HL-8

• Description :

  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].

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [2766352-64-9]