protac brd4 ligand-1

PROTAC BRD4 ligand-1 is a PROTAC and a BRD4-targeted inhibitor with BET inhibitory activity. This ligand is cell-permeable and is used for the synthesis of PROTAC GNE-987, possessing antitumor potential.

PROTACBRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu is a Target Protein Ligand-Linker Conjugate that comprises a BRD4 ligand and a PROTAC linker. This compound is utilized in the synthesis of PROTACBRD4 Degrader-14.

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.

KB02-JQ1 is a potent and specific proteolysis targeting chimera (PROTAC) that specifically degrades BRD4, acting as a molecular glue. It does not degrade BRD2 or BRD3. The mechanism of action involves covalent modification of the E3 ligase DCAF16, thereby promoting BRD4 degradation. Importantly, KB02-JQ1 demonstrates enhanced stability and durability in facilitating protein degradation within biological systems. The compound forms a complex with the ubiquitin E3 ligase ligand KB02 through a linker, resulting in the formation of KB02-JQ1[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].

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-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand via a linker, facilitating the formation of a PROTAC complex which efficiently degrades BRD4[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].

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.

MS83epimer 1 is the epimer of MS83, a proof-of-concept PROTAC compound. MS83 is created by linking a KEAP1 ligand to a BRD4/3/2 binder.

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.

KLHDC2-IN-1 (Compound 6) is a ligand that specifically targets the ubiquitin E3 ligase KLHDC2 with a dissociation constant (Kd) of 160 nM. It can be synthesized into a PROTAC capable of effectively degrading BRD4 within cells.

JQ-1-Azidopropylamine is a Target Protein Ligand-Linker Conjugate, composed of a BRD4 ligand and a PROTAC linker that recruits E3 ligase. It is used in the synthesis of PROTACJY-21.

FLT3/JAK2/BRD4 ligand-1 is a ligand for FLT3, JAK2, and BRD4. It serves as a component for synthesizing PROTAC [FLT3/JAK2/BRD4 Degrader-1].

JQ-1 (carboxylic acid)-amine-PEG8-cyanogen is a Target Protein Ligand-Linker Conjugate, comprising a BRD4 ligand and a PROTAC linker, which recruits E3 ligase. This compound is utilized for the synthesis of PROTAC BET Degrader-14.

CBP/p300/BRD4 ligand-1 is a small molecule inhibitor that targets CBP, p300, and BRD4. This compound competitively binds to the functional domains of the target proteins without disrupting essential interactions. CBP/p300/BRD4 ligand-1 is suitable for constructing dual-target PROTAC degraders, making it applicable to research related to prostate and other cancers.

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114 and binds specifically to cysteine 8 (C8) within its intrinsically disordered region, exhibiting an IC50 of 470 nM. EN219 inhibits RNF114-induced autoubiquitination and p21 ubiquitination in cell-free assays at 50 μM. At 1 μM, EN219 interacts with multiple proteins including the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60/HspD1), and histone H3.1 (HIST1H3A) in 231MFP breast cancer cells. Furthermore, EN219 has been linked to the bromodomain inhibitor (+)-JQ1 for the creation of a PROTAC capable of degrading BRD4 in 231MFP cells.