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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| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
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| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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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。 | |||||||||||||||||||
| 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. |
| 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. |
| 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. |
| 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 |
|
| 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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