ACY-738 | HDAC6 Inhibitor | AmBeed-信号通路专用抑制剂

ACY-738 {[allProObj[0].p_purity_real_show]}

货号：A213388

ACY-738是一种 HDAC6 抑制剂，IC50 值为 1.7 nM。

ACY-738 化学结构
CAS号：1375465-91-0

ACY-738 3D分子结构
CAS号：1375465-91-0

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组蛋白去乙酰化酶亚型比较

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 (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												Nrf2,NF-κB	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。

ACY-738 生物活性

靶点

HDAC6

HDAC6, IC50:1.7 nM

描述

ACY-738 at a concentration of 2.5 μM increases the acetylation of α-tubulin at lysine 40 in RN46A-B14 cells^[1].

体内研究

Administration of ACY-738 at a dose of 5 mg/kg results in a significant elevation of α-tubulin acetylation in whole-brain extracts. However, at a dose of 50 mg/kg, ACY-738 does not enhance locomotor activity in wild-type mice within a home cage setting^[1].

Administered at 5 mg/kg, ACY-738 achieves a peak plasma level of 1310 ng/mL at 0.0830 hours post-administration. At the same dosage (5 mg/kg body weight), it modifies BM B cell differentiation without significantly affecting IgG and C3 deposits in NZB/W mice. A higher dose of ACY-738 (20 mg/kg) markedly mitigates the severity of proteinuria in NZB/W F1 mice. At 5 mg/kg, there is a notable reduction in anti-dsDNA antibody production in aging NZB/W mice. Both 5 and 20 mg/kg doses of ACY-738 reduce serum IL-1β levels as NZB/W mice age. Furthermore, a 5 mg/kg dose significantly lowers glomerular IL-6 and IL-10 mRNA levels by over 50%, and a 20 mg/kg dose reduces these mRNA levels to undetectable quantities^[2].

体外研究

ACY-738 at a concentration of 2.5 μM increases the acetylation of α-tubulin at lysine 40 in RN46A-B14 cells^[1].

ACY-738 细胞实验

Cell Line RN46A-B14 cells RN46A-B14 cells Motor neurons Mec2 cells OSU-CLL cells B cells and T cells HCT-116 cells N2a cells Em-TCL1 B cells CLL patient B cells OSU-CLL cells Mouse neuroblastoma (N2a) cells Mouse mesangial cells (MES 13) Mouse mesangial cells (MES 13) Dorsal root ganglion (DRG) neurons	Concentration	Treated Time	Description	References
RN46A-B14 cells	2.5μM	1 hour	To test the effect of ACY-738 on GR nuclear translocation, results showed that ACY-738 significantly inhibited DEX-induced GR translocation.	Biol Psychiatry. 2015 Feb 15;77(4):345-55.
RN46A-B14 cells	2.5 μM	4 hours	To evaluate the effect of ACY-738 on α-tubulin acetylation. Results showed that ACY-738 significantly increased the acetylation of α-tubulin but had no significant effect on histone H3K9 acetylation.	Neuropsychopharmacology. 2014 Jan;39(2):389-400.
Motor neurons	1 µM	overnight	ACY-738, an HDAC6 inhibitor, was used to rescue axonal transport defects in FUS-ALS patient-derived motor neurons. Results showed that ACY-738 treatment significantly increased the number of moving mitochondria and ER vesicles in motor neurons, restoring axonal transport function.	Nat Commun. 2017 Oct 11;8(1):861.
Mec2 cells	1 μM	24 hours	ACY738 treatment significantly delayed growth kinetics, reduced cell-cycle progression, and arrested cells in G1 phase, increasing apoptosis.	Blood Adv. 2018 Nov 13;2(21):3012-3024.
OSU-CLL cells	1 μM	24 hours	ACY738 treatment significantly delayed growth kinetics, reduced cell-cycle progression, and arrested cells in G1 phase, increasing apoptosis.	Blood Adv. 2018 Nov 13;2(21):3012-3024.
B cells and T cells	4 μM	24 hours	ACY-738 treatment significantly decreased CO2 production from glucose oxidation in B cells and reduced CO2 production from fatty acid oxidation in both T cells and B cells.	Front Immunol. 2019 Oct 25;10:2512.
HCT-116 cells	800 nM		ACY-738 induces tubulin acetylation (a marker of HDAC6 inhibition) at 800nM, whereas histone acetylation (a marker of Class 1 HDAC inhibition) at that concentration is minimal.	Front Immunol. 2019 Oct 25;10:2512.
N2a cells	3μM		ACY-738 significantly increased acetylation levels of α-tubulin and histone 3	Acta Neuropathol Commun. 2019 Jul 5;7(1):107.
Em-TCL1 B cells	0.5μM	24 hours	To assess the effect of HDAC6 inhibition on antigen presentation by CLL B cells, results showed that ACY738 pre-treatment dose-dependently enhanced T-cell activation.	Front Immunol. 2020 Nov 23;11:590072.
CLL patient B cells	0.5μM	24 hours	To assess the effect of HDAC6 inhibition on surface markers of CLL patient B cells, results showed increased expression of MHCII and MHCI, and decreased expression of PD-L1.	Front Immunol. 2020 Nov 23;11:590072.
OSU-CLL cells	0.5μM	24 hours	To evaluate the effect of HDAC6 inhibition on CLL B cell engagement with T cells, results showed increased expression of MHCI, MHCII, and CD86, and decreased expression of PD-L1 and 41BB-L.	Front Immunol. 2020 Nov 23;11:590072.
Mouse neuroblastoma (N2a) cells	1 μM	overnight	To assess the effect of ACY-738 on α-tubulin acetylation, results showed that ACY-738 significantly enhanced the acetylation of α-tubulin without affecting histone acetylation.	Neurotherapeutics. 2017 Apr;14(2):417-428.
Mouse mesangial cells (MES 13)	0.5, 1 or 5 nM	2 hours pretreatment followed by 24 hours stimulation	ACY-738 treatment increased Hsp90 acetylation, decreased iNOS protein, and reduced NF-κB nuclear translocation.	Int Immunopharmacol. 2015 Dec;29(2):494-503.
Mouse mesangial cells (MES 13)	1, 2, 5, 10 or 100 nM	24 hours	ACY-738 at 5 nM significantly increased α-tubulin acetylation with little to no effect on histone H3 acetylation.	Int Immunopharmacol. 2015 Dec;29(2):494-503.
Dorsal root ganglion (DRG) neurons	2.5 μM	overnight	To evaluate the ability of ACY-738 to restore mitochondrial axonal transport defects, results showed that ACY-738 significantly increased mitochondrial motility and total number.	Neurotherapeutics. 2017 Apr;14(2):417-428.

Cell Line

Concentration

Treated Time

Description

References

RN46A-B14 cells

2.5μM

1 hour

To test the effect of ACY-738 on GR nuclear translocation, results showed that ACY-738 significantly inhibited DEX-induced GR translocation.

Biol Psychiatry. 2015 Feb 15;77(4):345-55.

RN46A-B14 cells

2.5 μM

4 hours

To evaluate the effect of ACY-738 on α-tubulin acetylation. Results showed that ACY-738 significantly increased the acetylation of α-tubulin but had no significant effect on histone H3K9 acetylation.

Neuropsychopharmacology. 2014 Jan;39(2):389-400.

Motor neurons

1 µM

overnight

ACY-738, an HDAC6 inhibitor, was used to rescue axonal transport defects in FUS-ALS patient-derived motor neurons. Results showed that ACY-738 treatment significantly increased the number of moving mitochondria and ER vesicles in motor neurons, restoring axonal transport function.

Nat Commun. 2017 Oct 11;8(1):861.

Mec2 cells

1 μM

24 hours

ACY738 treatment significantly delayed growth kinetics, reduced cell-cycle progression, and arrested cells in G1 phase, increasing apoptosis.

Blood Adv. 2018 Nov 13;2(21):3012-3024.

OSU-CLL cells

1 μM

24 hours

ACY738 treatment significantly delayed growth kinetics, reduced cell-cycle progression, and arrested cells in G1 phase, increasing apoptosis.

Blood Adv. 2018 Nov 13;2(21):3012-3024.

B cells and T cells

4 μM

24 hours

ACY-738 treatment significantly decreased CO2 production from glucose oxidation in B cells and reduced CO2 production from fatty acid oxidation in both T cells and B cells.

Front Immunol. 2019 Oct 25;10:2512.

HCT-116 cells

800 nM

ACY-738 induces tubulin acetylation (a marker of HDAC6 inhibition) at 800nM, whereas histone acetylation (a marker of Class 1 HDAC inhibition) at that concentration is minimal.

Front Immunol. 2019 Oct 25;10:2512.

N2a cells

3μM

ACY-738 significantly increased acetylation levels of α-tubulin and histone 3

Acta Neuropathol Commun. 2019 Jul 5;7(1):107.

Em-TCL1 B cells

0.5μM

24 hours

To assess the effect of HDAC6 inhibition on antigen presentation by CLL B cells, results showed that ACY738 pre-treatment dose-dependently enhanced T-cell activation.

Front Immunol. 2020 Nov 23;11:590072.

CLL patient B cells

0.5μM

24 hours

To assess the effect of HDAC6 inhibition on surface markers of CLL patient B cells, results showed increased expression of MHCII and MHCI, and decreased expression of PD-L1.

Front Immunol. 2020 Nov 23;11:590072.

OSU-CLL cells

0.5μM

24 hours

To evaluate the effect of HDAC6 inhibition on CLL B cell engagement with T cells, results showed increased expression of MHCI, MHCII, and CD86, and decreased expression of PD-L1 and 41BB-L.

Front Immunol. 2020 Nov 23;11:590072.

Mouse neuroblastoma (N2a) cells

1 μM

overnight

To assess the effect of ACY-738 on α-tubulin acetylation, results showed that ACY-738 significantly enhanced the acetylation of α-tubulin without affecting histone acetylation.

Neurotherapeutics. 2017 Apr;14(2):417-428.

Mouse mesangial cells (MES 13)

0.5, 1 or 5 nM

2 hours pretreatment followed by 24 hours stimulation

ACY-738 treatment increased Hsp90 acetylation, decreased iNOS protein, and reduced NF-κB nuclear translocation.

Int Immunopharmacol. 2015 Dec;29(2):494-503.

Mouse mesangial cells (MES 13)

1, 2, 5, 10 or 100 nM

24 hours

ACY-738 at 5 nM significantly increased α-tubulin acetylation with little to no effect on histone H3 acetylation.

Int Immunopharmacol. 2015 Dec;29(2):494-503.

Dorsal root ganglion (DRG) neurons

2.5 μM

overnight

To evaluate the ability of ACY-738 to restore mitochondrial axonal transport defects, results showed that ACY-738 significantly increased mitochondrial motility and total number.

Neurotherapeutics. 2017 Apr;14(2):417-428.

ACY-738 动物实验

Species Mice Mice Mice NZB/W F1 mice Mice Mice Mice Mice Mice	Animal Model Chronic social defeat stress model NIH Swiss mice and HDAC6 KO mice on C57BL/6J background EuTCL1 transgenic mouse model Systemic lupus erythematosus model TgFUS+/+ mouse model Em-TCL1 adoptive transfer model Mutant HSPB1-induced CMT2 mouse model Amyloid precursor protein/presenilin 1 (APP/PS1) mouse model Transgenic FUS mice (FUS+/+) expressing wild-type human FUS under the control of the mouse prion promoter (PrP)	Administration	Dosage	Frequency	Description	References
Mice	Chronic social defeat stress model	Intraperitoneal injection	5 mg/kg	Once daily for 20 days	To test the resilience-promoting effect of ACY-738 in social defeat stress, results showed that ACY-738-treated mice maintained higher interaction ratios, indicating enhanced resilience to stress.	Biol Psychiatry. 2015 Feb 15;77(4):345-55.
Mice	NIH Swiss mice and HDAC6 KO mice on C57BL/6J background	Intraperitoneal injection	5 mg/kg and 50 mg/kg	Single or repeated administration (24 h, 4 h, and 30 min before killing)	To evaluate the effect of ACY-738 on α-tubulin acetylation in the brain and its antidepressant-like behavioral effects. Results showed that ACY-738 significantly increased α-tubulin acetylation in the brain and exhibited antidepressant-like effects in the tail suspension test and social defeat paradigm. These effects were fully abrogated in mice with a neural-specific loss of function of HDAC6.	Neuropsychopharmacology. 2014 Jan;39(2):389-400.
Mice	EuTCL1 transgenic mouse model	Oral	25 mg/kg/day	Once daily for 3 months	ACY738 treatment significantly prolonged overall survival, reduced tumor burden and splenomegaly, decreased proliferation of malignant B cells, and increased sensitivity to apoptosis.	Blood Adv. 2018 Nov 13;2(21):3012-3024.
NZB/W F1 mice	Systemic lupus erythematosus model	Dietary administration	200 mg/kg	Daily administration for 4 weeks	ACY-738 treatment significantly reduced manifestations of lupus nephritis in NZB/W mice, decreased IgG and C3 deposition in glomeruli, and reduced plasma cell and germinal center formation in the spleen.	Front Immunol. 2019 Oct 25;10:2512.
Mice	TgFUS+/+ mouse model	Oral	100 mg/kg	Daily administration starting at symptom onset (P30)	ACY-738 treatment significantly extended the lifespan of TgFUS+/+ mice, improved motor performance, and reduced weight loss	Acta Neuropathol Commun. 2019 Jul 5;7(1):107.
Mice	Em-TCL1 adoptive transfer model	Oral	25mg/kg/day	Once daily for 2 weeks	To evaluate the effect of HDAC6 inhibition on CLL progression, results showed that ACY738 delayed CLL progression, reduced PD-L1 expression, and lowered IL-10 levels.	Front Immunol. 2020 Nov 23;11:590072.
Mice	Mutant HSPB1-induced CMT2 mouse model	Intraperitoneal injection	3 mg/kg	Once daily for 21 days	To assess the ability of ACY-738 to reverse motor and sensory deficits, results showed that ACY-738 significantly improved action potential amplitudes in motor and sensory nerves and increased reinnervation of neuromuscular junctions.	Neurotherapeutics. 2017 Apr;14(2):417-428.
Mice	Amyloid precursor protein/presenilin 1 (APP/PS1) mouse model	Oral	100 mg/kg	Daily for 21 days or 90 days	To evaluate the effects of ACY-738 on axonal transport, behavior, and pathology. Results showed that ACY-738 treatment significantly improved axonal transport rates, recovered short-term learning and memory deficits, reduced hyperactivity, and modified tau and tubulin.	Alzheimers Dement (N Y). 2015 Oct 11;1(3):170-181
Mice	Transgenic FUS mice (FUS+/+) expressing wild-type human FUS under the control of the mouse prion promoter (PrP)	Oral	100 mg/kg	Daily administration starting at symptom onset (30 days) until 60 days	ACY-738 treatment restored histone acetylation, slowed down disease progression and significantly expanded the lifespan of transgenic FUS mice. Additionally, ACY-738 restored metabolic alterations in the spinal cord, specifically targeting glycerophospholipid metabolism and reducing cholesteryl esters accumulation.	Int J Mol Sci. 2021 Oct 18;22(20):11224

Species

Mice Mice Mice NZB/W F1 mice Mice Mice Mice Mice Mice

Animal Model

Chronic social defeat stress model NIH Swiss mice and HDAC6 KO mice on C57BL/6J background EuTCL1 transgenic mouse model Systemic lupus erythematosus model TgFUS+/+ mouse model Em-TCL1 adoptive transfer model Mutant HSPB1-induced CMT2 mouse model Amyloid precursor protein/presenilin 1 (APP/PS1) mouse model Transgenic FUS mice (FUS+/+) expressing wild-type human FUS under the control of the mouse prion promoter (PrP)

Administration

Dosage

Frequency

Description

References

Mice

Chronic social defeat stress model

Intraperitoneal injection

5 mg/kg

Once daily for 20 days

To test the resilience-promoting effect of ACY-738 in social defeat stress, results showed that ACY-738-treated mice maintained higher interaction ratios, indicating enhanced resilience to stress.

Biol Psychiatry. 2015 Feb 15;77(4):345-55.

Mice

NIH Swiss mice and HDAC6 KO mice on C57BL/6J background

Intraperitoneal injection

5 mg/kg and 50 mg/kg

Single or repeated administration (24 h, 4 h, and 30 min before killing)

To evaluate the effect of ACY-738 on α-tubulin acetylation in the brain and its antidepressant-like behavioral effects. Results showed that ACY-738 significantly increased α-tubulin acetylation in the brain and exhibited antidepressant-like effects in the tail suspension test and social defeat paradigm. These effects were fully abrogated in mice with a neural-specific loss of function of HDAC6.

Neuropsychopharmacology. 2014 Jan;39(2):389-400.

Mice

EuTCL1 transgenic mouse model

Oral

25 mg/kg/day

Once daily for 3 months

ACY738 treatment significantly prolonged overall survival, reduced tumor burden and splenomegaly, decreased proliferation of malignant B cells, and increased sensitivity to apoptosis.

Blood Adv. 2018 Nov 13;2(21):3012-3024.

NZB/W F1 mice

Systemic lupus erythematosus model

Dietary administration

200 mg/kg

Daily administration for 4 weeks

ACY-738 treatment significantly reduced manifestations of lupus nephritis in NZB/W mice, decreased IgG and C3 deposition in glomeruli, and reduced plasma cell and germinal center formation in the spleen.

Front Immunol. 2019 Oct 25;10:2512.

Mice

TgFUS+/+ mouse model

Oral

100 mg/kg

Daily administration starting at symptom onset (P30)

ACY-738 treatment significantly extended the lifespan of TgFUS+/+ mice, improved motor performance, and reduced weight loss

Acta Neuropathol Commun. 2019 Jul 5;7(1):107.

Mice

Em-TCL1 adoptive transfer model

Oral

25mg/kg/day

Once daily for 2 weeks

To evaluate the effect of HDAC6 inhibition on CLL progression, results showed that ACY738 delayed CLL progression, reduced PD-L1 expression, and lowered IL-10 levels.

Front Immunol. 2020 Nov 23;11:590072.

Mice

Mutant HSPB1-induced CMT2 mouse model

Intraperitoneal injection

3 mg/kg

Once daily for 21 days

To assess the ability of ACY-738 to reverse motor and sensory deficits, results showed that ACY-738 significantly improved action potential amplitudes in motor and sensory nerves and increased reinnervation of neuromuscular junctions.

Neurotherapeutics. 2017 Apr;14(2):417-428.

Mice

Amyloid precursor protein/presenilin 1 (APP/PS1) mouse model

Oral

100 mg/kg

Daily for 21 days or 90 days

To evaluate the effects of ACY-738 on axonal transport, behavior, and pathology. Results showed that ACY-738 treatment significantly improved axonal transport rates, recovered short-term learning and memory deficits, reduced hyperactivity, and modified tau and tubulin.

Alzheimers Dement (N Y). 2015 Oct 11;1(3):170-181

Mice

Transgenic FUS mice (FUS+/+) expressing wild-type human FUS under the control of the mouse prion promoter (PrP)

Oral

100 mg/kg

Daily administration starting at symptom onset (30 days) until 60 days

ACY-738 treatment restored histone acetylation, slowed down disease progression and significantly expanded the lifespan of transgenic FUS mice. Additionally, ACY-738 restored metabolic alterations in the spinal cord, specifically targeting glycerophospholipid metabolism and reducing cholesteryl esters accumulation.

Int J Mol Sci. 2021 Oct 18;22(20):11224

ACY-738 参考文献

ACY-738 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.70mL

0.74mL

0.37mL

18.50mL

3.70mL

1.85mL

37.00mL

7.40mL

3.70mL

ACY-738 技术信息

CAS号	1375465-91-0
分子式	C₁₄H₁₄N₄O₂
分子量	270.29
SMILES Code	O=C(C1=CN=C(NC2(C3=CC=CC=C3)CC2)N=C1)NO
MDL No.	MFCD28347706

别名
运输	蓝冰
InChI Key	LIIWIMDSZVNYHY-UHFFFAOYSA-N
Pubchem ID	57381425

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 30 mg/mL(110.99 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

方案三

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