PROTAC BRD4 Degrader 1

PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination compared to BRD3. It effectively suppresses solid tumors with minimal cytotoxic effects and comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN)/cullin 4A[1].

PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.

PROTACBRD4-DCAF1 degrader-1 (I-907) is a PROTAC degrader targeting BRD4-DCAF1, exhibiting a DC50 range of 10~100 nM.

PROTACFLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader targeting FLT3, JAK2, and BRD4, with DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It exhibits potent antiproliferative activity against MV4;11 cells (IC50= 0.79 nM) and FLT3-mutated Ba/F3 cells. Additionally, PROTACFLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells and demonstrates significant antitumor efficacy in an MV4;11 xenograft model established in NOD SCID mice. This compound is applicable for research in acute myeloid leukemia (AML).

BET-IN-6, a ligand with potent and high affinity for inhibiting BRD2/BRD4, plays a crucial role in the synthesis of PROTAC BRD2/BRD4 degrader-1 [1], targeting the protein BRD2/4.

PROTAC BRD9 Degrader-1 is a leading PROTAC BRD9 chemical degrader with an IC50 of 13.5 nM.

Azido-PEG1-CH2CO2H, a PROTAC linker characterized by an alkyl/ether combination, can be utilized to synthesize PROTAC BRD4 Degrader-1[1].

Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl/ether-based PROTAC linker commonly used in the synthesis of PROTAC BRD4 Degrader-1[1].

Lenalidomide-PEG1-azide is an E3 ligase ligand-linker complex comprising a cereblon ligand and linker, suitable for synthesising PROTACs and click chemistry reactions.

Pomalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that combines the cereblon ligand based on Pomalidomide with a linker. This compound is instrumental in designing PROTAC BRD4 Degrader-1[1].

Thalidomide-NH-C4-NH2 TFA (compound 29c) is a conjugate composed of an E3 ligase ligand-linker that integrates a Thalidomide-based cereblon ligand and a linker moiety. This compound is used as a component in PROTAC BRD2/BRD4 degrader-1, a highly potent and selective degrader targeting BET proteins BRD4 and BRD2[1].

SJ46421, a PROTAC protein degrader derived from (+)-JQ-1, targets KLHDC2. It efficiently forms a stable ternary complex with KLHDC2, exhibiting an IC50 of 7.8 nM. Furthermore, SJ46421 promotes the polyubiquitination of the BD2 domain of BRD2, BRD3, or BRD4.

JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 incorporates a BRD4 ligand and a PROTAC linker, and is used in the synthesis of PROTAC BRD4 Degrader-29.

SJ44236 is a BET PROTAC degrader capable of degrading BRD2 (DC50 = 0.127 nM), BRD3, and BRD4. It shows cytotoxicity in MV4-11 and HD-MB03 cells with IC50 values of 0.12 nM and 0.92 nM, respectively. The compound downregulates c-Myc expression and upregulates p53 expression. In mice, SJ44236 demonstrates good oral bioavailability (45%). [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonE3ligaseLigand 54]

BRD4 ligand 6 is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). It serves as a key component in synthesizing the PROTAC CBP/BRD4 degrader-1.

PROTACBRD4 Degrader-26 (PROTAC-2) is a photo-regulated PROTAC designed to degrade BRD4, achieving 80% degradation efficiency at a concentration of 1 μM. This compound can be inactivated by ultraviolet light.

Boc-Dipiperidine-KLHDC2 ligand 1 is an E3 ubiquitin ligase ligand-linker conjugate, incorporating a KLHDC2 ligand. It is utilized in the synthesis of PROTAC BRD4 Degrader-31.

LO-3-61 is a JQ-1 analog featuring a truncated fumarylamide group, classified as a BRD4 degrader with PROTAC (protein degradation targeting chimera) properties. It promotes the degradation of both long and short BRD4 isoforms via a CUL4DCAF16-dependent pathway. In MDA-MB-231 cells, LO-3-61 exhibits selectivity in degrading BRD3 and BRD4.

PROTACBRD4 Degrader-36 (Compound TrimTAC-1) is a BRD4 PROTAC degrader. It has a DC50 of 0.649 nM and a Dmax of 71% in PANC-1 cells. Additionally, PROTACBRD4 Degrader-36 exhibits cytotoxicity towards PANC-1 cells with a GI50 of 0.103 μM. This compound is applicable for tumor research.

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor with IC50 values of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively, effectively degrading the BRD4 protein in PC3 prostate cancer cells[1].

cis MZ 1 is a negative control for MZ 1 (1797406-69-9) and exhibits no binding affinity for VHL. MZ 1 is a PROTAC degrader targeting BRD4.

ARV-771 is an effective BET degrader based on PROTAC technology. The Kd for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1) and BRD4(2) are 34 and 4.7 respectively. , 8.3, 7.6, 9.6 and 7.6 nM.

MZ 1 is a BRD4 protein degrader based on PROTAC technology.