Wogonin | 汉黄芩黄酮 | BRN 0287152 | CDK Inhibitor | AmBeed-信号通路专用抑制剂

Wogonin/汉黄芩素 {[allProObj[0].p_purity_real_show]}

货号：A583686 同义名： 汉黄芩黄酮 / BRN 0287152; Vogonin

Wogonin 是一种天然黄酮类化合物，能够抑制 CDK8 和 Wnt 的活性。Wogonin 具有抗炎和抗肿瘤的功效，主要用于抗炎症和抗癌研究。

Wogonin/汉黄芩素化学结构
CAS号：632-85-9

Wogonin/汉黄芩素 3D分子结构
CAS号：632-85-9

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CDK 亚型比较

产品名称	Cdc ↓ ↑	CDK1 ↓ ↑	CDK19 ↓ ↑	CDK2 ↓ ↑	CDK3 ↓ ↑	CDK4 ↓ ↑	CDK5 ↓ ↑	CDK6 ↓ ↑	CDK7 ↓ ↑	CDK8 ↓ ↑	CDK9 ↓ ↑	CLK ↓ ↑	其他靶点	纯度
XL413 HCl	++++ Cdc7, IC50: 3.4 nM													99%+
SU9516		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 22 nM		++ CDK4, IC50: 200 nM								99%+
RO-3306		+++ CDK1, Ki: 20 nM											SGK,ERK	98%
R547		++++ CDK1/CyclinB, Ki: 2 nM		++++ CDK2/CyclinE, Ki: 3 nM		++++ CDK4/CyclinD1, Ki: 1 nM								99%+
BMS-265246		++++ CDK1/CyclinB, IC50: 6 nM		++++ CDK2/CyclinE, IC50: 9 nM		+ CDK4/CyclinD, IC50: 230 nM								99%+
NU6027		+ CDK1, Ki: 2.5 μM		+ CDK2, Ki: 1.3 μM									DNA-PK	98%
Purvalanol A	++++ Cdc2/CyclinB, IC50: 4 nM			+++ CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM		+ CDK4/CyclinD1, IC50: 850 nM								99%+
SCH900776				++ CDK2, IC50: 0.16 μM										99%+
AUZ 454				++++ CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM										99%+
A-674563 HCl				++ CDK2, Ki: 46 nM									PKA	99%
JNJ-7706621		++++ CDK1/CyclinB, IC50: 9 nM		++++ CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM	++ CDK3/CyclinE, IC50: 58 nM	+ CDK4/CyclinD1, IC50: 253 nM		++ CDK6/CyclinD1, IC50: 175 nM						99%+
AT7519		++ CDK1/CyclinB, IC50: 210 nM		++ CDK2/CyclinA, IC50: 47 nM	+ CDK3/CyclinE, IC50: 360 nM	++ CDK4/CyclinD1, IC50: 100 nM	+++ CDK5/p35, IC50: 13 nM	++ CDK6/CyclinD3, IC50: 170 nM			++++ CDK9/CyclinT, IC50: <10 nM			98+%
PHA-793887		++ CDK1/CyclinB, IC50: 60 nM		++++ CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM		++ CDK4/CyclinD1, IC50: 62 nM	++++ CDK5/p25, IC50: 5 nM		++++ CDK7/CyclinH, IC50: 10 nM		++ CDK9/CyclinT1, IC50: 138 nM			99%+
Milciclib		+ CDK1/CyclinB, IC50: 398 nM		++ CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM		++ CDK4/CyclinD1, IC50: 160 nM	+ CDK5/p35, IC50: 265 nM		++ CDK7/CyclinH, IC50: 150 nM					99%+
Kenpaullone		+ CDK1/CyclinB, IC50: 0.4μM		+ CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM			+ CDK5/p35, IC50: 0.85μM							98%
SNS-032				+++ CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM			+ CDK5/p35, IC50: 340 nM		++ CDK7/CyclinH, IC50: 62 nM		++++ CDK9/CyclinT, IC50: 4 nM			99%+
Dinaciclib		++++ CDK1, IC50: 3 nM		++++ CDK2, IC50: 1 nM			++++ CDK5, IC50: 1 nM				++++ CDK9, IC50: 4 nM			99%+
PHA-767491 HCl	++++ Cdc7, IC50: 10 nM	+ CDK1, IC50: 250 nM		+ CDK2, IC50: 240 nM			+ CDK5, IC50: 460 nM				+++ CDK9, IC50: 34 nM		MK2	99%
(R)-Roscovitine	+ Cdc2/CyclinB, IC50: 0.65 μM			+ CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM			++ CDK5/p35, IC50: 0.16 μM							99%+
Narazaciclib						++++ CDK4/CyclinD1, IC50: 3.87 nM		++++ CDK6/CyclinD1, IC50: 9.82 nM					RET	99%+
Palbociclib						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%
Abemaciclib						++++ CDK4, IC50: 2 nM		++++ CDK6, IC50: 10 nM						99%
Ribociclib						++++ CDK4, IC50: 10 nM		+++ CDK6, IC50: 39 nM						98%
Palbociclib isethionate						++++ CDK4/CyclinD3, IC50: 9 nM CDK4/CyclinD1, IC50: 11 nM		+++ CDK6/CyclinD2, IC50: 15 nM						99%+
BS-181 HCl									+++ CDK7, IC50: 21 nM					99%+
(E/Z)-THZ1 2HCl									++++ CDK7, IC50: 3.2 nM					99%+
LDC4297									++++ CDK7, IC50: 0.13 nM					99%+
Senexin A			+ CDK19, Kd: 0.31 μM							+ CDK8, Kd: 0.83 μM				99%
MSC2530818										++++ CDK8, IC50: 2.6 nM				99%+
Wogonin											✔			99%+
Riviciclib HCl		++ CDK1/CyclinB, IC50: 79 nM		+ CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM		++ CDK4/CyclinD1, IC50: 63 nM		+ CDK6/CyclinD3, IC50: 396 nM	+ CDK7/CyclinH, IC50: 2.87 μM		+++ CDK9/CyclinT1, IC50: 20 nM			98%
LDC000067				+ CDK2, IC50: 2.441 μM							++ CDK9, IC50: 44 nM			98%
Flavopiridol		+++ CDK1, IC50: 40 nM		+++ CDK2, IC50: 40 nM		+++ CDK4, IC50: 40 nM		+++ CDK6, IC50: 40 nM	+ CDK7, IC50: 300 nM		+++ CDK9, IC50: 20 nM			99%+
LY2857785									+ CDK7, IC50: 0.246 μM	+++ CDK8, IC50: 0.016 μM	+++ CDK9, IC50: 0.011 μM			99%+
AZD-5438		+++ CDK1, IC50: 16 nM		++++ CDK2, IC50: 6 nM							+++ CDK9, IC50: 20 nM			99%+
ML167												++ Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM		99%+
(E/Z)-TG003												+++ mCLK1, IC50: 200 nM mCLK4, IC50: 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。

Wogonin/汉黄芩素生物活性

靶点

CDK9

描述

Wogonin, a naturally occurring flavonoid derived from the root extract of Scutellaria baicalensis, used in the treatment of inflammatory diseases. In vivo, treatment of osteoarthritis chondrocytes with Wogonin (10-50 μM) significantly blocked the IL-1β induced production of NO in a dose dependent manner^[3]. Moreover, wogonin protected retinal ganglion cells survival and suppressed neuro-inflammation in retina after optic nerve crush by inhibiting TLR4-NF-κB pathways^[4]. In vitro, DNA intercalation by Wogonin may result in the stabilization of genomic DNA leading to protective activity^[6].

Wogonin/汉黄芩素细胞实验

Cell Line Human eosinophils 3T3-L1 adipocytes MPC5 cells HK-2 cells Mouse eosinophils	Concentration	Treated Time	Description	References
Human eosinophils	0–125 µM	0–20 hours	Wogonin induced apoptosis in human eosinophils in a time- and concentration-dependent manner, accompanied by caspase-3 activation.	Am J Respir Crit Care Med. 2015 Mar 15;191(6):626-36.
3T3-L1 adipocytes	10 µM	12 hours	To investigate the effect of Wogonin on OPN expression and secretion in 3T3-L1 adipocytes under high glucose conditions, results showed that Wogonin significantly inhibited OPN mRNA and protein expression and reduced OPN secretion.	Acta Pharmacol Sin. 2015 Aug;36(8):987-97.
MPC5 cells	4, 8, 16 µM	24 hours	Wogonin dose-dependently alleviated high glucose (HG)-induced MPC5 cell damage, accompanied by increased expression of WT-1, nephrin, and podocin proteins, and decreased expression of TNF-α, MCP-1, IL-1β as well as phosphorylated p65. Furthermore, wogonin significantly inhibited HG-induced apoptosis in MPC5 cells. Wogonin reversed HG-suppressed autophagy in MPC5 cells, evidenced by increased ATG7, LC3-II, and Beclin-1 protein, and decreased p62 protein.	Acta Pharmacol Sin. 2022 Jan;43(1):96-110.
HK-2 cells	8 µM	24 hours	To evaluate the protective effects of Wogonin on high glucose-induced toxicity in HK-2 cells. The results showed that Wogonin significantly alleviated high glucose-induced cell injury, reduced the production of inflammatory cytokines, ROS, and MDA, and increased the levels of SOD and GSH.	Mol Med. 2024 Jun 6;30(1):78.
Mouse eosinophils	10–100 µM	6 hours	Wogonin induced apoptosis in mouse eosinophils in a concentration-dependent manner, accompanied by caspase-3 activation.	Am J Respir Crit Care Med. 2015 Mar 15;191(6):626-36.

Cell Line

Human eosinophils 3T3-L1 adipocytes MPC5 cells HK-2 cells Mouse eosinophils

Concentration

Treated Time

Description

References

Human eosinophils

0–125 µM

0–20 hours

Wogonin induced apoptosis in human eosinophils in a time- and concentration-dependent manner, accompanied by caspase-3 activation.

Am J Respir Crit Care Med. 2015 Mar 15;191(6):626-36.

3T3-L1 adipocytes

10 µM

12 hours

To investigate the effect of Wogonin on OPN expression and secretion in 3T3-L1 adipocytes under high glucose conditions, results showed that Wogonin significantly inhibited OPN mRNA and protein expression and reduced OPN secretion.

Acta Pharmacol Sin. 2015 Aug;36(8):987-97.

MPC5 cells

4, 8, 16 µM

24 hours

Wogonin dose-dependently alleviated high glucose (HG)-induced MPC5 cell damage, accompanied by increased expression of WT-1, nephrin, and podocin proteins, and decreased expression of TNF-α, MCP-1, IL-1β as well as phosphorylated p65. Furthermore, wogonin significantly inhibited HG-induced apoptosis in MPC5 cells. Wogonin reversed HG-suppressed autophagy in MPC5 cells, evidenced by increased ATG7, LC3-II, and Beclin-1 protein, and decreased p62 protein.

Acta Pharmacol Sin. 2022 Jan;43(1):96-110.

HK-2 cells

8 µM

24 hours

To evaluate the protective effects of Wogonin on high glucose-induced toxicity in HK-2 cells. The results showed that Wogonin significantly alleviated high glucose-induced cell injury, reduced the production of inflammatory cytokines, ROS, and MDA, and increased the levels of SOD and GSH.

Mol Med. 2024 Jun 6;30(1):78.

Mouse eosinophils

10–100 µM

6 hours

Wogonin induced apoptosis in mouse eosinophils in a concentration-dependent manner, accompanied by caspase-3 activation.

Am J Respir Crit Care Med. 2015 Mar 15;191(6):626-36.

Wogonin/汉黄芩素动物实验

Species Mice C57BL/6 mice C57BL/6J mice C57BLKS/J mice Sprague-Dawley rats	Animal Model OVA-induced allergic airway inflammation model STZ-induced type 1 diabetes model STZ-induced diabetic mice model Diabetic mouse model Traumatic brain injury model	Administration	Dosage	Frequency	Description	References
Mice	OVA-induced allergic airway inflammation model	Intraperitoneal injection	1 mg/mouse	Once daily for 4 days	Wogonin attenuated allergic airway inflammation, reduced eosinophil numbers in BAL and interstitial tissue, increased eosinophil apoptosis, and reduced airway mucus production and hyperresponsiveness.	Am J Respir Crit Care Med. 2015 Mar 15;191(6):626-36.
C57BL/6 mice	STZ-induced type 1 diabetes model	Intraperitoneal injection	10 mg/kg	Once every three days for 8 weeks	To investigate the effect of Wogonin on OPN expression in STZ-induced type 1 diabetic mice, results showed that Wogonin significantly reduced serum OPN levels and OPN expression in adipose tissue, and improved hyperglycemia.	Acta Pharmacol Sin. 2015 Aug;36(8):987-97.
C57BL/6J mice	STZ-induced diabetic mice model	Intragastrical gavage	10, 20, 40 mg/kg	Every other day for 12 weeks	Wogonin significantly alleviated albuminuria, histopathological lesions, and p65 NF-κB-mediated renal inflammatory response in STZ-induced diabetic mice. Wogonin dose-dependently inhibited podocyte apoptosis and promoted podocyte autophagy.	Acta Pharmacol Sin. 2022 Jan;43(1):96-110.
C57BLKS/J mice	Diabetic mouse model	Oral	40 mg/kg	Every other day for 12 weeks	To evaluate the protective effects of Wogonin on diabetic nephropathy in mice. The results showed that Wogonin significantly reduced blood glucose, urinary protein, serum creatinine, and blood urea nitrogen levels, while increasing the levels of SOD and GSH, alleviating renal inflammation and fibrosis.	Mol Med. 2024 Jun 6;30(1):78.
Sprague-Dawley rats	Traumatic brain injury model	Intraperitoneal injection	40 mg/kg	10 minutes, 24 hours, and 48 hours post-trauma	Wogonin treatment significantly reduced neurobehavioral disorders, brain edema, and hippocampal neuron damage caused by TBI.	Int J Mol Med. 2022 Apr;49(4):53

Species

Mice C57BL/6 mice C57BL/6J mice C57BLKS/J mice Sprague-Dawley rats

Animal Model

OVA-induced allergic airway inflammation model STZ-induced type 1 diabetes model STZ-induced diabetic mice model Diabetic mouse model Traumatic brain injury model

Administration

Dosage

Frequency

Description

References

Mice

OVA-induced allergic airway inflammation model

Intraperitoneal injection

1 mg/mouse

Once daily for 4 days

Wogonin attenuated allergic airway inflammation, reduced eosinophil numbers in BAL and interstitial tissue, increased eosinophil apoptosis, and reduced airway mucus production and hyperresponsiveness.

Am J Respir Crit Care Med. 2015 Mar 15;191(6):626-36.

C57BL/6 mice

STZ-induced type 1 diabetes model

Intraperitoneal injection

10 mg/kg

Once every three days for 8 weeks

To investigate the effect of Wogonin on OPN expression in STZ-induced type 1 diabetic mice, results showed that Wogonin significantly reduced serum OPN levels and OPN expression in adipose tissue, and improved hyperglycemia.

Acta Pharmacol Sin. 2015 Aug;36(8):987-97.

C57BL/6J mice

STZ-induced diabetic mice model

Intragastrical gavage

10, 20, 40 mg/kg

Every other day for 12 weeks

Wogonin significantly alleviated albuminuria, histopathological lesions, and p65 NF-κB-mediated renal inflammatory response in STZ-induced diabetic mice. Wogonin dose-dependently inhibited podocyte apoptosis and promoted podocyte autophagy.

Acta Pharmacol Sin. 2022 Jan;43(1):96-110.

C57BLKS/J mice

Diabetic mouse model

Oral

40 mg/kg

Every other day for 12 weeks

To evaluate the protective effects of Wogonin on diabetic nephropathy in mice. The results showed that Wogonin significantly reduced blood glucose, urinary protein, serum creatinine, and blood urea nitrogen levels, while increasing the levels of SOD and GSH, alleviating renal inflammation and fibrosis.

Mol Med. 2024 Jun 6;30(1):78.

Sprague-Dawley rats

Traumatic brain injury model

Intraperitoneal injection

40 mg/kg

10 minutes, 24 hours, and 48 hours post-trauma

Wogonin treatment significantly reduced neurobehavioral disorders, brain edema, and hippocampal neuron damage caused by TBI.

Int J Mol Med. 2022 Apr;49(4):53

Wogonin/汉黄芩素参考文献

Wogonin/汉黄芩素实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.59mL

3.52mL

1.76mL

35.18mL

7.04mL

3.52mL

Wogonin/汉黄芩素技术信息

CAS号	632-85-9
分子式	C₁₆H₁₂O₅
分子量	284.26
SMILES Code	COC1=C(O)C=C(O)C2=C1OC(C3=CC=CC=C3)=CC2=O
MDL No.	MFCD00017736

别名	汉黄芩黄酮 ;BRN 0287152; Vogonin
运输	蓝冰
InChI Key	XLTFNNCXVBYBSX-UHFFFAOYSA-N
Pubchem ID	5281703

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 60 mg/mL(211.07 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

配制的工作液建议现用现配，短期内尽快用完。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

细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源

RAW264.7 cells		Function assay		Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells by enzyme immunoassay, IC50=1.07 μM	19233646
SW1353 cells		Function assay		Antiinflammatory activity in PMA-stimulated human SW1353 cells assessed as inhibition of NF-kappaB activation, IC50=39 μM	19555121

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