Daphnetin | 7,8-Dihydroxycoumarin;NSC 633563 | Plant Standard | Tyrosine / EGF Receptor Protein Kinase Inhibitor | PKC | EGFR | TGF-beta/Smad | GAK

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瑞香素 /Daphnetin {[allProObj[0].p_purity_real_show]}

货号：A811058 同义名： 7,8-Dihydroxycoumarin;NSC 633563

Daphnetin is an inhibitor of EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM respectively. It derives from plants of the genus Daphne.

Daphnetin 化学结构
CAS号：486-35-1

Daphnetin 3D分子结构
CAS号：486-35-1

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Daphnetin 纯度/质量文件产品仅供科研

货号：A811058 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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EGFR 亚型比较
PKC 亚型比较
转化生长因子-β 亚型比较

产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750), IC50: 2 nM EGFR (E746_A750/T790M), IC50: 14 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKA,PKC	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		98%
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					Src,VEGFR	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						98%
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						98%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		98%
AZD3759	++++ EGFR (WT), IC50: 0.3 nM EGFR (L858R), IC50: 0.2 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR, IC50: 5 nM EGFR (L861Q), IC50: 4 nM						99%+
AG1557	✔						98%
Rociletinib	++ EGFR (L858R/T790M), Ki: 21.5 nM EGFR (wt), Ki: 303.3 nM						98%
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						98%
Osimertinib	++ WT EGFR, IC50: 12.92 nM L858R/T790M EGFR, IC50: 11.44 nM						99%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R), IC50: 2 nM EGFR (L858R/T790M), IC50: 8 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						98+%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						98%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						98%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L858R), IC50: 6 nM EGFR (L861Q) , IC50: <1 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						95%
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		98%
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		98+%
Lazertinib	++++ WT EGFR, IC50: 76 nM L858R/T790M EGFR, IC50: 2 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	98%
(E)-AG 99	✔						99%+
Licochalcone D	✔					PARP,Caspase	97%
Zipalertinib	+++ EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 nM		+++ HER4, IC50: 4 nM		++++ EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						98%
(Rac)-JBJ-04-125-02	✔						99%
(S)-Sunvozertinib	✔						98%
BLU-945	✔						95%
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			98%
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			98+%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			98%
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^L858R/T790M, IC50: 0.51 nM EGFR^T790M, IC50: 0.79 nM		98+%
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	98%
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			99+%
Tucatinib				+++ ErbB2, IC50: 8 nM			98%
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Src,Raf	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM			++ HER2, IC50: 14 nM			98%
Canertinib dihydrochloride	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			98%
Allitinib tosylate	++++ EGFR, IC50: 0.5 nM EGFR (T790M/L858R), IC50: 12 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			98%
Afatinib	++++ EGFR (L858R), IC50: 10 nM EGFR (wt), IC50: 0.5 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			98%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			98%
ALK-IN-1					++ EGFR(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM	ALK	98+%
Brigatinib					+ EGFR(del19), IC50: 39.9 nM EGFR(C797S/T790M/del19), IC50: 67.2 nM	FLT3,ALK	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		97%
Almonertinib					✔		98%
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^L858R/T790M, IC50: 0.19 nM EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM		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。

产品名称	PKC ↓ ↑	PKCα ↓ ↑	PKCβ ↓ ↑	PKCγ ↓ ↑	PKCδ ↓ ↑	PKCε ↓ ↑	PKCζ ↓ ↑	PKCη ↓ ↑	PKCθ ↓ ↑	其他靶点	纯度
Daphnetin	+ PKC, IC50: 25.01 μM									EGFR,PKA	95%
Dequalinium Chloride											99%+
Quercetin	✔									Sirtuin,Src	97%
Myricetrin		✔									96%
Go 6983		+++ PKCα, IC50: 7 nM	+++ PKCβ, IC50: 7 nM	+++ PKCγ, IC50: 6 nM	+++ PKCδ, IC50: 10 nM		++ PKCζ, IC50: 60 nM				99%+
Go6976	+++ PKC, IC50: 7.9 nM	++++ PKCα, IC50: 2.3 nM	+++ PKCβ1, IC50: 6.2 nM							FLT3	99%+
Bisindolylmaleimide I		+++ PKCα, IC50: 20 nM	+++ PKCβ1, IC50: 17 nM PKCβ2, IC50: 16 nM	+++ PKCγ, IC50: 20 nM							99%+
Lawsone methyl ether			✔								99%
Sotrastaurin		++++ PKCα, Ki: 0.95 nM	++++ PKCβ1, Ki: 0.64 nM		++++ PKCδ, Ki: 2.1 nM	++++ PKCε, Ki: 3.2 nM		++++ PKCη, Ki: 1.8 nM	++++ PKCθ, Ki: 0.22 nM		99%+
Enzastaurin		++ PKCα, IC50: 39 nM	+++ PKCβ, IC50: 6 nM	+ PKCγ, IC50: 83 nM		+ PKCε, IC50: 110 nM					98%
Midostaurin		++ PKCα, IC50: 22 nM	++ PKCβ1, IC50: 30 nM PKCβ2, IC50: 31 nM	++ PKCγ, IC50: 24 nM	+ PKCδ, IC50: 330 nM	+ PKCε, IC50: 1.25 μM		+ PKCη, IC50: 160 nM			99%
Ro 31-8220 mesylate		++++ PKCα, IC50: 5 nM	+++ PKCβ1, IC50: 24 nM PKCβ2, IC50: 14 nM	++ PKCγ, IC50: 27 nM		++ PKCε, IC50: 24 nM					99%+
Staurosporine		++++ PKCα, IC50: 2 nM		++++ PKCγ, IC50: 5 nM	+++ PKCδ, IC50: 20 nM	++ PKCε, IC50: 73 nM		++++ PKCη, IC50: 4 nM			99%+
Ruboxistaurin HCl		+ PKCα, IC50: 0.36 μM	++++ PKCβ1, IC50: 4.7 nM PKCβ2, IC50: 5.9 nM	+ PKCγ, IC50: 0.3 μM	+ PKCδ, IC50: 0.25 μM			++ PKCη, IC50: 0.052 μM			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	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 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。

Daphnetin 生物活性

靶点

PKC

PKC, IC50:25.01 μM
EGFR/ErbB1

EGFR, IC50:7.67 μM
PKA

PKA, IC50:9.33 μM

描述

Daphnetin (7,8-dihydroxycoumarin, DAP) is a 7, 8 dihydroxy coumarin isolated from different medicinal plants of the Thymelaeaceae family and exhibits copious pharmacological activities including neuroprotection, anti-cancer, anti-malarial, anti-inflammatory, anti-parasitic and anti-arthritic activity, The inhibition of EGF receptor tyrosine kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate^[3]. DAP markedly decreased cell viability and induced the apoptosis of CIA-FLS along with typical morphological and ultrastructural changes; moreover, DAP increased FasL, cytochrome c (Cyt-c), Bax, caspase-3, caspase-8, and caspase-9 mRNA expression and Bax, caspase-3, caspase-8, and caspase-9 protein expression^[4]. Daphnetin attenuated H2O2-induced apoptosis in a concentration-dependent manner, reduced the cleavage of poly ADP ribose polymerase and caspase 3, and inhibited the phosphorylation of p38 MAPK and c-Jun N-terminal kinases (JNK) in H2O2-induced PC12 cells. In addition, daphnetin induced the expression of HSP70 in a dose- and time-dependent manner, and daphnetin-induced HSP70 expression was reduced by ERK 1/2 inhibitor U0126 in PC12 cells^[5]. Both in vitro and in vivo results indicate that DAP exerts a protective effect against IL-1β in chondrocytes. In vitro ,DAP inhibits the expression of IL-6, IL-12, MMP-3, MMP-9 and MMP-13, induced by IL-1β in rabbit chondrocytes, and stimulates the production of IL-10. The inhibitory effect of DAP on the MMPs is partially regulated by the inhibition of the PI3K/AKT, MAPK and NF-κB signaling pathways. The effect of DAP on OA may be attributed to the suppression of inflammatory factor secretion, chondrocyte apoptosis observed by the decrease in pro-apoptotic Caspase-3 and BAX, and the activation of anti-apoptotic BCL-2^[6].

Daphnetin 参考文献

[1]Jimenez-Orozco FA, Rosales AA, et al. Differential effects of esculetin and daphnetin on in vitro cell proliferation and in vivo estrogenicity. Eur J Pharmacol. 2011 Oct 1;668(1-2):35-41.

[2]J Yang EB, Zhao YN, et al. Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor. Biochem Biophys Res Commun. 1999 Jul 14;260(3):682-5.

[3] Lovedeep Singh,et al. Mechanistic interplay of various mediators involved in mediating the neuroprotective effect of daphnetin. Pharmacol Rep. 2021 Apr 16.

[4]Mao Zheng,et al. Daphnetin induces apoptosis in fibroblast-like synoviocytes from collagen-induced arthritic rats mainly via the mitochondrial pathway, Cytokine. 2020 Sep;133:155146.

[5]Zhilin Qi,et al. Daphnetin protects oxidative stress-induced neuronal apoptosis via regulation of MAPK signaling and HSP70 expression. Oncol Lett. 2016 Sep;12(3):1959-1964.

[6]Xiaohan Zhang,et al. Chondroprotective and antiarthritic effects of Daphnetin used in vitro and in vivo osteoarthritis models. Life Sci. 2020 Jan 1;240:116857.

Daphnetin 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

5.61mL

1.12mL

0.56mL

28.07mL

5.61mL

2.81mL

56.13mL

11.23mL

5.61mL

Daphnetin 技术信息

CAS号	486-35-1
分子式	C₉H₆O₄
分子量	178.142

别名	7,8-Dihydroxycoumarin;NSC 633563
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 50 mg/mL(280.68 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

动物实验配方

瑞香素 /Daphnetin {[allProObj[0].p_purity_real_show]}

Daphnetin 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Daphnetin 质控信息

Daphnetin 生物活性

Daphnetin 参考文献

Daphnetin 实验方案

Daphnetin 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

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PKC	PKC, IC50:25.01 μM
EGFR/ErbB1	EGFR, IC50:7.67 μM
PKA	PKA, IC50:9.33 μM

瑞香素 /Daphnetin {[allProObj[0].p_purity_real_show]}

Daphnetin 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Daphnetin 质控信息

Daphnetin 生物活性

Daphnetin 参考文献

Daphnetin 实验方案

Daphnetin 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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Daphnetin 纯度/质量文件产品仅供科研