BG45 | HDAC3 Inhibitor | AmBeed-信号通路专用抑制剂

BG45 {[allProObj[0].p_purity_real_show]}

货号：A304243

BG45是一种选择性的 HDAC3 抑制剂，IC50 为 289 nM，能够靶向多发性骨髓瘤 (MM) 细胞并诱导 caspase 依赖性凋亡。

BG45 化学结构
CAS号：926259-99-6

BG45 3D分子结构
CAS号：926259-99-6

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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-A, IC50: 16 nM HD1-B, IC50: 7.5 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-A (Maize), IC50: 100 nM HD1-B (Maize), IC50: 3.4 μM															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	HER2,EGFR	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				✔											p53,NF-κB	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。

BG45 生物活性

靶点

HDAC3

HDAC3, IC50:289 nM
HDAC2

HDAC2, IC50:2.2 μM
HDAC1

HDAC1, IC50:2 μM

描述

BG45 is a selective HDAC3 with IC50 value of 289nM. It triggered significant MM cell growth inhibition via apoptosis at 15μM post 48h, shown by caspase and PARP cleavage. BG45 at 10μM or 20μM in a dose-dependent fashion significantly induced acetylation of histone H2A, H3, and H4 (Ac-H3K9, Ac-H4K8, Ac-H4K12, Ac-H2AK5), reduced IL-6-induced p-STAT3-Y705, and triggered hyperacetylation of STAT3 at 20μM in MM.1S cells. Administration of BG45 at dose of 15mg/kg or 50mg/kg, i.p., 5 days a week for 3 weeks, significantly inhibited tumor growth in a murine xenograft model of human MM, and potentiated bortezomib-induced cytotoxicity in vivo^[2].

BG45 细胞实验

Cell Line MM.1S cells NCI-H929 cells RPMI 8226 cells NCI-H929 cells RPMI 8226 cells MM.1S cells MM.1S RPMI8226 SH-SY5Y cells SH-SY5Y cells primary cortical neurons	Concentration	Treated Time	Description	References
MM.1S cells	20 μM	24 h	BG45 treatment downregulated DNMT1 protein levels.	Leukemia. 2017 Dec;31(12):2670-2677.
NCI-H929 cells	20 μM	24 h	BG45 treatment downregulated DNMT1 protein levels.	Leukemia. 2017 Dec;31(12):2670-2677.
RPMI 8226 cells	20 μM	24 h	BG45 treatment downregulated DNMT1 protein levels.	Leukemia. 2017 Dec;31(12):2670-2677.
NCI-H929 cells	20 μM	10 h	BG45 treatment downregulated c-Myc protein levels without altering mRNA levels.	Leukemia. 2017 Dec;31(12):2670-2677.
RPMI 8226 cells	20 μM	10 h	BG45 treatment downregulated c-Myc protein levels without altering mRNA levels.	Leukemia. 2017 Dec;31(12):2670-2677.
MM.1S cells	20 μM	10 h	BG45 treatment downregulated c-Myc protein levels without altering mRNA levels.	Leukemia. 2017 Dec;31(12):2670-2677.
MM.1S	15 µM		To evaluate the effect of BG45 on apoptosis in MM.1S cells, results showed that BG45 induced cleavage of caspase-3 and PARP.	Leukemia. 2014 Mar;28(3):680-9.
RPMI8226	1.875 – 30 µM	48 h and 72 h	To evaluate the inhibitory effect of BG45 on MM cell growth, results showed that BG45 significantly inhibited MM cell growth.	Leukemia. 2014 Mar;28(3):680-9.
SH-SY5Y cells	15 μM	36 h	BG45 increased cell viability, increased the expression of PSD-95 and spinophilin, and improved the cytoskeleton	Front Aging Neurosci. 2021 Jan 19;12:619866.
SH-SY5Y cells	15 μM	36 h	BG45 significantly increased the viability of APPsw-positive cells and decreased the expression of HDAC1, HDAC2, and HDAC3	Molecules. 2022 Jun 29;27(13):4160.
primary cortical neurons	10 μM	48 h	BG45 can upregulate the expression levels of synaptotagmin-1 (SYT-1) and neurofilament light chain (NF-L) in primary neurons	Pharmaceuticals (Basel). 2022 Nov 28;15(12):1481.

Cell Line

Concentration

Treated Time

Description

References

MM.1S cells

20 μM

24 h

BG45 treatment downregulated DNMT1 protein levels.

Leukemia. 2017 Dec;31(12):2670-2677.

NCI-H929 cells

20 μM

24 h

BG45 treatment downregulated DNMT1 protein levels.

Leukemia. 2017 Dec;31(12):2670-2677.

RPMI 8226 cells

20 μM

24 h

BG45 treatment downregulated DNMT1 protein levels.

Leukemia. 2017 Dec;31(12):2670-2677.

NCI-H929 cells

20 μM

10 h

BG45 treatment downregulated c-Myc protein levels without altering mRNA levels.

Leukemia. 2017 Dec;31(12):2670-2677.

RPMI 8226 cells

20 μM

10 h

BG45 treatment downregulated c-Myc protein levels without altering mRNA levels.

Leukemia. 2017 Dec;31(12):2670-2677.

MM.1S cells

20 μM

10 h

BG45 treatment downregulated c-Myc protein levels without altering mRNA levels.

Leukemia. 2017 Dec;31(12):2670-2677.

MM.1S

15 µM

To evaluate the effect of BG45 on apoptosis in MM.1S cells, results showed that BG45 induced cleavage of caspase-3 and PARP.

Leukemia. 2014 Mar;28(3):680-9.

RPMI8226

1.875 – 30 µM

48 h and 72 h

To evaluate the inhibitory effect of BG45 on MM cell growth, results showed that BG45 significantly inhibited MM cell growth.

Leukemia. 2014 Mar;28(3):680-9.

SH-SY5Y cells

15 μM

36 h

BG45 increased cell viability, increased the expression of PSD-95 and spinophilin, and improved the cytoskeleton

Front Aging Neurosci. 2021 Jan 19;12:619866.

SH-SY5Y cells

15 μM

36 h

BG45 significantly increased the viability of APPsw-positive cells and decreased the expression of HDAC1, HDAC2, and HDAC3

Molecules. 2022 Jun 29;27(13):4160.

primary cortical neurons

10 μM

48 h

BG45 can upregulate the expression levels of synaptotagmin-1 (SYT-1) and neurofilament light chain (NF-L) in primary neurons

Pharmaceuticals (Basel). 2022 Nov 28;15(12):1481.

BG45 动物实验

Species Mice CB17 SCID mice Kunming mice APP/PS1 transgenic mice APP/PS1 transgenic mice APPswe/PS1dE9 transgenic mice	Animal Model Murine xenograft model of human MM Human MM.1S xenograft model Alzheimer's disease-related model Alzheimer's disease model APP/PS1 transgenic mice Alzheimer's disease model	Administration	Dosage	Frequency	Description	References
Mice	Murine xenograft model of human MM		20 mg/kg	5 days/week, 3 weeks	Combination of BG45 and AZA significantly inhibited tumor growth and prolonged survival.	Leukemia. 2017 Dec;31(12):2670-2677.
CB17 SCID mice	Human MM.1S xenograft model	Intraperitoneal injection	15 mg/kg and 50 mg/kg	5 days a week for 3 weeks	To evaluate the inhibitory effect of BG45 alone or in combination with bortezomib on tumor growth, results showed that BG45 significantly inhibited tumor growth, and the combination with bortezomib was more effective.	Leukemia. 2014 Mar;28(3):680-9.
Kunming mice	Alzheimer's disease-related model	Intraperitoneal injection	30 mg/kg	9 consecutive days	BG45 decreased the expression of HDAC1 and 2, increased the expression of PSD-95, spinophilin, and synaptophysin (SYP)	Front Aging Neurosci. 2021 Jan 19;12:619866.
APP/PS1 transgenic mice	Alzheimer's disease model	Intraperitoneal injection	30 mg/kg	Once daily for 12 days	BG45 alleviates inflammation and improves synaptic protein expression by regulating the CREB/BDNF/NF-kB pathway, with more significant effects observed with early and repeated administration.	Int J Mol Sci. 2023 Mar 2;24(5):4805
APP/PS1 transgenic mice	APP/PS1 transgenic mice	Intraperitoneal injection	30 mg/kg	12 consecutive days	BG45 alleviated the apoptosis-mediated loss of hippocampal neurons, upregulated synapse-related proteins, reduced Aβ deposition and phosphorylation of tau, and increased the levels of the synapse-related genes GRIK2, SCN3B, SYP, Grm2, and Grid2IP	Molecules. 2022 Jun 29;27(13):4160.
APPswe/PS1dE9 transgenic mice	Alzheimer's disease model	Intraperitoneal injection	30 mg/kg	Once daily for 12 days	BG45 can alleviate damage to dendritic spines, reduce Aβ deposition, and improve learning and memory function	Pharmaceuticals (Basel). 2022 Nov 28;15(12):1481.

Species

Mice CB17 SCID mice Kunming mice APP/PS1 transgenic mice APP/PS1 transgenic mice APPswe/PS1dE9 transgenic mice

Animal Model

Murine xenograft model of human MM Human MM.1S xenograft model Alzheimer's disease-related model Alzheimer's disease model APP/PS1 transgenic mice Alzheimer's disease model

Administration

Dosage

Frequency

Description

References

Mice

Murine xenograft model of human MM

20 mg/kg

5 days/week, 3 weeks

Combination of BG45 and AZA significantly inhibited tumor growth and prolonged survival.

Leukemia. 2017 Dec;31(12):2670-2677.

CB17 SCID mice

Human MM.1S xenograft model

Intraperitoneal injection

15 mg/kg and 50 mg/kg

5 days a week for 3 weeks

To evaluate the inhibitory effect of BG45 alone or in combination with bortezomib on tumor growth, results showed that BG45 significantly inhibited tumor growth, and the combination with bortezomib was more effective.

Leukemia. 2014 Mar;28(3):680-9.

Kunming mice

Alzheimer's disease-related model

Intraperitoneal injection

30 mg/kg

9 consecutive days

BG45 decreased the expression of HDAC1 and 2, increased the expression of PSD-95, spinophilin, and synaptophysin (SYP)

Front Aging Neurosci. 2021 Jan 19;12:619866.

APP/PS1 transgenic mice

Alzheimer's disease model

Intraperitoneal injection

30 mg/kg

Once daily for 12 days

BG45 alleviates inflammation and improves synaptic protein expression by regulating the CREB/BDNF/NF-kB pathway, with more significant effects observed with early and repeated administration.

Int J Mol Sci. 2023 Mar 2;24(5):4805

APP/PS1 transgenic mice

Intraperitoneal injection

30 mg/kg

12 consecutive days

BG45 alleviated the apoptosis-mediated loss of hippocampal neurons, upregulated synapse-related proteins, reduced Aβ deposition and phosphorylation of tau, and increased the levels of the synapse-related genes GRIK2, SCN3B, SYP, Grm2, and Grid2IP

Molecules. 2022 Jun 29;27(13):4160.

APPswe/PS1dE9 transgenic mice

Alzheimer's disease model

Intraperitoneal injection

30 mg/kg

Once daily for 12 days

BG45 can alleviate damage to dendritic spines, reduce Aβ deposition, and improve learning and memory function

Pharmaceuticals (Basel). 2022 Nov 28;15(12):1481.

BG45 动物研究

Dose

Mice: 15 mg/kg, 50 mg/kg^[1] (i.p.)

Administration

i.p.

BG45 参考文献

BG45 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

4.67mL

0.93mL

0.47mL

23.34mL

4.67mL

2.33mL

46.68mL

9.34mL

4.67mL

BG45 技术信息

CAS号	926259-99-6
分子式	C₁₁H₁₀N₄O
分子量	214.22
SMILES Code	O=C(C1=NC=CN=C1)NC2=CC=CC=C2N
MDL No.	MFCD09046162

别名
运输	蓝冰
InChI Key	LMWPVSNHKACEKW-UHFFFAOYSA-N
Pubchem ID	16773791

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 50 mg/mL(233.4 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

BG45 {[allProObj[0].p_purity_real_show]}

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BG45 质控信息

BG45 生物活性

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BG45 技术信息

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HDAC3	HDAC3, IC50:289 nM
HDAC2	HDAC2, IC50:2.2 μM
HDAC1	HDAC1, IC50:2 μM

BG45 {[allProObj[0].p_purity_real_show]}

BG45 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

BG45 质控信息

BG45 生物活性

BG45 细胞实验

BG45 动物实验

BG45 动物研究

BG45 参考文献

BG45 实验方案

BG45 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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BG45 纯度/质量文件产品仅供科研