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Epigenetics

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Cat. No. Product Name Field of Application Chemical Structure
DC80359 C11-BODIPY 505/515 Ceramide-1-phosphate ammonium
C11-BODIPY 505/515 Ceramide-1-phosphate ammonium is a C11-BODIPY 505/515-labeled ceramide-1-phosphate ammonium that can be used to prepare lipid nanoparticles for drug delivery (Ex/Em = 505/515 nm).
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DC80358 BYBC-1
BYBC‑1 is a selective G4‑RNA‑targeting ligand with high affinity forKRAS and NRAS G4‑RNAs (Kd = 0.05-0.28 μM). BYBC‑1 stabilizes G4‑RNA structures in KRAS and NRAS mRNA, blocks thePI3K/AKT and MAPK/ERK pathways, activates the DNA damage response (DDR), suppresses energy metabolism, and induces S‑phase arrest and apoptosis. BYBC‑1 exhibits high selectivity over non‑malignant fibroblasts and significantly inhibits the growth of HCT‑116 xenograft tumors in vivo. BYBC‑1 can be used for the study of colorectal cancer.
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DC80319 BLT1-IN-1
BLT1-IN-1 is an orally active and selective BLT1 inhibitor with an IC50 of 8.7 nM and a Kd of 121 nM. BLT1-IN-1 exerts protective effects against acute lung injury and sepsis in in vivo models. BLT1-IN-1 can be used in research related to acute lung injury and sepsis.
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DC80302 Bentioflumin
Bentioflumin is a fluoroalkylthiobenzene acaricide with excellent leaf penetration, and its control validity period against mites exceeds 25 days. Bentioflumin can be used in studies related to mite infestation.
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DC80196 AMPK activator 18
AMPK activator 18 is a potent allosteric activator of AMPK complexes containing the β2 isoform. AMPK activator 18activates α2-containing AMPK α2β2γ1 and α2β2γ3 complexes, with EC50 values of 17.2 and 82.1 nM. AMPK activator 18 stimulates β2-AMPK in cells, and glucose uptake by isolated skeletal muscle. AMPK activator 18 induces acetyl-coenzyme A carboxylase (ACC) and AMPK α-T172 phosphorylation. AMPK activator 18 can be used for the research of type 2 diabetes.
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DC80174 AL-38022A
AL-38022A is a potent and selective 5-HT2 receptor agonist (Ki ≤2.2 nM), but a significantly lower (>100-fold less) affinity for other 5-HT receptors. AL-38022A potently stimulates functional responses via 5-HT2 receptor subtypes including [Ca2+]i mobilization and tissue contractions with apparently similar potencies and intrinsic activities. AL-38022A fully generalizes to the (±)-1-(2,5-dimethoxy 4-methylphenyl)-2-aminopropane hydrochloride (DOM) stimulus in drug discrimination paradigms. AL-38022A can be used for the glaucoma research.
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DC79946 1,2-Linolein-3-caprylin
1,2-Linolein-3-caprylin is an acylglycerol.
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DC77830 PB94
PB94 is a potent and selective inhibitor of HDAC11 with an IC50 of 108 nM and exhibits >40-fold selectivity over other HDAC isoforms. It ameliorates neuropathic pain in mouse models and can be radiolabeled with carbon-11 as [¹¹C]this compound for PET imaging, demonstrating significant brain uptake and potential for in vivo imaging applications.
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DC77829 SKLB-11A
SKLB-11A is a selective, first-in-class allosteric activator of SIRT3 that binds with a Kd of 4.7 μM and enhances its deacetylase activity with EC50 of 21.95 μM. It improves cardiac function and alleviates myocardial damage in vivo.
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DC73354 MDL-811 Featured
MDL-811 (MDL811) is a potent, selective and allosteric SIRT6 activator with EC50 of 5.7 uM (activated SIRT6 deacetylation), two-fold greater activity than MDL-800 (EC50=12.3 uM, Cat# 35760).
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DC5147 Molibresib(I-BET-762) Featured
GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4).
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DC70537 KDOBA67 Featured
KDOBA67 is a novel cell-permeable inhibitor of H3K27 lysine demethylase KDM6A/B, inhibits TBXT expression chordoma cell lines.KDOBA67 displayed in vitro inhibitory activity in the low micromolar range with IC50 values of 2 to 5 uM in various chordoma cell lines, leading to induction of apoptosis.H3K27 demethylase inhibition via KDOBA67 alters chromatin state at TBXT and inhibits its expression.TBXT was a KDM6A/B target gene, and chromatin changes at TBXT following KDOBA67 treatment were associated with a reduction in TBXT protein levels.KDOBA67 treatment downregulated expression of a network of transcription factors critical for chordoma survival and upregulated pathways dominated by ATF4-driven stress and proapoptotic responses.
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DC11041 QCA276 Featured
QCA276 is a novel potent BET proteins inhibitor with IC50/Ki of 10/.3 nM, QCA276 is the BET ligand for PROTAC QCA570.
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DC8293 UNC0224 Featured
UNC-0224 is a potent inhibitor of G9a histone lysine methyltransferase (IC50 = 15 nM).
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DC7658 C646 Featured
C646 is an inhibitor for histone acetyltransferase, and inhibits p300 with a Ki of 400 nM. Preferentially selective for p300 versus other acetyltransferases.
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DC10656 (+)-JQ1 carboxylic acid Featured
(+)-JQ1 carboxylic acid is the carboxylic acid form of (+)-JQ1 for derivative synthesis.
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DC7143 GSK-343 Featured
GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.
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DC71504 Thalidomide-NH-C4-NH-Boc Featured
Thalidomide-NH-C4-NH-Boc is a novel, potent, and selective class of Bromodomain-containing protein 4 (BRD4) and Bromodomain-containing protein 2 (BRD2) degrader for the development of therapeutics to treat cancers.
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DC8261 (-)-JQ-1 Featured
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains,it is the negative control of +JQ-1.
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DC5019 (+)-JQ1 Featured
(+)-JQ1 is a BET bromodomain inhibitor, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family.
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DC12024 ARV-825 Featured
ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
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DC73285 GSK-3484862(GSK862) Featured
GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity.
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DC9724 BI-7273 Featured
BI-7273 is a potent, selective, and cell-permeable BRD9 BD Inhibitor.
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DC28688 UNC6852 Featured
UNC6852 is a selective rolycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a VHL ligand, with an IC50 of 247 nM for EED.
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DC79850 DW34
DW34 is an orally active pan-BRD4-D1 biased inhibitor with additional BRD4-D2 inhibitive activity. DW34 displays comparable inhibitive efficacy to I-BET151 (EC50 = 0.16 μM) with low nanomolar EC50 values of 0.14 μM. DW34 significantly reduces liver inflammation induced by LPS and APAP via reducing chemokine expression and cellular necrosis.
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DC79811 (2R,4R,6S)-Tubacin
(2R,4R,6S)-Tubacin is the 2R,4R,6S enantiomer of Tubacin. Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1. Tubacin also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).
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DC79682 rel-A-395 hydrochloride
rel-A-395 hydrochloride is the relative configuration of A-395) hydrochloride. A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
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DC79522 TAF1 ligand 1
TAF1 ligand 1 is a TAF1 ligand. TAF1 ligand 1 can be used as a Ligands for Target Protein for PROTAC synthesis, such as ZS3-046.
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DC79518 Repibresib
Repibresib (VYN201) is a bromodomain and extra-terminal motif (BET) inhibitor. Repibresib shows antineoplastic activity.
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DC79506 KB-0118
KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.
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