Chemical Structure : CAS-010
CAS No.:
CAS-010
(CAS010, CAS-13312-010)
Catalog No.: PC-25366Not For Human Use, Lab Use Only.
CAS-010 (CAS-13312-010) is a potent, selective and ubiquitin-competitive inhibitor of USP28 with IC50 of 4.2 nM in UbRho assays, disrupts the 53BP1-USP28 interaction and reduces p53 target gene transactivation.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CAS-010 (CAS-13312-010) is a potent, selective and ubiquitin-competitive inhibitor of USP28 with IC50 of 4.2 nM in UbRho assays, disrupts the 53BP1-USP28 interaction and reduces p53 target gene transactivation.
CAS-010 inhibits recombinant full-length (FL) USP28 with single-digit nanomolar potency (IC50=2.2 nM).
CAS-010 inhibits closely related USP25 with IC50 of 75 nM (USP25 CD) and 51 nM (USP25 FL).
CAS-010 blocks ABP labeling of USP28 and USP25 in a dose dependent manner in ABPP-MS experiment in HCT116 lysate, but not binding the other 57 DUBs de tected.
CAS-010 recapitulates the effects of USP28 genetic loss, both with respect to viability and p53 relationship.
CAS-010 attenuates p53 gene transactivation.
CAS-010 significantly decreases 53BP1-USP28 PLA foci in both cell lines and conditions in RPE-1 and U2OS cells, both with and without IR-induced DNA damage.
Physicochemical Properties
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M.Wt
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448.63
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Formula
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C26H32N4OS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(4-(8-azabicyclo[3.2.1]octan-3-yl)phenethyl)-3-amino-6-propylthieno[2,3-b]pyridine-2-carboxamide
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References
1. Bratt AS, et al. Cell Chem Biol. 2025 Sep 1:S2451-9456(25)00232-6.
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