Cas(58880-19-6), Trichostatin A-阿拉丁试剂, TSA;曲古抑菌素 A,Trichostatin A,

货号 (SKU)	包装规格	是否现货
T129665-1mg	1mg	现货
T129665-5mg	5mg	现货
T129665-10mg	10mg	现货
T129665-25mg	25mg	现货
T129665-50mg	50mg	现货

基本描述

规格或纯度	≥98%
英文名称	Trichostatin A
别名	TSA;曲古抑菌素 A
英文别名	TSA; R-(E,E)]-7-[4-(Dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide
生化机理	Trichostatin A (TSA) is a potent and non-competitive reversible inhibitor of histone deacetylases (HDAC) with a Ki of 3.4 nM. In HeLa cells, TSA blocked cell cycle progression at G1 and induced a 12-fold increase in intracellular levels of gelsolin. In cells latently infected with HIV-1, TSA induced the transcriptional activation of the HIV-1 promoter, which resulted in a marked increase in virus production. In NIH 3T3 cells, TSA induced reversion of oncogenic ras-transformed cells to a normal morphology. In Jurkat cells, TSA inhibited IL-2 gene expression and displayed immunosuppressive activity in a mouse model. Induces increased acetylation of GATA4, a cardiac-specific transcription factor and increases cardiac muscle cell differentiation. In normal fibroblasts, induced Friend cell differentiation and inhibited the G1 and G2 phases of the cell cycle.Potent, selective histone deacetylase (HDAC) inhibitor (K i = 3.4 nM). Induces cell proliferation, differentiation and apoptosis in vitro . Anticancer and antifungal agent. Active in vivo and in vitro .
应用	A potent and non-competitive reversible inhibitor of HDAC.
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	Trichostatin A (TSA)是一种HDAC抑制剂，IC50为1.8 nM左右，HDAC8是HDAC家族中唯一不受TSA影响的成员。A potent and non-competitive reversible inhibitor of HDAC. Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM – HDAC8 is the only known member of the HDAC-family that is not affected by TSA. A potent and non-competitive reversible inhibitor of HDAC.

名称和标识符

IUPAC Name	(2E,4E,6R)-7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamide
INCHI	InChI=1S/C17H22N2O3/c1-12(5-10-16(20)18-22)11-13(2)17(21)14-6-8-15(9-7-14)19(3)4/h5-11,13,22H,1-4H3,(H,18,20)/b10-5+,12-11+/t13-/m1/s1
InChi Key	RTKIYFITIVXBLE-QEQCGCAPSA-N
Canonical SMILES	CC(C=C(C)C=CC(=O)NO)C(=O)C1=CC=C(C=C1)N(C)C
分子式	C₁₇H₂₂N₂O₃
PubChem CID	444732
分子量	302.37

数据库链接

DrugBank Ligand	DB04297
PubChem CID	444732
CAS Registry No.	58880-19-6
ChEMBL Ligand	CHEMBL99
Wikipedia	Trichostatin_A
RCSB PDB Ligand	TSN

化学和物理性质

溶解性	Soluble in water (Partly Miscible), ethanol (2 mg/mL), DMSO (20 mg/mL), acetonitrile, DMF (30 mg/mL), and methanol
敏感性	对热敏感
熔点	144 °C(dec.)
比旋光度	136° (C=0.3,MeOH)

安全信息

象形图	Harmful
信号词	Warning
危险声明	H315: Causes skin irritation H319: Causes serious eye irritation H335: May cause respiratory irritation H302: Harmful if swallowed H317: May cause an allergic skin reaction H312: Harmful in contact with skin H332: Harmful if inhaled H302+H312+H332: Harmful if swallowed, in contact with skin or if inhaled
预防措施声明	P261,P305+P351+P338,P280,P302+P352,P321,P405,P501,P264,P271,P270,P304+P340,P403+P233,P272,P333+P313,P362+P364,P330,P264+P265,P301+P317,P317,P337+P317,P332+P317,P319
WGK Germany	3
RTECS	MI5215000
Reaxy-Rn	2391788
Merck Index	9649
个人防护装备	dust mask type N95 (US), Eyeshields, Faceshields, Gloves

靶标

Target ID

2616

名称

histone deacetylase 2

缩写名

SHP2

家族

3.5.1.- Histone deacetylases (HDACs)

别名

EP₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	488	6q21	HDAC2	histone deacetylase 2
Mouse	2	488	10 B1	Hdac2	histone deacetylase 2
Rat	2	147	20q12	Hdac2	histone deacetylase 2

Entrez Gene

3066 (Hs) , 15182 (Mm) , 84577 (Rn)

UniProtKB

P70288 (Mm) , Q92769 (Hs)

Ensembl Gene

ENSG00000196591 (Hs) , ENSMUSG00000019777 (Mm) , ENSRNOG00000000604 (Rn)

RefSeq Nucleotide

NM_001527 (Hs) , NM_008229 (Mm) , NM_053447 (Rn)

RefSeq Protein

NP_001518 (Hs) , NP_032255 (Mm) , NP_445899 (Rn)

OMIM

605164 (Hs)

Protein GI

293336691 (Hs) , 87162464 (Mm) , 208022663 (Rn)

DrugBank Target

Q92769 (Hs)

CATH/Gene3D

3.40.800.20 (N/A)

ChEMBL Target

CHEMBL1937 (Hs)

Target ID

2617

名称

histone deacetylase 3

缩写名

SHP2

家族

3.5.1.- Histone deacetylases (HDACs)

别名

EP₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	428	5q31.3	HDAC3	histone deacetylase 3
Mouse	2	424	18 B3	Hdac3	histone deacetylase 3
Rat	2	428	18p11	Hdac3	histone deacetylase 3

Entrez Gene

8841 (Hs) , 15183 (Mm) , 84578 (Rn)

UniProtKB

O15379 (Hs) , O88895 (Mm) , Q6P6W3 (Rn)

Ensembl Gene

ENSG00000171720 (Hs) , ENSMUSG00000024454 (Mm) , ENSRNOG00000019618 (Rn)

RefSeq Nucleotide

NM_003883 (Hs) , NM_010411 (Mm) , NM_053448 (Rn)

RefSeq Protein

NP_003874 (Hs) , NP_034541 (Mm) , NP_445900 (Rn)

OMIM

605166 (Hs)

Protein GI

13128862 (Hs) , 89257352 (Mm) , 16758192 (Rn)

DrugBank Target

O15379 (Hs)

CATH/Gene3D

3.40.800.20 (N/A)

ChEMBL Target

CHEMBL5142 (Mm) , CHEMBL1829 (Hs)

Target ID

2618

名称

histone deacetylase 6

缩写名

SHP2

家族

3.5.1.- Histone deacetylases (HDACs)

别名

EP₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	1215	Xp11.23	HDAC6	histone deacetylase 6
Mouse	2	1149	X 3.58 cM	Hdac6	histone deacetylase 6
Rat	2	147	Xq13	Hdac6	histone deacetylase 6

Entrez Gene

10013 (Hs) , 15185 (Mm) , 84581 (Rn)

UniProtKB

Q9UBN7 (Hs) , Q9Z2V5 (Mm)

Ensembl Gene

ENSG00000094631 (Hs) , ENSMUSG00000031161 (Mm) , ENSRNOG00000048738 (Rn)

RefSeq Nucleotide

NM_006044 (Hs) , NM_010413 (Mm)

RefSeq Protein

NP_006035 (Hs) , NP_034543 (Mm)

OMIM

300272 (Hs)

Orphanet

248481 (Hs)

Protein GI

13128864 (Hs) , 194353997 (Mm)

DrugBank Target

Q9UBN7 (Hs)

CATH/Gene3D

3.30.40.10 (N/A) , 3.40.800.20 (N/A)

ChEMBL Target

CHEMBL2878 (Mm) , CHEMBL1865 (Hs)

Target ID

2619

名称

histone deacetylase 8

缩写名

SHP2

家族

3.5.1.- Histone deacetylases (HDACs)

别名

EP₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	377	Xq13.1	HDAC8	histone deacetylase 8
Mouse	2	377	X D	Hdac8	histone deacetylase 8
Rat	2	377	Xq22	Hdac8	histone deacetylase 8

Entrez Gene

55869 (Hs) , 70315 (Mm) , 363481 (Rn)

UniProtKB

B1WC68 (Rn) , Q8VH37 (Mm) , Q9BY41 (Hs)

Ensembl Gene

ENSG00000147099 (Hs) , ENSMUSG00000067567 (Mm) , ENSRNOG00000003122 (Rn)

RefSeq Nucleotide

NM_001126373 (Rn) , NM_018486 (Hs) , NM_027382 (Mm)

RefSeq Protein

NP_001119845 (Rn) , NP_060956 (Hs) , NP_081658 (Mm)

OMIM

300269 (Hs)

Orphanet

290272 (Hs)

Protein GI

8923769 (Hs) , 58037203 (Mm) , 270288778 (Rn)

CATH/Gene3D

3.40.800.20 (N/A)

ChEMBL Target

CHEMBL3192 (Hs) , CHEMBL2347 (Mm)

Target ID

2620

名称

histone deacetylase 9

缩写名

SHP2

家族

3.5.1.- Histone deacetylases (HDACs)

别名

EP₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	1011	7p21.1	HDAC9	histone deacetylase 9
Mouse	2	588	12 A3	Hdac9	histone deacetylase 9
Rat	2	1068	6q16	Hdac9	histone deacetylase 9

Entrez Gene

9734 (Hs) , 79221 (Mm) , 687001 (Rn)

UniProtKB

Q99N13 (Mm) , Q9UKV0 (Hs)

Ensembl Gene

ENSG00000048052 (Hs) , ENSMUSG00000004698 (Mm) , ENSRNOG00000004158 (Rn)

RefSeq Nucleotide

NM_001200045 (Rn) , NM_001271386 (Mm) , NM_058176 (Hs)

RefSeq Protein

NP_001186974 (Rn) , NP_001258315 (Mm) , NP_478056 (Hs)

OMIM

606543 (Hs)

Orphanet

122391 (Hs)

Protein GI

17158039 (Hs) , 405978897 (Mm) , 317689947 (Rn)

DrugBank Target

Q9UKV0 (Hs)

CATH/Gene3D

3.40.800.20 (N/A)

ChEMBL Target

CHEMBL4145 (Hs)

Target ID

2658

名称

histone deacetylase 1

缩写名

SHP2

家族

3.5.1.- Histone deacetylases (HDACs)

别名

EP₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	482	1p35.2-p35.1	HDAC1	histone deacetylase 1
Mouse	2	482	4 63.26 cM	Hdac1	histone deacetylase 1
Rat	2	482	5q36	Hdac1	histone deacetylase 1

RefSeq Protein

NP_004955 (Hs) , NP_032254 (Mm) , NP_001020580 (Rn)

RefSeq Nucleotide

NM_004964 (Hs) , NM_008228 (Mm) , NM_001025409 (Rn)

Entrez Gene

3065 (Hs) , 297893 (Rn) , 433759 (Mm)

UniProtKB

O09106 (Mm) , Q13547 (Hs)

Ensembl Gene

ENSG00000116478 (Hs) , ENSMUSG00000028800 (Mm) , ENSRNOG00000009568 (Rn)

OMIM

601241 (Hs)

Protein GI

13128860 (Hs) , 6680193 (Mm) , 70794768 (Rn)

DrugBank Target

Q13547 (Hs)

CATH/Gene3D

3.40.800.20 (N/A)

ChEMBL Target

CHEMBL4001 (Mm) , CHEMBL325 (Hs)

Target ID

2659

名称

histone deacetylase 4

缩写名

SHP2

家族

3.5.1.- Histone deacetylases (HDACs)

别名

EP₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	1084	2q37.3	HDAC4	histone deacetylase 4
Mouse	2	1076	1 D	Hdac4	histone deacetylase 4
Rat	2	1077	9q36	Hdac4	histone deacetylase 4

RefSeq Protein

NP_006028 (Hs) , NP_997108 (Mm) , NP_445901 (Rn)

RefSeq Nucleotide

NM_006037 (Hs) , NM_207225 (Mm) , NM_053449 (Rn)

Entrez Gene

9759 (Hs) , 208727 (Mm) , 363287 (Rn)

UniProtKB

P56524 (Hs) , Q6NZM9 (Mm)

Ensembl Gene

ENSG00000068024 (Hs) , ENSRNOG00000020372 (Rn) , ENSMUSG00000026313 (Mm)

OMIM

605314 (Hs)

Protein GI

153085395 (Hs) , 46402201 (Mm) , 402744248 (Rn)

CATH/Gene3D

3.40.800.20 (N/A)

ChEMBL Target

CHEMBL3524 (Hs)

Target ID

2660

名称

histone deacetylase 5

缩写名

SHP2

家族

3.5.1.- Histone deacetylases (HDACs)

别名

EP₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	1122	17q21.31	HDAC5	histone deacetylase 5
Mouse	2	1113	11 D	Hdac5	histone deacetylase 5
Rat	2	1113	10q32.1	Hdac5	histone deacetylase 5

RefSeq Protein

NP_005465 (Hs) , NP_001071164 (Mm) , NP_445902 (Rn)

RefSeq Nucleotide

NM_005474 (Hs) , NM_001077696 (Mm) , NM_053450 (Rn)

Entrez Gene

10014 (Hs) , 15184 (Mm) , 84580 (Rn)

UniProtKB

Q9UQL6 (Hs) , Q9Z2V6 (Mm)

Ensembl Gene

ENSG00000108840 (Hs) , ENSMUSG00000008855 (Mm) , ENSRNOG00000020905 (Rn)

OMIM

605315 (Hs)

Protein GI

62750347 (Hs) , 118136295 (Mm) , 281306754 (Rn)

CATH/Gene3D

3.40.800.20 (N/A)

ChEMBL Target

CHEMBL2563 (Hs) , CHEMBL2768 (Mm)

Target ID

2661

名称

histone deacetylase 7

缩写名

SHP2

家族

3.5.1.- Histone deacetylases (HDACs)

别名

EP₂

基因和蛋白信息

Species	Transmembrane Domains	Amino Acids	Chromosomal Location	Gene Symbol	Gene Name
Human	2	952	12q13.11	HDAC7	histone deacetylase 7
Mouse	2	938	15 F1	Hdac7	histone deacetylase 7
Rat	2	238	7q36	Hdac7	histone deacetylase 7

RefSeq Protein

NP_056216 (Hs) , NP_001191204 (Mm)

RefSeq Nucleotide

NM_015401 (Hs) , NM_001204275 (Mm)

Entrez Gene

51564 (Hs) , 56233 (Mm) , 84582 (Rn)

UniProtKB

Q8C2B3 (Mm) , Q8WUI4 (Hs) , Q99P96 (Rn)

Ensembl Gene

ENSG00000061273 (Hs) , ENSMUSG00000022475 (Mm) , ENSRNOG00000055597 (Rn)

OMIM

606542 (Hs)

Protein GI

169234807 (Hs) , 324073114 (Mm) , 30913010 (Rn)

CATH/Gene3D

3.40.800.20 (N/A)

ChEMBL Target

CHEMBL2716 (Hs)

关联配体

Ligand ID	7005
名称	trichostatin A
类别	Synthetic organic
学名	(2E,4E,6R)-7-[4-(dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxohepta-2,4-dienamide
生物活性评价	K_i values of trichostatin A across HDACs 1-9 varies from 0.2 nM to 1400nM .
评价	Trichostatin A Inhibits Class I and II histone deacetylases (HDACs), but NOT the Class III HDACs (sirtuins (SIRTs) 1-7), so is therefore a useful probe of histone deacetylase activity. HDAC1 has been tagged as the drug's primary target for data retrieval purposes only and in no way infers that this is the only target of this drug.

参考文献

1. Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R. (2010) Chemical phylogenetics of histone deacetylases.. Nat Chem Biol, 6 (3): (238-243). [PMID:20139990]
2. Gehring KB et al.. (2016) Involvement of phosphorylated Apis mellifera CREB in gating a honeybee's behavioral response to an external stimulus.. Learn Mem, 23 (5): (195-207). [PMID:27084927]
3. Wang Y et al.. (2019) Dexmedetomidine attenuates the toxicity of ?-amyloid on neurons and astrocytes by increasing BDNF production under the regulation of HDAC2 and HDAC5.. Mol Med Rep, 19 (): (533-540). [PMID:30483749]
4. Hu JX et al.. (2022) Macrophage migration inhibitory factor (MIF) acetylation protects neurons from ischemic injury.. Cell Death Dis, 13 (5): (466). [PMID:35585040]

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曲古柳菌素A

库存信息

库存信息

库存信息

库存信息

库存信息

基本描述

名称和标识符

数据库链接

化学和物理性质

安全信息

靶标

关联配体

参考文献

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曲古柳菌素A

库存信息

库存信息

库存信息

库存信息

库存信息

基本描述

名称和标识符

数据库链接

化学和物理性质

安全信息

靶标

关联配体

参考文献

相关文档

质检报告COA

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产品问答

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