1,3bis(carboxyethoxy)2,2bis(carboxyethoxy)propane

1,3-bis(carboxyethoxy)-2,2-bis(carboxyethoxy)propane is a polyethylene glycol (PEG)-based linker compound suitable for the synthesis of proteolysis-targeting chimeras (PROTACs) [1].

Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.

Thalidomide-NH-C2-PEG3-OH (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-4-[[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethyl]amino]-) is an E3 ligase ligand-linker conjugate.

Hydroxy-PEG1-C2-methyl ester, a polyethylene glycol (PEG) derived linker, is widely used in the production of PROTACs (proteolysis targeting chimeras). [1]

DBCO-NHS ester 3 (Compound 12) is a cleavable linker utilized in the synthesis of antibody-drug conjugate (ADC). It is a derivative of Dibenzylcyclooctyne (DBCO) resulting from the activation of N-hydroxysuccinimide by the carboxylic acid moiety of both methyl-oxanorbornadiene (MeOND) and dibenzoazacyclooctyne (DIBAC)[1][2].

PROTAC SMARCA2 4-degrader-26 is a PROTAC targeting the SMARCA2 4 proteins. It is composed of the ligand for PROTAC targeting proteins, 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid, an E3 ligase component (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide, and a PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid. The coupled complex of the E3 ubiquitin ligase ligand + Linker is referred to as (S,R,S)-AHPC.

3-(2-Pyridyldithio)propanoic Acid is an alkyl chain-derived PROTAC linker used for synthesizing PROTACs [1].

Azido-PEG3-Val-Cit-PAB-PNP is a cleavable 3-unit PEG ADC linker used for synthesizing antibody-drug conjugates (ADCs) [1] and also functions as a PEG-based PROTAC linker for PROTAC synthesis [2].

N-Succinimidyl 3-(Bromoacetamido)propionate is a PEG-based PROTAC linker used in the synthesis of PROTACs and antibody-drug conjugates (ADCs) [1, 2], serving as a cleavable ADC linker to facilitate drug-antibody conjugation for targeted delivery [2].

KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM for IRAK4 and 5 nM for Ikaros. It effectively induces apoptosis in MYD88 MT DLBCL and has demonstrated efficacy in inducing in vivo tumor regressions in a lymphoma model [1] [2] [3].

SLF TFA, a synthetic ligand for FK506-binding protein (FKBP), exhibits affinity toward FKBP51 with a value of 3.1 μM and demonstrates an IC50 of 2.6 μM for FKBP12. This compound is utilized in the synthesis of PROTAC [1] [2] [3].

1-Boc-azetidine-3-carboxylic acid is a valuable organic compound for life sciences research (catalog number T67359, CAS number 142253-55-2).

E3 Ligase Ligand-linker Conjugate 147 is a conjugate of an E3 ligase ligand and a PROTAC linker, utilized in the synthesis of BRD9 Degrader-1 (Compound 13-7). Comprising the E3 ligase ligand BRD9 ligand-7 and the PROTAC linker 2-((1R,5S,6s)-3-Azabicyclo[3.1.0]hexan-6-yl)ethan-1-ol, this conjugate plays a critical role in biochemical applications.

BI-3802, a highly potent BCL6 degrader, targets and inhibits the Bric-à-brac (BTB) domain of BCL6, exhibiting an IC50 value of ≤3 nM. It induces polymerization of BCL6 and facilitates its degradation in a manner dependent on the E3 ligase SIAH1, demonstrating notable antitumor activity[1][2].

Azide-PEG3-Tos is a PEG-based PROTAC linker used in the synthesis of PROTACs[1], and a non-cleavable 3-unit PEG ADC linker employed in the synthesis of antibody-drug conjugates (ADCs)[2].

PPC-NHS ester, a cleavable linker crucial in ADC synthesis, facilitates the attachment of cytotoxic drugs to antibodies for precise delivery to cells or proteins. Its cleavable nature ensures controlled drug release, thereby optimizing the effectiveness of ADCs (Antibody-Drug Conjugates).

MS15 is a potent, selective degrader of AKT PROTAC, effectively inhibiting activities of AKT1, AKT2, and AKT3. It exhibits IC50 values of 798 nM for AKT1, 90 nM for AKT2, and 544 nM for AKT3, respectively [1].

ChREBPα 14-3-3 regulator-1 (Compound 43) is a selective molecular glue that stabilizes the interaction between carbohydrate response element-binding protein (ChREBP) and 14-3-3 proteins, with an EC50 of 3.8 μM. It effectively safeguards β cells from glucolipotoxicity, preserving cell function and making it relevant for type 2 diabetes research.

PROTAC ER Degrader-14 (compound 86) is a PROTAC-type estrogen receptor ERR degrader. It comprises an E3 ubiquitin ligase ligand (blue part) (S)-Deoxy-thalidomide, a PROTAC linker (black part) N-Boc-piperazine, and a target protein ligand (red part) ER ligand-6. The combination of the E3 ligase and linker forms tert-Butyl (S)-4-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperazine-1-carboxylate.

DM4-SPDP, a drug-linker conjugate, integrates the antitubulin agent DM4 with the linker SMCC, facilitating the creation of antibody drug conjugates[1]. Additionally, SPDP serves as a short-chain crosslinker enabling amine-to-sulfhydryl conjugation, leveraging NHS-ester and pyridyldithiol groups to establish cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].

BCN-PEG3-Val-Cit is a PEG-based linker widely used in PROTAC synthesis[1] and as a cleavable 3-unit PEG linker in the production of antibody-drug conjugates (ADCs)[2].

Propargyl-PEG4-acid is a PEG-based PROTAC linker used in the synthesis of BTK-IAP PROTACs, including Ibrutinib-based PROTAC 2 and its analogue PROTAC 3. PROTAC 3 induces BTK degradation with a DC50 of 200 nM in THP-1 cells[1].

Pomalidomide-C2-NH2 (4-[(2-Aminoethyl)amino]-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione) is a synthesized E3 ligase ligand-linker conjugate containing a Pomalidomide-based cereblon ligand and a linker.

FLT3 ligand-2 serves as a ligand for the target protein in PROTAC. It is utilized for synthesizing PROTAC FLT-3 degrader 1.