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