propargyl-peg1-ss-peg1-propargyl

Propargyl-PEG1-SS-PEG1-propargyl refers to a cleavable di-functional polyethylene glycol (PEG) linker composed of two units. This specific linker is employed in the synthesis of antibody-drug conjugates (ADCs), where it plays a critical role in linking the antibody to the drug. [1]

Propargyl-PEG1-SS-PEG1-PFP ester is a cleavable linker consisting of a 1-unit polyethylene glycol (PEG) backbone, designed for use in the synthesis of antibody-drug conjugates (ADCs)[1].

Propargyl-PEG1-SS-PEG1-acid is a two-unit polyethylene glycol (PEG) linker that is cleavable and commonly employed in the synthesis of antibody-drug conjugates (ADCs) [1].

Propargyl-PEG1-SS-PEG1-C2-Boc is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

Propargyl-PEG1-SS-alcohol is a 1-unit PEG ADC linker that is cleavable. It finds application in the synthesis of antibody-drug conjugates (ADCs)[1].

(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1/2) (IC50=77/33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

Propargyl-PEG17-methane (MPEG16-Propyne) is a PEG-based PROTAC linker. Propargyl-PEG17-methane can be used in the synthesis of PROTACs.

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

Propargyl-PEG12-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

DSPE-PEG-OH (MW 2000) is a PEG-based PROTAC linker for PROTAC synthesis.

SMARCA-BD ligand 1 for Protac is a compound capable of binding to SMARCA2, the BAF ATPase subunit, based on the Protac technology for degrading SMARCA2

Propargyl-PEG5-Ms (Propargyl-PEG6-Ms) is a PEG-based PROTAC linker. Propargyl-PEG5-Ms can be used in the synthesis of PROTACs.

Propargyl-PEG11-methane is a PEG-based PROTAC linker that can be used to synthesize PROTACs[1].

Thalidomide-PEG4-Propargyl (Thalidomide-O-PEG4-Propargyl) is a synthetic E3 ligase ligand-linker conjugate containing a Thalidomide-based cereblon ligand and a linker which can be used in PROTAC technology[1].

Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

PROTAC BRD4 ligand-1 is a ligand for PROTAC GNE-987 targeting the BRD4 protein and is an inhibitor of BET.

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.

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM)[1].

PROTAC eDHFR Degrader-1 is a potent degrader targeting eDHFR-YFP and various proteins of interest (POIs), such as YFP and Luciferase [1].

Cereblon inhibitor 1, an isoindoline derivative, serves as a modulator of the cereblon E3 ubiquitin ligase and shows promise for applications in cancer research.

Azido-PEG8-propargyl is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

DBCO-(PEG)3-VC-PAB-MMAE is a chemical compound where monomethyl auristatin E (MMAE), a potent tubulin inhibitor acting as a toxin payload in antibody-drug conjugates, is conjugated to a DBCO-(PEG)3-vc-PAB linker.

Desthiobiotin-PEG4-propargyl is a PEG-coupled PROteolysis TArgeting Chimeric (PROTAC) linker, employed for PROTAC synthesis.

1-Isothiocyanato-PEG3-azide is a PEG-based PROTAC linker utilized for PROTAC synthesis[1].

m-PEG-azide (MW 5000) is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

U7D-1, a groundbreaking and selective ubiquitin-specific protease 7 (USP7) PROTAC degrader, exhibits a DC50 value of 33 nM in RS4;11 cells, demonstrating its potent anticancer properties. Furthermore, U7D-1 effectively induces apoptosis in Jeko-1 cells [1].

Biotin-PEG-amine (MW 2000) is a polyethylene glycol (PEG) derivative commonly employed as a linker in the synthesis of proteolysis targeting chimeras (PROTACs)[1].

PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.

Bis-propargyl-PEG10 is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

Amine-PEG-CH2COOH (MW 5000) is a PEG-based PROTAC linker that can be used in PROTAC synthesis.

PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) (IC50 of 6.5 nM).

Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1].

Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL)-binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells. Hydrochloride salt (Cat.No. 7374) available; suitable for in vivo use. Negative control dTAGV-1-NEG (Cat. No. 6915) also available. FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email TPD@bio-techne.com to enquire. Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.

Propargyl-PEG4-thiol is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].

Amine-PEG-CH2COOH (MW 2000) is a polyethylene glycol (PEG) derivative employed as a linker in the synthesis of proteolysis targeting chimeras (PROTACs)[1].

Bis-propargyl-PEG7 is a polyethylene glycol (PEG)-based linker utilized in the synthesis of proteolysis targeting chimeras (PROTACs). It is particularly employed for the synthesis of polymer-linked multimers of guanosine-3',5'-cyclic monophosphates[1].

Azide-PEG-amine (MW 2000) is a Polyethylene Glycol (PEG) derived linker compound utilized in the synthesis of Proteolysis Targeting Chimeras (PROTACs)[1].

PROTAC NSD3 degrader-1 (compound 56) is a targeted degradation agent for the Nuclear receptor binding SET domain protein NSD3. It effectively induces the degradation of NSD3 in NCI-H1703 and A549 lung cancer cell lines, with DC50 values of 1.43 and 0.94 μM, respectively. Additionally, it hinders H3K36 methylation, triggers apoptosis, and arrests the cell cycle. Furthermore, PROTAC NSD3 degrader-1 diminishes the expression of NSD3-related genes, including CDC25A, ALDH1A1, and IGFBP.

PROTAC GDI2 Degrader-1 (Compound 21) is a potent degrader of PROTAC GDI2, demonstrating outstanding antitumor activity in vivo within pancreatic xenograft models that overexpress GDI2 [1].

PROTAC BET Degrader-1 is a potent degrader of BET based on PROTAC.

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.

PROTAC SOS1 degrader-1, a potent compound, demonstrates an effective degradation of PROTAC SOS1 with a DC50 value of 98.4 nM. It exhibits antiproliferative activity against cancer cells harboring diverse KRAS mutations and has shown an antitumor effect with low toxicity [1].

Bis-propargyl-PEG11 is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

m-PEG-thiol (MW 5000) is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).

N-Boc-4-pentyne-1-amine is an alkyl chain-based PROTAC linker compound utilized in the synthesis of PROTAC MG-277[1].

N-(Propargyl-PEG2)-N-Boc-PEG3-t-butyl ester is a polyethylene glycol (PEG)-based linker employed for the synthesis of proteolysis-targeting chimeras (PROTACs) [1].

S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate, an ADC linker, is a glutathione cleavable compound used for the attachment of monoclonal antibodies (mAb) in antibody-drug conjugates (ADCs). It specifically refers to the Alkyl-Chain composition of the linker portion of these molecules [1].

Propargyl-PEG5-Br is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.