e3 ligase ligand 13

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].

(S,R,S)-AHPC-C4-NH2 hydrochloride (E3 ligase Ligand-Linker Conjugates 28) is a synthesized E3 ligase ligand-linker conjugate comprising the (S,R,S)-AHPC-based VHL ligand and a linker.

Thalidomide-O-C6-NH2 hydrochloride (4-((6-aminohexyl)oxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione hydrochloride) is a synthesized E3 ligase ligand-linker conjugate.

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].

(S,R,S)-AHPC-PEG2-N3 (VHL Ligand-Linker Conjugates 6) is a synthesized E3 ligase ligand-linker conjugate comprising a (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker.

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].

E3 Ligase Ligand 41 (Compound SI-13) serves as a ligand for the E3 ubiquitin ligase DCAF16. It is designed to connect with SLF through a linker, enabling the formation of KB03-SLF.

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]

CRBN ligand-13, a CRBN-type E3 ubiquitin ligase ligand, is applicable in the preparation of PROTAC.

PROTAC BTK Degrader-13 (Compound 25) is a targeted BTK PROTAC degrader with a DC50 of 0.27 μM. It inhibits BTK activity with an IC50 of 0.44 μM and suppresses IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. This compound also inhibits the p38 MAPK signaling pathway, thereby blocking the activation of the BCR (B cell receptor) signaling pathway. [Pink: ligand for target protein BTK ligand 15; Black: linker; Blue: ligand for E3 ligase cereblon]

Ethanolamine-Thalidomide-4-OH is an E3 ligase ligand-linker conjugate used in the synthesis of PROTACs, such as [PROTAC BTK Degrader-13].

dBRD9 is a PROTAC. dBRD9 is a double-acting molecule, partially containing Bromodomain-containing protein 9 (BRD9), ligand that recruits the cereblon E3 ubiquitin ligase. Ligand that recruits the cereblon E3 ubiquitin ligase. dBRD9 can inhibit the degradation of BRD9 in MOLM-13 cells, and the IC50 is 104 nM.

dBRD9 HCl is a PROTAC composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . dBRD9 HCl is a potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 HCl does not degrade BRD4 or BRD7 at concentrations up to 5 μM. dBRD9 HCl displays antiproliferative effects in human AML cell lines.

Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. This product has been recently renamed. The previous name for this product was VH 032 - linker 13 PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

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.