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Chemical Structure| 1316214-52-4 Chemical Structure| 1316214-52-4

Structure of Ricolinostat
CAS No.: 1316214-52-4

Chemical Structure| 1316214-52-4

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Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor with an IC50 of 5 nM. It also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.

Synonyms: ACY-1215; Rocilinostat; ACY-63

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Product Details of Ricolinostat

CAS No. :1316214-52-4
Formula : C24H27N5O3
M.W : 433.50
SMILES Code : O=C(C1=CN=C(N(C2=CC=CC=C2)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O
Synonyms :
ACY-1215; Rocilinostat; ACY-63
MDL No. :MFCD22666356
InChI Key :QGZYDVAGYRLSKP-UHFFFAOYSA-N
Pubchem ID :53340666

Safety of Ricolinostat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Ricolinostat

epigenetics

Isoform Comparison

Biological Activity

Target
  • HDAC8

    HDAC8, IC50:100 nM

  • HDAC3

    HDAC3, IC50:51 nM

  • HDAC6

    HDAC6, IC50:4.7 nM

  • HDAC2

    HDAC2, IC50:48 nM

  • HDAC1

    HDAC1, IC50:58 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human neutrophils 10, 2, 0.4, 0.08 µM 1 h Ricolinostat significantly reduced the release of CitH3 in PMA-treated human neutrophils, indicating its inhibition of NETosis. PMC8567386
Mouse neutrophils 10, 2, 0.4, 0.08 µM 1 h Ricolinostat efficiently decreased the release of CitH3 in PMA-treated mouse neutrophils, demonstrating its efficacy in inhibiting NETosis. PMC8567386
Peripheral blood mononuclear cells (PBMCs) 2.5 μM 24 h Ricolinostat significantly reduced the proportion of CD4+FOXP3+ Tregs and upregulated the expression of the CD69 activation marker on CD8+ and CD4+ T cells, indicating it promoted T cell activation. PMC5540748
PBMCs from NSCLC patients 2.5 μM 24 h Ricolinostat significantly reduced the proportion of Tregs in PBMCs from NSCLC patients and upregulated the expression of the CD69 activation marker on CD8+ and CD4+ T cells, indicating it promoted T cell activation. PMC5540748
MDA-MB-453 2.5 μM 72 h Induced apoptosis PMC9992270
MDA-MB-436 2.5 μM 72 h No significant apoptosis observed PMC9992270
HEK-293 cells 2.5 µM 24 h Assess the cytotoxicity of Ricolinostat on HEK-293 cells PMC8421147
HT1080 cells 2.5 µM 24 h Assess the cytotoxicity of Ricolinostat on HT1080 cells PMC8421147
HeLa cells 2.5 µM 24 h Assess the cytotoxicity of Ricolinostat on HeLa cells PMC8421147
WSU-NHL 0.01–100 µM 24–72 h Ricolinostat significantly inhibited cell viability with IC50 values ranging from 1.51 to 8.65 µM. PMC5401712
Hut-78 0.01–100 µM 24–72 h Ricolinostat significantly inhibited cell viability with IC50 value of 1.51 µM. PMC5401712
Jeko-1 0.01–100 µM 24–72 h Ricolinostat significantly inhibited cell viability with IC50 values ranging from 1.51 to 8.65 µM. PMC5401712
MM.1S cells 5 µM and 10 µM 72 h In flow cytometry, there was a 2.5-fold (5 µM) and 3.1-fold (10 µM) increase in CD38 expression at 72 h of treatment by mean fluorescence intensity (MFI) ( p<0 . 0 0 0 1 , n=13) PMC8318885
OPM-2 cells 5 µM and 10 µM 72 h Similar trends were observed on the MM cell line OPM-2 PMC8318885
U266 cells 1, 5, and 10 µM 48 h CD38 expression on U266 cells before and after treatment with ricolinostat, ACY-241, and WT-161 at fcs of 1, 5, and 10 µM PMC8318885
CD34+ HSPCs 2 μM 7 days To study the effect of Ricolinostat on the differentiation of CD34+ HSPCs into megakaryocytes, Ricolinostat significantly increased the percentage of CD34+CD41a+ MkPs and CD41a+CD61+ MKs. PMC8817546

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice EL4 lymphoma and LLC lung carcinoma models Intraperitoneal injection 50 mg/kg Once daily for 10 days Ricolinostat alone did not significantly affect tumor growth, but in combination with entinostat, it substantially delayed tumor progression. PMC7765083
Mouse Endotoxic shock model Intraperitoneal injection 30 mg/kg Administered on day 2, day 4, and 3 hours before the endpoint Ricolinostat significantly reduced NETosis and inflammation in a mouse model of endotoxic shock, improving lung functionality and reducing systemic inflammation. PMC8567386
Mice KP mice (genetically engineered mice with KrasG12D mutation and p53 loss) Intraperitoneal injection 50 mg/kg Once daily for 7 days Ricolinostat treatment significantly increased the proportion of tumor-infiltrating CD8+ T cells and decreased the proportion of CD4+Foxp3+ Tregs, while upregulating the CD69 activation marker and IFN-γ secretion, indicating it promoted T cell activation and effector function. PMC5540748
Mice MDA-MB-453 and MDA-MB-436 xenograft models Intraperitoneal injection 50 mg/kg 6 days a week for 1 month Significant antitumor activity was observed in the MDA-MB-453 model, but no significant effect was observed in the MDA-MB-436 model PMC9992270
Mice eGFP-expressing mouse embryos Embryo culture medium 2.5 µM 24 hours Evaluate the enhancement of gene editing efficiency in mouse embryos by Ricolinostat PMC8421147

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02088398 Healthy PHASE1 COMPLETED 2025-04-14 Covance Clinical Research Unit... More >> Incorporated, Madison, Wisconsin, 53704, United States Less <<
NCT05229042 Peripheral Nervous System Dise... More >>ases Less << PHASE1 COMPLETED 2023-11-10 Beijing3ERegenacy, Beijing, Ch... More >>ina Less <<
NCT01323751 Multiple Myeloma PHASE1|PHASE2 COMPLETED 2016-12-03 Winship Cancer Institute, Emor... More >>y University, Atlanta, Georgia, 30322, United States|Massachusetts General Hospital, Boston, Massachusetts, 02115, United States|Mt. Sinai Medical Center, New York, New York, 10029, United States|University of Pennsylvania, Philadelphia, Pennsylvania, 19104, United States|MD Anderson Cancer Center, Houston, Texas, 77030, United States|Medical College of Wisconsin - Clinical Cancer Center, Milwaukee, Wisconsin, 53226, United States Less <<
NCT02091063 Lymphoma|Lymphoid Malignancies PHASE1|PHASE2 TERMINATED 2019-05-05 Moffit Cancer Center, Tampa, F... More >>lorida, 33612, United States|Columbia University Medical Center, New York, New York, 10019, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.53mL

2.31mL

1.15mL

23.07mL

4.61mL

2.31mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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