ET-JQ1-OH
Featured
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ET-JQ1-OH is an allele-specific BET inhibitor. |
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| DC71501 |
S1427 |
S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC50 of 390 nM and Ki of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells. |
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| DC71502 |
FY-56 |
FY-56 is a highly potent and selective LSD1/KDM1A inhibitor (IC50=42 nM) and exhibits high selectivity over MAO-A/B. FY-56 induces differentiation of MOLM-13 and MV4-11 cell and has the potential for AML research. |
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