Tubastatin A TFA | TSA TFA | HDAC6 Inhibitor | AmBeed-信号通路专用抑制剂

Tubastatin A TFA {[allProObj[0].p_purity_real_show]}

货号：A531870 同义名： TSA TFA; Tubastatin A (trifluoroacetate salt)

Tubastatin A (TSA) TFA是一种高效、选择性的 HDAC6 抑制剂，在无细胞试验中的 IC50 为 15 nM，相对于所有其他同工酶具有 1000 倍的选择性，除 HDAC8 (57 倍)。TSA TFA 还抑制 HDAC10 和金属-β-内酰胺酶结构域蛋白 2 (MBLAC2)。

Tubastatin A TFA 化学结构
CAS号：1239262-52-2

Tubastatin A TFA 3D分子结构
CAS号：1239262-52-2

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自噬亚型比较

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半胱天冬酶亚型比较

产品名称	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK2, IC50: 711 nM ULK1, IC50: 108 nM		95%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 HCl	++++ ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		99%
Lys05	✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	HD1 ↓ ↑	HD2 ↓ ↑	HDAC ↓ ↑	HDAC1 ↓ ↑	HDAC10 ↓ ↑	HDAC11 ↓ ↑	HDAC2 ↓ ↑	HDAC3 ↓ ↑	HDAC4 ↓ ↑	HDAC5 ↓ ↑	HDAC6 ↓ ↑	HDAC7 ↓ ↑	HDAC8 ↓ ↑	HDAC9 ↓ ↑	其他靶点	纯度
Givinostat HCl monohydrate	++++ HD1-B, IC50: 7.5 nM HD1-A, IC50: 16 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM															96%
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													99%+
Scriptaid			✔													99%+
Valproic acid sodium			✔												Autophagy	97%
AR-42			+++ HDAC, IC50: 30 nM													99%+
Dacinostat			+++ HDAC, IC50: 32 nM													98+%
CUDC-101			++++ HDAC, IC50: 4.4 nM	++++ HDAC1, IC50: 4.5 nM	+++ HDAC10, IC50: 26.1 nM		+++ HDAC2, IC50: 12.6 nM	++++ HDAC3, IC50: 9.1 nM	+++ HDAC4, IC50: 13.2 nM	+++ HDAC5, IC50: 11.4 nM	++++ HDAC6, IC50: 5.1 nM	+ HDAC7, IC50: 373 nM	++ HDAC8, IC50: 79.8 nM	++ HDAC9, IC50: 67.2 nM	EGFR,HER2	99%+
M344			++ HDAC, IC50: 100 nM													99%+
Splitomicin			+ Sir2p, IC50: 60 μM													99%
Panobinostat			++++ HDAC (MOLT-4 cells), IC50: 5 nM HDAC (Reh cells), IC50: 20 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												NF-κB,Nrf2	98%
Belinostat			+++ HDAC, IC50: 27 nM													98%
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								98%
Valproic acid				+ HDAC1, IC50: 0.4 mM												98%
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								99%+
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								98%
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					98+%
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									99%+
Parthenolide				✔											NF-κB,p53	97% HPLC
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								98%
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								98%
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					99%+
Fimepinostat				++++ HDAC1, IC50: 1.7 nM	++++ HDAC10, IC50: 2.8 nM	++++ HDAC11, IC50: 5.4 nM	++++ HDAC2, IC50: 5.0 nM	++++ HDAC3, IC50: 1.8 nM			+++ HDAC6, IC50: 27 nM					99%+
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								99%+
Santacruzamate A							++++ HDAC2, IC50: 119 pM									99%+
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								99%+
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						99%+
Tasquinimod									✔							99%+
CAY10603											++++ HDAC6, IC50: 2 pM					98%
Tubastatin A											+++ HDAC6, IC50: 15 nM					98%
Tubacin											++++ HDAC6, IC50: 4 nM					99%+
ACY-738											++++ HDAC6, IC50: 1.7 nM					99%+
Nexturastat A											++++ HDAC6, IC50: 5 nM					99%+
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			99%
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			98%
PCI-34051													+++ HDAC8, IC50: 10 nM			99%+
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			99%+
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			99%+
Abexinostat				++++ HDAC1, Ki: 7 nM	+++ HDAC10, IC50: 24 nM		+++ HDAC2, Ki: 19 nM	++++ HDAC3/SMRT, Ki: 8.2 nM			+++ HDAC6, Ki: 17 nM		+ HDAC8, IC50: 280 nM			98%+
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			99%+
HPOB				+ HDAC1, IC50: 2.9 μM	+ HDAC10, IC50: 3.0 μM		+ HDAC2, IC50: 4.4 μM	+ HDAC3, IC50: 1.7 μM			++ HDAC6, IC50: 56 nM		+ HDAC8, IC50: 2.8 μM			97%
Quisinostat 2HCl				++++ HDAC1, IC50: 0.11 nM	++++ HDAC10, IC50: 0.46 nM	++++ HDAC11, IC50: 0.37 nM	++++ HDAC2, IC50: 0.33 nM	++++ HDAC3, IC50: 4.86 nM	++++ HDAC4, IC50: 0.64 nM	++++ HDAC5, IC50: 3.69 nM			++++ HDAC8, IC50: 4.26 nM			97%
Domatinostat				+ HDAC1, IC50: 1.20 μM	+ HDAC10, IC50: 21 μM	+ HDAC11, IC50: 9.7 μM	+ HDAC2, IC50: 1.12 μM	+ HDAC3, IC50: 0.57 μM		+ HDAC5, IC50: 11.3 μM				+ HDAC9, IC50: 50 μM		99%+
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		99%+
Pracinostat				++ HDAC1, IC50: 49 nM	+++ HDAC10, IC50: 40 nM	++ HDAC11, IC50: 93 nM	++ HDAC2, IC50: 96 nM	+++ HDAC3, IC50: 43 nM	++ HDAC4, IC50: 56 nM	+++ HDAC5, IC50: 47 nM	+ HDAC6, IC50: 1.008 μM	++ HDAC7, IC50: 137 nM	++ HDAC8, IC50: 140 nM	++ HDAC9, IC50: 70 nM		99%+
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Capase-7 ↓ ↑	Caspase ↓ ↑	Caspase-1 ↓ ↑	Caspase-10 ↓ ↑	Caspase-2 ↓ ↑	Caspase-3 ↓ ↑	Caspase-4 ↓ ↑	Caspase-5 ↓ ↑	Caspase-6 ↓ ↑	Caspase-8 ↓ ↑	Caspase-9 ↓ ↑	纯度
Emricasan		✔										99%+
Z-VAD(OMe)-FMK		✔										99%+
Z-VAD-FMK		✔										99%+
Q-VD-OPh												97%
VX-765			++++ Caspase-1, Ki: 0.8 nM				++++ Caspase-4, Ki: <0.6 nM					99%+
Ac-DEVD-CHO	+++ caspase-7, Ki: 1.6 nM		+++ Caspase-1, Ki: 18 nM	+++ caspase-10, Ki: 12 nM	+ caspase-2, Ki: 1.71 μM	++++ Caspase-3, Ki: 230 pM	++ Caspase-4, Ki: 132 nM	++ caspase-5, Ki: 205 nM	+++ caspase-6, Ki: 31 nM	++++ caspase-8, Ki: 0.92 nM	++ Caspase-9, Ki: 60 nM	98%+
Z-DEVD-FMK						✔						98%
Z-IETD-FMK										✔		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Tubastatin A TFA 生物活性

描述

Tubastatin A exhibits significant selectivity towards all 11 HDAC isoforms, maintaining over 1000-fold selectivity against all isoforms except HDAC8, for which it demonstrates approximately 57-fold selectivity. In assays assessing homocysteic acid (HCA)-induced neurodegeneration, Tubastatin A demonstrates dose-dependent protection against HCA-induced neuronal cell death, with significant protection observed at 5 μM and near-complete protection at 10 μM^[1]. Treatment of CC12 cells with Tubastatin A results in impaired myotube formation when alpha-tubulin undergoes early hyperacetylation during the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyperacetylated in mature myotubes^[3]. A recent study suggests that treatment with Tubastatin A enhances cell elasticity, as demonstrated by atomic force microscopy (AFM) tests, without causing significant alterations to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L^[4].

体内研究

Daily administration of Tubastatin A at a dose of 0.5 mg/kg suppresses HDAC6, thereby enhancing the suppressive function of Tregs in mouse models of inflammation and autoimmunity, including various experimental colitis models and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection^[2].

体外研究

Treatment of CC12 cells with Tubastatin A results in impaired myotube formation when alpha-tubulin undergoes early hyperacetylation during the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyperacetylated in mature myotubes^[3].

A recent study suggests that treatment with Tubastatin A enhances cell elasticity, as demonstrated by atomic force microscopy (AFM) tests, without causing significant alterations to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L^[4].

Tubastatin A TFA 细胞实验

Cell Line MDA-MB-231-ACSL4-WT cells MDA-MB-231 cells Primary cortical neuron IPS-CM cells CD8+ T cells MCF-7 cells U251-MG cells 661W cells HEK293 cells Dorsal root ganglion neurons N2a cells Primary cortical neuron	Concentration	Treated Time	Description	References
MDA-MB-231-ACSL4-WT cells	8 µM	20 hours	Tubastatin A significantly induced cell death in ferroptosis-sensitive cell lines without affecting cell viability of ferroptosis-resistant cell line.	Redox Biol. 2023 Jun;62:102677.
MDA-MB-231 cells	8 µM	20 hours	Tubastatin A induced ferroptosis and lipid peroxidation in MDA-MB-231 cells, and this effect could be fully rescued by the ferroptosis inhibitor Fer-1 or DFO.	Redox Biol. 2023 Jun;62:102677.
Primary cortical neuron	5 µM and 10 µM	24 hours	Exhibited dose-dependent neuroprotection in an oxidative stress model and showed no neurotoxicity when used alone	J Am Chem Soc. 2010 Aug 11;132(31):10842-6.
IPS-CM cells	3 µM	24 hours	Increase α-tubulin acetylation levels and improve cardiomyocyte contraction function	Nat Commun. 2022 Dec 22;13(1):7886.
CD8+ T cells	10 µM	24 hours	To screen compounds that promote IFN-γ expression in CD8+ T cells, Tubastatin A significantly promoted IFN-γ expression.	Immunity. 2019 Sep 17;51(3):491-507.e7.
MCF-7 cells	10 µM	28 hours	Tubastatin A induced ferroptosis and lipid peroxidation in MCF-7 cells, and this effect could be fully rescued by the ferroptosis inhibitor Fer-1 or DFO.	Redox Biol. 2023 Jun;62:102677.
U251-MG cells	10 nM and 100 nM	48 hours	Compared the inhibitory effects of JOC1, SAHA, and Tubastatin A on HDAC6, finding that JOC1 at 10 nM induced hyperacetylation of α-tubulin, while other HDAC inhibitors did not. 100 nM JOC1 induced stronger α-tubulin acetylation than SAHA and Tubastatin A.	Cell Death Dis. 2020 Jun 2;11(6):417.
661W cells	10 µM	8 hours	To evaluate the protective effects of TST against oxidative stress in photoreceptor cells.	Cell Death Dis. 2017 Aug 31;8(8):e3028.
HEK293 cells	10 µM	8 hours	Inhibit the activity of HDAC6 and increase the acetylation level of SCIN	Autophagy. 2023 Nov;19(11):2934-2957.
Dorsal root ganglion neurons	1 µM	Overnight	Tubastatin A treatment increased acetylated α-tubulin levels and restored mitochondrial axonal transport in mutant GlyRS-expressing neurons.	Brain. 2018 Mar 1;141(3):673-687.
N2a cells	1 µM	Overnight	Tubastatin A treatment increased acetylated α-tubulin levels and blocked the interaction between GlyRS and HDAC6.	Brain. 2018 Mar 1;141(3):673-687.
Primary cortical neuron	2.5 µM and 10 µM		Induced α-tubulin hyperacetylation, indicating selective inhibition of HDAC6	J Am Chem Soc. 2010 Aug 11;132(31):10842-6.

Cell Line

Concentration

Treated Time

Description

References

MDA-MB-231-ACSL4-WT cells

8 µM

20 hours

Tubastatin A significantly induced cell death in ferroptosis-sensitive cell lines without affecting cell viability of ferroptosis-resistant cell line.

Redox Biol. 2023 Jun;62:102677.

MDA-MB-231 cells

8 µM

20 hours

Tubastatin A induced ferroptosis and lipid peroxidation in MDA-MB-231 cells, and this effect could be fully rescued by the ferroptosis inhibitor Fer-1 or DFO.

Redox Biol. 2023 Jun;62:102677.

Primary cortical neuron

5 µM and 10 µM

24 hours

Exhibited dose-dependent neuroprotection in an oxidative stress model and showed no neurotoxicity when used alone

J Am Chem Soc. 2010 Aug 11;132(31):10842-6.

IPS-CM cells

3 µM

24 hours

Increase α-tubulin acetylation levels and improve cardiomyocyte contraction function

Nat Commun. 2022 Dec 22;13(1):7886.

CD8+ T cells

10 µM

24 hours

To screen compounds that promote IFN-γ expression in CD8+ T cells, Tubastatin A significantly promoted IFN-γ expression.

Immunity. 2019 Sep 17;51(3):491-507.e7.

MCF-7 cells

10 µM

28 hours

Tubastatin A induced ferroptosis and lipid peroxidation in MCF-7 cells, and this effect could be fully rescued by the ferroptosis inhibitor Fer-1 or DFO.

Redox Biol. 2023 Jun;62:102677.

U251-MG cells

10 nM and 100 nM

48 hours

Compared the inhibitory effects of JOC1, SAHA, and Tubastatin A on HDAC6, finding that JOC1 at 10 nM induced hyperacetylation of α-tubulin, while other HDAC inhibitors did not. 100 nM JOC1 induced stronger α-tubulin acetylation than SAHA and Tubastatin A.

Cell Death Dis. 2020 Jun 2;11(6):417.

661W cells

10 µM

8 hours

To evaluate the protective effects of TST against oxidative stress in photoreceptor cells.

Cell Death Dis. 2017 Aug 31;8(8):e3028.

HEK293 cells

10 µM

8 hours

Inhibit the activity of HDAC6 and increase the acetylation level of SCIN

Autophagy. 2023 Nov;19(11):2934-2957.

Dorsal root ganglion neurons

1 µM

Overnight

Tubastatin A treatment increased acetylated α-tubulin levels and restored mitochondrial axonal transport in mutant GlyRS-expressing neurons.

Brain. 2018 Mar 1;141(3):673-687.

N2a cells

1 µM

Overnight

Tubastatin A treatment increased acetylated α-tubulin levels and blocked the interaction between GlyRS and HDAC6.

Brain. 2018 Mar 1;141(3):673-687.

Primary cortical neuron

2.5 µM and 10 µM

Induced α-tubulin hyperacetylation, indicating selective inhibition of HDAC6

J Am Chem Soc. 2010 Aug 11;132(31):10842-6.

Tubastatin A TFA 动物实验

Species Mice Nude mice Mice Mice Mice	Animal Model Lmna p.H222P/H222P mice MDA-MB-231 xenograft model High-fat diet-induced obese mouse model C201R mutant Gars mouse model B16-OVA tumor model	Administration	Dosage	Frequency	Description	References
Mice	Lmna p.H222P/H222P mice	Intraperitoneal injection	10 mg/kg	Once daily for 1 month	Restore proper Cx43 localization in cardiomyocytes and improve cardiac function	Nat Commun. 2022 Dec 22;13(1):7886.
Nude mice	MDA-MB-231 xenograft model	Subcutaneous injection	2.5 mg/kg	Once daily until the end of the experiment	Tubastatin A significantly enhanced IR-induced ferroptosis in vivo, and Lipro-1 treatment substantially restored the reduced tumour growth and increased lipid peroxidation in mice.	Redox Biol. 2023 Jun;62:102677.
Mice	High-fat diet-induced obese mouse model	Intraperitoneal injection	25 mg/kg	Daily for two weeks	Tubastatin significantly reduced body weight and food intake in obese mice and improved their metabolic function	Nat Metab. 2022 Jan;4(1):44-59.
Mice	C201R mutant Gars mouse model	Intraperitoneal injection	50 mg/kg	Daily injections for 40 days	Tubastatin A treatment partially restored nerve conduction and motor behavior, and increased acetylated α-tubulin levels in peripheral nerves.	Brain. 2018 Mar 1;141(3):673-687.
Mice	B16-OVA tumor model	IntratumOral injection	60 μg/mouse	Daily until the end of the experiment	To evaluate the inhibitory effect of Tubastatin A and acetate combination therapy on tumor growth, the results showed that the combination therapy significantly inhibited tumor growth.	Immunity. 2019 Sep 17;51(3):491-507.e7.

Species

Mice Nude mice Mice Mice Mice

Animal Model

Lmna p.H222P/H222P mice MDA-MB-231 xenograft model High-fat diet-induced obese mouse model C201R mutant Gars mouse model B16-OVA tumor model

Administration

Dosage

Frequency

Description

References

Mice

Lmna p.H222P/H222P mice

Intraperitoneal injection

10 mg/kg

Once daily for 1 month

Restore proper Cx43 localization in cardiomyocytes and improve cardiac function

Nat Commun. 2022 Dec 22;13(1):7886.

Nude mice

MDA-MB-231 xenograft model

Subcutaneous injection

2.5 mg/kg

Once daily until the end of the experiment

Tubastatin A significantly enhanced IR-induced ferroptosis in vivo, and Lipro-1 treatment substantially restored the reduced tumour growth and increased lipid peroxidation in mice.

Redox Biol. 2023 Jun;62:102677.

Mice

High-fat diet-induced obese mouse model

Intraperitoneal injection

25 mg/kg

Daily for two weeks

Tubastatin significantly reduced body weight and food intake in obese mice and improved their metabolic function

Nat Metab. 2022 Jan;4(1):44-59.

Mice

C201R mutant Gars mouse model

Intraperitoneal injection

50 mg/kg

Daily injections for 40 days

Tubastatin A treatment partially restored nerve conduction and motor behavior, and increased acetylated α-tubulin levels in peripheral nerves.

Brain. 2018 Mar 1;141(3):673-687.

Mice

B16-OVA tumor model

IntratumOral injection

60 μg/mouse

Daily until the end of the experiment

To evaluate the inhibitory effect of Tubastatin A and acetate combination therapy on tumor growth, the results showed that the combination therapy significantly inhibited tumor growth.

Immunity. 2019 Sep 17;51(3):491-507.e7.

Tubastatin A TFA 参考文献

Tubastatin A TFA 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.13mL

2.23mL

1.11mL

22.25mL

4.45mL

2.23mL

Tubastatin A TFA 技术信息

CAS号	1239262-52-2
分子式	C₂₂H₂₂F₃N₃O₄
分子量	449.42
SMILES Code	O=C(NO)C1=CC=C(CN2C3=C(CN(C)CC3)C4=C2C=CC=C4)C=C1.O=C(O)C(F)(F)F
MDL No.	MFCD24873137

别名	TSA TFA; Tubastatin A (trifluoroacetate salt); Tubastatin A trifluoroacetate salt
运输	蓝冰
InChI Key	AVAOVICSJJIYRZ-UHFFFAOYSA-N
Pubchem ID	50898504

存储条件	In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C

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最近浏览的产品

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