Product apis-epigentics

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Catalog	name	Description	price
R-R-2474	I-CBP112 CAS No.1640282-31-0	I-CBP112/CAS No.1640282-31-0 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.	price>
R-R-2475	SGC-iMLLT CAS No.2255338-25-9	SGC-iMLLT/CAS No.2255338-25-9 is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with Kds of 0.129 and 0.077 μM, respectively.	price>
R-R-2476	GNE-272 CAS No.1936428-93-1	GNE-272/CAS No.1936428-93-1 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03, and 13 μM for CBP, EP300, and BRD4, respectively. GNE-272 is also an in vivo selective probe for CBP/EP300.	price>
R-R-2477	GNE-987 CAS No.2417371-71-0	GNE-987/CAS No.2417371-71-0 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).	price>
R-R-2478	MS645 CAS No.2250091-96-2	MS645/CAS No.2250091-96-2 is a bivalent BET bromodomains (BrD) inhibitor with a Ki of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells.	price>
R-R-2479	dBET57 CAS No.1883863-52-2	dBET57/CAS No.1883863-52-2 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4Cereblon E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2.	price>
R-R-2480	ZL0580 CAS No.2377151-10-3	ZL0580/CAS No.2377151-10-3, a structurally close analog of ZL0590, induces epigenetic suppression of HIV via selectively binding to BD1 domain of BRD4. ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter.	price>
R-R-2481	PROTAC BRD4 ligand-1 CAS No.2313230-51-0	PROTAC BRD4 ligand-1/CAS No.2313230-51-0 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT GNE-987 (HY-129937A).	price>
R-R-2482	CBP/p300-IN-12 CAS No.2738688-57-6	CBP/p300-IN-12/CAS No.2738688-57-6 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.	price>
R-R-2483	PF-CBP1 hydrochloride CAS No.2070014-93-4	PF-CBP1 hydrochloride/CAS No.2070014-93-4 is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β, IL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders.	price>

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