1. Metabolic Enzyme/Protease Anti-infection Apoptosis
  2. Xanthine Oxidase Influenza Virus Ferroptosis
  3. Baicalein

Baicalein  (Synonyms: 黄芩素; 5,6,7-Trihydroxyflavone)

目录号: HY-N0196 纯度: 98.94%
COA 产品使用指南

Baicalein (5,6,7-Trihydroxyflavone) 是黄嘌呤氧化酶抑制剂,其 IC50 值为 3.12 μM。

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Baicalein Chemical Structure

Baicalein Chemical Structure

CAS No. : 491-67-8

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Customer Review

Other Forms of Baicalein:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Baicalein (5,6,7-Trihydroxyflavone) is a xanthine oxidase inhibitor with an IC50 value of 3.12 μM.

IC50 & Target

IC50: 3.12 μM (xanthine oxidase)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
3T3-L1 IC50
29.81 μM
Compound: Baicalein
Cytotoxicity against mouse 3T3L1 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
Cytotoxicity against mouse 3T3L1 cells assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay
[PMID: 28818460]
A549 IC50
13 μM
Compound: 1, Baicalein
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells after 48 hrs by MTT assay
[PMID: 24507925]
BALB/3T3 IC50
342.3 μM
Compound: 3
Growth inhibition of BALB/c mouse cloned 3T3/A31 cells after 72 hrs by nigrosin assay
Growth inhibition of BALB/c mouse cloned 3T3/A31 cells after 72 hrs by nigrosin assay
[PMID: 10096863]
BJ EC50
> 86.2069 μM
Compound: 3
Antiproliferative activity against human BJ cells after 72 hrs by CelTiter-Glo assay
Antiproliferative activity against human BJ cells after 72 hrs by CelTiter-Glo assay
[PMID: 29407975]
C8166 EC50
1.67 μg/mL
Compound: 2
Antiviral activity against HIV-1 3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity by measuring syncytial cell number after 3 days by inverted microscopic analysis
Antiviral activity against HIV-1 3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathogenicity by measuring syncytial cell number after 3 days by inverted microscopic analysis
[PMID: 24794743]
C8166 CC50
30.3 μg/mL
Compound: 2
Cytotoxicity against human C8166 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
Cytotoxicity against human C8166 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
[PMID: 24794743]
DLD-1 IC50
> 20 μM
Compound: 1; Baicalein
Antiproliferative activity against human DLD1 cells after 24 hrs by MTT assay
Antiproliferative activity against human DLD1 cells after 24 hrs by MTT assay
10.1039/C5MD00163C
DLD-1 IC50
> 20 μM
Compound: 1; Baicalein
Antiproliferative activity against human DLD1 cells after 72 hrs by MTT assay
Antiproliferative activity against human DLD1 cells after 72 hrs by MTT assay
10.1039/C5MD00163C
DLD-1 IC50
27.88 μM
Compound: 1; Baicalein
Antiproliferative activity against human DLD1 cells after 48 hrs by MTT assay
Antiproliferative activity against human DLD1 cells after 48 hrs by MTT assay
10.1039/C5MD00163C
HEK293 IC50
4.4 μM
Compound: Baicalein
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in estradiol 3-glucuronidation by LC-MS/MS method
[PMID: 21030469]
HEK293 IC50
7 μM
Compound: Baicalein
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
Inhibition of human recombinant UGT1A1 expressed in HEK293 cells assessed as reduction in bilirubin glucuronidation by LC-MS/MS method
[PMID: 21030469]
HepG2 IC50
28.09 μM
Compound: 1; Baicalein
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
10.1039/C5MD00163C
HepG2 IC50
28.3 μM
Compound: 1, Baicalein
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 24507925]
HepG2 EC50
60 μM
Compound: 3
Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay
Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay
[PMID: 29407975]
HT-29 IC50
> 20 μM
Compound: 1; Baicalein
Antiproliferative activity against human HT-29 cells after 24 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 24 hrs by MTT assay
10.1039/C5MD00163C
HT-29 EC50
10.3 μM
Compound: Baicalein
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
[PMID: 24900447]
HT-29 IC50
18.05 μM
Compound: 1; Baicalein
Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
10.1039/C5MD00163C
HT-29 IC50
18.36 μM
Compound: 1; Baicalein
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
10.1039/C5MD00163C
HT-29 IC50
28.2 μM
Compound: Baicalein
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
[PMID: 24900447]
Huh-7 CC50
> 100 μM
Compound: BE
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
[PMID: 35738350]
Huh-7 CC50
> 100 μM
Compound: Baicalein
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by CCK8 assay relative to control
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability by CCK8 assay relative to control
[PMID: 36804408]
Huh-7 CC50
> 50 μM
Compound: 16
Cytotoxicity against human Huh7.5.1 cells by MTT assay
Cytotoxicity against human Huh7.5.1 cells by MTT assay
[PMID: 22445328]
Huh-7 EC50
33.9 μM
Compound: 16
Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay
Antiviral activity against HCV JFH-1 J399EM infected in Human Huh7.5.1 cells assessed as suppression of viral replication after 72 hrs by EGFP assay
[PMID: 22445328]
HUVEC IC50
3.7 μM
Compound: 1
Inhibition of trypsin-induced elevation in PAI1 production in HUVEC by ELISA
Inhibition of trypsin-induced elevation in PAI1 production in HUVEC by ELISA
[PMID: 9214730]
KB IC50
62.3 μM
Compound: S1
Cytotoxicity against human KB cells after 3 days
Cytotoxicity against human KB cells after 3 days
[PMID: 18722769]
KB IC50
62.3 μM
Compound: 1
Inhibitory activity against KB cell line after 72 h of drug exposure
Inhibitory activity against KB cell line after 72 h of drug exposure
[PMID: 15481991]
KB IC50
87.1 μM
Compound: S1
Cytotoxicity against multi-drug resistant human KB cells overexpressing mdr1 after 3 days
Cytotoxicity against multi-drug resistant human KB cells overexpressing mdr1 after 3 days
[PMID: 18722769]
KB 3-1 IC50
87.1 μM
Compound: 1
Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure
Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure
[PMID: 15481991]
KOPN-8 EC50
16 μM
Compound: 3
Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay
Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay
[PMID: 29407975]
MCF7 GI50
32.8 μM
Compound: 1
Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human MCF7 cells after 48 hrs by sulforhodamine B assay
[PMID: 21496973]
MCF7 IC50
5.3 μg/mL
Compound: Baicalein
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 3 days by beta scintillation counting based [3H]-thymidine incorporation assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 3 days by beta scintillation counting based [3H]-thymidine incorporation assay
[PMID: 33257172]
NCI-H460 GI50
26.7 μM
Compound: 1
Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay
Growth inhibition of human NCI-H460 cells after 48 hrs by sulforhodamine B assay
[PMID: 21496973]
RAW264.7 IC50
13.01 μM
Compound: Baicalein
Antiosteoporotic activity in mouse RAW264.7 cells assessed as inhibition of RANKL-stimulated osteoclastogenesis by TRAP assay
Antiosteoporotic activity in mouse RAW264.7 cells assessed as inhibition of RANKL-stimulated osteoclastogenesis by TRAP assay
[PMID: 19339083]
RBL-2H3 IC50
179 μM
Compound: 2
Antihistaminic activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge
Antihistaminic activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced beta-hexosaminidase release preincubated for 10 mins before DNP-BSA challenge
[PMID: 14510616]
SUP-B15 EC50
103 μM
Compound: 3
Antiproliferative activity against human SUP-B15 cells after 72 hrs by CelTiter-Glo assay
Antiproliferative activity against human SUP-B15 cells after 72 hrs by CelTiter-Glo assay
[PMID: 29407975]
SW480 IC50
11.55 μM
Compound: 1; Baicalein
Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay
Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay
10.1039/C5MD00163C
SW480 IC50
14.05 μM
Compound: 1; Baicalein
Antiproliferative activity against human SW480 cells after 48 hrs by MTT assay
Antiproliferative activity against human SW480 cells after 48 hrs by MTT assay
10.1039/C5MD00163C
SW480 IC50
16.95 μM
Compound: 1; Baicalein
Antiproliferative activity against human SW480 cells after 24 hrs by MTT assay
Antiproliferative activity against human SW480 cells after 24 hrs by MTT assay
10.1039/C5MD00163C
U2OS EC50
22.7 μM
Compound: Baicalein
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
[PMID: 24900447]
Vero IC50
6.46 μg/mL
Compound: baicalein
Antiviral activity against dengue virus 2 infected in african green monkey Vero cells assessed as reduction in viral replication dosed after adsorption with 200 FFU of virus for 1 hour by foci forming unit reduction assay
Antiviral activity against dengue virus 2 infected in african green monkey Vero cells assessed as reduction in viral replication dosed after adsorption with 200 FFU of virus for 1 hour by foci forming unit reduction assay
[PMID: 25564380]
Vero C1008 CC50
> 200 μM
Compound: Baicalein
Cytotoxicity against African green monkey Vero E6 cells incubated for 3 hrs by CCK-8 assay
Cytotoxicity against African green monkey Vero E6 cells incubated for 3 hrs by CCK-8 assay
[PMID: 33186044]
Vero C1008 CC50
> 200 μM
Compound: 211
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction of cell viability by CellTiterGlo assay
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction of cell viability by CellTiterGlo assay
[PMID: 34798775]
ZR-75-1 EC50
25 μM
Compound: 1, Baicalein
Increase in intracellular Ca2+ level in human ZR-75-1 cells treated for 25 secs by fura-2-AM dye-based spectrofluorophotometric analysis in presence of Ca2+ containing medium
Increase in intracellular Ca2+ level in human ZR-75-1 cells treated for 25 secs by fura-2-AM dye-based spectrofluorophotometric analysis in presence of Ca2+ containing medium
[PMID: 26154615]
ZR-75-1 EC50
35 μM
Compound: 1, Baicalein
Increase in intracellular Ca2+ level in human ZR-75-1 cells treated for 25 secs by fura-2-AM dye-based spectrofluorophotometric analysis in presence of Ca2+-free medium
Increase in intracellular Ca2+ level in human ZR-75-1 cells treated for 25 secs by fura-2-AM dye-based spectrofluorophotometric analysis in presence of Ca2+-free medium
[PMID: 26154615]
体外研究
(In Vitro)

Baicalein 体外抑制有丝分裂原诱导的 T 细胞增殖和细胞因子分泌。在 25 μM 时,用 Baicalein 预处理可显著抑制 Con A 或抗 CD3/CD28 mAb 诱导的增殖和细胞因子分泌。Baicalein 处理可诱导 NF-κB 与 DNA 结合,但会抑制核区室中的硫氧还蛋白活性[2]
Baicalein 以时间和剂量依赖性方式抑制 MDA-MB-231 细胞的增殖、迁移和侵袭。Baicalein 显著降低 MDA-MB-231 细胞中 SATB1 的表达。Baicalein 还下调 Wnt1 和 β-catenin 蛋白的表达以及 Wnt/β-catenin 靶向基因的转录水平[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Baicalein 抑制移植物抗宿主病的诱导,但不抑制小鼠 T 细胞的稳态增殖。这一观察清楚地表明 Baicalein 在体内具有强大的抗炎活性[2]
用 Baicalein 处理的大鼠可防止心脏体重比、脑利钠肽血浆水平、室间隔厚度、左心室心肌胶原体积增加 (分别为 P < 0.05)。Baicalein 的抗纤维化作用进一步表现为左心室前胶原 I 和 III 的表达受到抑制,伴随着 12-脂氧合酶的表达降低,以及基质金属肽酶 9 和细胞外信号调节激酶的表达和活性降低。Baicalein 可抑制高血压大鼠心肌纤维化[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

270.24

Formula

C15H10O5

CAS 号
性状

固体

颜色

Light yellow to brown

中文名称

黄芩素

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (185.02 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.7004 mL 18.5021 mL 37.0041 mL
5 mM 0.7401 mL 3.7004 mL 7.4008 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (9.25 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (9.25 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂: 0.5% CMC-Na/saline water

    Solubility: 20 mg/mL (74.01 mM); 悬浊液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 98.94%

参考文献
Cell Assay
[3]

MTT assay is conducted to evaluate the effect of baicalein on proliferation of breast cancer cells. MDA-MB-231 cells are routinely digested, collected, and then seeded in 96-well plates at a density of 8×103 cells/well. After incubation for 12-24 hours, cells are treated with 0, 20, 40, 60, 80, 100, and 120 μM baicalein according to their experimental grouping and then incubated at 37°C for 24, 48, and 72 hours[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2][4]

Rats: Baicalein is suspended in 1% methylcellulose. Rats are treated with baicalein suspension via oral garvage. SHR and WKY rats are divided into 4 groups (n=8 per group): 12-week treatment with high-dose (200 mg/kg/day) or low-dose (50 mg/kg/day) group; and 4-week treatment with high-dose or low-dose group. The 12-week and 4-week negative control groups of SHR and WKY rats (n=8 per group) receive vehicle while positive control groups (Val group, n=8 per group) receive valsartan (20 mg/kg/day) for comparison[4].

Mice: To study the in vivo anti-inflammatory efficacy of baicalein, graft-versus-host disease (GVHD) model is used. Splenic lymphocytes from C57BL/6 mice are incubated with baicalein in vitro (25 μM, 4h) and adoptively transferred to immune-compromised Balb/c mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 1 year; -20°C, 6 months (protect from light)。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7004 mL 18.5021 mL 37.0041 mL 92.5104 mL
5 mM 0.7401 mL 3.7004 mL 7.4008 mL 18.5021 mL
10 mM 0.3700 mL 1.8502 mL 3.7004 mL 9.2510 mL
15 mM 0.2467 mL 1.2335 mL 2.4669 mL 6.1674 mL
20 mM 0.1850 mL 0.9251 mL 1.8502 mL 4.6255 mL
25 mM 0.1480 mL 0.7401 mL 1.4802 mL 3.7004 mL
30 mM 0.1233 mL 0.6167 mL 1.2335 mL 3.0837 mL
40 mM 0.0925 mL 0.4626 mL 0.9251 mL 2.3128 mL
50 mM 0.0740 mL 0.3700 mL 0.7401 mL 1.8502 mL
60 mM 0.0617 mL 0.3084 mL 0.6167 mL 1.5418 mL
80 mM 0.0463 mL 0.2313 mL 0.4626 mL 1.1564 mL
100 mM 0.0370 mL 0.1850 mL 0.3700 mL 0.9251 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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