BRD4 Degrader
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SNIPER(BRD)-1
0 ImagesSNIPER (BRD)-1 is a BRD2/3/4 SNIPER degrader. SNIPER (BRD)-1 induces ubiquitin-proteasome-dependent degradation of the epigenetic regulatory proteins BRD2/3/4 as well as the IAP family E3 ligase itself with its IC50 values for cIAP1, cIAP2 and XIAP of 6.8 nM, 17 nM and 49 nM, respectively. SNIPER (BRD)-1 can be used in the research of prostate cancer.
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DP-15
0 ImagesDP-15 is a BRD4 and GSPT1 PROTAC degrader with DC50 values of 0.48 nM and 5.25 nM, respectively. DP-15 induces ubiquitination and degradation of BRD4 and GSPT1. DP-15 induces Apoptosis. DP-15 exerts anticancer activity against acute myeloid leukemia and non-Hodgkin's lymphoma cells. DP-15 can be used in studies related to acute myeloid leukemia and non-Hodgkin's lymphoma.
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ML 2-14
0 ImagesCat. No.: HY-132991Purity: 99.43%ML 2-14 is a PROTAC targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219 (HY-115715) (bule part), the target protein ligand JQ-1 (HY-13030) (red part), and the PROTAC linker (balck part). ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells, and this effect can be reversed by the proteasome inhibitor Bortezomib (HY-10227) and the E1 activase inhibitor TAK-243 (HY-100487). ML 2-14 can be used for breast cancer-related research.
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PROTAC BRD4 Degrader linker conjugate-1
0 ImagesCat. No.: HY-138632CAS No.: 2417370-42-2PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC50 values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845)).\n
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dHTC3
0 ImagesCat. No.: HY-181976dHTC3 is a selective BRD4 molecular glue degrader. dHTC3 selectively binds to BRD4 BD1 to form a BRD4-dHTC3 complex, which cooperatively recruits the SCFFBXO3 E3 ubiquitin ligase and mediates the degradation of BRD4 via the ubiquitin-proteasome pathway. dHTC3 induces proteasome- and CRL-dependent BRD4 degradation with no hook effect. dHTC3 can be used in related research on acute myeloid leukemia.
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TrimTAC1
0 ImagesTrimTAC1 is a TRIM21-based PROTAC degrader targeting BRD4, with a DC50 of 0.649 nM. TrimTAC1 selectively degrades multimeric proteins, including those localized in biomolecular condensates, while exerting no effect on monomeric proteins in the dilute phase. This degradation effect can be blocked by Bortezomib (HY-10227) or TAK-243 (HY-100487). TrimTAC1 can be used in research related to pancreatic cancer and autoimmune diseases.
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MS83
0 ImagesCat. No.: HY-139620CAS No.: 2762181-19-9MS83 is a selective degrader of BRD4/BRD3 belonging to the PROTAC class. MS83 hijacks the KEAP1-dependent CUL3 ligase complex by binding to KEAP1 and forming a ternary complex with BRD4/BRD3. MS83 induces polyubiquitination and degradation of BRD4/BRD3 in a concentration-, time- and ubiquitin-proteasome system-dependent manner. MS83 inhibits c-MYC protein levels and suppresses the proliferation of triple-negative breast cancer cells.
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CFT-2718
0 ImagesCat. No.: HY-132941Purity: 99.87%CFT-2718 is a selective CRBN-dependent BRD4 PROTAC degrader. CFT-2718 mediates rapid, selective BRD4 degradation, reduces total and phosphorylated Ser2 RPB1 levels, and reduces MYC protein levels. CFT-2718 can inhibit cancer cells proliferation and induce apoptosis. CFT-2718 reduces growth of lung cancer and pancreatic patient-derived xenograft models. CFT-2718 can be used for the research of cancer, such as small-cell lung cancer and pancreatic cancer.
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L134
0 ImagesL134 is a BRD4 PROTAC degrader with a DC50 of 7.36 nM. L134 induces BRD4 protein degradation without inhibiting BRD4 gene expression, and recruits the E3 ubiquitin ligase DCAF11 to mediate this process, which can be blocked by proteasome inhibitors (MG132 (HY-13259), PS341 (HY-10227)) and E1 ubiquitin ligase inhibitors (PYR41 (HY-13296), MLN4924 (HY-70062)). L134 inhibits cancer cell migration, promotes cancer cell apoptosis and exerts antiproliferative activity. L134 can be used in studies related to triple-negative breast cancer.
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JQ1-S(GlcNAc)Cq
0 ImagesCat. No.: HY-178510JQ1-S (GlcNAc) Cq is a sugar-modified BRD4 PROTAC degrader with a DC50 of 2.1 μM. JQ1-S (GlcNAc) Cq inhibits the formation of the ternary complex between CRBN and BRD4 (BD1/BD2). JQ1-S (GlcNAc) Cq serves as a substrate for O-GlcNAcase, which cleaves its O-GlcNAc domain to restore binding ability with CRBN, thereby forming a BRD4-containing ternary complex and triggering ubiquitination and proteasomal degradation of BRD4. JQ1-S (GlcNAc) Cq is applicable for cancer research.
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PROTAC BRD4 Degrader-36
0 ImagesCat. No.: HY-175224PROTAC BRD4 Degrader-36 is a BRD4 PROTAC degrader with a DC50 of 0.649 nM. It has a Kd of 123 nM for TRIM21. PROTAC BRD4 Degrader-36 recruits the E3 ubiquitin ligase TRIM21 (Kd = 123 nM) to BRD4, leading to ubiquitination and subsequent degradation of BRD4. PROTAC BRD4 Degrader-36 exhibits cytotoxicity against PANC-1 cells (GI50 = 0.103 μM). It can be used in research related to pancreatic cancer.
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PROTAC FLT3/JAK2/BRD4 Degrader-1
0 ImagesCat. No.: HY-175610CAS No.: 3067695-20-6PROTAC FLT3/JAK2/BRD4 Degrader-1 is a FLT3/JAK2/BRD4 PROTAC degrader with DC50 values of 5.23, 0.68, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces cereblon- and proteasome-dependent degradation of FLT3, JAK2, and BRD4 via the ubiquitin-proteasome system. PROTAC FLT3/JAK2/BRD4 Degrader-1 is used in studies related to FLT3 inhibitor-resistant leukemia and acute myeloid leukemia.
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PROTAC BRD4 Degrader-26
0 ImagesCat. No.: HY-161650CAS No.: 3050769-37-1PROTAC BRD4 Degrader-26 is a light-regulated BRD4 PROTAC degrader. PROTAC BRD4 Degrader-26 induces targeted degradation of BRD4 via the ubiquitin-proteasome system. PROTAC BRD4 Degrader-26 is a degrader that can be inactivated in response to ultraviolet light. PROTAC BRD4 Degrader-26 can be used in breast cancer-related research.
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phoBET1
0 ImagesCat. No.: HY-149328CAS No.: 3033545-34-2phoBET1 is a photolabile PROTAC molecule that, upon photoactivation, functions as a BRD4 PROTAC degrader to trigger BRD4 degradation via the ubiquitin-proteasome system. Activated phoBET1 induces cancer cell apoptosis and inhibits tumor growth in xenograft mouse models. In its inactive caged state, phoBET1 exhibits only extremely low antiproliferative activity against cancer cells. phoBET1 can be applied in studies related to acute myeloid leukemia.
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PROTAC BRD4 Degrader-17
0 ImagesCat. No.: HY-143328CAS No.: 2585561-49-3PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells.
