PI3K Degrader
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HaloPROTAC-E
0 ImagesHaloPROTAC-E is a SGK3/VPS34 HaloPROTAC degrader that degrades Halo-tagged SGK3 and VPS34, with a DC50 of 3-10 nM in HEK293 cells. HaloPROTAC-E induces ubiquitination and proteasomal degradation of target proteins. HaloPROTAC-E blocks downstream phosphorylation of SGK3 substrate NDRG1. HaloPROTAC-E is applicable for cancer research.
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PROTAC PI3Kα degrader-1
0 ImagesCat. No.: HY-174461Purity: 99.21%PROTAC PI3Kα degrader-1 is a PI3Kα PROTAC degrader that recruits CRBN, with a DC50 of 0.08 μM in T47D breast cancer cells. PROTAC PI3Kα degrader-1 inhibits the phosphorylation of AKT at the Ser473 site in cancer cells and exhibits in vivo anticancer efficacy in xenograft models. PROTAC PI3Kα degrader-1 can be used in cancer-related research.
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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 PI3K/110β degrader-1
0 ImagesCat. No.: HY-176421CAS No.: 3070438-85-3PROTAC PI3K/110β degrader-1 is a VHL-recruiting PROTAC degrader targeting PI3K/110β, with DC50 values of 0.416 μM (MCF-7) and 19.66 μM (A549), respectively. PROTAC PI3K/110β degrader-1 recruits VHL to induce proteasomal degradation of PI3K/110β. It activates endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis via the PERK/ATF4/CHOP unfolded protein response (UPR) pathway, downregulates p-AKT and Bcl-2, upregulates Bax, cleaved-caspase-9 and cleaved-caspase-3, inhibits the expression and activity of P-gp, and exerts synergistic anti-tumor effects with Doxorubicin (Adriamycin, ADM) (HY-15142A) and Cisplatin (DDP) (HY-17394). PROTAC PI3K/110β degrader-1 can be used in research related to multidrug-resistant cancers.
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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 VHL-recruiting PI3K/110β PROTAC degrader, with DC50 values of 1.258 μM and 2.185 μM in MCF-7/ADM and A549/DDP cells, respectively. PROTAC PI3K/110β degrader-2 induces proteasomal degradation of PI3K/110β, inhibits phosphorylation of AKT and expression of Bcl-2, while suppressing the activity and expression of P-gp. It also induces endoplasmic reticulum stress and mitochondrial apoptosis via the PERK/CHOP pathway. PROTAC PI3K/110β degrader-2 exerts anti-tumor activity against multidrug-resistant cancer cells both in vitro and in vivo, and produces a synergistic effect when combined with Doxorubicin (HY-15142A) or Cisplatin (HY-17394), making it applicable for the research of multidrug-resistant cancers.
