HL-8

HL-8 is a PI3Kα PROTAC degrader. HL-8 promotes the ubiquitination and degradation of PI3Kα. HL-8 reduces pAKT levels. HL-8 has anticancer activity against colon and cervical cancer (Pink: PI3Kα ligand (HY-143277) ; Blue: E3 ligase VHL ligand (HY-138678) ; Black: linker (HY-W002042) ) [1].

Product Specifications

CAS Number

[2766352-64-9]

UNSPSC

12352005

Target

Akt; PI3K; PROTACs

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/hl-8.html

Purity

99.17

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

COC1=NC=C(C=C1NS(=O)(C2=C(C=C(C=C2)F)F)=O)C3=CN4C(C5=NN=C(O5)C6=C(C=CC=C6)C(NCCCCCCC(N[C@@H](C(C)(C)C)C(N7C[C@H](C[C@@H]7C(NCC8=CC=C(C=C8)C9=C(N=CS9)C)=O)O)=O)=O)=O)=CN=C4C=C3

Molecular Formula

C57H59F2N11O9S2

Molecular Weight

1144.27

References & Citations

[1]Wang H, et al. Design, synthesis and activity study of a novel PI3K degradation by hijacking VHL E3 ubiquitin ligase. Bioorg Med Chem. 2022 May 1;61:116707.