Protein Information

General Information of the Protein

Protein ID	PT01499
Protein Name	Histone deacetylase 8
Secondarily Protein Name	Protein deacetylase HDAC8 Protein decrotonylase HDAC8
Gene Name	HDAC8
Secondarily Gene Name	HDACL1 CDA07
Sequence	MEEPEEPADSGQSLVPVYIYSPEYVSMCDSLAKIPKRASMVHSLIEAYALHKQMRIVKPKVASMEEMATFHTDAYLQHLQKVSQEGDDDHPDSIEYGLGYDCPATEGIFDYAAAIGGATITAAQCLIDGMCKVAINWSGGWHHAKKDEASGFCYLNDAVLGILRLRRKFERILYVDLDLHHGDGVEDAFSFTSKVMTVSLHKFSPGFFPGTGDVSDVGLGKGRYYSVNVPIQDGIQDEKYYQICESVLKEVYQAFNPKAVVLQLGADTIAGDPMCSFNMTPVGIGKCLKYILQWQLATLILGGGGYNLANTARCWTYLTGVILGKTLSSEIPDHEFFTAYGPDYVLEITPSCRPDRNEPHRIQQILNYIKGNLKHVV Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Epigenetic regulator > Eraser > Histone deacetylase > HDAC class I
Function	Histone deacetylase that catalyzes the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4) (PubMed:10748112, PubMed:10922473, PubMed:10926844, PubMed:14701748, PubMed:28497810). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events (PubMed:10748112, PubMed:10922473, PubMed:10926844, PubMed:14701748). Histone deacetylases act via the formation of large multiprotein complexes (PubMed:10748112, PubMed:10922473, PubMed:10926844, PubMed:14701748). Also involved in the deacetylation of cohesin complex protein SMC3 regulating release of cohesin complexes from chromatin (PubMed:22885700). May play a role in smooth muscle cell contractility (PubMed:15772115). In addition to protein deacetylase activity, also has protein-lysine deacylase activity: acts as a protein decrotonylase by mediating decrotonylation ((2E)-butenoyl) of histones (PubMed:28497810). Show/Hide
Uniprot ID	Primary ID: Q9BY41 Secondarily ID: A6ND12 A6ND61 A6NET3 A6NJR3 A8MQ62 B4DKN0 B4DV22 Q86VC8 Q9NP76 Q9NYH4 Show/Hide
Ensembl ID	ENSG00000147099
HGNC ID	HGNC:13315
Subcellular Location	Nucleus Chromosome Cytoplasm

Map of Molecular Bioactivity Related to the Protein

Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity

Table of Molecular Bioactivities Related to the Protein

Cell Line ID: CL000023 , BTI-Tn-5B1-4

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0444962 Compound Info	5-cyclopropyl-N-[(1S)-1-[4-(hydroxycarbamoyl)phenyl]ethyl]-2-(5-phenyl-1,3-thiazol-2-yl)-1,3-thiazole-4-carboxamide Show/Hide	C25H22N4O3S2	1
1	IC50 = 16.84 nM Bioactivity Info	TI LI LO TS
CP0003580 Compound Info	Faridak Show/Hide	C21H23N3O2	1
1	IC50 = 19.79 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000314 , HEK293T/17

Cell Line Info

Cell Line ID: CL000017 , HeLa

Cell Line Info

Cell Line ID: CL000012 , Sf21

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0008777 Compound Info	JNJ-26481585 Show/Hide	C21H26N6O2	3
1	IC50 = 4.26 nM
2	Ki = 0.5 nM
3	Ki = 24 nM
CP0003580 Compound Info	Faridak Show/Hide	C21H23N3O2	9
1	IC50 = 5 nM
2	IC50 = 277 nM
3	IC50 = 550 nM
4	IC50 = 1780 nM
5	IC50 = 1864 nM
6	IC50 < 300 nM
7	Ki = 22 nM
8	Ki = 105 nM
9	Ki = 170 nM
CP0003832 Compound Info	N'-hydroxy-N-phenyloctanediamide Show/Hide	C14H20N2O3	91
1	IC50 = 10 nM
2	IC50 = 45 nM
3	IC50 = 82.96 nM
4	IC50 = 110 nM
5	IC50 = 119 nM
6	IC50 = 161 nM
7	IC50 = 172 nM
8	IC50 = 180 nM
9	IC50 = 188 nM
10	IC50 = 191.5 nM
11	IC50 = 193 nM
12	IC50 = 195 nM
13	IC50 = 205.2 nM
14	IC50 = 230 nM
15	IC50 = 232 nM
16	IC50 = 239 nM
17	IC50 = 240 nM
18	IC50 = 243 nM
19	IC50 = 250 nM
20	IC50 = 261 nM
21	IC50 = 272 nM
22	IC50 = 290 nM
23	IC50 = 300 nM
24	IC50 = 306 nM
25	IC50 = 310 nM
26	IC50 = 370 nM
27	IC50 = 400 nM
28	IC50 = 410 nM
29	IC50 = 425 nM
30	IC50 = 440 nM
31	IC50 = 442 nM
32	IC50 = 500 nM
33	IC50 = 540 nM
34	IC50 = 640 nM
35	IC50 = 645 nM
36	IC50 = 646 nM
37	IC50 = 660 nM
38	IC50 = 780 nM
39	IC50 = 820 nM
40	IC50 = 827 nM
41	IC50 = 960 nM
42	IC50 = 1000 nM
43	IC50 = 1020 nM
44	IC50 = 1030 nM
45	IC50 = 1100 nM
46	IC50 = 1140 nM
47	IC50 = 1152 nM
48	IC50 = 1200 nM
49	IC50 = 1260 nM
50	IC50 = 1279.3 nM
51	IC50 = 1337 nM
52	IC50 = 1350 nM
53	IC50 = 1374.7 nM
54	IC50 = 1500 nM
55	IC50 = 1524 nM
56	IC50 = 1532 nM
57	IC50 = 1600 nM
58	IC50 = 1680 nM
59	IC50 = 1700 nM
60	IC50 = 1800 nM
61	IC50 = 1860 nM
62	IC50 = 1890 nM
63	IC50 = 1989 nM
64	IC50 = 2000 nM
65	IC50 = 2185 nM
66	IC50 = 2290 nM
67	IC50 = 2736.9 nM
68	IC50 = 2800 nM
69	IC50 = 3295.01 nM
70	IC50 = 3970 nM
71	IC50 = 4300 nM
72	IC50 = 4800 nM
73	IC50 = 4890 nM
74	IC50 = 5120 nM
75	IC50 = 5300 nM
76	IC50 = 5600 nM
77	IC50 = 7468.5 nM
78	IC50 = 9590 nM
79	IC50 > 500 nM
80	IC50 > 1000 nM
81	IC50 > 5000 nM
82	IC50 > 10000 nM
83	Ka = 581395.3488 nM
84	Kd = 580 nM
85	Kd = 2900 nM
86	Ki = 173 nM
87	Ki = 205 nM
88	Ki = 396 nM
89	Ki = 480 nM
90	Ki = 700 nM
91	Ki = 5330 nM
CP0115609 Compound Info	N-hydroxy-2-[2-[6-(6-methoxypyridin-3-yl)-4-methylquinazolin-8-yl]oxyethyl-methylamino]pyrimidine-5-carboxamide Show/Hide	C23H23N7O4	1
1	IC50 = 12 nM
CP0005479 Compound Info	CHEBI:46024 Show/Hide	C17H22N2O3	30
1	IC50 = 25 nM
2	IC50 = 89.5 nM
3	IC50 = 89.53 nM
4	IC50 = 90 nM
5	IC50 = 100 nM
6	IC50 = 125 nM
7	IC50 = 160 nM
8	IC50 = 165 nM
9	IC50 = 170 nM
10	IC50 = 196 nM
11	IC50 = 232 nM
12	IC50 = 280 nM
13	IC50 = 290 nM
14	IC50 = 300 nM
15	IC50 = 314 nM
16	IC50 = 360 nM
17	IC50 = 390 nM
18	IC50 = 427 nM
19	IC50 = 566 nM
20	IC50 = 770 nM
21	IC50 = 790 nM
22	IC50 = 820 nM
23	IC50 = 1020 nM
24	IC50 = 1360 nM
25	IC50 = 1380 nM
26	IC50 = 4550 nM
27	IC50 = 73100 nM
28	Ki = 45 nM
29	Ki = 69.65 nM
30	Ki = 130 nM
CP0081453 Compound Info	(2R)-2-amino-3-(2,4-dichlorophenyl)-1-(1,3-dihydroisoindol-2-yl)propan-1-one Show/Hide	C17H16Cl2N2O	2
1	IC50 = 90 nM
2	IC50 = 1090 nM
CP0004475 Compound Info	RICOLINOSTAT Show/Hide	C24H27N5O3	4
1	IC50 = 100 nM
2	IC50 = 254 nM
3	IC50 = 436 nM
4	IC50 > 5000 nM
CP0004955 Compound Info	(5R,8S,11S)-5-methyl-8-propan-2-yl-11-[(E)-4-sulfanylbut-1-enyl]-10-oxa-3,17-dithia-7,14,19,20-tetrazatricyclo[14.2.1.12,5]icosa-1(18),2(20),16(19)-triene-6,9,13-trione Show/Hide	C21H28N4O4S3	2
1	IC50 = 102 nM
2	IC50 = 228.4 nM
CP0363242 Compound Info	US8609678, 2-((2-chlorophenyl)(phenyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide [89] Show/Hide	C24H26ClN5O3	1
1	IC50 = 137 nM
CP0013235 Compound Info	(E)-3-[2-butyl-1-[2-(diethylamino)ethyl]benzimidazol-5-yl]-N-hydroxyprop-2-enamide Show/Hide	C20H32Cl2N4O2	2
1	IC50 = 140 nM
2	Ki = 48 nM
CP0004988 Compound Info	pyridin-3-ylmethyl N-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate Show/Hide	C21H20N4O3	10
1	IC50 = 181 nM
2	IC50 = 1440 nM
3	IC50 = 3200 nM
4	IC50 = 9880 nM
5	IC50 = 9884 nM
6	IC50 = 14120 nM
7	IC50 = 44900 nM
8	IC50 = 63400 nM
9	IC50 > 10000 nM
10	IC50 > 40000 nM
CP0003676 Compound Info	N-hydroxy-2-[[2-(6-methoxypyridin-3-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]methyl-methylamino]pyrimidine-5-carboxamide Show/Hide	C23H24N8O4S	2
1	IC50 = 191 nM
2	IC50 = 426 nM
CP0207767 Compound Info	(3S,6R,9S,12R)-3-[(2S)-butan-2-yl]-6-[(4-methoxyphenyl)methyl]-9-(7,7,7-trifluoro-6-oxoheptyl)-1,4,7,10-tetrazabicyclo[10.3.0]pentadecane-2,5,8,11-tetrone Show/Hide	C30H41F3N4O6	1
1	IC50 = 370 nM
CP0007846 Compound Info	N-hydroxy-4-[(2-methyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl)methyl]benzamide Show/Hide	C20H21N3O2	11
1	IC50 = 681 nM
2	IC50 = 695 nM
3	IC50 = 755 nM
4	IC50 = 814 nM
5	IC50 = 850 nM
6	IC50 = 854 nM
7	IC50 = 1270 nM
8	IC50 = 1899 nM
9	IC50 = 2340 nM
10	IC50 > 5000 nM
11	Ki = 96.2 nM
CP0207768 Compound Info	(3S,6R,9S,12R)-3-[(2S)-butan-2-yl]-6-[(4-methoxyphenyl)methyl]-9-(7,7,8,8,8-pentafluoro-6-oxooctyl)-1,4,7,10-tetrazabicyclo[10.3.0]pentadecane-2,5,8,11-tetrone Show/Hide	C31H41F5N4O6	1
1	IC50 = 780 nM
CP0057110 Compound Info	4-[[butyl(phenylcarbamoyl)amino]methyl]-N-hydroxybenzamide Show/Hide	C19H23N3O3	2
1	IC50 = 954 nM
2	IC50 = 988 nM
CP0004959 Compound Info	S-[(E)-4-[(5R,8S,11S)-5-methyl-6,9,13-trioxo-8-propan-2-yl-10-oxa-3,17-dithia-7,14,19,20-tetrazatricyclo[14.2.1.12,5]icosa-1(18),2(20),16(19)-trien-11-yl]but-3-enyl] octanethioate Show/Hide	C29H42N4O5S3	3
1	IC50 = 1068 nM
2	IC50 > 10000 nM
3	IC50 > 30000 nM
CP0013041 Compound Info	HPOB Show/Hide	C17H18N2O4	1
1	IC50 = 2800 nM
CP0010599 Compound Info	UF010 Show/Hide	C11H15BrN2O	1
1	IC50 = 3970 nM
CP0053451 Compound Info	6-(2-Mercapto-acetylamino)-hexanoic acid quinolin-8-ylamide Show/Hide	C17H21N3O2S	1
1	IC50 = 6120 nM
CP0053450 Compound Info	6-(3-adamantan-1-yl-ureido)hexanoic acid hydroxyamide Show/Hide	C17H29N3O3	1
1	IC50 = 6800 nM
CP0070180 Compound Info	tert-butyl N-[4-[3-[[7-(hydroxyamino)-7-oxoheptyl]carbamoyl]-1,2-oxazol-5-yl]phenyl]carbamate Show/Hide	C22H30N4O6	1
1	IC50 = 6851 nM
CP0124688 Compound Info	N-hydroxy-9H-fluorene-9-carboxamide Show/Hide	C14H11NO2	1
1	IC50 = 15000 nM
CP0066173 Compound Info	N-hydroxy-2,2-diphenylacetamide Show/Hide	C14H13NO2	3
1	IC50 = 45000 nM
2	IC50 = 66000 nM
3	IC50 > 50000 nM
CP0085832 Compound Info	(1R,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone Show/Hide	C24H36N4O6S2	1
1	IC50 > 1000 nM
CP0544056 Compound Info	N-hydroxy-4-[[(2,3,4,5,6-pentafluorophenyl)sulfonylamino]methyl]benzamide Show/Hide	C14H9F5N2O4S	1
1	IC50 > 1000 nM
CP0016939 Compound Info	N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide Show/Hide	C23H20N6O	2
1	IC50 > 10000 nM
2	IC50 > 25000 nM
CP0015005 Compound Info	S-[(E)-4-[(4Z,7S,10S)-4-ethylidene-2,5,8,12-tetraoxo-7-propan-2-yl-9-oxa-16-thia-3,6,13,18-tetrazabicyclo[13.2.1]octadeca-1(17),15(18)-dien-10-yl]but-3-enyl] octanethioate Show/Hide	C29H42N4O6S2	1
1	IC50 > 10000 nM
CP0008165 Compound Info	N'-(2-aminophenyl)-N-[3-(1-phenyltriazol-4-yl)phenyl]octanediamide Show/Hide	C28H30N6O2	1
1	IC50 > 30000 nM
CP0013905 Compound Info	[6-(diethylaminomethyl)naphthalen-2-yl]methyl N-[4-(hydroxycarbamoyl)phenyl]carbamate Show/Hide	C24H27N3O4	1
1	Ki = 39 nM
CP0008445 Compound Info	3-[(dimethylamino)methyl]-N-{2-[4-(hydroxycarbamoyl)phenoxy]ethyl}-1-benzofuran-2-carboxamide Show/Hide	C21H23N3O5	1
1	Ki = 280 nM

Clinical Information about the Protein

Target 1 ( Histone deacetylase 8 (HDAC8) )

Target Type	Clinical trial Target
Disease	1 Target-related Disease				1
1	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Investigative Drug(s)	2 Investigative Drugs				2
1	PCI-34051	Drug Info	Investigative	Solid tumour/cancer
2	ST-2987	Drug Info	Investigative	Solid tumour/cancer

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han