1834513-65-3
Chemical Structure
Bocodepsin
Synonym(s): OKI-179
- CAS No.: 1834513-65-3
- Formula:C26H39N5O6S2
- Molecular Weight:581.75
InChIKey: YBLKKAYDPCHCJG-IQGTVIFDSA-N
SMILES: O=C1C2=CSC(CNC(C[C@H](OC([C@@H](NC(C(C)(N1)C)=O)C(C)C)=O)/C=C/CCSC([C@@H](N)C(C)C)=O)=O)=N2
Biological Activity: Bocodepsin (OKI-179) is an orally active class I HDAC inhibitor. Bocodepsin is metabolized in vivo to the active metabolite OKI-006 (HY-144893), which then targets and inhibits class I HDAC (HDAC-1, 2, 3, 8), activating the apoptosis pathway by increasing the acetylation levels of histone H3 and p21 (upregulating BIM, decreasing BCL-XL, and inducing Caspase-3 cleavage), while also upregulating the expression of MHC class I and class II molecules and PD-L1 on tumor cells in the immune microenvironment, thereby increasing intratumoral CD4+ and CD8+ T cell infiltration and restoring their antitumor immunity. Bocodepsin can be used for research on colorectal cancer, triple-negative breast cancer, and B-cell lymphoma[1][2][3].
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Bocodepsin | 98.01% | Bocodepsin (OKI-179) is an orally active class I HDAC inhibitor. Bocodepsin is metabolized in vivo to the active metabolite OKI-006 (HY-144893), which then targets and inhibits class I HDAC (HDAC-1, 2, 3, 8), activating the apoptosis pathway by increasing the acetylation levels of histone H3 and p21 (upregulating BIM, decreasing BCL-XL, and inducing Caspase-3 cleavage), while also upregulating the expression of MHC class I and class II molecules and PD-L1 on tumor cells in the immune microenvironment, thereby increasing intratumoral CD4+ and CD8+ T cell infiltration and restoring their antitumor immunity. Bocodepsin can be used for research on colorectal cancer, triple-negative breast cancer, and B-cell lymphoma. | ||||||||||||||||||||
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Similarity Score 0.99
HY-156602ABocodepsin hydrochloride -
Similarity Score 0.82
HY-144893OKI-006 -
Similarity Score 0.82
HY-185584OKI-005 -
Similarity Score 0.61
HY-13906Largazole -
Similarity Score 0.60
HY-170890Largazole thiol -
Similarity Score 0.45
HY-15149Romidepsin -
Similarity Score 0.44
HY-P2792Beauveriolide III -
Similarity Score 0.43
HY-N12591Iso-isariin B -
Similarity Score 0.43
HY-N8355Beauveriolide I -
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References
- [1]. Diamond JR, et al. Preclinical Development of the Class-I-Selective Histone Deacetylase Inhibitor OKI-179 for the Treatment of Solid Tumors. Molecular cancer therapeutics. 2022 Mar 01;21(3):397-406. [Content Brief]
- [2]. Smoots SG, et al. Overcoming doxorubicin resistance in triple-negative breast cancer using the class I-targeting HDAC inhibitor bocodepsin/OKI-179 to promote apoptosis. Breast Cancer Res. 2024 Mar 1;26(1):35. [Content Brief]
- [3]. Wang X, et al. Histone Deacetylase Inhibition Sensitizes PD1 Blockade-Resistant B-cell Lymphomas. Cancer immunology research. 2019 Aug;7(8):1318-1331.
