CBP/p300 Degrader
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JET-209
0 ImagesJET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia.
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QC-182
0 ImagesQC-182 is a p300/CBP PROTAC degrader with a DC50 of 93 nM against p300. QC-182 induces ubiquitination and proteasomal degradation of p300 and CBP in a CRBN-dependent manner. QC-182 induces Apoptosis. QC-182 exhibits anticancer activity against liver cancer cells. QC-182 can be used for the research of hepatocellular carcinoma.
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MJP6412
0 ImagesCat. No.: HY-168201CAS No.: 3105406-14-9MJP6412 is a p300 and CBP PROTAC degrader that potently degrades p300 and CBP in 22Rv1 cells with DC50 values of 1.6 nM and 1.2 nM, respectively. MJP6412 downregulates the expression of AR-FL, AR-V7 and c-MYC, as well as androgen receptor target genes (KLK3, FKBP5, TMPRSS2). MJP6412 completely abolishes p300/CBP-dependent histone acetylation (H3K27Ac and H2BNTAC) and induces G1 cell cycle arrest. MJP6412 inhibits cancer cell proliferation and tumor growth. MJP6412 can be used in prostate cancer-related research.
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PROTAC CBP/p300/BRD4 Degrader-1
0 ImagesCat. No.: HY-181758CAS No.: 3109024-12-3PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader with DC50 values of 8.8 pM (BRD4), 6.55 nM (CBP), and 1.05 nM (p300). PROTAC CBP/p300/BRD4 Degrader-1 induces CRBN- and proteasome-dependent degradation of BRD4 and CBP/p300, downregulates c-Myc and acetyl-H3K27, induces apoptosis. PROTAC CBP/p300/BRD4 Degrader-1 acts as an antiproliferative and antitumor agent, induces tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 can be used for the research of prostate cancer and colorectal cancer.
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PROTAC CBP/P300 Degrader-4
0 ImagesCat. No.: HY-183802PROTAC CBP/P300 Degrader-4 is a p300/CBP PROTAC degrader with DC50 of 17.4 nM and 10.2 nM against p300 and CBP in U2OS cells, respectively. PROTAC CBP/P300 Degrader-4 forms ternary complexes with p300 or CBP and an E3 ligase, drives ubiquitination, and mediates proteasomal degradation. PROTAC CBP/P300 Degrader-4 can be used for the research of hematological malignancies.
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PROTAC CBP/EP300 degrader-1
0 ImagesCat. No.: HY-184453PROTAC CBP/EP300 Degrader-5 is a CBP and EP300 PROTAC degrader. PROTAC CBP/EP300 Degrader-5 relies on the ubiquitin-proteasome pathway to preferentially induce ubiquitination and degradation of EP300 rather than CBP. PROTAC CBP/EP300 Degrader-5 induces G1 phase cell cycle arrest and triggers Apoptosis. PROTAC CBP/EP300 Degrader-5 is applicable to research related to EP300-dependent malignant tumors.
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dCBP-30
0 ImagesCat. No.: HY-184556dCBP-30 is an orally active, selective and dual-acting CBP/p300 PROTAC degrader with DC50 values of 0.05 nM (CBP) and 0.04 nM (p300), respectively. dCBP-30 reduces the acetylation levels of histone substrates H3K27, H3K18, H2BK5 and H2BK20, downregulates multiple myeloma-specific dependency programs, and induces multiple myeloma cell apoptosis. dCBP-30 triggers tumor regression and prolongs survival in multiple myeloma xenograft mouse models, and exhibits synergistic antiproliferative activity with dexamethasone. dCBP-30 can be used for the research of multiple myeloma.
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XYD129
0 ImagesCat. No.: HY-161710XYD129 is a CBP/p300 PROTAC degrader. XYD129 potently binds to CBP, p300 and CRBN proteins, with IC50 values of 0.021 μM, 0.03 μM and 0.18 μM, respectively. XYD129 forms a ternary CRBN-CBP/p300 complex and induces CBP/p300 degradation via the ubiquitin-proteasome system. XYD129 inhibits tumor growth and suppresses the proliferation of acute myeloid leukemia cells. XYD129 can be used in studies related to acute myeloid leukemia.
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Pomalidomide-NH-PEG6-amide-C2-CPI-1612
0 ImagesCat. No.: HY-161250Pomalidomide-NH-PEG6-amide-C2-CPI-1612 is a CBP/EP300 PROTAC degrader with a DC50 value of 1.3 μM. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 mediates the formation of a ternary complex between CRBN and the core of CBP, with an EC50 of 1.2 μM. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 inhibits cancer cell growth and exhibits cell line-specific degradation activity. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 can be used in research related to multiple myeloma and leukemia.
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