Baicalein (Synonyms: 5,6,7-Trihydroxyflavone)

Name: Baicalein
Brand: MedChemExpress
SKU: HY-N0196
Rating: 5.0 (37 reviews)

Cat. No.: HY-N0196 Purity: 98.51%: Data Sheet
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Baicalein (5,6,7-Trihydroxyflavone) is a xanthine oxidase inhibitor with an IC₅₀ value of 3.12 μM.

For research use only. We do not sell to patients.

CAS No. : 491-67-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 37 publication(s) in Google Scholar

Other Forms of Baicalein:

Baicalein (Standard) In-stock
Baicalein hydrate Get quote

37 Publications Citing Use of MCE Baicalein

Bio/Physico-chemical Assay

Cell Proliferation/Viability Assay

Flow Cytometry

In Vivo Efficacy Study

Histological Imaging/Staining

: Baicalein purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Feb:188:106666. [Abstract]; Intracellular drug release of 80 μg/mL cPBA-BE in HepaRG cells injured by 3 mg/mL APAP (8 h) was observed.

: Baicalein purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Feb:188:106666. [Abstract]; Representative flow cytometry curves and quantitative data illustrating time-dependent internalization of 10 mg/mL Cy5-labeled cPBA-BE in HepaRG cells until 24 h.

: Baicalein purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Feb:188:106666. [Abstract]; After mice were injured by 200 mg/kg APAP for 6 h, a single intravenous injection of 100 μL 20 mg/mL cPBA-BE in PBS or 5.1 mg/mL BE in 5% DMSO (equal to 20 mg/mL cPBA-BE) was administered. The expression levels of representative factors of inflammation and oxidative stress in the liver were measured. After 18 h of treatment, homogenates of the hepatic tissues were prepared, and the concentrations of GSH, H2O2, MDA, and MPO were separately measured.

: Baicalein purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Feb:188:106666. [Abstract]; After mice were injured by 200 mg/kg APAP for 6 h, a single intravenous injection of 100 μL 20 mg/mL cPBA-BE in PBS or 5.1 mg/mL BE in 5% DMSO (equal to 20 mg/mL cPBA-BE) was performed. Masson trichrome (MT) staining of liver sections.

: Baicalein purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Jul 13;11(17):8301-8321. [Abstract]; Fluorescence quenching of cPBA after an interaction with various concentrations (0, 3, 6, 12, 24 μg/mL) of BE was observed.

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Description

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]

Cellular Effect

Cell Line	Type	Value	Description	References
3T3-L1	IC₅₀	29.81 3 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]
3T3-L1	IC₅₀	29.81 3 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 3 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]
A549	IC₅₀	13 3 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 3 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]
BALB/3T3	IC₅₀	342.3 3 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 3 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]
BJ	EC₅₀	> 86.2069 3 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	CC₅₀	30.3 6 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]
3T3-L1	IC₅₀	29.81 3 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]
C8166	EC₅₀	1.67 6 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	EC₅₀	1.67 6 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]
A549	IC₅₀	13 3 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]
C8166	CC₅₀	30.3 6 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 3 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
Caco-2	IC₅₀	3.5 × 10^-5 41 Compound: 2	Inhibition of human intestinal sucrase in human Caco-2 cell membrane Inhibition of human intestinal sucrase in human Caco-2 cell membrane	[PMID: 9834167]
BALB/3T3	IC₅₀	342.3 3 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]
DLD-1	IC₅₀	> 20 3 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
Caco-2	IC₅₀	2.6 × 10^-4 41 Compound: 2	Inhibition of rat intestinal sucrase expressed in human Caco-2 cells Inhibition of rat intestinal sucrase expressed in human Caco-2 cells	[PMID: 9834167]
BJ	EC₅₀	> 86.2069 3 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]
DLD-1	IC₅₀	27.88 3 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
Calu-3	CC₅₀	91 3 Compound: 1	Cytotoxicity against human Calu-3 cells assessed as inhibition of cell growth incubated for 4 days by MTS assay Cytotoxicity against human Calu-3 cells assessed as inhibition of cell growth incubated for 4 days by MTS assay	[PMID: 36965227]
C8166	CC₅₀	30.3 6 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]
CHO	IC₅₀	>350 3 Compound: 1	Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells	[PMID: 12713409]
HEK293	IC₅₀	4.4 3 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]
C8166	EC₅₀	1.67 6 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]
HEK293	IC₅₀	7 3 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]
DLD-1	IC₅₀	>20 3 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	27.88 3 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
CHO	IC₅₀	> 350 3 Compound: 1	Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells Displacement of [3H]LSD from human 5HT7 receptor expressed in CHO cells	[PMID: 12713409]
HepG2	IC₅₀	28.09 3 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
HEK293	IC₅₀	7 3 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	28.3 3 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 3 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]
HEK293	IC₅₀	4.4 3 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]
HT-29	IC₅₀	> 20 3 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
Caco-2	IC₅₀	2.6 x 10^-4 41 Compound: 2	Inhibition of rat intestinal sucrase expressed in human Caco-2 cells Inhibition of rat intestinal sucrase expressed in human Caco-2 cells	[PMID: 9834167]
HepG2	EC₅₀	60 3 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]
Caco-2	IC₅₀	3.5 x 10^-5 41 Compound: 2	Inhibition of human intestinal sucrase in human Caco-2 cell membrane Inhibition of human intestinal sucrase in human Caco-2 cell membrane	[PMID: 9834167]
HepG2	IC₅₀	28.09 3 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
HT-29	EC₅₀	10.3 3 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]
HepG2	IC₅₀	28.3 3 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]
HT-29	IC₅₀	18.05 3 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
Calu-3	CC₅₀	9.1 3 Compound: Baicalein	Cytotoxicity against human Calu-3 cells incubated for 4 days by MTS assay Cytotoxicity against human Calu-3 cells incubated for 4 days by MTS assay	[PMID: 37437351]
HT-29	EC₅₀	10.3 3 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	18.36 3 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	>20 3 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
Calu-3	CC₅₀	91 3 Compound: 1	Cytotoxicity against human Calu-3 cells assessed as inhibition of cell growth incubated for 4 days by MTS assay Cytotoxicity against human Calu-3 cells assessed as inhibition of cell growth incubated for 4 days by MTS assay	[PMID: 36965227]
HT-29	IC₅₀	28.2 3 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]
HT-29	IC₅₀	18.05 3 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
DLD-1	IC₅₀	27.88 3 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
Huh-7	CC₅₀	> 100 3 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]
HT-29	IC₅₀	18.36 3 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
DLD-1	IC₅₀	> 20 3 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
Huh-7	CC₅₀	> 100 3 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]
HT-29	IC₅₀	28.2 3 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]
DLD-1	IC₅₀	> 20 3 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
Huh-7	CC₅₀	> 50 3 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 3 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]
Huh-7	CC₅₀	>100 3 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	>100 3 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]
HUVEC	IC₅₀	3.7 3 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]
Huh-7	CC₅₀	>50 3 Compound: 16	Cytotoxicity against human Huh7.5.1 cells by MTT assay Cytotoxicity against human Huh7.5.1 cells by MTT assay	[PMID: 22445328]
KB	IC₅₀	62.3 3 Compound: S1	Cytotoxicity against human KB cells after 3 days Cytotoxicity against human KB cells after 3 days	[PMID: 18722769]
Huh-7	EC₅₀	33.9 3 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]
KB	IC₅₀	62.3 3 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]
HUVEC	IC₅₀	3.7 3 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	87.1 3 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	IC₅₀	62.3 3 Compound: S1	Cytotoxicity against human KB cells after 3 days Cytotoxicity against human KB cells after 3 days	[PMID: 18722769]
HEK-293T	CC₅₀	<= 200 3 Compound: Baicalein	Cytotoxicity against HEK293T cells expressing human ACE2 assessed as reduction in cell viability incubated for 4 hrs by MTT assay Cytotoxicity against HEK293T cells expressing human ACE2 assessed as reduction in cell viability incubated for 4 hrs by MTT assay	[PMID: 37437351]
KB 3-1	IC₅₀	87.1 3 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 3 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]
KB	IC₅₀	87.1 3 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]
HEK293	IC₅₀	4.4 3 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]
MCF7	GI₅₀	32.8 3 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]
HEK293	IC₅₀	7 3 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]
KB	IC₅₀	62.3 3 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]
MCF7	IC₅₀	5.3 6 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]
KB 3-1	EC₅₀	41 3 Compound: 1	Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h	[PMID: 15481991]
NCI-H460	GI₅₀	26.7 3 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]
HT-29	EC₅₀	10.3 3 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]
KB 3-1	IC₅₀	87.1 3 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]
RAW264.7	IC₅₀	13.01 3 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]
KOPN-8	EC₅₀	16 3 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]
RBL-2H3	IC₅₀	179 3 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]
HT-29	IC₅₀	18.05 3 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
MCF7	GI₅₀	32.8 3 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]
HT-29	IC₅₀	18.36 3 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
SUP-B15	EC₅₀	103 3 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]
MCF7	IC₅₀	5.3 6 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]
HT-29	IC₅₀	28.2 3 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]
NCI-H460	GI₅₀	26.7 3 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]
SW480	IC₅₀	11.55 3 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
HT-29	IC₅₀	> 20 3 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
RAW264.7	IC₅₀	30.4 3 Compound: 7	Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as reduction in NO production Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as reduction in NO production	[PMID: 37778427]
SW480	IC₅₀	14.05 3 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
RAW264.7	IC₅₀	13.01 3 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]
HUVEC	IC₅₀	3.7 3 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]
SW480	IC₅₀	16.95 3 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
RAW264.7	IC₅₀	>100 3 Compound: 2	Cytotoxicity against mouse RAW264.7 cells Cytotoxicity against mouse RAW264.7 cells	[PMID: 22101131]
U2OS	EC₅₀	22.7 3 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]
RBL-2H3	IC₅₀	179 3 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]
Vero	IC₅₀	6.46 6 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]
SUP-B15	EC₅₀	103 3 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]
Vero C1008	CC₅₀	> 200 3 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]
SW480	IC₅₀	16.95 3 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
Vero C1008	CC₅₀	> 200 3 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 3 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]
SW480	IC₅₀	14.05 3 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
HepG2	EC₅₀	60 3 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]
ZR-75-1	EC₅₀	35 3 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]
HepG2	IC₅₀	28.09 3 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
SW480	IC₅₀	11.55 3 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
HepG2	IC₅₀	28.3 3 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]
U2OS	EC₅₀	22.7 3 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]
Huh-7	CC₅₀	> 100 3 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]
Vero	IC₅₀	6.46 6 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]
Huh-7	CC₅₀	> 100 3 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]
Vero C1008	CC₅₀	8.6 3 Compound: 1	Cytotoxicity against african green monkey Vero E6 cells assessed as inhibition of cell growth incubated for 4 days by MTS assay Cytotoxicity against african green monkey Vero E6 cells assessed as inhibition of cell growth incubated for 4 days by MTS assay	[PMID: 36965227]
Vero C1008	CC₅₀	>200 3 Compound: 1	Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability by CCK8 assay Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability by CCK8 assay	[PMID: 37257024]
Huh-7	CC₅₀	> 50 3 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 3 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]
Vero C1008	CC₅₀	>200 3 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]
Vero C1008	CC₅₀	>50 3 Compound: 14	Cytotoxicity against african green monkey Vero E6 cells by CCK-8 assay Cytotoxicity against african green monkey Vero E6 cells by CCK-8 assay	[PMID: 37257212]
KB	IC₅₀	62.3 3 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]
Vero C1008	CC₅₀	>200 3 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]
KB	IC₅₀	62.3 3 Compound: S1	Cytotoxicity against human KB cells after 3 days Cytotoxicity against human KB cells after 3 days	[PMID: 18722769]
ZR-75-1	EC₅₀	25 3 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]
KB	IC₅₀	87.1 3 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]
ZR-75-1	EC₅₀	35 3 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]
KB 3-1	EC₅₀	41 3 Compound: 1	Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h	[PMID: 15481991]
KB 3-1	IC₅₀	87.1 3 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 3 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 3 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 6 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 3 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 3 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]
RAW264.7	IC₅₀	30.4 3 Compound: 7	Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as reduction in NO production Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as reduction in NO production	[PMID: 37778427]
RAW264.7	IC₅₀	> 100 3 Compound: 2	Cytotoxicity against mouse RAW264.7 cells Cytotoxicity against mouse RAW264.7 cells	[PMID: 22101131]
RBL-2H3	IC₅₀	179 3 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 3 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 3 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 3 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 3 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 3 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	CC₅₀	8.6 3 Compound: Baicalein	Cytotoxicity against African green monkey Vero cells incubated for 4 days by MTS assay Cytotoxicity against African green monkey Vero cells incubated for 4 days by MTS assay	[PMID: 37437351]
Vero	CC₅₀	> 200 3 Compound: Baicalein	Cytotoxicity against African green monkey Vero cells Cytotoxicity against African green monkey Vero cells	[PMID: 37437351]
Vero	CC₅₀	> 500 3 Compound: Baicalein	Cytotoxicity against African green monkey Vero cells by CCK8 assay Cytotoxicity against African green monkey Vero cells by CCK8 assay	[PMID: 37437351]
Vero	IC₅₀	6.46 6 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	8.6 3 Compound: 1	Cytotoxicity against african green monkey Vero E6 cells assessed as inhibition of cell growth incubated for 4 days by MTS assay Cytotoxicity against african green monkey Vero E6 cells assessed as inhibition of cell growth incubated for 4 days by MTS assay	[PMID: 36965227]
Vero C1008	CC₅₀	> 200 3 Compound: 1	Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability by CCK8 assay Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability by CCK8 assay	[PMID: 37257024]
Vero C1008	CC₅₀	> 200 3 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]
Vero C1008	CC₅₀	> 200 3 Compound: 86	Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell growth incubated for 24 hrs by WST-8 assay Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell growth incubated for 24 hrs by WST-8 assay	[PMID: 37597436]
Vero C1008	CC₅₀	> 200 3 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	> 50 3 Compound: 14	Cytotoxicity against african green monkey Vero E6 cells by CCK-8 assay Cytotoxicity against african green monkey Vero E6 cells by CCK-8 assay	[PMID: 37257212]
ZR-75-1	EC₅₀	25 3 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 3 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]

In Vitro

Baicalein suppresses mitogen induced T cell proliferation and cytokine secretion in vitro. Pre-treatment with baicalein significantly suppresses Con A or anti-CD3/CD28 mAb induced proliferation as well as cytokine secretion at 25 μM. Baicalein treatment induces DNA binding of NF-κB but inhibits thioredoxin activity in the nuclear compartment^[2]. Baicalein suppresses proliferation, migration, and invasion of MDA-MB-231 cells in a time- and dose-dependent manner. Baicalein significantly decreases the expression of SATB1 in MDA-MB-231 cells. Baicalein also downregulates the expression of Wnt1 and β-catenin proteins and transcription level of Wnt/β-catenin-targeted genes^[3].

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

In Vivo

Baicalein suppresses induction of graft versus host disease but does not inhibit homeostatic proliferation of T-cells in mice. This observation clearly shows potent anti-inflammatory activity of baicalein in vivo^[2]. Rats treated with baicalein are protected against an increase in heart to body weight ratio, plasma level of brain natriuretic peptides, intraventricular septum thickness, myocardial collagen volume of left ventricle (all P<0.05, respectively). The antifibrotic effects of baicalein are further illustrated by the suppressed expression of left ventricle pro-collagens I and III accompanied by the decreased expression of 12-lipoxygenase, and by reduced expression and activity of matrix metallopeptidase 9 and extracellular signal-regulated kinases. Baicalein can inhibit cardiac fibrosis in hypertensive rats^[4].

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

Molecular Weight

270.24

Formula

C₁₅H₁₀O₅

CAS No.

491-67-8

Appearance

Solid

Color

Light yellow to brown

SMILES

O=C1C=C(C2=CC=CC=C2)OC3=CC(O)=C(O)C(O)=C13

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (185.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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
10 mM	0.3700 mL	1.8502 mL	3.7004 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (9.25 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (9.25 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (74.01 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.72%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (250 KB) HNMR (251 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Shieh DE,et al. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res. 2000 Sep-Oct;20(5A):2861-5. [Content Brief]

[2]. Patwardhan RS, et al. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation. Biochem Pharmacol. 2016 May 15;108:75-89. [Content Brief]

[3]. Ma X, et al. Baicalein suppresses metastasis of breast cancer cells by inhibiting EMT via downregulation of SATB1 and Wnt/β-catenin pathway. Drug Des Devel Ther. 2016 Apr 18;10:1419-41. [Content Brief]

[4]. Kong EK, et al. A novel anti-fibrotic agent, baicalein, for the treatment of myocardial fibrosis in spontaneously hypertensiverats. Eur J Pharmacol. 2011 May 11;658(2-3):175-81. [Content Brief]

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.
References	[1]. Shieh DE,et al. Antioxidant and free radical scavenging effects of baicalein, baicalin and wogonin. Anticancer Res. 2000 Sep-Oct;20(5A):2861-5. [Content Brief] [2]. Patwardhan RS, et al. Baicalein exhibits anti-inflammatory effects via inhibition of NF-κB transactivation. Biochem Pharmacol. 2016 May 15;108:75-89. [Content Brief] [3]. Ma X, et al. Baicalein suppresses metastasis of breast cancer cells by inhibiting EMT via downregulation of SATB1 and Wnt/β-catenin pathway. Drug Des Devel Ther. 2016 Apr 18;10:1419-41. [Content Brief] [4]. Kong EK, et al. A novel anti-fibrotic agent, baicalein, for the treatment of myocardial fibrosis in spontaneously hypertensiverats. Eur J Pharmacol. 2011 May 11;658(2-3):175-81. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	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

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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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Baicalein491-67-85,6,7-TrihydroxyflavoneXanthine OxidaseInfluenza VirusFerroptosisXOInhibitorinhibitorinhibit

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Baicalein (Synonyms: 5,6,7-Trihydroxyflavone)

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