13-tetradecyn-1-oic acid

Alkynyl myristic acid (13-Tetradecyn-1-oic acid) is an alkyl chain-based PROTAC linker.

Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.

2-(Azido-PEG2-amido)-13-propandiol is a Polyethylene glycol (PEG)-based PROTAC linker used for synthesizing PROTACs[1].

2-(Biotin-amido)-13-bis(carboxylethoxy)propane is a polyethylene glycol (PEG)-based PROteolysis TArgeting Chimera (PROTAC) linker used in the synthesis of PROTACs[1].

m-PEG4-azide, also referred to as 13-Azido-2,5,8,11-tetraoxatridecane, functions as a PEG-based PROTAC linker suitable for PROTACs synthesis[1].

Propynol Ethoxylate is a PEG-based linker for PROTACs [Proteolysis Targeting Chimeras] that connects two essential ligands, facilitating the formation of PROTAC molecules and enabling selective protein degradation via the ubiquitin-proteasome system within cells.

Boc-NH-PEG2-C2-NH2 (PROTAC Linker 13) is a PEG-based linker used in PROTAC synthesis, essential for connecting the targeted protein and the E3 ubiquitin ligase to facilitate selective protein degradation[1].

E3 ligase Ligand 13 is an E3 ubiquitin ligase ligand that can be employed to create PROTACs, which are connected to the ligand for the protein through a linker. PROTACs serve as inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].

Lenalidomide-C4-NH2 hydrochloride is a Cereblon ligand derived from Lenalidomide. It serves as a recruiting agent for the CRBN protein. The compound, known as PROTAC (Compound 24), can be formed by linking Lenalidomide-C4-NH2 hydrochloride to the ligand for the protein. It exhibits inhibitory effects with IC50s of 0.98 nM and 13.7 nM against the growth of RS4;11 and MOLM-13 acute leukemia cell lines, respectively[1].

cIAP1 Ligand-Linker Conjugates 13, containing an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker, are utilized in the development of SNIPERs[1].

Pomalidomide-PEG1-C2-N3, a conjugate of an E3 ligase ligand-linker, incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, commonly used in PROTAC technology. This compound enables the design of the selective CDK6 PROTAC degrader CP-10, which effectively induces CDK6 degradation with a DC50 value of 2.1 nM[1].

Thalidomide-O-C6-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12F36V and BET[1].

Thalidomide-O-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate used in the PROTAC dTAG-13, a degrader of FKBP12F36V and BET[1].

PROTAC METTL3 degrader 1 (Compound KH12) is a VHL-based degrader of METTL3, demonstrating a DC50 of 220 nM in MOLM-13 cells. This compound inhibits the METTL3/14 complex with an IC50 of 341 nM and exhibits antiproliferative activity against AML cells.

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.

DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]

PROTAC K-Ras Degrader-4 (Compound 4) is a proteolysis-targeting chimera (PROTAC) molecule designed to selectively degrade oncogenic mutants of K-Ras, effectively degrading KRASG12D in the GP5d cell line and KRASG12V in SW620 cells with DC50 of 1 nM and 13 nM, respectively; it concomitantly inhibits the downstream MAPK signaling pathway and represents a novel therapeutic strategy for cancer research targeting previously undruggable Ras mutations.

PROTACPIN1degrader-2 (1) is a PROTAC degrader of PIN1. The IC50 values of PROTACPIN1degrader-2 (1) against various cancer cells are as follows: 2248 nM for MV-4-11 cells, 3984 nM for MOLM-13 cells, and 3925 nM for HL-60 cells.

SR-1114, a first-in-class PROTAC ENL degrader, induces rapid CRBN-dependent ENL degradation with DC50 values of 150 nM in MV4;11 cells, 311 nM in MOLM-13 cells, and 1.65 μM in OCI/AML-2 cells [1].

PROTAC SOS1 degrader-5 (compound 4) serves as an effective degrader of PROTAC SOS1, exhibiting a DC50 of 13 nM. It robustly suppresses the proliferation of NCI-H358 cells, with an IC50 value of 5 nM [1].

PTOTAC HSD17B13 Degrader 1, a PROTAC designed to target 17β-HSD 13 (HSD17B13), incorporates several key components. These include the PROTAC target protein ligand HSD17B13 Degrader 2, the PROTAC Linker tert-Butyl 5-bromoisoindoline-2-carboxylate, and the E3 ubiquitin ligase ligand E3 Ligase Ligand 31. Notably, the conjugate formed by the E3 ubiquitin ligase ligand and the linker is recognized as E3 Ligase Ligand-linker Conjugate 114.