Phellopterin, a natural product isolated and purified from the roots of Saposhnikovia divaricata, is a partial agonist of the central benzodiazepine receptors in vitro, shows cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM, and reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
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产品名称 | ALK1 ↓ ↑ | ALK2 ↓ ↑ | ALK3 ↓ ↑ | ALK4 ↓ ↑ | ALK6 ↓ ↑ | Smad3 ↓ ↑ | TGF-β ↓ ↑ | TGFβRI/ALK5 ↓ ↑ | TGFβRII ↓ ↑ | 其他靶点 | 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。 |
产品名称 | Akt ↓ ↑ | Akt1 ↓ ↑ | Akt2 ↓ ↑ | Akt3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Honokiol | ✔ | MEK | 98% | ||||||||||||||||
PF-04691502 |
++++
P-Akt (S473), IC50: 3.8 nM P-Akt (T308), IC50: 7.5 nM |
98+% | |||||||||||||||||
PHT-427 |
+
Akt, Ki: 2.7 μM |
99%+ | |||||||||||||||||
Deguelin | ✔ | PI3K | 99%+ | ||||||||||||||||
TIC10 isomer | ✔ | ERK | 98+% | ||||||||||||||||
Perifosine |
+
Akt, IC50: 4.7 μM |
98% | |||||||||||||||||
Miltefosine | ✔ | PI3K,PKC | 98% | ||||||||||||||||
Triciribine |
+
Akt, IC50: 130 nM |
99%+ | |||||||||||||||||
Uprosertib |
+
Akt1, IC50: 180 nM |
+
Akt2, IC50: 328 nM |
++
Akt3, IC50: 38 nM |
99%+ | |||||||||||||||
Afuresertib |
++++
Akt1, Ki: 0.08 nM |
++++
Akt2, Ki: 2 nM |
++++
Akt3, Ki: 2.6 nM |
99%+ | |||||||||||||||
Miransertib |
++++
Akt1, IC50: 5 nM |
++++
Akt2, IC50: 4.5 nM |
++
Akt3, IC50: 16 nM |
98+% | |||||||||||||||
GSK-690693 |
++++
Akt1, IC50: 2 nM |
+++
Akt2, IC50: 13 nM |
+++
Akt3, IC50: 9 nM |
99%+ | |||||||||||||||
AT7867 |
++
Akt1, IC50: 32 nM |
++
Akt2, IC50: 17 nM |
++
Akt3, IC50: 47 nM |
PKA | 99%+ | ||||||||||||||
AKT inhibitor VIII |
++
Akt1, IC50: 58 nM |
+
Akt2, IC50: 210 nM |
+
Akt3, IC50: 2119 nM |
98+% | |||||||||||||||
MK-2206 2HCl |
+++
Akt1, IC50: 8 nM |
+++
Akt2, IC50: 12 nM |
+
Akt3, IC50: 65 nM |
99%+ | |||||||||||||||
Ipatasertib |
++++
Akt1, IC50: 5 nM |
++
Akt2, IC50: 18 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
AT13148 |
++
Akt1, IC50: 38 nM |
+
Akt2, IC50: 402 nM |
++
Akt3, IC50: 50 nM |
PKA | 98+% | ||||||||||||||
Capivasertib |
++++
Akt1, IC50: 3 nM |
+++
Akt2, IC50: 8 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
A-674563 HCl |
+++
Akt1, Ki: 11 nM |
PKA | 98% | ||||||||||||||||
CCT128930 |
+++
Akt2, IC50: 6 nM |
PKA | 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 |
PKA,EGFR | 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。 |
描述 | Phellopterin, a natural product isolated and purified from the roots of Saposhnikovia divaricata, is a partial agonist of the central benzodiazepine receptors in vitro, shows cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM, and reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.33mL 0.67mL 0.33mL |
16.65mL 3.33mL 1.66mL |
33.30mL 6.66mL 3.33mL |
CAS号 | 2543-94-4 |
分子式 | C17H16O5 |
分子量 | 300.306 |
别名 | |
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: 105 mg/mL(349.64 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 |