Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
76 Results for "
BRD4-PROTAC
" in MedChemExpress (MCE) Product Catalog:
Products (76)
76 Results for "BRD4-PROTAC" in MCE Product Catalog:
4
4 Cited Publications
Target:
Research Areas:
KB02-JQ1 is a potent and selective BRD4 PROTAC degrader. KB02-JQ1 degrades BRD4 via the ubiquitin-proteasome pathway by bridging DCAF16 E3 ubiquitin ligase and BRD4. KB02-JQ1 can be used for cancer research .
3
3 Cited Publications
Research Areas:
A1874 is an orally active BRD4 PROTAC degrader with a DC50 of 32 nM. A1874 degrades BRD4 via the ubiquitin-proteasome system by recruiting the MDM2 E3 ligase, while disrupting the MDM2-p53 interaction to stabilize p53 and upregulate p21, thereby inducing cell cycle arrest and apoptosis. A1874 exhibits selectivity for wild-type p53 cells and MDM2-amplified tumors, and it can be used in research on breast cancer, colorectal cancer, melanoma, lung cancer, lymphoma, myeloid leukemia, osteosarcoma, and glioblastoma [4] .
3
3 Cited Publications
Target:
Research Areas:
ZXH-3-26 is a CRBN-recruiting BRD4 PROTAC degrader with a DC50/5h of approximately 5 nM. ZXH-3-26 drives the ubiquitination and degradation of BRD4 by recruiting BRD4BD1 to the CRL4 CRBN E3 ubiquitin ligase complex, thereby inhibiting the dynamic distribution of super-enhancers. ZXH-3-26 reverses TNF-α-induced impairment of the immunosuppressive function of mesenchymal stem cells, and affects RNA synthesis and the transcriptional elongation process of Pol II. ZXH-3-26 can be used in studies related to inflammatory arthritis, malignant tumors, and HIV latency [4] .
2
2 Cited Publications
Target:
Research Areas:
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 .
1
1 Cited Publications
Target:
Research Areas:
GNE-987 is a VHL-dependent BRD4 PROTAC degrader. 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 can be used for the research of cancer .
Target:
Research Areas:
BD-9136 is a selective BRD4 PROTAC degrader with a DC50 of 1.2 nM, and exhibits a selectivity of ≥1000-fold over BRD2 and BRD3. BD-9136 preferentially forms a ternary complex with the BD1 domain of BRD4, and downregulates the expression of B7-H4 by disrupting the PR-P300-BRD4 axis. BD-9136 depletes BRD4 protein in tumor tissues, inhibits tumor growth, reduces B7-H4 protein expression, increases CD8+ T cell infiltration, and enhances tumor sensitivity to anti-PD-L1. Degradation of BRD4 by BD-9136 rescues the erythroid differentiation block induced by LSD1 inhibition, and transient administration restores erythroid output while retaining HbF induction. BD-9136 causes no adverse effects in mice at effective doses. BD-9136 can be used in studies related to acute myeloid leukemia, acute lymphoblastic leukemia and breast cancer .
Target:
Research Areas:
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation .
Cat. No.: HY-132941
Research Areas:
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 .
Synonyms: PROTAC BRD4 Degrader-5
Target:
Research Areas:
GAL-02-221 is a BRD4 PROTAC degrader with blood-brain barrier permeability, with a DC50 of 0.009 μM (Jurkat BRD4-HiBiT). GAL-02-221 induces proteasome-catalyzed BRD4 degradation, binds to VHL to trigger BRD4 ubiquitination, and recruits the VHL E3 ligase complex to participate in protein degradation. GAL-02-221 degrades BRD4 in breast cancer cells as well as mouse liver and brain tissues. GAL-02-221 is applicable to research related to breast cancer .
Cat. No.: HY-164995
CAS No.: 2417370-68-2
Research Areas:
L1BC8 (Compound 13a) is a drug-linker conjugate for ADC. L1BC8 is obtained by conjugating a BRD4 PROTAC degrader with a peptidomimetic protease-cleavable linker for the preparation of ADC, which can be conjugated to STEAP1 antibodies and CLL1 antibodies, respectively. L1BC8 can be used in research related to prostate cancer and acute myeloid leukemia .
Research Areas:
PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136) . PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Target:
Research Areas:
SJ995973 is a BRD4 PROTAC degrader with DC50 values of 0.87 nM (12 h) and 0.16 nM (24 h), respectively. SJ995973 induces the formation of a ternary complex between purified BRD4 and CRBN-DDB1 proteins, with an IC50 of 17 nM against CRBN. SJ995973 inhibits the viability of human acute myeloid leukemia cells. SJ995973 can be used in studies related to acute myeloid leukemia and medulloblastoma .
Cat. No.: HY-174996
CAS No.: 3031840-36-2
Target:
Research Areas:
NEP162 is a BRD4 PROTAC degrader based on the E3 ubiquitin ligase GID4, with DC50 values of 1.2 μM and 1.6 μM in SW480 and U2OS cells, respectively, and a Kd value of 0.13 µM for GID4. NEP162 bridges the E3 ligase GID4 and BRD4 to form a ternary complex, promotes polyubiquitination and subsequent degradation of BRD4 via the ubiquitin-proteasome system, reduces the proliferation capacity of tumor cells and induces apoptosis. NEP162 can be used for research on cancers such as osteosarcoma, colorectal cancer and non-small cell lung cancer .
Cat. No.: HY-161651A
CAS No.: 2763548-61-2
Target:
Research Areas:
BRD4 ligand 6 TFA is the TFA salt form of BRD4 ligand 6 (HY-161651). BRD4 ligand 6 TFA is a BRD4 ligand and can be used for synthesis of BRD4 PROTACs, such as PROTAC BRD4 Degrader-26 (HY-161650) .
Target:
Research Areas:
dBET23 is a highly potent and selective BRD4 PROTAC degrader, with a DC50/5h of approximately 50 nM against the BRD4BD1 protein. dBET23 induces the formation of a ternary complex consisting of CRBN, itself, and BRD4BD1, thereby mediating the degradation of BRD4BD1. dBET23 causes downregulation of BRD4 expression in cancer cells. dBET23 can be used for research on malignant tumors .
Cat. No.: HY-131203
CAS No.: 2410947-56-5
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research .
Cat. No.: HY-156774
CAS No.: 2361142-23-4
Target:
Research Areas:
CCW 28-3 is a BRD4 PROTAC degrader. CCW 28-3 recruits RNF4 to BRD4, inducing RNF4-dependent ubiquitination and proteasomal degradation of BRD4. CCW 28-3 can be used in breast cancer-related research .
Cat. No.: HY-168546
CAS No.: 2154353-03-2
Target:
Research Areas:
CFT-1297 is a CRBN-recruiting BRD4 PROTAC degrader with a DC50 of 5 nM; it has KD values of 2.1 μM, 0.68 μM and 58 nM for CRBN, BRD4 (BD2) and BRD4 (BD1), respectively. CFT-1297 binds weakly to CRBN-DDB1, with a KD value of 2.1 μM .
Cat. No.: HY-174210
Target:
Research Areas:
PROTAC BRD4 Degrader-3 is a potent BRD4 PROTAC degrader with DC50 values of 164 nM and 80 nM at 4 h and 24 h, respectively. PROTAC BRD4 Degrader-3 induces the ubiquitination and subsequent proteasomal degradation of BRD4 by recruiting the ubiquitin E3 ligase KLHDC2. PROTAC BRD4 Degrader-3 can be used in breast cancer research .
Cat. No.: HY-160694
CAS No.: 2417369-73-2
Synonyms: cBu-Cit-PROTAC BRD4 Degrader-5
Research Areas:
cBu-Cit-GAL-02-221 (cBu-Cit-PROTAC BRD4 Degrader-5) is a BRD4 PROTAC-linker conjugate with a protease-cleavable cBu-Cit linker. cBu-Cit-GAL-02-221 can be conjugated with antibodies to form PACs, and releases a VHL-recruiting BRD4 degrader inside cells. cBu-Cit-GAL-02-221 is applicable to studies on BRD4-targeted degradation, antibody-mediated PROTAC delivery and PAC construction .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
