heterobifunctional

dCBP-1 is a chemical degrader of p300/CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300/CBP. Degradation of p300/CBP by dCBP-1 leads to effective multiple myeloma cell killing.

Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER.

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

EMCS (6-Maleimidohexanoic acid N-hydroxysuccinimide ester) is a heterobifunctional crosslinking agent, which is a compound for the preparation of hapten conjugate and enzyme immune conjugate, and an effective protective group in antibody drug conjugate.

SMCC (N-Succinimidyl 4-(N-maleimidomethyl)cycl) is a heterobifunctional protein crosslinker.

AMAS is a non-claevable heterobifunctional crosslinker with NHS ester and maleimide groups that enables covalent conjugation of amine- and sulfhydryl-containing molecules.

FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader that can be used for target validation during drug discovery by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.

3,4-Dibromo-Mal-PEG2-N-Boc is a PEGylated PROTAC linker that enables conjugation between target-binding ligands and E3 ligase ligands during PROTAC assembly. 3,4-Dibromo-Mal-PEG2-N-Boc supports the design of heterobifunctional degraders that exploit the ubiquitin–proteasome system for selective protein degradation。

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

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 used in the design and synthesis of PROTACs, which are heterobifunctional molecules that facilitate targeted protein degradation[1].

m-PEG3-Sulfone-PEG4-propargyl is a polyethylene glycol (PEG)-based prodrug-induced degradation (PROTAC) linker utilized in the efficient synthesis 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.

Sulfo-SMPB sodium is a non-cleavable, heterobifunctional chemical cross-linking reagent that combines N-hydroxysuccinimide ester and maleimide groups, enabling the covalent conjugation of molecules possessing (amine) and (sulfhydryl) functionalities.

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.

EN171, a covalent ligand, selectively binds to C38 and C96 on 14-3-3, intensifying 14-3-3's interactions with ERα, YAP, and TAZ. This action impairs both estrogen receptor and Hippo pathway transcriptional activities. Beyond serving as a molecular glue to augment native protein interactions, EN171 also functions as a covalent recruiter for 14-3-3 in heterobifunctional molecules. This facilitates the sequestration of nuclear neo-substrates, such as BRD4 and BLC6, into the cytosol.

TMX-2172 is a heterobifunctional CDK2 degrader, selectively degrading CDK2 and CDK5, with minimal effects on CDK1, transcriptional CDKs (CDK7 and CDK9), and cell cycle CDKs (CDK4 and CDK6). In ovarian cancer cells (OVCAR8), its anti-proliferative activity is dependent on CDK2 degradation and is linked to high expression of cyclin E1 (CCNE1), which acts as a regulatory subunit of CDK2. As a lead compound for further development, TMX-2172 demonstrates that CDK2 degradation could be a potentially effective strategy for treating ovarian and other cancers with elevated CCNE1 expression.

HEMTACWEE1degrader-1 is a WEE1-targeting heterobifunctional chimeric degrader (HEMTAC) facilitated by HSP90, exhibiting an HSP90 enzyme inhibitory activity with an IC50 of 16.76 nM. It enhances the ubiquitination and subsequent degradation of WEE1, effectively blocking the G2/M cell cycle transition. This compound shows anticancer properties in patient-derived xenograft (PDX) models of acute myeloid leukemia (AML). HEMTACWEE1degrader-1 is utilized in AML research.

dTAG-47-NEG is an analogue of dTAG-47 that is unable to bind and recruit cereblon (CRBN), serving as a heterobifunctional negative control for dTAG-47.

iRGD–CPT is an iRGD-camptothecin conjugate covalently linked via a heterobifunctional linker. It exhibits anticancer activity both in vivo and in vitro and can be utilized in colon cancer research.

ARM165 is a heterobifunctional molecule that degrades the protein PIK3CG and inhibits the PI3Kγ-Akt signaling pathway, thereby exerting anti-leukemic effects. It is capable of suppressing the proliferation of AML cells, with an IC50 of less than 1 μM.

HL435 is a heterobifunctional molecule that degrades BRD4 by linking with JQ1, with DC50 values of 11.9 nM and 21.9 nM in MDA-MB-231 and MCF-7 cells, respectively. It inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1, and A549 cells, arrests the cell cycle, and induces apoptosis. Additionally, HL435 exhibits antitumor activity in mouse models.