1,1,1 trifluoroethyl peg4 azide

111-Trifluoroethyl-PEG4-azide is a polyethylene glycol (PEG) derivative featuring a trifluoroethyl moiety and an azide functional group. It is utilized as a PROTAC linker, specifically designed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

1-Bromo-6-chlorohexane (Hexane, 1-bromo-6-chloro-) is used as PROTAC linker.

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

Azido-PEG4-azide is a PEG-based PROTAC linker used for synthesizing PROTACs.

SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.

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.

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

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

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

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.

Biotin-PEG4-Amide-C6-Azide is a PEG-based PROTAC linker utilized in PROTAC synthesis.

PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.

PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50 values of 0.04 μM for ERRα and 2.8 μM for ERRγ.

Pomalidomide 4'-PEG2-azide is a synthetic E3 ligase ligand-linker conjugate, comprising a Pomalidomide-based cereblon ligand and a linker.

SMARCA-BD ligand 1 for Protac dihydrochloride binds to the BAF ATPase subunit SMARCA2 and is used for degrading SMARCA2 based on PROTAC.

PROTAC BCR-ABL1 ligand 1 is the ligand of PROTAC .

Biotin-PEG4-azide, a biotin-labeled, PEG-based PROTAC linker, is utilized in PROTAC synthesis.

UAA crosslinker 1 hydrochloride is an Amber codon-activating agent used for incorporating non-canonical amino acids (ncAAs) into proteins in vivo by leveraging the promiscuous activity of specific wildtype and engineered aminoacyl-tRNA synthetases[1].

Compound X10g (PROTAC Hsp90α degrader 1) is a selective agent targeting Hsp90α for degradation and is utilized in breast cancer research. It demonstrates inhibitory effects on the proliferation of breast cancer cell lines, MDA-MB-231, MDA-MB-468, MCF-7, and MX-1, with respective IC50 values of 51.48 μM, 16.46 μM, 8.93 μM, and 11.95 μM [1].

Lenalidomide 4'-PEG2-azide, a Lenalidomide-derived Cereblon ligand, facilitates the recruitment of CRBN protein. This compound can be tethered via a linker to a protein ligand, enabling the formation of PROTAC [1].

Lenalidomide 4'-alkyl-C3-azide (compound 4a), a chemically modified version of the orally active immunomodulator lenalidomide, is engineered for the synthesis of PROTACs. This compound, serving as a ligand for the ubiquitin E3 ligase cereblon (CRBN), integrates an Azide group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with alkyne-bearing molecules. Additionally, it can undergo strain-promoted alkyne-azide cycloaddition reactions (SPAAC) with molecules containing DBCO or BCN groups [1].

PROTAC IRAK4 ligand-1 is a synthetic ligand targeting interleukin-1 receptor-associated kinase 4 (IRAK4).

PROTAC MDM2 Degrader-1 is a chemical compound that employs PROTAC technology to degrade MDM2, comprising a highly effective MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].

PROTAC CRABP-II Degrader-1 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on cIAp1.

Aminooxy-PEG4-azide, a PEG-based linker for PROTACs, connects two essential ligands critical for forming PROTAC molecules, facilitating selective protein degradation via the ubiquitin-proteasome system within cells.

ERRα Ligand-Linker Conjugates 1 refers to a chemical compound that consists of a ligand targeting estrogen-related receptor alpha (ERRα), and a PROTAC linker that facilitates the recruitment of E3 ligases MDM2. It finds utility in the synthesis of a range of PROTACs, including one known as PROTAC ERRalpha Degrader-1. With its capability to induce degradation of ERRα, PROTAC ERRalpha Degrader-1 functions as an ERRα degrader[1].

PROTAC PD-1 PD-L1 degrader-1, a Cereblon E3 ligand-based compound, is a PD-1 PD-L1 PROTAC that effectively inhibits the PD-1 PD-L1 interaction with an IC50 of 39.2 nM. It restores the suppressed immune response in a co-culture model of Hep3B OS-8 hPD-L1 cells and CD3 T cells and moderately decreases PD-L1 protein levels through a lysosome-dependent mechanism.

1-Cbz-azetidine-3-carboxylic acid (catalog number: T66609, CAS number: 97628-92-7) is a valuable organic compound for life sciences research.

dTAGV-1-NEG TFA, a diastereomer, serves as the heterobifunctional negative control for dTAGV-1. It acts specifically as an FKBP12 F36V-selective degrader [1].

PROTAC CYP1B1 Degrader-1 (Compound 6C), an α-naphthoflavone chimera derivative, effectively targets and degrades cytochrome P450 (CYP) 1B1 to overcome agent resistance, displaying half-maximal inhibitory concentrations (IC50s) of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2. This compound is suitable for investigating prostate cancer characterized by overexpression of CYP1B1 [1].

PROTAC ERα Y537S degrader-1 consists of a ubiquitin E3 ligase binding group, a linker, and a protein binding group, functioning as an estrogen receptor-alpha (ERα) Y537S degrader [1].

PROTAC STING Degrader-1 (Compound SP23) is a STING-targeted PROTAC degrader with a DC50 of 3.2 μM, demonstrating anti-inflammatory activity [1].

HEMTAC CDK4 6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4 6 with a ( K_d ) value of 35.7 μM. It induces CDK4 6 degradation in B16F10 melanoma cells, arrests the cell cycle at the G0 G1 phase, and induces apoptosis. HEMTAC CDK4 6 degrader 1 can be used in cancer research [1].

BacPROTAC-1, a potent mSA BacPROTAC degrader, exhibits high affinity for both mSA and the N-terminal domain (NTD) of ClpC, with dissociation constants (K D) of 3.9 μM and 2.8 μM, respectively [1].

PROTAC PARP EGFR ligand 1 is a potent compound used in developing dual PARP-EGFR degraders via Proteolytic Targeting Chimera (PROTAC) technology [1].

PROTAC Axl Degrader 1 is a potent and selective compound with an IC50 of 0.92 µM, exhibiting in vitro anti-proliferative and anti-migratory activities, and inducing mehuosis [1].

Negative control for dTAGV-1.

Tetraethyl butane- 1, 4- diylbis(phosphoramid ate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

PROTAC BET-binding moiety 1 is a crucial intermediate used in synthesizing high-affinity BET inhibitors.

PROTAC CDK9 ligand-1, a CDK9 ligand, is used in the synthesis of PROTACs.

PROTAC CDK2/9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

N-(m-PEG4)-N'-(azide-PEG4)-Cy3 is a polyethylene glycol (PEG)-derived linker, specifically designed for the synthesis of proteolysis-targeting chimeras (PROTACs) [1].

PROTAC BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

PROTAC BRD4-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand via a linker, facilitating the formation of a PROTAC complex which efficiently degrades BRD4[1].

1,1,1-Trifluoroethyl-PEG4-aminooxy is a polyethylene glycol (PEG)-based linker designed for the development of proteolysis targeting chimeras (PROTACs) [1].

ZXH-1-161 is a potent regulator of cereblon (CRBN) with an IC50 of 39 μM in wild-type MM1.S cells, selectively degrading GSPT1, and is useful for studying multiple myeloma.

Ald-C2-PEG4-azide is a PEG-based linker for PROTACs that joins two essential ligands, enabling selective protein degradation through the ubiquitin-proteasome system within cells.