MS99-β-Gal
MS99-β-Gal (Gal-MS99) is a galactose-modified NPM-ALK PROTAC degrader. MS99-β-Gal is only hydrolyzed by SA-β-gal and esterase in senescent cancer cells, releasing MS99, which specifically degrades the NPM-ALK fusion protein. MS99-β-Gal shows an IC50 of 454.8 nM for aging Karpas 299 cells, significantly lower than that of normal Karpas 299 cells (IC50 = 2.162 μM). MS99-β-Gal can be used for the research of cancer.
(Pink: NPM-ALK ligand (HY-15656); Blue: VHL ligand (HY-112078); Black: linker).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3055593-63-7
- Formule: C78H96ClN9O20S2
- Masse moléculaire:1579.23
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| KARPAS-299 | IC50 |
2162 nM
Compound: Gal-MS99
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Antiproliferative activity against human normal (non-senescent) KARPAS-299 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human normal (non-senescent) KARPAS-299 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
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[PMID: 38635879] |
Chemical Information
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CAS No. 3055593-63-7
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Masse moléculaire 1579.23
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Formule C78H96ClN9O20S2
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SMILES
CC(O[C@@H]1[C@H]([C@H]([C@H](O[C@H]1OC2=CC=C(C=C2)COC(O[C@H]3CN([C@@H](C3)C(N[C@H](C4=CC=C(C5=C(C)N=CS5)C=C4)C)=O)C([C@H](C(C)(C)C)NC(CCCC(N6CCC(CC6)C7=CC(OC(C)C)=C(NC8=NC=C(C(NC9=C(S(=O)(C(C)C)=O)C=CC=C9)=N8)Cl)C=C7C)=O)=O)=O)=O)COC(C)=O)OC(C)=O)OC(C)=O)=O
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Synonyms
Gal-MS99
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Senescence-associated β-galactosidase staining
Senescence-associated β-galactosidase staining detects β-galactosidase activity that is histochemically visible at pH 6. 0 in senescent cells, where X-gal cleavage produces an insoluble blue precipitate observable by bright-field microscopy. This activity reflects increased lysosomal β-galactosidase/lysosomal mass rather than a senescence-essential enzyme, because GLB1 depletion or genetic lysosomal β-galactosidase deficiency can abolish SA-β-gal staining while cells still undergo senescence. SA-β-gal was originally reported in senescent but not presenescent fibroblasts and keratinocytes, absent from quiescent fibroblasts and terminally differentiated keratinocytes, and increased with donor age in human skin samples. Because SA-β-gal can also appear in some non-senescent or tissue-specific contexts, interpretation should be paired with experimental controls and, when possible, independent senescence markers.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)