Ricolinostat
Based on 45 publication(s) in Google Scholar
Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 1316214-52-4
- Formula: C24H27N5O3
- Molecular Weight:433.50
-
Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
Publications Citing Use of MedChemExpress (MCE) Ricolinostat
More- Blood. 2019 Oct 17;134(16):1323-1336. [Abstract]
- Nat Commun. 2023 Oct 17;14(1):6547. [Abstract]
- Leukemia. 2019 Jul;33(7):1675-1686. [Abstract]
- J Exp Clin Cancer Res. 2025 Feb 24;44(1):67. [Abstract]
- J Control Release. 2025 Feb 5:380:125-137. [Abstract]
- Cell Mol Biol Lett. 2024 Jan 3;29(1):8. [Abstract]
- J Neuroinflammation. 2025 Mar 11;22(1):74. [Abstract]
- Cancer Lett. 2016 Aug 28;379(1):134-142. [Abstract]
- NPJ Precis Oncol. 2024 Mar 7;8(1):66. [Abstract]
- Biomed Pharmacother. 2019 Jan:109:2464-2471. [Abstract]
- Oncogene. 2021 Mar;40(12):2323-2334. [Abstract]
- Oncogene. 2018 Nov;37(45):5952-5966. [Abstract]
- Cell Death Discov. 2024 Jun 8;10(1):275. [Abstract]
- J Med Chem. 2025 Feb 20. [Abstract]
- Fluids Barriers CNS. 2025 May 7;22(1):45. [Abstract]
- Cells. 2026 Apr 10;15(8):673. [Abstract]
- Life Sci. 2025 Apr 1:366-367:123498. [Abstract]
- Commun Biol. 2024 Oct 4;7(1):1257. [Abstract]
- Pharmaceuticals (Basel). 2025 Aug 29;18(9):1303. [Abstract]
- Int Immunopharmacol. 2026 Mar 1:172:116254. [Abstract]
- Int Immunopharmacol. 2025 May 18:158:114884. [Abstract]
- Int Immunopharmacol. 2024 Sep 30;143(Pt 1):113270. [Abstract]
- Cancers (Basel). 2022 Feb 3;14(3):782. [Abstract]
- Cancers. 2019 Sep 7;11(9):1327. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Jun;1870(5):167137. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- iScience. 2024 Apr 6;27(5):109678. [Abstract]
- Oncol Rep. 2017 Feb;37(2):1270-1276. [Abstract]
- Med Oncol. 2016 May;33(5):50. [Abstract]
- Theriogenology. 2022 Apr 15:183:98-107. [Abstract]
- Anticancer Res. 2022 Jan;42(1):471-482. [Abstract]
- SSRN. 2026 May 21.
- bioRxiv. 2025 Oct 30.
- bioRxiv. 2025 Oct 4:2025.10.03.680349. [Abstract]
- University of Pittsburgh. 2025.
- Patent. US20250161243A1.
- bioRxiv. 2025 April 26.
- McGill University. 2023 Dec.
- Research Square Print. 2023 Mar 9.
- Res Sq. 2023 Jan 27:rs.3.rs-2440581. [Abstract]
- bioRxiv. 2021 Dec.
- Patent. US20210290612A1.
- bioRxiv. 2021 Jan 5.
- Albert-ludwigs-university Of Freiburg. 2019 Dec.
- Patent. US20180263995A1.
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Biological Activity
|
HDAC6 4.7 nM (IC50) |
HDAC2 48 nM (IC50) |
HDAC3 51 nM (IC50) |
HDAC1 58 nM (IC50) |
HDAC8 100 nM (IC50) |
HDAC7 1400 nM (IC50) |
HDAC5 5000 nM (IC50) |
HDAC4 7000 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 697 | IC50 |
201 nM
Compound: Ricolinostat
|
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human 697 cells after 48 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 31710483] |
| A2780 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
Cytotoxicity against human A2780 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| A549 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| A549 | IC50 |
7.7 μM
Compound: ACY1215
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 30525585] |
| HAL-01 | IC50 |
>25 μM
Compound: Ricolinostat
|
Anticancer activity against human HAL-01 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
Anticancer activity against human HAL-01 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
|
[PMID: 34582215] |
| HAL-01 | IC50 |
2.04 μM
Compound: Ricolinostat
|
Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human HAL-01 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 36351184] |
| HCT-116 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| HCT-116 | IC50 |
1.85 μM
Compound: ACY-1215
|
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 36182802] |
| HEL | IC50 |
2.54 μM
Compound: 28; ACY1215
|
Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
|
[PMID: 29940115] |
| HEL | IC50 |
3.75 μM
Compound: 28; ACY1215
|
Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay
|
[PMID: 29940115] |
| HeLa | IC50 |
>5000 nM
Compound: ACY-1215
|
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| HepG2 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| HL-60 | IC50 |
2.54 μM
Compound: 28; ACY1215
|
Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
|
[PMID: 29940115] |
| HL-60 | IC50 |
3.75 μM
Compound: 28; ACY1215
|
Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay
|
[PMID: 29940115] |
| HL-60 | IC50 |
2.36 μM
Compound: Ricolinostat
|
Cytotoxicity against human HL60 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human HL60 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 30365892] |
| HL-60 | IC50 |
>10000 nM
Compound: Ricolinostat
|
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability for 72 hrs by Celltitre-Glo luminescent assay
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability for 72 hrs by Celltitre-Glo luminescent assay
|
[PMID: 33360560] |
| HL-60 | IC50 |
10.37 μM
Compound: Ricolinostat
|
Anticancer activity against human HL-60 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
Anticancer activity against human HL-60 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
|
[PMID: 34582215] |
| HL-60 | IC50 |
1.54 μM
Compound: Ricolinostat
|
Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human HL-60 cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 36351184] |
| HPBALL | IC50 |
6.7 μM
Compound: Ricolinostat
|
Anticancer activity against human HPBALL cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
Anticancer activity against human HPBALL cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
|
[PMID: 34582215] |
| HT-29 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| HUVEC | IC50 |
13.62 μM
Compound: ACY-1215
|
Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay
Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 36182802] |
| Jurkat | IC50 |
2.42 μM
Compound: Ricolinostat
|
Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 36351184] |
| K562 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| K562 | IC50 |
2.54 μM
Compound: 28; ACY1215
|
Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay
|
[PMID: 29940115] |
| K562 | IC50 |
3.75 μM
Compound: 28; ACY1215
|
Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay
|
[PMID: 29940115] |
| K562 | IC50 |
6.02 μM
Compound: Ricolinostat
|
Anticancer activity against human K562 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
Anticancer activity against human K562 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
|
[PMID: 34582215] |
| KCL-22 | IC50 |
3.38 μM
Compound: Ricolinostat
|
Cytotoxicity against imatinib-resistant human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against imatinib-resistant human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 30365892] |
| KCL-22 | IC50 |
3.75 μM
Compound: Ricolinostat
|
Cytotoxicity against human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 30365892] |
| KCL-22 | IC50 |
3.75 μM
Compound: Ricolinostat
|
Cytotoxicity against human KCL-22 cells
Cytotoxicity against human KCL-22 cells
|
[PMID: 33077264] |
| KM12 | IC50 |
2.15 μM
Compound: ACY-1215
|
Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 36182802] |
| MDA-MB-468 | IC50 |
4.919 μM
Compound: ACY-1215
|
Cytotoxicity against human MDA-MB-468 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay
Cytotoxicity against human MDA-MB-468 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay
|
[PMID: 37797564] |
| MM1.S | IC50 |
2 μM
Compound: 18; ACY-1215
|
Cytotoxicity against human MM1.S cells incubated for 48 hrs by MTT assay
Cytotoxicity against human MM1.S cells incubated for 48 hrs by MTT assay
|
[PMID: 29133060] |
| MM1.S | EC50 |
0.85 nM
Compound: ACY-1215
|
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability after 144 hrs
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability after 144 hrs
|
[PMID: 33359604] |
| MM1.S | IC50 |
0.84 μM
Compound: ACY-1215
|
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
|
[PMID: 35119267] |
| MV4-11 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human MV4-11 cells after 72 hrs by MTT assay
Cytotoxicity against human MV4-11 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| MV4-11 | IC50 |
0.656 μM
Compound: 5
|
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
|
[PMID: 32615502] |
| MV4-11 | IC50 |
0.81 μM
Compound: ACY-1215
|
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
|
[PMID: 34101461] |
| MV4-11 | IC50 |
0.656 μM
Compound: ACY-1215
|
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
|
[PMID: 35119267] |
| MV4-11 | EC50 |
0.71 μM
Compound: ACY-1215
|
Antiproliferative activity against human MV4-11 cells assessed as cell viability by measuring amount of ATP after 72 hrs incubation by CellTiteer-Glo Cell viability assay
Antiproliferative activity against human MV4-11 cells assessed as cell viability by measuring amount of ATP after 72 hrs incubation by CellTiteer-Glo Cell viability assay
|
[PMID: 39067437] |
| NCI-H460 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human H460 cells after 72 hrs by MTT assay
Cytotoxicity against human H460 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| NCI-H929 | GI50 |
>100 μM
Compound: 3; ACY-1215
|
Antiproliferative activity against human NCI-H929 cells after 48 hrs by SRB assay
Antiproliferative activity against human NCI-H929 cells after 48 hrs by SRB assay
|
[PMID: 29304284] |
| OPM-2 | IC50 |
2 μM
Compound: 18; ACY-1215
|
Cytotoxicity against human OPM-2 cells incubated for 48 hrs by MTT assay
Cytotoxicity against human OPM-2 cells incubated for 48 hrs by MTT assay
|
[PMID: 29133060] |
| PBMC | IC50 |
<3.6 μM
Compound: Ricolinostat
|
Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 30365892] |
| Ramos | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human Ramos cells after 72 hrs by MTT assay
Cytotoxicity against human Ramos cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| REH | IC50 |
>25 μM
Compound: Ricolinostat
|
Anticancer activity against human REH cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
Anticancer activity against human REH cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
|
[PMID: 34582215] |
| RPMI-8226 | IC50 |
1468 nM
Compound: ACY-1215
|
Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay
Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| RPMI-8226 | GI50 |
6.4 μM
Compound: 3; ACY-1215
|
Antiproliferative activity against human RPMI8226 cells after 48 hrs by SRB assay
Antiproliferative activity against human RPMI8226 cells after 48 hrs by SRB assay
|
[PMID: 29304284] |
| RPMI-8226 | IC50 |
11 μM
Compound: ACY-1215
|
Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay
Growth inhibition of human RPMI8226 cells after 72 hrs by MTT assay
|
[PMID: 30594434] |
| RPMI-8226 | IC50 |
9.26 μM
Compound: ACY-1215
|
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay
|
[PMID: 31865013] |
| RPMI-8226 | IC50 |
1.5 μM
Compound: 1; ACY-1215
|
Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue dye based assay
Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition incubated for 72 hrs by alamar blue dye based assay
|
[PMID: 37660484] |
| RPMI-8226 | IC50 |
1.191 μM
Compound: ACY-1215
|
Cytotoxicity against human RPMI-8226 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay
Cytotoxicity against human RPMI-8226 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay
|
[PMID: 37797564] |
| SEM | IC50 |
1.61 μM
Compound: Ricolinostat
|
Cytotoxicity against human SEM cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human SEM cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 30365892] |
| SEM | IC50 |
1.61 μM
Compound: Ricolinostat
|
Cytotoxicity against human SEM cells
Cytotoxicity against human SEM cells
|
[PMID: 33077264] |
| Sf9 | IC50 |
5 nM
Compound: ACY-1215
|
Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay
Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay
|
[PMID: 30594434] |
| Sf9 | IC50 |
74 nM
Compound: ACY-1215
|
Inhibition of full length recombinant human C-terminal FLAG-tagged HDAC1 expressed in sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay
Inhibition of full length recombinant human C-terminal FLAG-tagged HDAC1 expressed in sf9 cells preincubated for 5 mins followed by biotinylated H3K9-Ac substrate addition and measured after 60 mins by HTRF assay
|
[PMID: 30594434] |
| Sf9 | IC50 |
4.7 nM
Compound: ACY-1215
|
Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a
Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a
|
[PMID: 31414801] |
| Sf9 | IC50 |
58 nM
Compound: ACY-1215
|
Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr
Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr
|
[PMID: 31414801] |
| Sf9 | IC50 |
12 nM
Compound: Ricolinostat
|
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
Inhibition of recombinant full length human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 insect cells pretreated with compound followed by Fluor de Lys deacetylase substrate addition by fluorescence method
|
[PMID: 31710483] |
| Sf9 | IC50 |
>1 μM
Compound: ACY1215
|
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
|
[PMID: 31938464] |
| Sf9 | IC50 |
0.379 μM
Compound: ACY1215
|
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
|
[PMID: 31938464] |
| SK-BR-3 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay
Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| SK-OV-3 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| SU-DHL-6 | IC50 |
0.83 μM
Compound: ACY-1215
|
Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 36182802] |
| SUP-B15 | IC50 |
1.92 μM
Compound: Ricolinostat
|
Cytotoxicity against human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 30365892] |
| SUP-B15 | IC50 |
3.54 μM
Compound: Ricolinostat
|
Cytotoxicity against imatinib-resistant human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against imatinib-resistant human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 30365892] |
| T47D | IC50 |
0.71 μM
Compound: ACY-1215
|
Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay
|
[PMID: 36182802] |
| TALL-1 | IC50 |
3.88 μM
Compound: Ricolinostat
|
Anticancer activity against human TALL-1 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
Anticancer activity against human TALL-1 cells assessed as cell growth inhibition by CellTiter-Glo luminescent assay
|
[PMID: 34582215] |
| U-266 | IC50 |
>5000 nM
Compound: ACY-1215
|
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
|
[PMID: 26443078] |
| U-266 | GI50 |
>100 μM
Compound: 3; ACY-1215
|
Antiproliferative activity against human U266 cells after 48 hrs by SRB assay
Antiproliferative activity against human U266 cells after 48 hrs by SRB assay
|
[PMID: 29304284] |
| U-266 | IC50 |
3.52 μM
Compound: Ricolinostat
|
Cytotoxicity against human U266 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human U266 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 30365892] |
| U-266 | IC50 |
21.2 μM
Compound: ACY-1215
|
Growth inhibition of human U266 cells after 72 hrs by MTT assay
Growth inhibition of human U266 cells after 72 hrs by MTT assay
|
[PMID: 30594434] |
| U-266 | IC50 |
>100 μM
Compound: ACY-1215
|
Antiproliferative activity against human U-266 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay
Antiproliferative activity against human U-266 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay
|
[PMID: 31865013] |
Ricolinostat (ACY-1215) has slight activity against HDAC8 (IC50=0.1 μM), and has minimal activity (IC50>1 μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2. The effect of Ricolinostat (ACY-1215) on multiple myeloma (MM) cell viability is determined with MTT assays using MM cell lines. Exposure of MM cell lines for 48 hours results in dose-dependent decreased viability, with IC50 values ranging from 2-8μM. Ricolinostat (ACY-1215) demonstrates significant activity in the MM PS-341-resistant cell line (ANBL-6.BR), demonstrating the ability of Ricolinostat (ACY-1215) to overcome PS-341 resistance[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1316214-52-4
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Appearance Solid
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Molecular Weight 433.50
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Formula C24H27N5O3
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Color White to off-white
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SMILES
O=C(C1=CN=C(N(C2=CC=CC=C2)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O
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Synonyms
ACY-1215; Rocilinostat
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
Publications (45)
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Journal Impact Factor
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Most Recent
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Blood
Suz12 inactivation cooperates with JAK3 mutant signaling in the development of T-cell acute lymphoblastic leukemia. [Abstract]2019 Oct 17;134(16):1323-1336. PMID: 31492675 -
Nat Commun
Neural deficits in a mouse model of PACS1 syndrome are corrected with PACS1- or HDAC6-targeting therapy. [Abstract]2023 Oct 17;14(1):6547. PMID: 37848409 -
Leukemia
Functional cooperativity of p97 and histone deacetylase 6 in mediating DNA repair in mantle cell lymphoma cells. [Abstract]2019 Jul;33(7):1675-1686. PMID: 30664664 -
J Exp Clin Cancer Res
CD47 blockade reverses resistance to HDAC inhibitor by liberating anti-tumor capacity of macrophages. [Abstract]2025 Feb 24;44(1):67. PMID: 39994810 -
J Control Release
Polymer-based nanodrugs enhance sonodynamic therapy through epigenetic reprogramming of the immunosuppressive tumor microenvironment. [Abstract]2025 Feb 5:380:125-137. PMID: 39892649 -
Cell Mol Biol Lett
2024 Jan 3;29(1):8. PMID: 38172700 -
J Neuroinflammation
Inhibition of histone deacetylase 6 alleviates neuropathic pain via direct regulating post-translation of spinal STAT3 and decreasing downstream C-C Motif Chemokine Ligand 7 synthesis. [Abstract]2025 Mar 11;22(1):74. PMID: 40069860 -
Cancer Lett
HDAC6 promotes cell proliferation and confers resistance to temozolomide in glioblastoma. [Abstract]2016 Aug 28;379(1):134-142. PMID: 27267806
Ricolinostat purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2016 Aug 28;379(1):134-142. [Abstract]
Inhibition of HDAC6 by HDAC6-selective inhibitors impairs the proliferation of glioblastoma cells. U87 and U251 cells are treated with HDAC6 selective inhibitors and the cells are harvested for subsequent western blot analysis.
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NPJ Precis Oncol
Connectivity mapping-based identification of pharmacological inhibitor targeting HDAC6 in aggressive pancreatic ductal adenocarcinoma. [Abstract]2024 Mar 7;8(1):66. PMID: 38454151 -
Biomed Pharmacother
ACY-1215 exhibits anti-inflammatory and chondroprotective effects in human osteoarthritis chondrocytes via inhibition of STAT3 and NF-κB signaling pathways. [Abstract]2019 Jan:109:2464-2471. PMID: 30551507
Ricolinostat purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2019 Jan:109:2464-2471. [Abstract]
The expression of IL-1β and IL-6 in human primary chondrocytes and C28/I2 cells is tested by western blot analysis with the treatment of IL-1β, DMSO and ACY-1215.
Ricolinostat purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2019 Jan:109:2464-2471. [Abstract]
The expression of MMP-1, MMP-13 and COL2 A1 in C28/I2 cells is tested by western blot analysis with the treatment of IL-1β, DMSO and ACY-1215.
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Oncogene
Tektin4 loss promotes triple-negative breast cancer metastasis through HDAC6-mediated tubulin deacetylation and increases sensitivity to HDAC6 inhibitor. [Abstract]2021 Mar;40(12):2323-2334. PMID: 33654196 -
Oncogene
Histone deacetylase 6 regulates the immunosuppressive properties of cancer-associated fibroblasts in breast cancer through the STAT3-COX2-dependent pathway. [Abstract]2018 Nov;37(45):5952-5966. PMID: 29980788
Ricolinostat purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 Nov;37(45):5952-5966. [Abstract]
Mouse CAFs are treated with increasing concentrations of ACY1215 for 24 h. Western blot analysis of tubulin, histone H3, histone H4, acetylated tubulin, acetylated histone H3, and acetylated histone H4.
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Cell Death Discov
Deacetylated MDH1 and IDH1 aggravates PANoptosis in acute liver failure through endoplasmic reticulum stress signaling. [Abstract]2024 Jun 8;10(1):275. PMID: 38851781 -
J Med Chem
Discovery of Novel and Highly Potent Dual PD-L1/Histone Deacetylase 6 Inhibitors with Favorable Pharmacokinetics for Cancer Immunotherapy. [Abstract]2025 Feb 20. PMID: 39979078 -
Fluids Barriers CNS
Inhibition of histone deacetylase 6 activity mitigates neurological impairment and post-hemorrhagic hydrocephalus after intraventricular hemorrhage by modulating pyroptosis and autophagy pathways. [Abstract]2025 May 7;22(1):45. PMID: 40336077 -
Cells
HDAC Inhibition Induces Transient Phenotypic Inertia in Dormant OCCC Spheroids by Derepression of Cell Cycle Genes. [Abstract]2026 Apr 10;15(8):673. PMID: 42041541 -
Life Sci
Targeting the HDAC6/Hint2/MICU1 axis to ameliorate acute liver failure via inhibiting NETosis. [Abstract]2025 Apr 1:366-367:123498. PMID: 39983829 -
Commun Biol
Selective inhibition of HDAC class IIA as therapeutic intervention for KMT2A-rearranged acute lymphoblastic leukemia. [Abstract]2024 Oct 4;7(1):1257. PMID: 39362994 -
Pharmaceuticals (Basel)
Discovery of a Promising Hydroxyamino-Piperidine HDAC6 Inhibitor via Integrated Virtual Screening and Experimental Validation in Multiple Myeloma. [Abstract]2025 Aug 29;18(9):1303. PMID: 41011174 -
Int Immunopharmacol
Acetylation of Hint2 mitigates acute liver failure by suppressing neutrophil chemotaxis and NETosis through maintaining mitochondrial calcium and protein homeostasis. [Abstract]2026 Mar 1:172:116254. PMID: 41570743 -
Int Immunopharmacol
IDH1/MDH1 deacetylation activates the cGAS-STING pathway by promoting NETosis in acute liver failure. [Abstract]2025 May 18:158:114884. PMID: 40388861 -
Int Immunopharmacol
2024 Sep 30;143(Pt 1):113270. PMID: 39353390 -
Cancers (Basel)
Uveal Melanoma Cell Line Proliferation Is Inhibited by Ricolinostat, a Histone Deacetylase Inhibitor. [Abstract]2022 Feb 3;14(3):782. PMID: 35159049 -
Cancers
Selective Inhibition of Histone Deacetylases 1/2/6 in Combination with Gemcitabine: A Promising Combination for Pancreatic Cancer Therapy. [Abstract]2019 Sep 7;11(9):1327. PMID: 31500290 -
Biochim Biophys Acta Mol Basis Dis
Hippocampal HDAC6 promotes POCD by regulating NLRP3-induced microglia pyroptosis via HSP90/HSP70 in aged mice. [Abstract]2024 Jun;1870(5):167137. PMID: 38527593 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
iScience
The acetylation of MDH1 and IDH1 is associated with energy metabolism in acute liver failure. [Abstract]2024 Apr 6;27(5):109678. PMID: 38660411 -
Oncol Rep
ACY-1215 accelerates vemurafenib induced cell death of BRAF-mutant melanoma cells via induction of ER stress and inhibition of ERK activation. [Abstract]2017 Feb;37(2):1270-1276. PMID: 28035401
Ricolinostat purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2017 Feb;37(2):1270-1276. [Abstract]
A375 cells are treated with indicated concentrations of ACY-1215. After 72 h, Western blotting assay are utilized to detect apoptosis.
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Med Oncol
HDAC6-mediated EGFR stabilization and activation restrict cell response to sorafenib in non-small cell lung cancer cells. [Abstract]2016 May;33(5):50. PMID: 27090797
Ricolinostat purchased from MedChemExpress. Usage Cited in: Med Oncol. 2016 May;33(5):50. [Abstract]
H460 cells are treated with 0.5 μM Aorafenib and indicated concentration of HDAC6 inhibitors, CAY10603 (CAY, 0.05 μM) or ACY1215 (ACY,1 μM). The cleavage of PARP and caspase 3 also increased after cotreatment.
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Theriogenology
Effect of ACY-1215 on cytoskeletal remodeling and histone acetylation in bovine somatic cell nuclear transfer embryos. [Abstract]2022 Apr 15:183:98-107. PMID: 35231828 -
Anticancer Res
Blockade of GRP78 Translocation to the Cell Surface by HDAC6 Inhibition Suppresses Proliferation of Cholangiocarcinoma Cells. [Abstract]2022 Jan;42(1):471-482. PMID: 34969757 -
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bioRxiv
2025 Oct 4:2025.10.03.680349. PMID: 41256453 -
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Res Sq
2023 Jan 27:rs.3.rs-2440581. PMID: 36747781 -
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Solvent & Solubility
DMSO : ≥ 50 mg/mL (115.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The effect of Ricolinostat with or without PS-341 on the viability of MM cell lines, patient MM cells, and PBMCs is assessed by measuring MTT dye absorbance. PBMCs from healthy donors are isolated and stimulated with 2.5 μg/mL of phytohemagglutinin (PHA) for 48 hours in the presence of increasing concentrations of Ricolinostat (ACY-1215). DNA synthesis is measured by tritiated thymidine uptake. CD4+ T cells are purified from human blood with the Rosette Sep negative-selection kit. Cells are stimulated by CD3/CD28 Dynabeads for 7 days in the presence of compounds. Cell viability is assessed using alamarBlue. MM cells (2-3×104 cells/well) are incubated in 96-well culture plates with medium and different concentrations of Ricolinostat (ACY-1215), PS-341, and/or recombinant IL-6 (10 ng/mL) or IGF-1 (50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
To evaluate the in vivo anti-MM activity of Ricolinostat, male SCID mice are inoculated subcutaneously with 5×106 MM.1S cells in 100 μL of serum-free RPMI 1640 medium. When tumors are measurable, mice are treated IP with Ricolinostat 50 mg/kg dissolved in 10% DMSO in 5% dextrose in water consecutively for 5 days a week for 3 weeks; PS-341 0.5 mg/kg dissolved in 0.9% saline solution biweekly (IV) for 3 consecutive weeks; or combination with the same dosing regimen used for the individual agents. The control group receive the carrier alone at the same schedule as the combination group. Tumor size is measured every other day in 2 dimensions using calipers, and tumor volume is calculated with the formula: V=0.5(a×b2) where a is the long diameter of the tumor and b is the short diameter of the tumor. Mice are killed when the tumor reaches 2 cm3 or is ulcerated. Survival and tumor growth are evaluated from the first day of treatment until death.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3068 mL | 11.5340 mL | 23.0681 mL | 57.6701 mL |
| 5 mM | 0.4614 mL | 2.3068 mL | 4.6136 mL | 11.5340 mL | |
| 10 mM | 0.2307 mL | 1.1534 mL | 2.3068 mL | 5.7670 mL | |
| 15 mM | 0.1538 mL | 0.7689 mL | 1.5379 mL | 3.8447 mL | |
| 20 mM | 0.1153 mL | 0.5767 mL | 1.1534 mL | 2.8835 mL | |
| 25 mM | 0.0923 mL | 0.4614 mL | 0.9227 mL | 2.3068 mL | |
| 30 mM | 0.0769 mL | 0.3845 mL | 0.7689 mL | 1.9223 mL | |
| 40 mM | 0.0577 mL | 0.2884 mL | 0.5767 mL | 1.4418 mL | |
| 50 mM | 0.0461 mL | 0.2307 mL | 0.4614 mL | 1.1534 mL | |
| 60 mM | 0.0384 mL | 0.1922 mL | 0.3845 mL | 0.9612 mL | |
| 80 mM | 0.0288 mL | 0.1442 mL | 0.2884 mL | 0.7209 mL | |
| 100 mM | 0.0231 mL | 0.1153 mL | 0.2307 mL | 0.5767 mL |