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HLDA-212

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].

Product Specifications

CAS Number

3077339-88-6

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

Frequently Asked Questions

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