heterobifunctional

dCBP-1 是基于Cereblon 配体的p300/CBP 的选择性双功能降解剂。dCBP-1可以有效的杀死多发性骨髓瘤细胞，并降低驱动 MYC 表达的致癌增强子活性。

Vepdegestrant （ARV-471） 是一种雌激素受体 (ER) α PROTAC 分子，可降解 ER 阳性乳腺癌细胞系中的 ER，DC50 约为 1 nM。它可以通过降解 ER 来降低经典调节的 ER 靶基因的表达并抑制 ER 依赖性细胞系（包括表达 ESR1 变体的细胞系，例如 Y537S 和 D538G）的生长。

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by connecting BET bromodomains to the E3 ubiquitin ligase CRBN. Additionally, it serves as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

SMCC (N-Succinimidyl 4-(N-maleimidomethyl)cycl) 是一种异双功能蛋白质交联剂。它接合抗原耦合脾脏细胞来诱导抗原特异性免疫反应。

AMAS 是一种不可裂解的异双功能交联剂，具有 NHS 酯和马来酰亚胺基团，可实现含胺和巯基分子的共价结合。

FKBP12 PROTAC dTAG-13是一种PROTAC和选择性降解剂，通过接合FKBP12 F36V和CRBN从而降解 FKBP12 F36V，可用于药物发现过程中的靶标验证。

3,4-Dibromo-Mal-PEG2-N-Boc 是一种 PEG 化的 PROTAC 连接子，可在 PROTAC 组装过程中实现靶蛋白配体与 E3 泛素连接酶配体之间的偶联。3,4-Dibromo-Mal-PEG2-N-Boc 可应用于设计利用泛素–蛋白酶体系统，合成选择性蛋白降解的双功能降解剂。

Bromo-PEG5-phosphonic acid diethyl ester is a polyethylene glycol (PEG)-based linker for PROTAC synthesis[1]. It is utilized in the construction of PROteolysis TArgeting Chimeras (PROTACs), which are heterobifunctional molecules designed to induce protein degradation.

GMBS, a heterobifunctional cross-linker, possesses an N-hydroxysuccinimide (NHS) ester at one end and a maleimide group at the other. It is commonly used in bioconjugation to link amines and sulfhydryls [thiols], forming stable amide and thioether bonds, respectively, which are useful in creating protein and peptide conjugates.

m-PEG4-phosphonic acid ethyl ester is a PEGylation-based linker for the design and synthesis of PROTACs, which are heterobifunctional molecules facilitating targeted protein degradation[1].

m-PEG3-Sulfone-PEG4-propargyl is a polyethylene glycol (PEG)-based prodrug-induced degradation (PROTAC) linker. It is utilized in the efficient synthesis of PROTACs, a class of heterobifunctional molecules designed to selectively target and degrade specific protein targets[1].

Sulfo-LC-SPDP is a heterobifunctional crosslinker characterized by its thiol-cleavable and membrane impermeable properties.

Sulfo-SPP is a heterobifunctional, thiol-cleavable, and membrane-impermeable crosslinker.

SBA crosslinker is a sulfhydryl and amino reactive heterobifunctional protein crosslinking reagent. SBA protein crosslinker is non-cleavable and is among the shortest amine and sulfhydryl reactive crosslinking reagents known with a spacer arm length of on

SMPB crosslinker is a heterobifunctional protein crosslinking reagent that is reactive toward sulfhydryl and amino groups. The SMPB protein crosslinker is an extended chain length analog of MBS crosslinker. SMPB crosslinker's spacer arm is non-cleavable.

dTAG-47-NEG 是 dTAG-47 的相似物，无法结合或募集 cereblon (CRBN)，被用作 dTAG-47 的异双功能阴性对照。

ARM165 是一种异双功能分子，通过降解蛋白 PIK3CG 来抑制 PI3Kγ-Akt 信号通路，从而展现抗白血病的能力。ARM165 可有效抑制 AML 细胞增殖，IC50<1 μM。

HL435是一种异双功能分子，通过与JQ1连接来降解BRD4，其在MDA-MB-231和MCF-7细胞中的DC50分别为11.9 nM和21.9 nM。HL435能够抑制MDA-MB-231、MCF-7、22Rv1和A549细胞的增殖，阻滞细胞周期并诱导细胞凋亡 (apoptosis)。此外，HL435在小鼠模型中展现出抗肿瘤活性。

Mal-PEG3-NH2 TFA 是一种线性异双功能的 PEG 交联剂，含有马来酰亚胺和胺基团。这种化合物是一种不可降解的 (non-cleavable) ADC linker。

Sulfo-MBS Crosslinker is a non-cleavable, water-soluble, heterobifunctional protein crosslinking reagent. It is commonly used to crosslink haptens to carrier proteins and enzymes to antibodies.

Sulfo-SIA Crosslinker is a non-cleavable, heterobifunctional protein crosslinker. Sulfo-SIA Crosslinker is useful in making antibody-drug conjugates.

Piperidine-GNE-049-N-Boc is a ligand that specifically binds to the target protein dCBP, enabling it to be degraded by a selective and potent heterobifunctional degrader, p300/CBP.

Thalidomide-NH-PEG4-COOH is a conjugate comprising an E3 ligase ligand-linker, utilized in the synthesis of dCBP-1. dCBP-1 itself functions as a powerful and selective heterobifunctional degrader targeting p300/CBP.

CBP/p300 ligand 2 是 PROTAC dCBP-1 的靶蛋白配体，后者为高效选择性 p300/CBP 降解剂。