HLDA-212

• Target:

  Apoptosis|||Aurora Kinase

• Related Pathways:

  Cell Cycle/Checkpoint|||Chromatin/Epigenetic|||Apoptosis

• Bioactivity:

  HLDA-212 (Compound 43) is a bifunctional small molecule designed to target HaloTag-tagged protein (target protein, TP) and Aurora kinase A/B (AURKA/B, effector protein, EP) . By binding TP and EP, it forms a stable ternary complex (TP:RIPTAC:EP) that inhibits the cell survival functions of EP, inducing apoptosis in cancer cells expressing TP. In 293_HFL cells, HLDA-212 demonstrates antiproliferative activity with a GI50 of 0.011 ?M. This compound holds promise for treating cancers with high TP expression, such as prostate cancer and hematological malignancies.

• Smiles:

  [C@H] (C (=O) N1[C@H] (C (O[C@H] (CCC2=CC (OC) =C (OC) C=C2) C3=CC (OCC (N (CCOCCOCCOCCOCCOCCOCCNS (=O) (=O) C4=CC=C (NC=5N=C (NC6=C (C (N) =O) C (F) =CC=C6) C (Br) =CN5) C=C4) C) =O) =CC=C3) =O) CCCC1) (CC) C7=CC (OC) =C (OC) C (OC) =C7

• Molecular Formula:

  C70H90BrFN8O19S

• Molecular Weight:

  1478.47

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  3077339-88-6