Ricolinostat (Synonyms: ACY-1215; Rocilinostat)

Name: Ricolinostat
Brand: MedChemExpress
SKU: HY-16026
Rating: 5.0 (36 reviews)

Cat. No.: HY-16026 Purity: 99.83%: FAQs
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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.

Ricolinostat Chemical Structure

CAS No. : 1316214-52-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 36 publication(s) in Google Scholar

30 Publications Citing Use of MCE Ricolinostat

: 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.

: 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.

: 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.

: 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.

: 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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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

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)

Cellular Effect

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	> 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	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]
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	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	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]
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]
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]
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]
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	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]
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	0.656 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	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]
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	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	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	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]
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]
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]
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	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	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	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	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]
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	> 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]
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	> 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	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	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]

In Vitro

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.

In Vivo

Mice treated with Ricolinostat (ACY-1215), PS-341, or Ricolinostat plus PS-341 show a significant delay in tumor growth (P=0.01, P=0.006, and P<0.0001, respectively). Combined treatment with Ricolinostat and PS-341 shows significant suppression of tumor growth and significantly prolonged overall survival (OS) compare with the control group (17 days in the control vs 40 days in the combination-treated group, P<0.0001) and the Ricolinostat (ACY-1215)-treated group (22 days in the PS-341 group vs 40 days in the combination-treated group, P<0.0001). Weight loss in the combination-treated group is between 4% and 12% compare with the same-day control group values during treatment, with complete recovery after the last injection. As is observed in the plasmacytoma model, a significant therapeutic advantage is found by combining Ricolinostat with PS-341 compare with either agent alone^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

433.50

Formula

C₂₄H₂₇N₅O₃

CAS No.

1316214-52-4

Appearance

Solid

Color

White to pink

SMILES

O=C(C1=CN=C(N(C2=CC=CC=C2)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3068 mL	11.5340 mL	23.0681 mL
5 mM	0.4614 mL	2.3068 mL	4.6136 mL
10 mM	0.2307 mL	1.1534 mL	2.3068 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

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:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.83%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (244 KB) LCMS (262 KB)

Handling Instructions (2659 KB)

References

[1]. Santo L, et al. Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with PS-341 in multiple myeloma. Blood. 2012 Mar 15;119(11):2579-89. [Content Brief]

Cell Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Santo L, et al. Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with PS-341 in multiple myeloma. Blood. 2012 Mar 15;119(11):2579-89. [Content Brief]

Complete Stock Solution Preparation Table

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

Ricolinostat Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ricolinostat1316214-52-4ACY-1215 RocilinostatACY1215ACY 1215HDACApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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Ricolinostat (Synonyms: ACY-1215; Rocilinostat)

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