YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.
tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Azido-PEG2-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Thalidomide-O-amido-C8-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs[1].
N,N-Diethanol amine-PEG4-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Fmoc-Val-Phe-Boc is a PROTAC linker and a maleimide-GGFG peptide linker. Fmoc-Val-Phe-Boc can be used in the synthesis of the Deruxtecan[1].
Bis-Mal-Lysine-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Tos-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
BCN-exo-PEG3-NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Thalidomide-5-methyl is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein[1].
Boc-PEG2-ethoxyethane-PEG2-benzyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader[1].
N-Mal-N-bis(PEG4-amine) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader based on PROTAC technology with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively.
Mal-amido-PEG2-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression[1].
Oleic-DBCO is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
N-(m-PEG4)-N'-(m-PEG4)-O-(m-PEG4)-O'-(propargyl-PEG4)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Mal-PEG8-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Bromo-PEG7-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
m-PEG16-SH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Amino-PEG2-(CH2)3COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
TL12-186 is a CRBN-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM)[1].
Thalidomide-O-C6-azide is a synthesized E3 ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugates) that incorporates the Thalidomide (Thalidomide (HY-14658)) based cereblon ligand and a linker used in PROTAC technology[1].
Bromo-PEG3-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs[1].
Cl-PEG2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CH2COOH-PEG6-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
N-(Azido-PEG4)-biocytin is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ms-PEG2-C2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].