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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
44 Results for "
PROTAC AKT degrader
" in MedChemExpress (MCE) Product Catalog:
Products (44)
44 Results for "PROTAC AKT degrader" in MCE Product Catalog:
2
2 Cited Publications
LC-2 is an orally active PROTAC-class degrader targeting KRAS G12C and a MAPK inhibitor. LC-2 shows higher selectivity for KRAS G12C than wild-type KRAS and other KRAS mutants. LC-2 covalently binds to KRAS G12C via the MRTX849 (HY-130149) warhead, recruits the VHL E3 ligase to form a ternary complex, and induces ubiquitination and degradation of KRAS G12C. Meanwhile, LC-2 inhibits the MAPK signaling pathway, reduces the phosphorylation levels of CRAF and AKT, thereby inducing apoptosis and suppressing cancer cell and tumor growth. LC-2 can be used for the research of KRAS G12C-positive cancers, including non-small cell lung cancer and colorectal cancer .
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2 Cited Publications
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
2
2 Cited Publications
TL13-112 is a ALK PROTAC degrader. TL13-112 degrades the NPM-ALK protein by recruiting the CRBN E3 ligase, thereby blocking oncogenic signal transduction such as STAT3, ERK and AKT, and relieving the transcriptional repression of CD45, CCR7 and PI3Kδ. TL13-112 can be used in related research on anaplastic large cell lymphoma .
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2 Cited Publications
Cat. No.: HY-133120A
Purity: 99.27%
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
1
1 Cited Publications
MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively .
Synonyms: ASP-3082; KRAS G12D inhibitor 17
Setidegrasib (ASP-3082) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib suppresses p-ERK, p-AKT, p-S6 levels in AsPC-1 cells. Setidegrasib exhibits anti-tumor activity in various cancer xenograft models in mice. Setidegrasib can be used in studies involving KRAS(G12D)-mutated solid tumors, such as non-small cell lung cancer .
MS21 is an effective AKT PROTAC degrader. MS21 can inhibit mutations in the PI3K/PTEN pathway, suppress the proliferation and induce cell cycle arrest of tumor cells. MS21 has anti-tumor activity. (Pink: AKT ligand-2 (HY-48682); Black: Linker (HY-W014125); Blue: (S,R,S)-AHPC (HY-125845)) .
Cat. No.: HY-168555
CAS No.: 3053716-98-3
YJ1206 is an orally active selective CDK12/CDK13 PROTAC degrader. YJ1206 induces DNA damage and genomic instability, activates the AKT pathway, and triggers apoptosis. YJ1206 reduces tumor cell viability, inhibits tumor growth, and attenuates tumor cell dissemination. YJ1206 is applicable to research related to prostate cancer and high-grade serous tubo-ovarian cancer .
Cat. No.: HY-174461
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 Ser 473 site in cancer cells and exhibits in vivo anticancer efficacy in xenograft models. PROTAC PI3Kα degrader-1 can be used in cancer-related research .
Cat. No.: HY-177008
CAS No.: 2897640-93-4
PROTAC HER2 degrader-1 is a selective HER2 PROTAC degrader with a DC50 of 69 nM. PROTAC HER2 degrader-1 induces ubiquitination and degradation of HER2 via the ubiquitin-proteasome system, thereby inhibiting the downstream PI3K/AKT/mTOR and RAS/RAF/MEK/ERK signaling pathways. PROTAC HER2 degrader-1 inhibits the proliferation of HER2-positive cancer cells, induces apoptosis and arrests the cell cycle. PROTAC HER2 degrader-1 suppresses the growth of HER2-positive xenografts. PROTAC HER2 degrader-1 can be used in HER2-positive cancer-related research .
Cat. No.: HY-143883
CAS No.: 2376137-41-4
MS143 is a VHL-recruiting AKT protein PROTAC degrader with a DC50 of 46 nM in PC3 prostate cancer cells. MS143 preferentially binds to AKT1 and AKT3, with weaker binding activity towards AKT2. MS143 degrades AKT and blocks the phosphorylation of downstream signaling molecules in the PI3K/AKT/mTOR pathway. MS143 inhibits cancer cell growth and xenograft tumor growth. MS143 can be used for research on prostate cancer, triple-negative breast cancer, and breast cancer .
Research Areas:
PTD10 is a selective and potent BTK PROTAC degrader (DC50 = 0.5 nM, KD = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease .
Synonyms: VH032-C8-NH2
Research Areas:
(S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) is a synthesized?E3 ligase ligand-linker conjugate?that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1 .
Cat. No.: HY-W998345
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models .
Cat. No.: HY-175975
CAS No.: 3048204-93-6
PROTAC Akt3 Degrader-1 is a highly efficient and selective PROTAC degrader targeting Akt3. PROTAC Akt3 Degrader-1 shows weak antiproliferative activity in 36 cell lines. PROTAC Akt3 Degrader-1 can be used for the study of Triple-negative breast cancer and melanoma .
Cat. No.: HY-176239
PROTAC 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 .
Cat. No.: HY-162589
Lw13 is a Hsp90 PROTAC degrader. Lw13 induces Hsp90 degradation via the ubiquitin-proteasome system, destabilizes client proteins HER2 and AKT, and blocks the activation of the HER2/AKT/mTOR signaling pathway. Lw13 inhibits the metastasis of cervical cancer cells, induces cell cycle arrest and apoptosis (apoptosis). Lw13 exerts synergistic anti-tumor activity with Cisplatin (HY-17394). Lw13 is applicable to cervical cancer-related research .
Cat. No.: HY-152145
CAS No.: 3029320-99-5
PROTAC SOS1 degrader-3 is a PROTAC degrader targeting SOS1, which induces the targeted degradation of SOS1 via the ubiquitin-proteasome system, with DC50 values ranging from 0.19 μM to 0.75 μM in multiple distinct colorectal cancer cell lines. PROTAC SOS1 degrader-3 inhibits the phosphorylation of AKT and ERK. PROTAC SOS1 degrader-3 induces apoptosis and morphological changes in KRAS-mutant colorectal cancer organoids. PROTAC SOS1 degrader-3 can be applied in studies related to kras-mutant colorectal cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
