dCBP-1 |
| Katalog-Nr.GC62211 |
dCBP-1 ist ein potenter und selektiver heterobifunktioneller Abbauer von p300/CBP auf der Basis von Cereblon-Liganden. dCBP-1 ist außergewÖhnlich wirksam bei der AbtÖtung multipler Myelomzellen und schwÄcht die onkogene Enhancer-AktivitÄt ab, die die MYC-Expression antreibt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2484739-25-3
Sample solution is provided at 25 µL, 10mM.
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dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression[1].
dCBP-1 (10-1000 nM; 6 hours) treatment shows near-complete degradation of p300/CBP in MM1S cells. dCBP-1 is also able to induce near-complete p300/CBP degradation across other multiple myeloma cell lines tested, including MM1R, KMS-12-BM, and KMS34[1].Treatment of the human haploid cell line HAP1 for 6 h with dCBP-1 reveals almost complete loss of both CBP and p300 between 10 and 1000 nM doses. A time course analysis with 250 nM dCBP-1 revealed almost complete degradation of p300/CBP within an hour of treatment[1].
[1]. Raghu Vannam, et al. Targeted degradation of the enhancer lysine acetyltransferases CBP and p300. Cell Chem Biol. 2020 Dec 31;S2451-9456(20)30513-4.
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