HLDA-212

• Description:

  HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP) . HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies) [1].

• UNSPSC:

  12352005

• Target:

  Apoptosis; Aurora Kinase

• Related Pathways:

  Apoptosis; Cell Cycle/DNA Damage; Epigenetics

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Smiles:

  CC[C@H](C(N1CCCC[C@H]1C(O[C@H](CCC2=CC=C(OC)C(OC)=C2)C3=CC=CC(OCC(N(C)CCOCCOCCOCCOCCOCCOCCNS(=O)(C4=CC=C(NC5=NC=C(Br)C(NC6=C(C(N)=O)C(F)=CC=C6)=N5)C=C4)=O)=O)=C3)=O)=O)C7=CC(OC)=C(OC)C(OC)=C7

• Molecular Formula:

  C70H90BrFN8O19S

• Molecular Weight:

  1478.47

• References & Citations:

  [1]Ma Z, et al. RIPTACs: A groundbreaking approach to drug discovery. Drug Discov Today. 2023 Nov;28 (11) :103774.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  Aurora A; Aurora B

• CAS Number:

  [3077339-88-6]