Reaction Details |
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Target | Histone deacetylase 6 |
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Ligand | BDBM19152 |
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Substrate/Competitor | BDBM19150 |
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Meas. Tech. | HDAC Enzyme Activity Assay |
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pH | 8±n/a |
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Temperature | 310.15±n/a K |
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IC50 | 881±138 nM |
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Comments | MCF7 cells growth inhibition, IC50=37 +/- 4 nM.HeLa nuclear HDACs inhibition, IC50=15 +/- 7 nM. |
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Citation | Yurek-George, A; Cecil, AR; Mo, AH; Wen, S; Rogers, H; Habens, F; Maeda, S; Yoshida, M; Packham, G; Ganesan, A The First Biologically Active Synthetic Analogues of FK228, the Depsipeptide Histone Deacetylase Inhibitor. J Med Chem50:5720-5726 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Histone deacetylase 6 |
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Name: | Histone deacetylase 6 |
Synonyms: | HD6 | HDAC6_MOUSE | Hdac6 | Histone Deacetylase 6 (HDAC6) | Histone deacetylase | Histone deacetylase mHDA2 |
Type: | PROTEIN |
Mol. Mass.: | 125762.28 |
Organism: | Mus musculus |
Description: | ChEMBL_1460074 |
Residue: | 1149 |
Sequence: | MTSTGQDSSTRQRKSRHNPQSPLQESSATLKRGGKKCAVPHSSPNLAEVKKKGKMKKLSQ
PAEEDLVVGLQGLDLNPETRVPVGTGLVFDEQLNDFHCLWDDSFPESPERLHAIREQLIL
EGLLGRCVSFQARFAEKEELMLVHSLEYIDLMETTQYMNEGELRVLAETYDSVYLHPNSY
SCACLATGSVLRLVDALMGAEIRNGMAVIRPPGHHAQHNLMDGYCMFNHLAVAARYAQKK
HRIQRVLIVDWDVHHGQGTQFIFDQDPSVLYFSIHRYEHGRFWPHLKASNWSTIGFGQGQ
GYTINVPWNQTGMRDADYIAAFLHILLPVASEFQPQLVLVAAGFDALHGDPKGEMAATPA
GFAHLTHLLMGLAGGKLILSLEGGYNLRALAKGVSASLHTLLGDPCPMLESCVVPCASAQ
TSIYCTLEALEPFWEVLERSVETQEEDEVEEAVLEEEEEEGGWEATALPMDTWPLLQNRT
GLVYDEKMMSHCNLWDNHHPETPQRILRIMCHLEEVGLAARCLILPARPALDSELLTCHS
AEYVEHLRTTEKMKTRDLHREGANFDSIYICPSTFACAKLATGAACRLVEAVLSGEVLNG
IAVVRPPGHHAEPNAACGFCFFNSVAVAARHAQIIAGRALRILIVDWDVHHGNGTQHIFE
DDPSVLYVSLHRYDRGTFFPMGDEGASSQVGRDAGIGFTVNVPWNGPRMGDADYLAAWHR
LVLPIAYEFNPELVLISAGFDAAQGDPLGGCQVTPEGYAHLTHLLMGLAGGRIILILEGG
YNLASISESMAACTHSLLGDPPPQLTLLRPPQSGALVSISEVIQVHRKYWRSLRLMKMED
KEECSSSRLVIKKLPPTASPVSAKEMTTPKGKVPEESVRKTIAALPGKESTLGQAKSKMA
KAVLAQGQSSEQAAKGTTLDLATSKETVGGATTDLWASAAAPENFPNQTTSVEALGETEP
TPPASHTNKQTTGASPLQGVTAQQSLQLGVLSTLELSREAEEAHDSEEGLLGEAAGGQDM
NSLMLTQGFGDFNTQDVFYAVTPLSWCPHLMAVCPIPAAGLDVSQPCKTCGTVQENWVCL
TCYQVYCSRYVNAHMVCHHEASEHPLVLSCVDLSTWCYVCQAYVHHEDLQDVKNAAHQNK
FGEDMPHSH
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BDBM19152 |
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BDBM19150 |
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Name | BDBM19152 |
Synonyms: | (1S,7R,10S,16E,21R)-21-methyl-7-(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone | FK228 Analogue, 8a |
Type | Small organic molecule |
Emp. Form. | C20H30N4O6S2 |
Mol. Mass. | 486.605 |
SMILES | CC(C)[C@H]1NC(=O)[C@H]2CSSCC\C=C\[C@H](CC(=O)N[C@H](C)C(=O)N2)OC(=O)CNC1=O |r,t:13| |
Structure |
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