HLDA-212
HLDA-212 is a non-covalent RIPTAC that targets FKBP (target protein, TP) and multiple CDK (effector protein, EP). HLDA-212 binds to FKBP and CDK to form a stable ternary complex (TP:RIPTAC:EP), and induces cell death by blocking FKBP function. HLDA-212 selectively inhibits the proliferation of CDK-expressing cells and accumulates in CDK-expressing cells in a CDK-dependent manner. HLDA-212 exhibits antiproliferative activity in 293_HFL cells (with a GI50 of 0.011 μM). HLDA-212 holds promise for the treatment of cancers with high FKBP expression.
For research use only. We do not sell to patients.
- CAS No.: 3077339-88-6
- Formula: C70H90BrFN8O19S
- Molecular Weight:1478.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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Aurora A |
Aurora B |
In Vitro
HLDA-212 (Compound 43) (7 days; or 4 hours, followed by 7 days of cultivation without compound) selectively inhibits the proliferation of TP-expressing 293_HFL cells with a GI50 of 0.011 μM, showing a >900-fold greater potency than in TP-absent 293_GFPL cells[1].
HLDA-212 accumulates specifically in TP-expressing 293_HFL cells in a target protein-dependent manner[1].
HLDA-212 has reduced anti-proliferative potency in 293_MYRHF cells expressing plasma membrane-localized TP, indicating dependence on subcellular localization of target and effector proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3077339-88-6
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Molecular Weight 1478.47
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Formula C70H90BrFN8O19S
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HLDA-212 Related Classifications
HY-173499 Related Classifications
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