Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
For research use only. We do not sell to patients.
Romidepsin Chemical Structure
CAS No. : 128517-07-7
This product is a controlled substance and not for sale in your territory.
Based on 47 publication(s) in Google Scholar
Romidepsin purchased from MedChemExpress. Usage Cited in:
Cancer Cell. 2023 Mar 13;41(3):602-619.e11.
[Abstract]
The triple combination of E + R + iC significantly decreases tumor volume compared with double combinations, in mice. E: enzalutamide (30 mg/kg; p.o.; single daily for 10 days); R: Romidepsin (0.3 mg/kg; i.p.; single daily for 10 days); iC: CXCR2 inhibitor.
Immunoblot analysis for vIL-6, ORF45, or actin is performed on lysates from BCBL-1 cells treated with NaB+TPA, Romidepsin or LBH589.
Romidepsin purchased from MedChemExpress. Usage Cited in:
Neurosci Lett. 2017 May 12;653:12-18.
[Abstract]
Romidepsin increases histone acetylation in SH-SY5Y neuroblastoma cells. Western blots of pAcH3 and β-actin levels in SH-SY5Y cells cultured for 24 h with 0-40 nM of Romidepsin. 20 nM and 40 nM Romidepsin significantly increase the levels of pAcH3 relative to control, which is measured by densitometric quantification of pAcH3 protein levels relative to β-actin loading control.
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Description
Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively[1]. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis[2].
IC50 & Target[1]
HDAC1
36 nM (IC50)
HDAC2
47 nM (IC50)
HDAC4
510 nM (IC50)
HDAC6
14000 nM (IC50)
In Vitro
Romidepsin (0-72 hours; 0-80 nM) inhibits proliferation of HCC cells in dose-dependent manner[2].
Romidepsin (0-48 hours; 0-60 nM) leads to a time- and dose-dependent induction of cell cycle arrest in the G2/M phase in HCC cells[2].
Romidepsin (0-48 hours; 0-60 nM) promotesapoptosis in HCC cells, increases c-caspase-3, c-caspase-9, and c-PARP protein expression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Increaesd c-caspase-3, c-caspase-9, and c-PARP expression in HCC cells.
In Vivo
Romidepsin (intraperitoneal injection; 0.5 and 1 mg/kg; every 3 day; 21 days) inhibited the tumor growth, reveals a higher expression of p-cdc25C, ki67, c-caspase-3 and c-PARP, and a lower expression of Ki-67 in Romidepsin treated tumors [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Nude mice with Huh7 cells[2]
Dosage:
0.5 and 1 mg/kg
Administration:
Intraperitoneal injection; 0.5 and 1 mg/kg; every 3 day; 21 days
Result:
Suppressed tumor growth in mouse xenograft models.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
*The compound is unstable in solutions, freshly prepared is recommended.
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (184.95 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
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.8495 mL
9.2473 mL
18.4945 mL
5 mM
0.3699 mL
1.8495 mL
3.6989 mL
10 mM
0.1849 mL
0.9247 mL
1.8495 mL
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 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: 2.08 mg/mL (3.85 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (20.8 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
This protocol yields a clear solution of ≥ 2.08 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 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
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).
*The compound is unstable in solutions, freshly prepared is recommended.
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.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
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.
[1]. Furumai R, et al. FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res. 2002 Sep 1;62(17):4916-21.
[Content Brief]
[2]. Sun WJ, et al. Romidepsin induces G2/M phase arrest via Erk/cdc25C/cdc2/cyclinB pathway and apoptosis induction through JNK/c-Jun/caspase3 pathway in hepatocellular carcinoma cells. Biochem Pharmacol. 2017 Mar 1;127:90-100.
[Content Brief]
[1]. Furumai R, et al. FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res. 2002 Sep 1;62(17):4916-21.
[2]. Sun WJ, et al. Romidepsin induces G2/M phase arrest via Erk/cdc25C/cdc2/cyclinB pathway and apoptosis induction through JNK/c-Jun/caspase3 pathway in hepatocellular carcinoma cells. Biochem Pharmacol. 2017 Mar 1;127:90-100.
Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
1.8495 mL
9.2473 mL
18.4945 mL
46.2364 mL
5 mM
0.3699 mL
1.8495 mL
3.6989 mL
9.2473 mL
10 mM
0.1849 mL
0.9247 mL
1.8495 mL
4.6236 mL
15 mM
0.1233 mL
0.6165 mL
1.2330 mL
3.0824 mL
20 mM
0.0925 mL
0.4624 mL
0.9247 mL
2.3118 mL
25 mM
0.0740 mL
0.3699 mL
0.7398 mL
1.8495 mL
30 mM
0.0616 mL
0.3082 mL
0.6165 mL
1.5412 mL
40 mM
0.0462 mL
0.2312 mL
0.4624 mL
1.1559 mL
50 mM
0.0370 mL
0.1849 mL
0.3699 mL
0.9247 mL
60 mM
0.0308 mL
0.1541 mL
0.3082 mL
0.7706 mL
80 mM
0.0231 mL
0.1156 mL
0.2312 mL
0.5780 mL
100 mM
0.0185 mL
0.0925 mL
0.1849 mL
0.4624 mL
Romidepsin 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.