Romidepsin (FK228, Depsipeptide)

For research use only.

Catalog No.S3020 Synonyms: FR 901228, NSC 630176

116 publications

Romidepsin (FK228, Depsipeptide) Chemical Structure

CAS No. 128517-07-7

Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.

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Selleck's Romidepsin (FK228, Depsipeptide) has been cited by 116 publications

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Choose Selective HDAC Inhibitors

Biological Activity

Description Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively. Romidepsin (FK228/depsipeptide) controls growth and induces apoptosis in neuroblastoma tumor cells.
Features More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.
Targets
HDAC1 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
36 nM 47 nM
In vitro

Unlike TSA, the active form redFK of Romidepsin strongly inhibits HDAC1 and HDAC2 with IC50 of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC50 25 nM and 790 nM, respectively. Romidepsin is 17-23 times weaker than redFK in inhibiting these HDACs with IC50 of 36 nM, 47 nM, 510 nM, and 14 μM, respectively. Romidepsin treatment in HeLa cells induces histone acetylation and p21 expression with EC50 of 3.0 nM, more strongly than redFK with EC50 of 11 nM due to the instability of redFK. [1] In addition to G2/M arrest, Romidepsin treatment causes cyclin D1 downregulation and a p53-independent p21 induction, leading to inhibition of CDK and dephosphorylation of Rb resulting in growth arrest in the early G1 phase. [2] Romidepsin is 100 times more potent than TSA and 1,000,000 times more potent than butyrate in inhibiting the proliferation of the A549 cells. [3] Romidepsin inhibits the growth of U-937, K562, and CCRF-CEM cells with IC50 of 5.92 nM, 8.36 nM, and 6.95 nM, respectively. [5] Romidepsin promotes apoptosis in chronic lymphocytic leukemia (CLL) cells at a concentration corresponding to that at which H3 and H4 acetylation and HDAC inhibition occurs, selectively involving activation of caspase 8 and effector caspase 3, as well as down-regulation of c-FLIP protein. [6] In 11 of 13 (85%) renal cell carcinoma cell lines and in 16 of 37 (43%) other cancer cell lines, Romidepsin treatment up-regulates tumor death receptors, and potentiates natural killer (NK)-mediated tumor killing. [7] Romidepsin exhibits concentration-dependent cytotoxicity against a panel of mantle cell lymphoma (MCL) cell lines. [9]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SU-DHL4 MlzjR4VtdCCYaXHibYxqfHliQYPzZZk> MXiyMlUuOTVibl2= M2P0dlczKGh? NW[2R3R{cW6mdXPld{BkgXSxdH;4bYNqfHliaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XMEoB?= MV:yOVc6ODlyNx?=
U2932  NHPl[JFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1fle|IvPS1zNTDuUS=> M4Lj[|czKGh? M4HUXIlv\HWlZYOgZ5l1d3SxeHnjbZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzyqB? NHLKPHkzPTd7MEmwOy=>
OCI-LY7 M1\3ZWNmdGxiVnnhZoltcXS7IFHzd4F6 NXTmS4hCOi53LUG1JI5O NWTHN5N1PzJiaB?= MkixbY5lfWOnczDjfZRwfG:6aXPpeJkhcW5iYTDjc45k\W62cnH0bY9vNWSncHXu[IVvfCCvYX7u[ZLDqA>? MmHaNlU4QTB7MEe=
Farage NUjkeGI{S2WubDDWbYFjcWyrdImgRZN{[Xl? NF\DeFIzNjVvMUWgcm0> NGPmS4s4OiCq NHTq[pVqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi MoPJNlU4QTB7MEe=
LY7/EBV NHnrTmJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn73Nk42NTF3IH7N M2n0VVczKGh? MW\pcoR2[2W|IHP5eI91d3irY3n0fUBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7lduKh MVWyOVc6ODlyNx?=
U2932/EBV MW\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUPPR|M5Oi53LUG1JI5O MYW3NkBp NHjSO5ZqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi MnTtNlU4QTB7MEe=
HCT116 MmWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M17aOFUuPTByMDDuUS=> M1LqZ|I1KGh? M2\jXWROW09? MkDXbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiY3;uZ4VvfHKjdHnvck1l\XCnbnTlcpQhdWGwbnXy MVSyOVQ6OjVzNR?=
ACH-2 MWfGeY5kfGmxbjDBd5NigQ>? M1vEe|EuQSCwTR?= NFTU[VIzPCCq M3XSNolv\HWlZYOgTGlXNTFiRX72JIV5eHKnc4Ppc44> MYiyOVE1QTR4Nx?=
MCF-10A MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml7nTWM2OD1yLkG3xtExNjBzIH7N NHi3O|UzPDl3NEi1Oi=>
MCF-7 M2mxeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTFwMUFCtVAvOjBibl2= NVjKSm1iOjR7NUS4OVY>
SK-BR-3 M1nkSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjUWYFKSzVyPUGuNFDDuTBwM{Wgcm0> NVrX[mp6OjR7NUS4OVY>
MDA-MB-231 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrFTm5KSzVyPUCuOljDuTBwMUSgcm0> NFfHengzPDl3NEi1Oi=>
PC3 NYn6NIg{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPnTWM2OD1zLk[1xtExNjN3IH7N M2\xclI1QTV2OEW2
HCT116 NI\lW45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTFwMEFCtVAvODBibl2= NVnpUZdwOjR7NUS4OVY>
HCT116-p21-/- MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTFwMkdCtVAvOzdibl2= NGr0fYIzPDl3NEi1Oi=>
S1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTdwNkhCtVAvOjlibl2= MWmyOFk2PDh3Nh?=
SW620 MmjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlraTWM2OD1yLkmzxtExNjJ7IH7N NUDq[VFKOjR7NUS4OVY>
LOX-IMVI MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPPTmJKSzVyPUCuPFfDuTBwMEOgcm0> Mn;1NlQ6PTR6NU[=
UACC-62 MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTBwNUdCtVAvOTZibl2= M2SxeFI1QTV2OEW2
MDA-MB-435 M{HwOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTBwOUFCtVAvODZibl2= MoOwNlQ6PTR6NU[=
SF-295 MnqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGm5VFFKSzVyPUCuPFjDuTBwMUWgcm0> M1\wZ|I1QTV2OEW2
A549 M3zFVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\5ZnhKSzVyPUGuNlbDuTBwMkSgcm0> NHnZO5kzPDl3NEi1Oi=>
H460 NGHUWINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHjZWJKSzVyPUKuOVjDuTBwOECgcm0> NWfV[FU5OjR7NUS4OVY>
EKVX NYfWfXVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLZdXB1UUN3ME2xMlM{yrFyLkO0JI5O NHX4RVYzPDl3NEi1Oi=>
H146 NVi5WJIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWxOYZ1UUN3ME2wMlIzyrFyLkC3JI5O M3zmW|I1QTV2OEW2
H526 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHmdpNKSzVyPUCuNVXDuTBwMEOgcm0> NVLod3ZiOjR7NUS4OVY>
HuT-78 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j5ZWlEPTB;MT63N:KyOC52NDDuUS=> MoLMNlQ6PTR6NU[=
HA M{DlOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn4W4FoOC54MkWtNVBvVQ>? MXi0PEBp Mn;2bY5lfWOnczDhJJNq\26rZnnjZY51dHlic4Tyc45o\XJiaX7obYJqfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[29vdILlZZRm\CC5aYToJIJwenSnen;tbYI> Moj1NlQ4PzF3MUC=
MS-275 NITnZ5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUSwMlYzPS1zMH7N Mor6OFghcA>? MYLpcoR2[2W|IHGgd4lodmmoaXPhcpRtgSC|dILvcodmeiCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBkdy22cnXheIVlKHerdHigZo9zfGW8b33pZi=> MXiyOFc4OTVzMB?=
CD4 T NVzZWXFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PjZlQ5KGh? MWXFR|UxRTRwNdMxNU4xKG6P M2[yO|I1PzJ{NEW0
CD4 T NUPWT|J4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIexcpk1QCCq MkC5R2M2OD1zMEhCtVEzPiCwTR?= MoTDNlQ4OjJ2NUS=
CD4+ T NXX2fpBVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7sSWM2OD1|IH7N MlzXNlQ1QTVzMEW=
A549 NGrtOYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXQUpRNOTEkgKOxNFDDqG6P NWLwVplbOjRxM{[vOFghcA>? NGXmNHNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDic5RpKGOxbnPlcpRz[XSrb36tJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M4TlSVI1PDh3N{m5
JJN3 NFrk[3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LzR|I1NzR6IHi= NHPlO4pGSzVyPEJihKlvVTtiNElihKlp MX2yOFA{ODF3MB?=
OPM-2 NF3jTWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVeyOE81QCCq NIDVZ2JGSzVyc{2x5qCKdk19IES45qCKcA>? NHHFdFUzPDB|MEG1NC=>
RPMI-8226 MmqxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYiweWtLOjRxNEigbC=> MU\FR|Uxez1zLklihKlvVTtiNElihKlp MVuyOFA{ODF3MB?=
U266 NYjVcWI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGD5e5AzPC92ODDo NIrXeHBGSzVyc{2xNQKBkW6POzC0PQKBkWh? MYCyOFA{ODF3MB?=
CA46 NGf6b3ZCeG:ydH;zbZMhSXO|YYm= MoS5OkBp M3Gwd4lv\HWlZYOgZox2dnRiYYDvdJRwe2m| NVnqfJZFOjN7Nk[xOlQ>
DG75 MUjBdI9xfG:|aYOgRZN{[Xl? M{jVelYhcA>? MYjpcoR2[2W|IH7vJIFxd3C2b4Ppdy=> NFHWSJQzOzl4NkG2OC=>
Ramos M{DiTGFxd3C2b4Ppd{BCe3OjeR?= NXTl[IFYPiCq NV3US|JQcW6mdXPld{BmgHSnboPpeoUh[XCxcITvd4l{ M1LzPFI{QTZ4MU[0
ST486 MWDBdI9xfG:|aYOgRZN{[Xl? NUPSPZNrPiCq M2ThVIlv\HWlZYOg[Zh1\W6|aY\lJIFxd3C2b4Ppdy=> MUmyN|k3PjF4NB?=
HuT78 M{HwbGFxd3C2b4Ppd{BCe3OjeR?= MUKxM|ExNzFyMDDuUS=> NFvzNpA1QCCq MkTCbY5lfWOnczDhdI9xfG:|aYOgZZQhOSCwTR?= M{GyVlI{PTN{N{Oy
DpVp35 MVPBdI9xfG:|aYOgRZN{[Xl? M{fj[lEwOTBxMUCwJI5O MUK0PEBp M2W0SYlv\HWlZYOgZox2dnRiYYDvdJRwe2m| MV[yN|U{Ojd|Mh?=
DpVp50 NEXWOJZCeG:ydH;zbZMhSXO|YYm= M1zSbFEwOTBxMUCwJI5O M{\ZO|Q5KGh? MljPbY5lfWOnczDicJVvfCCjcH;weI9{cXN? NWnxXppHOjN3M{K3N|I>
DpP75  Moq5RZBweHSxc3nzJGF{e2G7 M33XPVEwOTBxMUCwJI5O NEDFTmo1QCCq NHTl[XRqdmS3Y3XzJIJtfW62IHHwc5B1d3Orcx?= NI\tR|czOzV|MkezNi=>
SKOV-3 NUC3bG1ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmqyNgKBmzJybl2= MlTRO|IhcA>? MnHBSG1UVw>? MnrudoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjbH;u[UBidmRiY3;tZolv\WRid3n0bEBkcXOybHH0bY4> M1i3flI{ODFyM{S4
Brca1 WT NITZc4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXix5qCUOjCwTR?= Mnu5O|IhcA>? NF3TOGtFVVOR MVPy[YR2[2W|IHPlcIwhfmmjYnnsbZR6KGGub37lJIFv\CClb33ibY5m\CC5aYToJINqe3CuYYTpci=> M{LaVFI{ODFyM{S4
Brca1 Null NVvhd4R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWKx5qCUOjCwTR?= MVm3NkBp Mm\vSG1UVw>? MmHKdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjbH;u[UBidmRiY3;tZolv\WRid3n0bEBkcXOybHH0bY4> NEDjXGIzOzBzMEO0PC=>
OVCAR-8  NFOxUFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzsZ3gy6oDVMkDuUS=> MoSxO|IhcA>? M1fPNWROW09? M3r2R5Jm\HWlZYOgZ4VtdCC4aXHibYxqfHliYXzvcoUh[W6mIHPvcYJqdmWmIIfpeIgh[2m|cHzheIlv MXKyN|AyODN2OB?=
NCI/ADR-RES MmfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnRNgKBmzJybl2= MknjO|IhcA>? MXnEUXNQ MknjdoVlfWOnczDj[YxtKH[rYXLpcIl1gSCjbH;u[UBidmRiY3;tZolv\WRid3n0bEBkcXOybHH0bY4> MkTWNlMxOTB|NEi=
HCT116 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrvOUBvVS13MDFOwG0> MojRNlQhcA>? MlK5SG1UVw>? NYLrcGl[cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? M3\DSlIzQTJ2OUW4
RKO MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV21JI5ONTVyIN88US=> NHr6NGUzPCCq NUKyeYU4TE2VTx?= MXjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHPvcoNmdnS{YYTpc44u\GWyZX7k[Y51KG2jbn7ldi=> MkPpNlI6OjR7NUi=
CO115 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LveVUhdk1vNUCg{txO NV\qUXpjOjRiaB?= NUHOUnZyTE2VTx?= NE\oRWlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? M1TtPFIzQTJ2OUW4
HFS NGrrfWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTu[4JnPSCwTR?= M2\OZlI1NzR6L{eyJIg> NELLVlJqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lMYRmeGWwZHXueIx6 M2TCR|IzOTB4Mkiy
LNCaP MmS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nicVUhdk1? M1TFZlI1NzR6L{eyJIg> NHzDOlFqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lMYRmeGWwZHXueIx6 NILuNpczOjFyNkK4Ni=>
A549 MkeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3iybFUhdk1? MXWyOE81QC95MjDo MX;pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nLXTldIVv\GWwdHz5 NG[4ZmYzOjFyNkK4Ni=>
697  MlTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|Ux6oDLPfMAjVIvPcLibl2= NGnESJMzOTV|OEKxOi=>
697-R MljoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPselZsUUN3MPMAjV3jiIl6LkdCpI5OyqB? NUfieJNSOjF3M{iyNVY>
HUT78 Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTFibl2= M3vjT|IyOTl6NUS1
THJ-16T NWHQVXVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPBVXQ{OSCwTR?= NHXZWVUzPCCq MWTpcohq[mm2czDj[YxtKGe{b4f0bC=> M2nGZ|IxQDFyNU[4
HCT116 NXSyVIdjTnWwY4Tpc44hSXO|YYm= MYiyNEBvVQ>? NHXkWmo5KGh? NYq2ZlV1dW:mdXzheIV{KHS{YX7zZ5JqeHRibHX2[Yx{KG[xcjDoeY5lemWmczDv[kBo\W6nczDpckBmcXSqZYKg[Ilz\WO2aX;u Mn7aNlA4Ozl2NUS=
B104  MWDGeY5kfGmxbjDBd5NigQ>? NE\vOVYzKG6P MWiyOE81QC95MjDo NYHWN3hzcW6lcnXhd4V{KHSqZTDzeZJn[WOnIHX4dJJme3Orb36gc4YhS0R{MNMg MmDINlA3QDZ3MEW=
HL-60  MVrDfZRwfG:6aXPpeJkhSXO|YYm= NI\TPIEyNTVyMDDuUS=> MWeyOEBp M2\Odolv\HWlZYOgZ5l1d3SxeHnjbZR6KGmwIHGgZ49v[2WwdILheIlwdi2mZYDlcoRmdnRibXHucoVzyqB? NYfNbGNHOjB4MkSxOlM>
HP100 Ml60R5l1d3SxeHnjbZR6KEG|c3H5 M4Ph[FEuPTByIH7N NVu3W3I6OjRiaB?= NGHCN4dqdmS3Y3XzJIN6fG:2b4jpZ4l1gSCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5mesLi M3zyO|IxPjJ2MU[z
HL-60  MlvFSpVv[3Srb36gRZN{[Xl? MVixNEBvVQ>? MVq0M|YwOTZiaB?= MmrjbY5lfWOnczD0bIUh\2WwZYLheIlwdiCxZjDofYRzd2enbjDw[ZJwgGmmZTDmdo9uKDSq NXPrW4ZIOjB4MkSxOlM>
HP100 MVjGeY5kfGmxbjDBd5NigQ>? MVyxNEBvVQ>? NH\QfnU1NzZxMU[gbC=> NITYTGdqdmS3Y3XzJJRp\SCpZX7ldoF1cW:wIH;mJIh6\HKxZ3XuJJBmem:6aXTlJIZzd21iNHi= M1ToOlIxPjJ2MU[z
HL-60  MmnDSpVv[3Srb36gRZN{[Xl? M2DTZlExNTVyMDDuUS=> MXS0JIg> NVXoS|lb\GWlcnXhd4V{KHSqZTDobZN1d26nIHTlZYNmfHmuYYPlJEhJTEGFKTDhZ5Rqfmm2edMg MWGyNFYzPDF4Mx?=
HP100 NIfYNodHfW6ldHnvckBCe3OjeR?= NYqzRXh3OTBvNUCwJI5O MWq0JIg> NYTzOlhR\GWlcnXhd4V{KHSqZTDobZN1d26nIHTlZYNmfHmuYYPlJEhJTEGFKTDhZ5Rqfmm2edMg Ml74NlA3OjRzNkO=
11z MYXLbY5ie2ViQYPzZZk> MoDqN{0yODBibl2= M1fmdpJm\HWlZYOgTGRCSyCnbor5cYF1cWNiYXP0bZZqfHliKFnDOVDDqD1iNj61JOKyKDBwNjDucY9tN0xr MYmyNFYxPTF2NB?=
SKOV-3 NILkUXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWm0M|gwOTZibl2= NVH4TFBiPDhiaB?= NUPiZ3NrcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBkd26lZX70doF1cW:wLXTldIVv\GWwdDDtZY5v\XJ? MojaNlA1ODR3NkS=
OVCAR-3 MoHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HCZVQwQC9zNjDuUS=> NHXtdmc1QCCq NInCdldqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJINwdmOnboTyZZRqd25vZHXw[Y5l\W62IH3hco5meg>? NHLpVWMzODRyNEW2OC=>
HBL-2 NGfVW5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmm3Nk0yOCCwTR?= NVGxT2RXOjRiaB?= NGOxNWdKSzVyPUSuN{BvVQ>? NYnFNlZNOjByNkiwPFA>
Jeko-1 M1T4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV2yMVUxKG6P MkO1NlQhcA>? NVnZb4s4UUN3ME2xNUBvVQ>? NVvLSotNOjByNkiwPFA>
Granta-519 NFrrSFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEW4Uos2NTRyIH7N M{\OTFI1KGh? NEe4[YdKSzVyPUW4MlUhdk1? NH\SNYUzODB4OEC4NC=>
L1236 MV;DfZRwfG:6aXPpeJkhSXO|YYm= NWnodFE1OSCwTT2xNFAh|ryP NIrEOII1QCCq M4TnPGVEPTB;MD6wO{DPxE1? NEfTNXIyQTJ|M{S3NC=>
L428 MonMR5l1d3SxeHnjbZR6KEG|c3H5 MXWxJI5ONTFyMDFOwG0> MUK0PEBp NYrIZWd6TUN3ME2wMlQ{KM7:TR?= NGjQSGwyQTJ|M{S3NC=>
KM-H2 MoHlR5l1d3SxeHnjbZR6KEG|c3H5 MVuxJI5ONTFyMDFOwG0> MoXFOFghcA>? MXXFR|UxRTBwNUig{txO NX\JOYlGOTl{M{O0O|A>
L540Cy M2L4cGN6fG:2b4jpZ4l1gSCDc4PhfS=> Mm\jNUBvVS1zMECg{txO NFjYZW41QCCq MnfDSWM2OD1yLkG2JO69VQ>? MXixPVI{OzR5MB?=
G401 M4rjVWZ2dmO2aX;uJGF{e2G7 MWqxNEBvVQ>? M4LvXlI1NzR6L{eyJIg> MUPEUXNQ MYrpcoNz\WG|ZYOgR2RMVjGFIHX4dJJme3Orb36= Mn\JNVkzOjF3OE[=
STM91-01 NW\jN|c4TnWwY4Tpc44hSXO|YYm= MWWxNEBvVQ>? MoLINlQwPDhxN{KgbC=> NGfkWZVFVVOR NHHUVXlqdmO{ZXHz[ZMhS0SNTkHDJIV5eHKnc4Ppc44> NYjLd2ZzOTl{MkG1PFY>
SJSC  Mm\OSpVv[3Srb36gRZN{[Xl? NEnlWYoyOCCwTR?= M3rGZlI1NzR6L{eyJIg> Mle3SG1UVw>? MV3pcoNz\WG|ZYOgR2RMVjGFIHX4dJJme3Orb36= MVuxPVIzOTV6Nh?=
BT16  NXvR[IhwTnWwY4Tpc44hSXO|YYm= NX:3eHpnOTBibl2= NFj1eHczPC92OD:3NkBp MlX4SG1UVw>? M3y0fYlv[3KnYYPld{BETEuQMVOg[ZhxemW|c3nvci=> NHLuT|AyQTJ{MUW4Oi=>
NCI-H1299 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjwU4NKSzVyPUSuOuKyOC5{IH7nM41t NUjzcII1OTlzN{m4PVA>
NCI-2882 NE\qXmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFwNtMxNE4xPCCwZz;tcC=> M174eVE6OTd7OEmw
HCC95 NYjzfHQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPUVYMxUUN3ME2yMlXDuTBwMEWgcocwdWx? MVexPVE4QTh7MB?=
NCI-H23 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnyOXh[UUN3ME2yMlnDuTBwMjDu[{9udA>? NVzp[GNLOTlzN{m4PVA>
NCI-H157 NGDyO3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rafmlEPTB;MT62xtExNjB{IH7nM41t MnfVNVkyPzl6OUC=
NCI-H460 M2Plfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPSVpVKSzVyPUKuNeKyOC5yNzDu[{9udA>? MW[xPVE4QTh7MB?=
NCI-H1975 NUDES3NPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPJepRKSzVyPUGuN:KyOC5yNDDu[{9udA>? NGrVO2wyQTF5OUi5NC=>
NCI-H820 M3;vPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoniTWM2OD1{LkVCtVAvOSCwZz;tcC=> M1\NfFE6OTd7OEmw
NCI-H1650 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTRwOdMxNE4{KG6pL33s M4jDcFE6OTd7OEmw
DTC1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTBwNUGgcm0> MnjaNVg2PjZ{NE[=
KAO NUHRPXY1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLITWM2OD1yLkmxJI5O NYPYe3UyOTh3Nk[yOFY>
SU-CCS-1 MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzaTWM2OD1yLki5JI5O MX:xPFU3PjJ2Nh?=
SYO-1 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NID5OmdKSzVyPUCuOlchdk1? M3\PdlE5PTZ4MkS2
FUJI NETNXIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvZb|hmUUN3ME2xMlMyKG6P NGrVVHMyQDV4NkK0Oi=>
SKNMC MoHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnk[YNMUUN3ME2xMlE4KG6P M3;GXVE5PTZ4MkS2
402-91 NHjtXJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q3XWlEPTB;MT6yOkBvVQ>? Mk[wNVg2PjZ{NE[=
1765-92 MmTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnYWmlqUUN3ME2xMlc4KG6P NE\sXnMyQDV4NkK0Oi=>
JN-DSRCT-1 M3rufGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL4XmpRUUN3ME2xMlI2KG6P NGLnc4EyQDV4NkK0Oi=>
NMS-2PC MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVm1blNyUUN3ME2wMlgyKG6P NE\JOlcyQDV4NkK0Oi=>
HL60 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTFwOE[gcm0> M3v0bFE5PTZ4MkS2
A549 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDn[2VKSzVyPUOuNlQhdk1? Mn3wNVg2PjZ{NE[=
SW480 M{\LS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLTZnE4UUN3ME2yMlY6KG6P M1LN[lE5PTZ4MkS2
MCF7 M2L1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zuXGlEPTB;Mz61OUBvVQ>? NI\FXocyQDV4NkK0Oi=>
PC-3 MlnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTJwNUGgcm0> MYixPFU3PjJ2Nh?=
MMRU Mmm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjLUnVPUUN3ME2yMlU4KG6P MU[xPFU3PjJ2Nh?=
Hs68 NHnmfFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvuRWNKSzVyPU6xNEBvVQ>? NG\qfWEyQDV4NkK0Oi=>
hMSC-001F NEjGc2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[0NIRKSzVyPU6xNEBvVQ>? NGTw[3UyQDV4NkK0Oi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p21 / Cyclin D1; 

PubMed: 19682393     


NIH 3T3 cells stably expressing the indicated proteins were treated with DMSO (Vehicle) or the indicated concentration of romidepsin for 24 h. Cell lysates were analyzed by western blotting with antibodies to cyclin D1, p21 and β-actin (loading control). Data shown are representative of at least two independent experiments.

AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27); 

PubMed: 26473529     


Effects of romidepsin (Rom) on the levels of acetylated proteins and related enzymes. Cells were exposed to romidepsin for 48 h and total cell extracts were analyzed by western blot.

HDAC3 / HDAC4 / HDAC6 / HDAC2; 

PubMed: 26473529     


Effects of romidepsin (Rom) on the levels of acetylated proteins and related enzymes. Cells were exposed to romidepsin for 48 h and total cell extracts were analyzed by western blot.

γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP; 

PubMed: 26473529     


Western blot analysis of proteins involved in DNA-damage response and apoptosis. Established cell lines were exposed to different concentrations of romidepsin (Rom) for 48 h and total cell extracts were analyzed.

Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac; 

PubMed: 27444036     


Western blot analysis of the effects of panobinostat (25 nM), vorinostat (5 µM) and romidepsin (10 nM) on expression of cyclin E1, E2F1, BRCA1, cleaved PARP and acetylated histone H3 in OVCAR-3 cells. Actin and histone H3 were loading controls. 

pAKT(S473) / pAKT(T308) / AKT; 

PubMed: 25492515     


Western blot analysis of phosphorylated AKT in PC3 cells. Cells were treated for 3 h with various concentrations of FK228. 

19682393 26473529 27444036 25492515
Growth inhibition assay
Cell viability; 

PubMed: 27444036     


Concentration-dependent effects of panobinostat and vorinostat in SRB viability assays in OVCAR-3 cells (72 h). Values are mean+SE of 3 independent experiments. 

27444036
Immunofluorescence
SS18/TLE1; 

PubMed: 27120803     


A significant decrease in detectable PLA signal following HDAC inhibition in SYO-1 cells.

Cleaved caspase-3; 

PubMed: 22531354     


TDP-B activates cleaved caspase-3 by immunofluorescence. Representative immunofluorescence staining for cleaved caspase 3 (green) in SKOV-3 ovarian cancer cells treated with 10 nM FK228, TDP-A or TDP-B after 24 h of exposure. The nuclei are stained with DAPI (blue).

27120803 22531354
In vivo Romidepsin treatment potently inhibits the neovascularization of chick embryo and that of adult mice in the Matrigel plug assay. [4]Administration of Romidepsin at 0.1-1 mg/kg twice a week significantly prolongs the survival of mice bearing U-937 lymphoma, with median survival times of 30.5 (0.56 mg/kg) and 33 days (0.32 mg/kg), respectively (vs. 20 days in control mice). [5]

Protocol

Kinase Assay:

[1]

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HDAC-inhibitory activity:

For the enzyme assay, 10 μL of [3H]acetyl-labeled histones (25,000 cpm/10 μg) are added to 90 μL of the HDAC enzyme fraction extracted from 293T cells overexpressing HDAC1 or HDAC2 in the presence of increasing concentrations of Romidepsin, and the mixture is incubated at 37 °C for 15 minutes. The enzyme reaction is linear for at least 1 hour. The reaction is stopped by the addition of 10 μL of concentrated HCl. The released [3H]acetic acid is extracted with 1 mL of ethylacetate, and 0.9 mL of the solvent layer is taken into 5 mL of aqueous counting scintillant II solution for determination of radioactivity. The IC50 values are determined from at least three independent dose-response curves.
Cell Research:

[3]

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  • Cell lines: HL60, Jurkat, A549, and MCF-7
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are exposed to various concentrations of Romidepsin for 72 hours in 96-well plates. 20 μL of 5 mg/mL MTT solution in PBS is added to each well for 4 hours. After removal of the medium, 170 μL of DMSO is added to each well to dissolve the formazan crystals. The absorbance at 540 nm is determined. In addition, cells are incubated with trypan blue, and the numbers of blue (dead) cells and transparent (live) cells are counted in a hemocytometer. For cell cycle analysis, cells are incubated for 30 minutes in propidium iodide staining solution containing 0.05 mg/mL propidium iodide, 1 mM EDTA, 0.1% Triton X-100, and 1 mg/mL RNase A in PBS. The suspension is then passed through a nylon mesh filter and analyzed on a Becton Dickinson FACScan.


    (Only for Reference)
Animal Research:

[5]

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  • Animal Models: Male scid mice inoculated i.p. with U-937 cells
  • Dosages: ~1 mg/kg once or twice a week
  • Administration: Treated i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 10 mg/mL (18.49 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5%Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* 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.

Chemical Information

Molecular Weight 540.7
Formula

C24H36N4O6S2

CAS No. 128517-07-7
Storage powder
in solvent
Synonyms FR 901228, NSC 630176
Smiles CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03770000 Recruiting Drug: Tenalisib|Drug: Romidepsin T Cell Lymphoma Rhizen Pharmaceuticals SA March 12 2019 Phase 1|Phase 2
NCT02616965 Recruiting Drug: Romidepsin|Drug: Brentuximab vedotin Cutaneous T-cell Lymphoma (CTCL) Fox Chase Cancer Center|Seattle Genetics Inc.|Celgene Corporation February 22 2017 Phase 1
NCT02616874 Completed Drug: MVA.HIVconsv vaccine|Drug: Romidepsin HIV IrsiCaixa|Germans Trias i Pujol Hospital|Fundacio Lluita Contra la SIDA|Hospital Clinic of Barcelona|Hospital de Sant Pau|HIVACAT|University of Oxford|BCN Checkpoint February 2016 Phase 1
NCT03141203 Active not recruiting Drug: Romidepsin|Drug: Carfilzomib Peripheral T Cell Lymphoma University of Birmingham|Bloodwise|Celgene|Amgen July 13 2015 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID