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Formula | C24H27N5O3 |
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Molecular Weight | 433.5 | CAS No. | 1316214-52-4 | ||||
Solubility (25°C)* | In vitro | DMSO | 87 mg/mL (200.69 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2. | ||||||||||
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Targets |
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In vitro | ACY-1215 is a hydroxamic acid derivative. ACY-1215 is 12-, 10-, and 11-fold less active against HDAC1, HDAC2, and HDAC3 (class I HDACs), respectively. ACY-1215 has minimal activity (IC50 > 1μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2, and has slight activity against HDAC8 (IC50 = 0.1μM). The IC50 values for ACY-1215 for T-cell toxicity is 2.5μM. ACY-1215 overcomes tumor cell growth and survival conferred by BMSCs and cytokines in the BM milieu. |
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In vivo | ACY-1215 is readily absorbed by tumor tissue. Moreover, the drug does not accumulate in tumor tissue, as evidenced by the parallel decline of acetylated α-tubulin in blood cells and tumor tissue by 24 hours after dose. [1] |
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Features | Induced less cytotoxicity in PHA-stimulated PBMCs from 4 healthy donors compared with the pan-HDAC inhibitor SAHA. |
Kinase Assay: |
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, , Oncogene, 2017, 36(24):3450-3463
, , Mol Cancer Ther, 2015, 14(3):727-39.
Data from [Data independently produced by , , J Pathol, 2018, 246(2):141-153]
Data from [Data independently produced by , , Br J Cancer, 2018, 119(10):1278-1287]
HDAC6 inhibitor ACY-1215 enhances STAT1 acetylation to block PD-L1 for colorectal cancer immunotherapy [ Cancer Immunol Immunother, 2024, 73(1):7] | PubMed: 38231305 |
HDAC6 inhibitor ACY-1215 enhances STAT1 acetylation to block PD-L1 for colorectal cancer immunotherapy [ Cancer Immunol Immunother, 2024, 73(1):7] | PubMed: 38231305 |
HDAC Inhibition Induces CD26 Expression on Multiple Myeloma Cells via the c-Myc/Sp1-mediated Promoter Activation [ Cancer Res Commun, 2024, 4(2):349-364] | PubMed: 38284882 |
Histone Deacetylase 6 Inhibition Exploits Selective Metabolic Vulnerabilities in LKB1 Mutant, KRAS Driven NSCLC [ J Thorac Oncol, 2023, S1556-0864(23)00197-1] | PubMed: 36958689 |
The lysosomal Ragulator complex activates NLRP3 inflammasome in vivo via HDAC6 [ EMBO J, 2023, 42(1):e111389] | PubMed: 36444797 |
HDAC6 regulates human erythroid differentiation through modulation of JAK2 signalling [ J Cell Mol Med, 2023, 27(2):174-188] | PubMed: 36578217 |
Aggresome assembly at the centrosome is driven by CP110-CEP97-CEP290 and centriolar satellites [ Nat Cell Biol, 2022, 24(4):483-496] | PubMed: 35411088 |
Histone deacetylase 6 inhibition restores leptin sensitivity and reduces obesity [ Nat Metab, 2022, 4(1):44-59] | PubMed: 35039672 |
Uveal Melanoma Cell Line Proliferation Is Inhibited by Ricolinostat, a Histone Deacetylase Inhibitor [ Cancers (Basel), 2022, 14(3)782] | PubMed: 35159049 |
Ricolinostat enhances adavosertib‑induced mitotic catastrophe in TP53‑mutated head and neck squamous cell carcinoma cells [ Int J Oncol, 2022, 60(5)54] | PubMed: 35348191 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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