BI-78D3 | JNK Inhibitor X | JNK Inhibitor | AmBeed-信号通路专用抑制剂

BI-78D3 {[allProObj[0].p_purity_real_show]}

货号：A166355 同义名： JNK Inhibitor X; c-Jun N-terminal Kinase Inhibitor X

BI-78D3是一种选择性竞争性 JNK 抑制剂，IC50 为 280 nM，选择性高，对 p38α 的抑制作用低于 100 倍。

BI-78D3 化学结构
CAS号：883065-90-5

BI-78D3 3D分子结构
CAS号：883065-90-5

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

BI-78D3 质控信息

JNK 亚型比较

产品名称	JNK ↓ ↑	JNK1 ↓ ↑	JNK2 ↓ ↑	JNK3 ↓ ↑	其他靶点	纯度
Mulberroside A	✔					99%+
Loureirin B	✔				Calcium Channel,Potassium Channel	99%+
Ginsenoside Re	✔				NF-κB	98%
(+)-(3R,8S)-Falcarindiol	✔				ERK,STAT	99%+
trans-Zeatin	✔				ERK,p38 MAPK	95+%
Urolithin B	✔				ERK,NF-κB	95%
Cucurbitacin IIb	✔				NF-κB	99%
Astragaloside IV	✔				Akt,NF-κB,mTOR	98%
m-PEG25-NHS ester	✔					95%
NDMC101	✔					99%+
DB07268		++++ JNK1, IC50: 9 nM				99%+
SP600125	+ MKK4, IC50: 0.4 μM	+++ JNK1, IC50: 40 nM	+++ JNK2, IC50: 40 nM	+++ JNK3, IC50: 90 nM		98%
JNK-IN-7		++++ JNK1, IC50: 1.5 nM	++++ JNK2, IC50: 2 nM	++++ JNK3, IC50: 0.7 nM		99%
JNK-IN-8		++++ JNK1, IC50: 4.7 nM	+++ JNK2, IC50: 18.7 nM	++++ JNK3, IC50: 1 nM		99%+
3,3',5-Triiodo-L-thyronine		++ JNK1, Kd: 240 nM	++ JNK2, Kd: 290 nM	+++ JNK3, Kd: 66 nM		98%
IQ-1S free acid		+ JNK1, IC50: 390 nM	++ JNK2, IC50: 360 nM	+++ JNK3, IC50: 87 nM		99%
BI-78D3	++ JNK, IC50: 280 nM	++ JNK, IC50: 280 nM	++ JNK, IC50: 280 nM	++ JNK, IC50: 280 nM		99%+
Bentamapimod		+++ JNK1, IC50: 80 nM	+++ JNK2, IC50: 90 nM	++ JNK3, IC50: 230 nM		98%
Resveratrol		+ JNK1, IC50: 50 μM				98%
Indirubin-3′-oxime		✔				99%+
SU3327	+ JNK, IC50: 0.7 μM	+ JNK, IC50: 0.7 μM	+ JNK, IC50: 0.7 μM	+ JNK, IC50: 0.7 μM		99%+
JNK Inhibitor VIII		++++ JNK1, Ki: 2 nM JNK1, IC50: 45 nM	++++ JNK2, Ki: 4 nM JNK2, IC50: 160 nM	+++ JNK3, Ki: 52 nM		98%
Doramapimod			✔			99%+
RPI-1			✔			99%
TCS JNK 5a			++ JNK2, pIC50: 6.5	++ JNK3, pIC50: 6.7		98%
SP 600125, negative control			+ JNK2, IC50: 18 μM	+ JNK3, IC50: 24 μM		97%
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。

BI-78D3 生物活性

靶点

JNK1

JNK, IC50:280 nM
JNK

JNK, IC50:280 nM
JNK2

JNK, IC50:280 nM
JNK3

JNK, IC50:280 nM

描述

BI-78D3 is a competitive JNK inhibitor with IC50 of 280 nM that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K.

BI-78D3 细胞实验

Cell Line Primary human AML cells (IDH1R132C) HoxA9-IDH1R132C HoxA9-IDH1R132H HEK293 cells A375 human melanoma cells RL95-2 human endometrial cancer cells Porcine retinal arterioles Human prostate smooth muscle cells Osteoarthritis human MSCs Normal human MSCs HeLa cells	Concentration	Treated Time	Description	References
Primary human AML cells (IDH1R132C)	5 nM	24 hours	Inhibition of R-2HG production	J Immunol. 2018 May 15;200(10):3556-3567.
HoxA9-IDH1R132C	45 nM	8 days	Inhibition of intracellular R-2HG production	J Immunol. 2018 May 15;200(10):3556-3567.
HoxA9-IDH1R132H	60 nM	8 days	Inhibition of intracellular R-2HG production	J Immunol. 2018 May 15;200(10):3556-3567.
HEK293 cells	25 µM	2 hours	Covalent modification of ERK2 by BI-78D3	Nat Commun. 2019 Nov 19;10(1):5232.
A375 human melanoma cells	1 µM	1 hour	Inhibition of ERK phosphorylation and downstream signaling	Nat Commun. 2019 Nov 19;10(1):5232.
RL95-2 human endometrial cancer cells	50 µM	1 hour	BI-78D3 significantly abolished the PAE-induced increase in p-JNK expression but did not significantly affect the anti-proliferative effect of PAE	Exp Ther Med. 2017 Dec;14(6):5445-5451.
Porcine retinal arterioles	7 µM	2 hours	To investigate the effect of acute hyperglycemia on endothelium-dependent dilation of retinal arterioles, BI-78D3 preserved the impaired vasodilation induced by high glucose via inhibition of JIP1/JNK signaling pathway.	Invest Ophthalmol Vis Sci. 2016 Aug 1;57(10):4333-40.
Human prostate smooth muscle cells	30 µM	2 hours	To investigate the effect of BI-78D3 on noradrenaline- and phenylephrine-induced contractions of prostate strips, results showed that BI-78D3 significantly inhibited these contractions	Br J Pharmacol. 2012 Jul;166(6):1926-35.
Osteoarthritis human MSCs	1 µM	24 hours	To investigate the effect of BI-78D3 on Naproxen-induced COL10A1 expression. Results showed that BI-78D3 significantly suppressed Naproxen-induced COL10A1 expression.	Tissue Eng Part A. 2015 Jan;21(1-2):234-45.
Normal human MSCs	1 µM	24 hours	To investigate the effect of BI-78D3 on Naproxen-induced COL10A1 expression. Results showed that BI-78D3 significantly suppressed Naproxen-induced COL10A1 expression.	Tissue Eng Part A. 2015 Jan;21(1-2):234-45.
HeLa cells	12.4 µM (EC50)	60 min pretreatment, 30 min TNF-α stimulation	Inhibits TNF-α stimulated c-Jun phosphorylation	Proc Natl Acad Sci U S A. 2008 Oct 28;105(43):16809-13.

Cell Line

Concentration

Treated Time

Description

References

Primary human AML cells (IDH1R132C)

5 nM

24 hours

Inhibition of R-2HG production

J Immunol. 2018 May 15;200(10):3556-3567.

HoxA9-IDH1R132C

45 nM

8 days

Inhibition of intracellular R-2HG production

J Immunol. 2018 May 15;200(10):3556-3567.

HoxA9-IDH1R132H

60 nM

8 days

Inhibition of intracellular R-2HG production

J Immunol. 2018 May 15;200(10):3556-3567.

HEK293 cells

25 µM

2 hours

Covalent modification of ERK2 by BI-78D3

Nat Commun. 2019 Nov 19;10(1):5232.

A375 human melanoma cells

1 µM

1 hour

Inhibition of ERK phosphorylation and downstream signaling

Nat Commun. 2019 Nov 19;10(1):5232.

RL95-2 human endometrial cancer cells

50 µM

1 hour

BI-78D3 significantly abolished the PAE-induced increase in p-JNK expression but did not significantly affect the anti-proliferative effect of PAE

Exp Ther Med. 2017 Dec;14(6):5445-5451.

Porcine retinal arterioles

7 µM

2 hours

To investigate the effect of acute hyperglycemia on endothelium-dependent dilation of retinal arterioles, BI-78D3 preserved the impaired vasodilation induced by high glucose via inhibition of JIP1/JNK signaling pathway.

Invest Ophthalmol Vis Sci. 2016 Aug 1;57(10):4333-40.

Human prostate smooth muscle cells

30 µM

2 hours

To investigate the effect of BI-78D3 on noradrenaline- and phenylephrine-induced contractions of prostate strips, results showed that BI-78D3 significantly inhibited these contractions

Br J Pharmacol. 2012 Jul;166(6):1926-35.

Osteoarthritis human MSCs

1 µM

24 hours

To investigate the effect of BI-78D3 on Naproxen-induced COL10A1 expression. Results showed that BI-78D3 significantly suppressed Naproxen-induced COL10A1 expression.

Tissue Eng Part A. 2015 Jan;21(1-2):234-45.

Normal human MSCs

1 µM

24 hours

To investigate the effect of BI-78D3 on Naproxen-induced COL10A1 expression. Results showed that BI-78D3 significantly suppressed Naproxen-induced COL10A1 expression.

Tissue Eng Part A. 2015 Jan;21(1-2):234-45.

HeLa cells

12.4 µM (EC50)

60 min pretreatment, 30 min TNF-α stimulation

Inhibits TNF-α stimulated c-Jun phosphorylation

Proc Natl Acad Sci U S A. 2008 Oct 28;105(43):16809-13.

BI-78D3 动物实验

Species C57BL/6 mice Nude mice Pigs	Animal Model ConA-induced liver injury model A375 human melanoma xenograft model Streptozotocin-induced diabetic model	Administration	Dosage	Frequency	Description	References
C57BL/6 mice	ConA-induced liver injury model	Intravenous injection	10 mg/kg	Single dose, evaluated after 7.5 hours	Significantly reduced serum ALT levels, blocked ConA-induced liver damage	Proc Natl Acad Sci U S A. 2008 Oct 28;105(43):16809-13.
Nude mice	A375 human melanoma xenograft model	Intraperitoneal injection	15 mg/kg	Daily for 10 days	Suppression of tumor growth and ERK phosphorylation	Nat Commun. 2019 Nov 19;10(1):5232.
Pigs	Streptozotocin-induced diabetic model	Intraluminal administration	7 μM	Single dose, lasting 2 hours	To investigate the effect of chronic hyperglycemia on endothelium-dependent dilation of retinal arterioles, BI-78D3 restored the impaired vasodilation induced by high glucose via inhibition of JIP1/JNK signaling pathway.	Invest Ophthalmol Vis Sci. 2016 Aug 1;57(10):4333-40.

Species

C57BL/6 mice Nude mice Pigs

Animal Model

ConA-induced liver injury model A375 human melanoma xenograft model Streptozotocin-induced diabetic model

Administration

Dosage

Frequency

Description

References

C57BL/6 mice

ConA-induced liver injury model

Intravenous injection

10 mg/kg

Single dose, evaluated after 7.5 hours

Significantly reduced serum ALT levels, blocked ConA-induced liver damage

Proc Natl Acad Sci U S A. 2008 Oct 28;105(43):16809-13.

Nude mice

A375 human melanoma xenograft model

Intraperitoneal injection

15 mg/kg

Daily for 10 days

Suppression of tumor growth and ERK phosphorylation

Nat Commun. 2019 Nov 19;10(1):5232.

Pigs

Streptozotocin-induced diabetic model

Intraluminal administration

7 μM

Single dose, lasting 2 hours

To investigate the effect of chronic hyperglycemia on endothelium-dependent dilation of retinal arterioles, BI-78D3 restored the impaired vasodilation induced by high glucose via inhibition of JIP1/JNK signaling pathway.

Invest Ophthalmol Vis Sci. 2016 Aug 1;57(10):4333-40.

BI-78D3 参考文献

BI-78D3 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.18mL

2.64mL

1.32mL

26.36mL

5.27mL

2.64mL

BI-78D3 技术信息

CAS号	883065-90-5
分子式	C₁₃H₉N₅O₅S₂
分子量	379.37
SMILES Code	[O-][N+](=O)C1=CN=C(SC2=NNC(=O)N2C2=CC3=C(OCCO3)C=C2)S1
MDL No.	MFCD01313575

别名	JNK Inhibitor X; c-Jun N-terminal Kinase Inhibitor X
运输	蓝冰
InChI Key	QFRLDZGQEZCCJZ-UHFFFAOYSA-N
Pubchem ID	2747117

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, store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 105 mg/mL(276.77 mM)，配合低频超声助溶，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

靶点

靶点	数值

JNK1	JNK, IC50:280 nM
JNK	JNK, IC50:280 nM
JNK2	JNK, IC50:280 nM
JNK3	JNK, IC50:280 nM

BI-78D3 {[allProObj[0].p_purity_real_show]}

BI-78D3 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

BI-78D3 质控信息

BI-78D3 生物活性

BI-78D3 细胞实验

BI-78D3 动物实验

BI-78D3 参考文献

BI-78D3 实验方案

BI-78D3 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

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

靶点	JNK1 JNK, IC50:280 nM JNK JNK, IC50:280 nM JNK2 JNK, IC50:280 nM JNK3 JNK, IC50:280 nM
描述	BI-78D3 is a competitive JNK inhibitor with IC50 of 280 nM that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K.

BI-78D3 {[allProObj[0].p_purity_real_show]}

BI-78D3 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

BI-78D3 质控信息

BI-78D3 生物活性

BI-78D3 细胞实验

BI-78D3 动物实验

BI-78D3 参考文献

BI-78D3 实验方案

BI-78D3 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

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

BI-78D3 纯度/质量文件产品仅供科研