RIPTACs
Regulated Induced Proximity Targeting Chimeras; RIPTAC
RIPTAC (Regulated Induced Proximity Targeting Chimera) is a heterobifunctional small molecule based on the principle of molecular proximity. It induces the formation of a stable ternary complex between a target protein (TP)—selectively expressed in tumor cells—and an effector protein (EP) that is essential for cell survival. The resulting synergistic protein-protein interaction (PPI) inhibits the function of this essential protein, thereby selectively causing the death of cells that express the target protein (TP)[1][2].
Verweise:
- [1]. Raina K, et al. Regulated induced proximity targeting chimeras-RIPTACs-A heterobifunctional small molecule strategy for cancer selective therapies. Cell Chem Biol. 2024 Aug 15;31(8):1490-1502.e42. [Content Brief]
- [2]. Ma Z, et al. RIPTACs for Precision Cancer Therapy: A Novel Modality with the Inspiration of HLD-0915 as the First Candidate in Clinical Trials. J Med Chem. 2025 Jun 12;68(11):10503-10506.
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RIPTACs Verwandte Produkte (5)
Verwandte Produkte (5)
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AR/BRD4 RIPTAC-1
0 ImagesAR/BRD4 RIPTAC-1 (Compound II-5) is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 holds promise for use in prostate cancer research.
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AR/BRD4 RIPTAC-1 TFA
0 ImagesArt. -Nr.: HY-176521AAR/BRD4 RIPTAC-1 (Compound II-5) TFA is an orally active Regulatory-inducible proximity-targeting chimera (RIPTAC). AR/BRD4 RIPTAC-1 TFA induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 TFA inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 TFA holds promise for use in prostate cancer research.
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HLDA-212
0 ImagesArt. -Nr.: HY-173499CAS. Nr.: 3077339-88-6HLDA-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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(R)-AR/BRD4 RIPTAC-1
0 Images(R)-AR/BRD4 RIPTAC-1 is the R-enantiomer of AR/BRD4 RIPTAC-1 (HY-176521). AR/BRD4 RIPTAC-1 is an orally active Regulated Induced Proximity TArgeting Chimera (RIPTAC). AR/BRD4 RIPTAC-1 induces the formation of a stable ternary complex between the androgen receptor (AR) and BRD4, thereby blocking BRD4 function. AR/BRD4 RIPTAC-1 inhibits the growth and proliferation of tumor cells. AR/BRD4 RIPTAC-1 holds promise for research into prostate cancer.
