Entinostat (MS-275)

For research use only.

Catalog No.S1053 Synonyms: SNDX-275

337 publications

Entinostat (MS-275) Chemical Structure

CAS No. 209783-80-2

Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.

Selleck's Entinostat (MS-275) has been cited by 337 publications

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.
Targets
HDAC1 [2]
(Cell-free assay)
HDAC3 [2]
(Cell-free assay)
0.51 μM 1.7 μM
In vitro

MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. MS-275 inhibits the proliferation of human tumor cell lines including A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 with IC50 from 41.5 nM to 4.71 μM, which due to HAD-inhibition. [1] MS-275 is not sensitive to other HDACs (4, 6, 8 and 10) with IC50 about/above 100 μM. [2] MS-275 shows great inhibition to human leukemia and lymphoma cells, including U937, HL-60, K562, and Jurkat. MS-275 also decreases expression of cyclin D1 and the antiapoptotic proteins Mcl-1 and XIAP. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SCC-3 Mn3lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHOzXGNKSzVyPUCuNFYyKM7:TR?= M2XNZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
ALL-PO MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DDUmlEPTB;MD6wOlM2PSEQvF2= NE[yVZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
697 NUDWOWdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn21TWM2OD1yLkC5PVc3KM7:TR?= NFvZfoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
NCI-H748 M1Habmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTBwMUCzN|Qh|ryP M1\TeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
NKM-1 NEHGbGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwMUC5NVIh|ryP NE\HWpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
ES1 M{f3Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIP6c5JKSzVyPUCuNVEzPTVizszN MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
NCI-H1963 NEjpbWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwMUG1O|kh|ryP MkmyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NCI-H1417 NULQPXc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1roTWlEPTB;MD6xNlk4PCEQvF2= NHXIPGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
NEC8 NXfpO2VYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\lXWNKSzVyPUCuNVM2OjdizszN MkS0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
CRO-AP2 NEHGe4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1n5TWlEPTB;MD6xOlg5QSEQvF2= MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
A3-KAW NUmyV4hkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TLc2lEPTB;MD6xO|YzPyEQvF2= M2KwUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
SF539 NHnnUo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2iydGlEPTB;MD6xPVU6OyEQvF2= MkjNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
NOS-1 NIHwUVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTBwMUm2NVkh|ryP NYnwNYU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
NTERA-S-cl-D1 NGm4R49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HI[2lEPTB;MD6yNFEyOyEQvF2= NXq0T5FtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
COR-L88 NYHDe49XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17ETGlEPTB;MD6yNlk2QSEQvF2= NEHwTZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
EM-2 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYD1TGg4UUN3ME2wMlI1ODd7IN88US=> NXO2dVhPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
KARPAS-45 NYLsUXhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH1coNKSzVyPUCuNlc5OzNizszN MnHZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
DSH1 M4\3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrkTGc6UUN3ME2wMlI5PzB6IN88US=> NXT1RZhPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
HT-144 M{f0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkH4TWM2OD1yLkOwNlU3KM7:TR?= NV[yTWtQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
ATN-1 MofxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwM{C1O|Yh|ryP M4LvXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
HEL NHXp[m9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwM{GzOFgh|ryP NHy0[mo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
NB12 NVXKb5RbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDoe4NKSzVyPUCuN|E4PTZizszN NVLHO25VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
LU-139 M2PMeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTBwM{O1NUDPxE1? M2jMclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI4PzV7Lze+V2FPT0WUPD;hQi=>
J-RT3-T3-5 NGXZ[IdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwM{O3NVYh|ryP Mn3WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
MOLT-13 NHOxeXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{LqNGlEPTB;MD6zN|gyKM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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LB647-SCLC NETKfmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTOb4tKSzVyPUCuN|Y4OyEQvF2= NX;yVnVoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
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DEL NVfRTHN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\NWI8zUUN3ME2wMlM4PDh5IN88US=> MkjIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
ARH-77 M2DmT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TM[WlEPTB;MD6zPFE6OyEQvF2= NF7JTpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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RPMI-8402 NH3FOnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXqOm5rUUN3ME2wMlM5PzBzIN88US=> NFq3e4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
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SK-MM-2 M4XjRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHmydmxKSzVyPUCuN|k5PjhizszN NVPRd3pPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjd5NUmvK|5USU6JRWK8M4E,
CHP-126 MkG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y2R2lEPTB;MD60NFI{OSEQvF2= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
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NCI-H209 M4rWSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1[xXmlEPTB;MD60NFYyOyEQvF2= MnLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
MOLT-16 MlrES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zjTGlEPTB;MD60NVAyPyEQvF2= NFnTd4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPzd3OT:nQnNCVkeHUkyvZV4>
RPMI-6666 M3i5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfGXnNKSzVyPUCuOFEyOiEQvF2= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyO|c2QS9pPmPBUmdGWjxxYU6=
OPM-2 Mmn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHvhd3dKSzVyPUCuOFE2OTNizszN MlGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlc4PTlxJ{7TRW5ITVJ:L3G+
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MV4-11 NEPxbGRCeG:ydH;zbZMh[XO|YYm= MmrhOUB2VQ>? MYKyOEB1dyB2ODDodpM> MWfJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKE2YND2xNUBk\WyuczDheEA2KHWPIHHmeIVzKDJ2IITvJFQ5KGi{czDifUBCdm6neHnuJHYuWElic4ThbY5qdmdiYnHz[YQh\myxdzDjfZRwdWW2comu MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTd|OEm1N{c,Ojl5M{i5OVM9N2F-
MV4-11 NEHHT4FHfW6ldHnvckBie3OjeR?= MmH0NlAxKG6P Mkf3NlQhcHK| MoL5TY5pcWKrdHnvckBw\iClbHHzd{AyKEiGQVOgbY4hcHWvYX6gUXY1NTFzIHPlcIx{KGG|c3Xzd4VlKGG|IHj5dIVz[WOndInsZZRqd25ib3[gbIl{fG:wZTDIN{BifCB{MECgcm0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqey5? NYP2U2Z3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3N|g6PTNpPkK5O|M5QTV|PD;hQi=>
HL60 NGCye|hCeG:ydH;zbZMh[XO|YYm= MXW1JJVO NE\YU2E1QCCqcoO= NFTIVoVKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5icILvZ4F{eGG|ZT2zJIxmfmWuIHH0JFUhfU1iYX\0[ZIhPDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcz6= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDRzNUCwPUc,Ojh2MUWwNFk9N2F-
HL60 MkHCRZBweHSxc3nzJIF{e2G7 M2fadlUhfU1? NHvJbmg1QCCqcoO= NYfCdVZjUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIUFYxKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPs[YF3\WRiY3HzdIF{\S1|IHzleoVtKGG2IEWgeW0h[W[2ZYKgOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqey5? NHnadHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OESxOVAxQSd-Mki0NVUxODl:L3G+
HL60 MlHPRZBweHSxc3nzJIF{e2G7 Ml\LOUB2VQ>? MU[0PEBpenN? NYr2NVE{UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIUFYxKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPs[YF3\WRiUFHSVEBt\X[nbDDheEA2KHWPIHHmeIVzKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOu MlOzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2MUWwNFkoRjJ6NEG1NFA6RC:jPh?=
MV4-11 M2\y[WNmdGxiY4njcIUh[XK{ZYP0JIF{e2G7 MYK1JJVO Ml7yNlQhcHK| MVvD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDNWlQuOTFiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KHO3Yj3HNUBxcGG|ZTDheEA2KHWPIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtd3diY4n0c41mfHKrYzDt[ZRpd2Rw NYS2fXdRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1PFk1PDFpPkK5OVg6PDRzPD;hQi=>
HEL MUXD[YxtKGO7Y3zlJIFzemW|dDDhd5NigQ>? MnTuOUB2VQ>? MVGyOEBpenN? NGXnZZVE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBJTUxiY3XscJMh[XRiNTD1UUBi\nSncjCyOEBpenNiYomgdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZz3iZZNm\CCobH;3JIN6fG:vZYTybYMhdWW2aH;kMi=> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV6OUS0NUc,Ojl3OEm0OFE9N2F-
Jurkat NH7ySJdE\WyuIHP5Z4xmKGG{cnXzeEBie3OjeR?= MY[1JJVO M2PtPVI1KGi{cx?= MlfNR4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gTpVzc2G2IHPlcIx{KGG2IEWgeW0h[W[2ZYKgNlQhcHK|IHL5JJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnetZoF{\WRiZnzve{BkgXSxbXX0dolkKG2ndHjv[E4> NF3U[Gw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW4PVQ1OSd-Mkm1PFk1PDF:L3G+
MV4-11 MVTGeY5kfGmxbjDhd5NigQ>? NIKweVM2KHWP NYDmbJVGOjRiaILz MnjrTY5pcWKrdHnvckBw\iClbHHzd{AyKEiGQVOgbY4hcHWvYX6gUXY1NTFzIHPlcIx{KGG|c3Xzd4VlKGG|IHnu[JVkfGmxbjDv[kBpcXO2b37lJIh6eGW{YXPleJlt[XSrb36gZZQhPSC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZD6= M2nwSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUi5OFQyLz5{OUW4PVQ1OTxxYU6=
LNCAP M2HKTGZ2dmO2aX;uJIF{e2G7 NUjEdZVpOTBidV2= M4LWV|I1KGi{cx?= NFjwc5dKdmirYnn0bY9vKG:oIFjERWM3KGmwIHj1cYFvKEyQQ1HQJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiRFjUMYlv\HWlZXSgZYxxcGFvdIXieYxqdiCmZXHj[ZR6dGG2aX;uJIJ6KG2nYYP1dolv\yCrbnPy[YF{\SCrbjDhcJBp[S22dXL1cIlvKGGlZYT5cIF1cW:wIHH0JFExKHWPIH3lZZN2emWmIHHmeIVzKDJ2IHjyd{Bz\WyjdHn2[UB1dyClb370do9tNg>? NEf0W|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{exO|U1PCd-Mke3NVc2PDR:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
AcH3 / AcH4 / HDAC1 / HDAC2 / HDAC3; 

PubMed: 24203492     


HCT-15 or fresh primary NK cells were treated with entinostat for 24 h, and AcH3, AcH4, and HDAC1, 2, and 3 were detected by Western blotting. 

Cleaved PARP; 

PubMed: 19148581     


Induction of PARP cleavage in Daoy cells upon exposure to MS-275 was demonstrated by Western blot analyses using antibodies that recognize the cleaved 89 kDa PARP protein. Pan-Actin (45 kDa) was used as a loading control.

Caspase 8 ; 

PubMed: 19148581     


Cleavage of pro-Caspase-8 was demonstrated by Western blotting with extracts prepared from Daoy cells treated with 2.5 µM MS-275 for various time periods. Antibodies specific to human Caspase-8 or the loading control, pan-Actin were used to probe protein expression.

DR4 / DR5; 

PubMed: 19148581     


Western blotting to detect DR4 and DR5 expression upon treatment of Daoy cells with 2.5 µM MS-275 for 4, 8 and 24 h.

TopoIIα / TopoIIβ; 

PubMed: 21254166     


Upper panel, concentration-dependent effects of AR42, MS-275 and vorinostat on the expression of topoIIα versus topoIIβ after 48 h. Lower panel, time-dependent effect of 0.5 μM AR42 and 5 μM MS-275 on topoIIα versus topoIIβ expression in PLC-5 cells.

24203492 19148581 21254166
Immunofluorescence
phalloidin / snail; 

PubMed: 29855565     


(C) Effect of MS-275 treatment on Snail expression and localization. MCs (mesothelial cells) were treated with MS-275 (250 nM), or DMSO for 48 hr and then stimulated with TGFβ1 (2 ng/ml) for 24 h before processing for immunofluorescence with a monoclonal antibody against Snail. Cell nuclei are shown in blue (Hoechst 33342). Confocal images are shown from one representative experiment of three performed.

DR4 / DR5; 

PubMed: 19148581     


Flow Cytometry to measure cell surface expression of FAS, DR4 and DR5 using PE-labeled antibodies. Cells stained with isotype matched anti-human IgG antibodies served as controls.

H3K4Me3 / H3K9Me3; 

PubMed: 22468166     


Immunocytochemical analysis of the effects of AR42, SAHA, and MS-275 at the indicated concentrations on H3K4Me3 (upper panels) and H3K9Me3 (lower panels) after 24 h of treatment in LNCaP cells.

29855565 19148581 22468166
Growth inhibition assay
Cell proliferation; 

PubMed: 24203492     


(A) HCT-15 cells were cultured in indicated concentrations of entinostat for up to 72 h, and proliferation determined by MTT assay as indicated. (B) HCT-15, CCH-OS-D, COL and HOS cells were cultured in indicated concentrations of entinostat for 72 h, and viable cell number was determined using the Vi-cell assay and proliferation index calculated. (C) Freshly-isolated human NK cells were cultured in indicated concentrations of entinostat for up to 72 h, and viability was assessed by flow cytometry for 7-AAD uptake. *, P < 0.05, **; P ≤ 0.01; ***, P ≤ 0.001

Cell viability; 

PubMed: 28969017     


PANC-1, MIA PaCa-2, BxPC3, CFPAC-1, SUIT2 and SUIT2 Clone 1 cells were plated at a density of 3-5×103 per well in 96-well microtiter plates, allowed to adhere overnight and incubated for 72 hours in the presence of variable concentrations of entinostat (0-100μM). Cell viability was determined by XTT assays. The data presented are the mean values from triplicate wells from two independent experiments ±SE.

24203492 28969017
ELISA
GCP-2 / MCP-2 / MIF ; 

PubMed: 24241152     


MS-275 and SAHA suppressed the secretion of GCP-2, MCP-2 and MIF in E11 cells. (A) GCP suppression. (B) MCP-2 suppression. (C) MIF suppression. E11 cells were incubated with HDAC inhibitors at various concentrations for 1 h before they were stimulated by LPS. 24 h later, the secretion of GCP-2, MCP-2 and MIF were quantified by ELISA (n = 8). Bars show the mean and SD in (A–C).

24241152
In vivo MS-275 exhibits great antitumor activity against human tumor xenografts except HCT-15 at 49 mg/kg. [1] MS-275 demonstrates promising therapeutic potential in both solid and hematologic malignancies, as well as regulation of physiologic and aberrant gene expression. [4] MS-275, combination with IL-2, has great antitumor activity to renal cell carcinoma xenograft model, which due to decreased T regulatory cells and increased splenocytes. [5]

Protocol

Kinase Assay:

[6]

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Standard HDAC Assays:

Rat liver enzyme is diluted 1:6 with HDAC buffer. Recombinant human HDACs are diluted 1:4 in HDAC buffer. For standard HDAC assays, 60 μL of HDAC buffer is mixed with 10 μL of diluted enzyme solution at 30 °C. The HDAC reaction is started by adding 30 μL substrate solution in HDAC buffer followed by 30 min of incubation at 30 °C. The reaction is stopped by adding 100 μL trypsin solutions (10 mg/ml trypsin in 50 mM Tris-HCl [pH 8.0], 100 mM NaCl, 2 μM TSA). After a 20 min incubation period at 30 °C, the release of AMC is monitored by measuring the fluorescence at 460 nm (λex = 390 nm). Fluorescence intensity is calibrated using free AMC. For standard time course experiments, 20 pmol of substrate is used in the initial 100 μL HDAC reaction. Km and Vmax values are determined by measuring the fluorescence AMC generated by enzymatic cleavage of 2–50 pmol of substrate. The experimental data are analyzed using a Hanes plot. The AMC signals are recorded against a blank with buffer and substrate but without the enzyme.
Cell Research:

[2]

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  • Cell lines: A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 cells
  • Concentrations: ~ 10 μM
  • Incubation Time: 3 days
  • Method:

    Cancer cells (5 × 103) are seeded into each well of 96-well plates and cultured with graded concentrations of MS-275 for 3 days. The cells are stained with 0.1 mg/mL neutral red for 1 hour in a CO2-incubator, and, after aspiration of the medium, OD540 of the neutral red solubilized with 50 μL of ethanol and 150 μL of 0.1 M Na2HPO4 is measured. The IC50 value is determined by plotting growth inhibition of the cells against the logarithm of the drug concentration.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1 and Calu-3 cells are injected subcutaneously into the flank of nude mice.
  • Dosages: 12.3, 24.5 and 49 mg/kg
  • Administration: Administered orally once daily 5 days per week for 4 weeks
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (199.25 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+ddH2O
For best results, use promptly after mixing.
10mg/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 376.41
Formula

C21H20N4O3

CAS No. 209783-80-2
Storage powder
in solvent
Synonyms SNDX-275
Smiles C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC(=O)OCC3=CN=CC=C3

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
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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)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / 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 )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / 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):
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    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
NCT04708470 Recruiting Drug: Bintrafusp Alfa|Drug: NHS-IL12|Drug: Entinostat Cancer|Solid Tumor|Metastatic Checkpoint Refractory HPV Associated Malignancies|Microsatellite Stable Colon Cancer (MSS) National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) September 7 2021 Phase 1|Phase 2
NCT03829930 Terminated Drug: Entinostat|Drug: Enzalutamide Prostate Adenocarcinoma George Washington University May 1 2019 Phase 1
NCT03765229 Recruiting Drug: Entinostat|Drug: Pembrolizumab Melanoma UNC Lineberger Comprehensive Cancer Center|Syndax Pharmaceuticals Inc. March 22 2019 Phase 2
NCT03473639 Recruiting Drug: Entinostat|Drug: Capecitabine Metastatic Breast Cancer|Breast Cancer University of Virginia|Syndax Pharmaceuticals January 29 2019 Phase 1
NCT03361800 Terminated Drug: Entinostat Breast Cancer|Invasive Breast Cancer|ER-Negative PR-Negative HER2-Negative Breast Cancer UNC Lineberger Comprehensive Cancer Center|Syndax Pharmaceuticals|National Cancer Institute (NCI) November 28 2018 Early Phase 1

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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Frequently Asked Questions

  • Question 1:

    I would like to use Entinostat(Catalog No.S1053) for animal study. What is your recommendation for the solvent? What is the role of PEG 300 in this case? Can I use DMSO only and dilute it with PBS or HBSS?

  • Answer:

    2%DMSO/30%PEG/68%Water is recommended. PEG is an important polymer that helps with the solubility of hydrophobic drugs. If you use DMSO only and dilute it with PBS or HBSS, Entinostat will likely to precipitate out since it has very low solubility in water.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID