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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
14 Results for "
gsk protac
" in MedChemExpress (MCE) Product Catalog:
Products (14)
14 Results for "gsk protac" in MCE Product Catalog:
2
2 Cited Publications
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
Synonyms: Molibresib carboxylic acid; gsk525762A carboxylic acid; protac BRD4-binding moiety 2
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I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1 .
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PT-65 is a GSK3α and GSK3β PROTAC degrader with DC50 values of 28.3 nM and 34.2 nM, respectively. PT-65 inhibits excessive tau phosphorylation mediated by GSK3β, Aβ and Okadaic acid (HY-N6785). PT-65 is applicable for the research of Alzheimer's disease .
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PROTAC GSK-3β Degrader-1 (compound 1) is a degrader targets GSK-3β PROTAC degrader with an IC50 value of 833 nM. PROTAC GSK-3β Degrader-1 contains SB-216763 (a GSK-3β inhibitor), a PEG linker and a CRBN (E3 ligase liand). PROTAC GSK-3β Degrader-1 reduces the neurotoxicity induced by Aβ25-35 peptide and CuSO4. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease .
Cat. No.: HY-122822
CAS No.: 2260944-68-9
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GSK699 is a KAT2A/B/PCAF/GCN5 PROTAC degrader . GSK699 induces proteasome-dependent degradation of KAT2A, KAT2B, PCAF and GCN5, regulates the histone acetyltransferase activity of the SAGA complex, and reduces the level of histone H3K9ac. GSK699 inhibits the growth of neuroblastoma, acute myeloid leukemia and small cell lung cancer cells. GSK699 reduces the production of inflammatory cytokines and chemokines, and impairs LPS-stimulated immune cell responses. GSK699 is applicable to research related to acute myeloid leukemia, small cell lung cancer, neuroblastoma and inflammatory diseases .
Synonyms: (R)-Molibresib carboxylic acid; (R)-gsk525762A carboxylic acid; (R)-protac BRD4-binding moiety 2
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(R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 value of 5.1 .
Cat. No.: HY-185634
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PROTAC GSK3 degrader-1 is a potent, blood-brain barrier-permeable GSK3 PROTAC degrader, with a DC50 of 1.4 nM against GSK3β. PROTAC GSK3 degrader-1 exerts equally potent degradation activity against both GSK3α and GSK3β. It inhibits the phosphorylation of CRMP2, PRKAA1 and Tau, and stabilizes β-catenin. PROTAC GSK3 degrader-1 can be used in the research of Alzheimer's disease and Parkinson's disease .
Cat. No.: HY-185635
GSK3 ligand-1 (GSK3 binder reagent 2) is a GSK3 ligand that can be used for the synthesis of PROTACs, such as PROTAC GSK3 degrader-1 (HY-185634) .
Cat. No.: HY-185009
CAS No.: 2260944-69-0
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GSK702, a PROTAC, is a the less active cis-(S,S)-enantiomer of GSK983 (P300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) PROTAC). GSK702 induces only a small decrease of PCAF protein levels. GSK702 binds to CRBN and causes a reduction of IL-1β in macrophages. GSK702 can be used for the study of inflammatory mediators .
Cat. No.: HY-W068828
CAS No.: 7300-34-7
Synonyms: 4,9-Dioxa-1,12-dodecanediamine
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1,4-Butanediol bis(3-aminopropyl) ether (4,9-Dioxa-1,12-dodecanediamine) is a PROTAC linker. Pent-4-yn-1-ol can be used to synthesize PROTAC molecules (e.g., PROTAC GSK-3β Degrader-1 (HY-149845)) .
Cat. No.: HY-182978
CAS No.: 2138439-13-9
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Pomalidomide-C3-O-C4-O-C3-NH2 is an E3 ligase ligand-linker conjugate that contains Pomalidomide (HY-10984). Pomalidomide-C3-O-C4-O-C3-NH2 can be used for the synthesis of PROTACs targeting glycogen synthase kinase 3β (GSK-3β), such as PROTAC GSK-3β Degrader-1 (HY-149845) .
Cat. No.: HY-107443R
CAS No.: 1300019-38-8
Synonyms: Molibresib carboxylic acid (Standard); gsk525762A carboxylic acid (Standard); protac BRD4-binding moiety 2 (Standard)
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I-BET762 carboxylic acid (Standard) is the analytical standard of I-BET762 carboxylic acid (HY-107443). This product is intended for research and analytical applications. I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1 .
Cat. No.: HY-107443AR
CAS No.: 1786401-70-4
Synonyms: (R)-Molibresib carboxylic acid (Standard); (R)-gsk525762A carboxylic acid (Standard); (R)-protac BRD4-binding moiety 2 (Standard)
Research Areas:
(R)-I-BET762 carboxylic acid (Standard) is the analytical standard of (R)-I-BET762 carboxylic acid (HY-107443A). This product is intended for research and analytical applications. (R)-I-BET762 carboxylic acid, the R-enantiomer of I-BET762 carboxylic acid (HY-107443). I-BET762 carboxylic acid is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid is a BRD4 inhibitor with a pIC50 value of 5.1 .
Cat. No.: HY-W1137162
CAS No.: 3107976-26-8
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CRBN ligand-904 is a ligand for the E3 ubiquitin ligase cereblon (CRBN), which is used to recruit cereblon protein. CRBN ligand-904 can be linked to a target protein ligand via a linker to form a PROTAC, such as PROTAC GSK3 degrader-1 (HY-185634) .
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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
