PI3K Degrader
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PROTAC PI3Kα degrader-1
0 ImagesCat. No.: HY-174461Purity: 99.21%PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader (DC50 = 0.08 μM), demonstrating good selectivity for PI3Kα degradation over PI3Kβ, PI3Kγ, and PI3Kδ. PROTAC PI3Kα degrader-1 effectively degrades PI3Kα in a time- and concentration-dependent, over PI3Kβ, PI3Ky and PI3Kδ, and potently inhibited the phosphorylation of AKT at the Ser473site. PROTAC PI3Kα degrader-1 shows significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models.
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GP262
0 ImagesGP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. GP262 induces degradation of p110α and p110γ with a DC50 of 227.4 and 42.23 nM. GP262 efficient modulates the PI3K/AKT/mTOR pathway, achieving degradation through the ubiquitin-proteasome system (UPS). GP262 also exhibits robust antiproliferative activity and induces apoptosis in vitro. GP262 exhibits tumor growth suppression capability and biosafety profile. GP262 can be used for leukemia and triple-negative breast cancer (TNBC) .
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PROTAC PI3Kα/δ degrader-1
0 ImagesCat. No.: HY-182083PROTAC PI3Kα/δ degrader-1 is an orally active PI3Kα/δ PROTAC degrader, with an IC50 of 0.34 nM for PI3Kα and 1.85 nM for PI3Kδ. PROTAC PI3Kα/δ degrader-1 inhibits the proliferation and migration of cancer cells, induces G1-phase cell cycle arrest and PI3Kα degradation. PROTAC PI3Kα/δ degrader-1 suppresses tumor growth in breast cancer xenograft mouse models. PROTAC PI3Kα/δ degrader-1 can be used for the research of breast cancer.
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PROTAC PI3Kδ degrader-1
0 ImagesCat. No.: HY-176239PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model.
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PROTAC PI3K/110β degrader-2
0 ImagesCat. No.: HY-174469CAS No.: 3070438-79-5PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer.
