3077339-88-6
Chemical Structure
HLDA-212
- CAS No.: 3077339-88-6
- Formula:C70H90BrFN8O19S
- Molecular Weight:1478.47
InChIKey: RWOLQNVDQJTABL-KSYSBPRJSA-N
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
Biological Activity: 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[1].
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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. | |||||||||||||||||||||
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