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Chelerythrine/白屈菜红碱 {[allProObj[0].p_purity_real_show]}

货号:A164459 同义名: Toddaline; Broussonpapyrine

Chelerythrine 是一种天然生物碱,作为一种有效和选择性的 Ca2+/磷脂依赖性 PKC 拮抗剂,IC50 为 0.7 μM。它具有抗肿瘤、抗糖尿病和抗炎活性,抑制 BclXL-Bak BH3 肽结合,IC50 为 1.5 μM,置换 Bax 从 BclXL 并触发凋亡和自噬。

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Chelerythrine/白屈菜红碱 化学结构 CAS号:34316-15-9
Chelerythrine/白屈菜红碱 化学结构
CAS号:34316-15-9
Chelerythrine/白屈菜红碱 3D分子结构
CAS号:34316-15-9
Chelerythrine/白屈菜红碱 化学结构 CAS号:34316-15-9
Chelerythrine/白屈菜红碱 3D分子结构 CAS号:34316-15-9
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Chelerythrine/白屈菜红碱 纯度/质量文件 产品仅供科研

货号:A164459 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Bax Bcl-2 Bcl-B Bcl-w Bcl-xL Bfl-1 Mcl-1 其他靶点 纯度
BTSA1 99%+
HA14-1 +

Bcl-2, IC50: 9 μM

98%
Venetoclax ++++

Bcl-2, Ki: <0.01 nM

99%
Navitoclax 99%+
Obatoclax Mesylate +++

Bcl-2, Ki: 0.22 μM

99%
ABT-737 +++

Bcl-2, EC50: 30.3 nM

+

Bcl-B, EC50: 1.82 μM

+++

Bcl-w, EC50: 197.8 nM

+++

Bcl-xL, EC50: 78.7 nM

99%+
Gambogic Acid +

Bcl-2, IC50: 1.21 μM

Bfl-1, IC50: 1.06 μM

++

Bcl-B, IC50: 0.66 μM

++++

Bcl-w, IC50: 0.02 μM

+

Bcl-xL, IC50: 1.47 μM

+

Bfl-1, IC50: 1.06 μM

++

Mcl-1, IC50: 0.79 μM

Caspase 99% HPLC
BH3I-1 +

BH3-Bcl-xL interaction, Ki: 2.4 μM

99%
A-1331852 ++++

Bcl-xL, Ki: <0.01 nM

99%+
A-1210477 ++++

MCL-1, IC50: 26.2 nM

99%+
Maritoclax 97%
TW-37 +++

Bcl-2, Ki: 0.29 μM

+

Bcl-xL, Ki: 1.11 μM

+++

Mcl-1, Ki: 0.26 μM

98%
UMI-77 ++

Mcl-1, Ki: 490 nM

97%
(R)-(-)-Gossypol acetic acid ++

Bcl-2, Ki: 0.32 μM

++

Bcl-xL, Ki: 0.48 μM

+++

Mcl-1, Ki: 0.18 μM

99%
Sabutoclax ++

Bcl-2, IC50: 0.32 μM

Bfl-1, IC50: 0.62 μM

++

Bcl-xL, IC50: 0.31 μM

++

Bfl-1, IC50: 0.62 μM

+++

Mcl-1, IC50: 0.20 μM

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 95%
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

+++

PKCβ2, IC50: 16 nM

PKCβ1, IC50: 17 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

++

PKCβ2, IC50: 31 nM

PKCβ1, IC50: 30 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

+++

PKCβ2, IC50: 14 nM

PKCβ1, IC50: 24 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

++++

PKCβ2, IC50: 5.9 nM

PKCβ1, IC50: 4.7 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 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 2HCl ++++

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%
(E/Z)-SIS3 free base 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

99%
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 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK1, IC50: 108 nM

ULK2, IC50: 711 nM

95%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 HCl ++++

ULK1, IC50: 2.9 nM

ULK2, IC50: 1.1 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

99%
Lys05 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。

Chelerythrine/白屈菜红碱 生物活性

描述 Chelerythrine, a natural product isolated and purified from the herbs of Chelidonium majus with potent antimanic, antiproliferatvie and antitumor effect, can inhibit telomerase activity, and is a well-known protein kinase C inhibitor.

Chelerythrine/白屈菜红碱 细胞实验

Cell Line
Concentration Treated Time Description References
Hepatic stellate cells 0-5 µM 1 hour Enhanced leptin signaling, observed elevated tyrosine phosphorylation of JAK2 Nat Commun. 2018 Jan 18;9(1):283.
293T cells 2 µM 1 hour Enhanced insulin signaling, observed enhanced phosphorylation of the insulin receptor β-subunit (IR-β) and activation of AKT Nat Commun. 2018 Jan 18;9(1):283.
Aplysia sensory and motor neuron cocultures 10 µM 1 hour Inhibition of PKM Apl III reversed 5HT-induced synaptic growth, returning varicosity numbers to pretraining levels Elife. 2014 Nov 17;3:e03896.
Rat aortic vascular smooth muscle cells (VSMCs) 100 µM 1 hour Chelerythrine attenuated the dexmedetomidine-induced PKC phosphorylation Int J Mol Sci. 2016 Sep 30;17(10):1663.
Rat aortic vascular smooth muscle cells (VSMCs) 100 µM 1 hour Chelerythrine attenuated the dexmedetomidine-induced phosphorylation of MLC20 at Ser19 Int J Mol Sci. 2016 Sep 30;17(10):1663.
Rat aortic vascular smooth muscle cells (VSMCs) 100 µM 1 hour Chelerythrine attenuated the dexmedetomidine-induced phosphorylation of CPI-17 at Thr38 Int J Mol Sci. 2016 Sep 30;17(10):1663.
LO2 cells 10 µM 24 hours CHE had minimal cytotoxic effects on normal LO2 cells. J Cell Mol Med. 2020 Jan;24(1):50-60.
Jurkat WT cells 1 µg/mL 48 hours After CHE treatment, 45% of Jurkat WT cells died. Int J Mol Sci. 2023 Oct 20;24(20):15405.
RAW264.7 cells 0.5, 1, or 2 µM 1 hour To evaluate the inhibitory effect of CH on LPS-induced inflammatory responses. Results showed that CH pretreatment significantly inhibited LPS-induced production of TNF-α, IL-6, and IL-1β. Front Pharmacol. 2018 Sep 26;9:1047.
Human B-lymphocytes 10 µM 15 minutes To study the effect of chelerythrine on ATP- and PMA-induced PLD activity, results showed chelerythrine inhibited ATP-induced PLD activity by 94.2±21.9% and PMA-induced PLD activity by 68.2±7.4% Br J Pharmacol. 2004 Jul;142(6):1015-9.
A375 cells 1 µg/mL 2 and 3 hours After CHE treatment, A375 cells showed an increase in cPARP (apoptosis marker), indicating apoptosis induction. Int J Mol Sci. 2023 Oct 20;24(20):15405.
Human erythrocytes 1-10 µM 2 hours Chelerythrine was able to partially inhibit costunolide-induced phosphatidylserine exposure and cell shrinkage Apoptosis. 2020 Oct;25(9-10):674-685.
786-O cells 6, 9, 12 µM 20 hours CHE induced G2/M cell cycle arrest and apoptosis in 786-O cells by increasing Cle-PARP expression and decreasing the Bcl-2/Bax ratio. J Cell Mol Med. 2020 Jan;24(1):50-60.
Caki cells 6, 9, 12 µM 20 hours CHE induced G2/M cell cycle arrest and apoptosis in Caki cells by increasing Cle-PARP expression and decreasing the Bcl-2/Bax ratio. J Cell Mol Med. 2020 Jan;24(1):50-60.
HepG2 cells 1.25-10 µM 24 hours CHE induces apoptotic cell death in HepG2 cells involving the inhibition of Akt pathway and the activation of oxidative stress and mitochondrial apoptotic pathway Antioxidants (Basel). 2022 Sep 18;11(9):1837.
Non-small cell lung cancer NCI-H1299 cells 10, 15, 20 µM 24 hours To study the effect of CHE on cell viability, results showed CHE significantly reduced the viability of NCI-H1299 cells in a concentration-dependent manner Redox Biol. 2017 Aug;12:367-376.
Non-small cell lung cancer A549 cells 10, 15, 20 µM 24 hours To study the effect of CHE on cell viability, results showed CHE significantly reduced the viability of A549 cells in a concentration-dependent manner Redox Biol. 2017 Aug;12:367-376.
NCI-N87 cells 3.81 µM (IC50) 24 hours To evaluate the cytotoxicity of Chelerythrine on NCI-N87 cells, results showed Chelerythrine significantly reduced cell viability. Molecules. 2023 Sep 28;28(19):6842.
Mechanically skinned skeletal muscle fibres of the rat 12 µM 30 s Chelerythrine (12 μM) was shown to restore ECC in these fibres. Restored force responses were similar in peak but significantly broadened compared to initial control responses. Early exposure to chelerythrine prevented run-down of DIFRs. Chelerythrine also induced spontaneous force responses in some fibres. Br J Pharmacol. 2003 Feb;138(3):417-26.
MKN45 cells 5 µM 4 hours Chelerythrine significantly inhibited TXNRD1 activity in MKN45 cells. Molecules. 2023 Sep 28;28(19):6842.
Jurkat CASP3/7/6-/- cells 1 µg/mL 48 hours After CHE treatment, 13% of Jurkat CASP3/7/6-/- cells died. Int J Mol Sci. 2023 Oct 20;24(20):15405.
Jurkat FADD-/- cells 1 µg/mL 48 hours After CHE treatment, 81% of Jurkat FADD-/- cells died. Int J Mol Sci. 2023 Oct 20;24(20):15405.
Human B-lymphocytes 5 µM and 10 µM 5 minutes To study the effect of chelerythrine on ATP concentration-effect curves, results showed chelerythrine inhibited P2X7 receptor in a noncompetitive manner Br J Pharmacol. 2004 Jul;142(6):1015-9.
Human B-lymphocytes 10 µM 5 minutes To examine the effect of chelerythrine on P2X7 receptor function, results showed chelerythrine inhibited ATP-induced 86Rb+ efflux by 73.4±3.5% Br J Pharmacol. 2004 Jul;142(6):1015-9.

Chelerythrine/白屈菜红碱 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rat Isolated perfused heart model Perfusion 10 mM Started 5 min before ischemia, infused for 20 min together with 5–10-sP Chelerythrine abrogated the improvement in mitochondrial function induced by 5–10-sP, including ADP-stimulated respiration, ATP production, and prevention of ROS formation. Front Pharmacol. 2020 May 5;11:545
Aplysia californica Long-term sensitization model of siphon-withdrawal reflex Intrahemocoel injection 200 µl/100 g Single injection PKM Apl III inhibition erased behavioral expression of long-term sensitization memory, but memory could be reinstated with additional training Elife. 2014 Nov 17;3:e03896.
C57Bl6/J mice High fat diet-induced obesity model Intraperitoneal injection 3 mg/kg Once daily for 30 days Improved metabolism, promoted insulin and leptin signaling, and reduced body weight Nat Commun. 2018 Jan 18;9(1):283.
Sprague-Dawley rats Subarachnoid hemorrhage (SAH) model Cisterna magna injection 5 µM Injected once 2 days before SAH induction and on day 3 and day 5 after SAH induction To investigate the effect of PKC inhibitors on SAH-induced increase in Cx43 expression. Results showed that Cx43 expression in basilar arteries significantly increased at day 7 post-SAH, and pretreatment with PKC inhibitors (Chelerythrine or GF 109203X) reversed this increase. J Transl Med. 2019 Dec 30;17(1):433
BALB/c mice LPS-induced acute lung injury model Gavage 5 or 10 mg/kg 7 consecutive days To evaluate the protective effect of CH on LPS-induced acute lung injury. Results showed that CH significantly ameliorated LPS-induced pathological changes in the lung, reduced inflammatory cell infiltration, and inhibited the production of TNF-α, IL-6, and IL-1β. Front Pharmacol. 2018 Sep 26;9:1047.

Chelerythrine/白屈菜红碱 参考文献

[1]Vieira SM, de Oliveira VH, et al. Chelerythrine inhibits the sarco/endoplasmic reticulum Ca(2+)-ATPase and results in cell Ca(2+) imbalance. Arch Biochem Biophys. 2015 Mar 15;570:58-65.

[2]Ghosh S, Jana J, et al. Plant alkaloid chelerythrine induced aggregation of human telomere sequence--a unique mode of association between a small molecule and a quadruplex. Biochemistry. 2015 Feb 3;54(4):974-86.

Chelerythrine/白屈菜红碱 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.44mL

28.71mL

5.74mL

2.87mL

Chelerythrine/白屈菜红碱 技术信息

CAS号34316-15-9
分子式C21H18NO4
分子量 348.37
SMILES Code C[N+]1=CC2=C(OC)C(OC)=CC=C2C(C=CC3=C4)=C1C3=CC5=C4OCO5
MDL No. MFCD00270393
别名 Toddaline; Broussonpapyrine
运输蓝冰
InChI Key LLEJIEBFSOEYIV-UHFFFAOYSA-N
Pubchem ID 2703
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C

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