Epigenetic Reader Domain Inhibitor

EML 425 (Standard) is the analytical standard of EML 425 (HY-110263). This product is intended for research and analytical applications. EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC₅₀s of 2.9 and 1.1 μM, respectively.

dBET1 (Standard) is the analytical standard of dBET1 (HY-101838). This product is intended for research and analytical applications. dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker.

PROTAC BET Degrader-1 (Standard) is the analytical standard of PROTAC BET Degrader-1 (HY-103633). This product is intended for research and analytical applications. PROTAC BET Degrader-1 is a BRD2/BRD3/BRD4 PROTAC degrader. PROTAC BET Degrader-1 inhibits the growth of acute leukemia cells. PROTAC BET Degrader-1 is applicable to the research of acute leukemia.

KG-501 (Standard) is the analytical standard of KG-501 (HY-103299). This product is intended for research and analytical applications. KG-501 is a CREB inhibitor, with an IC₅₀ of 6.89 μM.

NVS-CECR2-1 (Standard) is the analytical standard of NVS-CECR2-1 (HY-110374). This product is intended for research and analytical applications. NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC₅₀=47 nM; K_d=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism. NVS-CECR2-1 is a chemical probe.

GNE-272 (Standard) is the analytical standard of GNE-272 (HY-100726). This product is intended for research and analytical applications. GNE-272 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 a selective in vivo probe for CBP/EP300.

Hexamethylene bisacetamide (Standard) is the analytical standard of Hexamethylene bisacetamide. This product is intended for research and analytical applications. Hexamethylene bisacetamide (HMBA) is a differentiation inducer and selective bromine domain inhibitor that can differentiate across the blood-brain barrier. Hexamethylene bisacetamide can induce tumor cell differentiation and inhibit cell proliferation, showing antitumor activity. Hexamethylene bisacetamide induces apoptosis by Notch1, Bcl-2 and p53 signaling pathways. In addition, Hexamethylene bisacetamide improves the obesity phenotype of mice.

RMM23 is an inhibitor targeting PfBDP1 with a K_d value of 1.24 μM. RMM23 against the wild-type strains 3D7 and NF54, and the multidrug-resistant K1 strain in vitro blood stage, with EC₅₀ values of 18 μM, 14 μM, 20 μM, respectively .

(+)-JQ-1 (Standard) is the analytical standard of (+)-JQ-1 (HY-13030). This product is intended for research and analytical applications. (+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.

Alobresib (Standard) is the analytical standard of Alobresib (HY-109050). This product is intended for research and analytical applications. Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.

Inobrodib (Standard) is the analytical standard of Inobrodib (HY-111784). This product is intended for research and analytical applications. Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with K_d values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a K_d of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.

CDD-1147 is a BRDT-BD2 inhibitor with an IC₅₀ of 94 nM. CDD-1147 can be used in the research of non-hormonal contraceptives for men.

AZD5153 (6-Hydroxy-2-naphthoic acid) (Standard) is the analytical standard of AZD5153 (6-Hydroxy-2-naphthoic acid) (HY-100653A). This product is intended for research and analytical applications. AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.

MI-2-2 (Standard) is the analytical standard of MI-2-2 (HY-108350). This product is intended for research and analytical applications. MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (K_d=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation.

BRPF1B/TRIM24-IN-1 (compound 34) is a potent TRIM24/BRPF1/BRPF2 inhibitor, with IC₅₀ values of 0.43, 0.34, 1.75 μM, respectively. BRPF1B/TRIM24-IN-1 binds the TRIM24 bromodomain with a K_D of 222 nM and has a K_D for the BRPF1 bromodomain of 137 nM and for BRD1 of 1130 nM.

TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with K_Ds of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC₅₀ of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026).

CBP/p300-IN-1 (Standard) is the analytical standard of CBP/p300-IN-1 (HY-111420). This product is intended for research and analytical applications. CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor.

EP300/CBP-IN-1 (compound 172) is a potent EP300/CBP inhibitor with IC₅₀s of 2.3 nM and 2.1 nM for CBP BRD and EP300 BRD, respectively. EP300/CBP-IN-1 has the inhibitory effect on the proliferation of prostate cancer CWR22RV1 cells.

SNIPER(BRD)-1 (Standard) is the analytical standard of SNIPER(BRD)-1 (HY-111875). This product is intended for research and analytical applications. SNIPER(BRD)-1 is a SNIPER degrader of BRD4, cIAP1 and XIAP. SNIPER(BRD)-1 has IC₅₀ values of 6.8 nM, 17 nM and 49 nM for cIAP1, cIAP2 and XIAP, respectively. SNIPER(BRD)-1 can be used for cancer research. (Blue: LCL161 (HY-15518); Black: linker (HY-W008005); Pink: (+)-JQ-1 (HY-13030))

GSK6853 (Standard) is the analytical standard of GSK6853 (HY-100220). This product is intended for research and analytical applications. GSK6853, a chemical probe, is a potent and selective inhibitor of the BRPF1 bromodomain. GSK6853 shows excellent BRPF1 potency (pKd = 9.5) and greater than 1600-fold selectivity over all other bromodomains.