Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12551 |
PROTAC BRD4 ligand-1
|
Epigenetic Reader Domain; Ligands for Target Protein for PROTAC | Chromatin/Epigenetic; PROTAC |
PROTAC BRD4 ligand-1 是 PROTAC GNE-987 靶向 BRD4 蛋白的配体,也是一种 BET 的抑制剂。 | |||
T18599 |
PROTAC BRD4-binding moiety 1
|
Others | Others |
PROTAC BRD4-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand through a linker, enabling the formation of a PROTAC complex. This complex efficiently degrades BRD4[1]. | |||
T18554 |
Pomalidomide-PEG1-azide
|
Others | Others |
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]. | |||
T10522 | BET-IN-6 | Epigenetic Reader Domain | Chromatin/Epigenetic |
BET-IN-6 是一种有效且高亲和力的BRD2/BRD4抑制剂。BET-IN-6 是靶蛋白 BRD2/4 的配体,可用于合成 PROTAC BRD2/BRD4 degrader-1 。 | |||
T18067 |
Lenalidomide-PEG1-azide
|
Others | Others |
Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1]. | |||
T18808 | Thalidomide-NH-C4-NH2 TFA | Others | Others |
Thalidomide-NH-C4-NH2 TFA (compound 29c) is a conjugate consisting of an E3 ligase ligand-linker, incorporating the Thalidomide-based cereblon ligand and a linker moiety. This compound, Thalidomide-NH-C4-NH2 TFA, is utilized as a component in PROTAC BRD2/BRD4 degrader-1, which is a highly potent and selective degrader targeting BET proteins BRD4 and BRD2[1]. | |||
T18598 |
PROTAC BRD2/BRD4 degrader-1
|
Others | Others |
PROTAC BRD2/BRD4 degrader-1 (compound 15) serves as a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination of BRD4 and BRD2 compared to BRD3. Its efficacy in suppressing solid tumors manifest with minimal cytotoxic effects. This compound comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN)/cullin 4A[1]. | |||
T18060 |
KB02-JQ1
|
Others | Others |
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 link... | |||
T36800 |
EN219
|
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EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 μM. EN219 (1 μM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP hum... |