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MedKoo Cat#: 561385 | Name: Baicalein
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Baicalein is a positive allosteric modulator of the benzodiazepine site and/or a non-benzodiazepine site of the GABAA receptor. It displays subtype selectivity for α2 and α3 subunit-containing GABAA receptors. Baicalein is also an antagonist of the estrogen receptor.

Chemical Structure

Baicalein
Baicalein
CAS#491-67-8

Theoretical Analysis

MedKoo Cat#: 561385

Name: Baicalein

CAS#: 491-67-8

Chemical Formula: C15H10O5

Exact Mass: 270.0528

Molecular Weight: 270.24

Elemental Analysis: C, 66.67; H, 3.73; O, 29.60

Price and Availability

Size Price Availability Quantity
1g USD 250.00 2 Weeks
5g USD 550.00 2 Weeks
10g USD 750.00 2 Weeks
25g USD 1,250.00 2 Weeks
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Related CAS #
352000-07-8 (hydrate) 491-67-8
Synonym
Baicalein; BaiKalein; Noroxylin;
IUPAC/Chemical Name
5,6,7-Trihydroxy-2-phenylchromen-4-one
InChi Key
FXNFHKRTJBSTCS-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H10O5/c16-9-6-11(8-4-2-1-3-5-8)20-12-7-10(17)14(18)15(19)13(9)12/h1-7,17-19H
SMILES Code
O=C1C=C(C2=CC=CC=C2)OC3=C1C(O)=C(O)C(O)=C3
Appearance
Solid powder
Purity
>95% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Baicalein is a xanthine oxidase inhibitor with an IC50 of 3.12 μM.
In vitro activity:
To measure the effect of baicalein on the proliferation of MCF-7 and MDA-MB-231 cells that were exposed to 0, 10, 20, and 40 µM of baicalein for 24, 48, and 72 hours, MTT assay was implemented. The results showed that baicalein significantly inhibited the proliferation of MCF-7 and MDA-MB-231 cells in a dose- and time-dependent manner (P<0.05, P<0.01, Figure 1B). Baicalein also suppressed the colony formation of MCF-7 and MDA-MB-231 cells as shown by the plate colony formation assay. As shown in Figure 1C, the numbers of colonies that formed for preparations treated with baicalein at 10, 20, and 40 µM were 118±2.6, 63±6.2, 25±3.7 and 85±1.6, 51±6.7, 19±3.6 in MCF-7 and MDA-MB-231 cells respectively (P<0.05). These results suggest that baicalein has anti-proliferative effects on breast cancer cells. Reference: Drug Des Devel Ther. 2018 Nov 16;12:3961-3972. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6248272/
In vivo activity:
The anticancer potential of baicalein was evaluated using breast xenografts models (BALB/c-nude) as the testing model. After therapeutic treatment with baicalein, tumor tissues from breast xenograft models were collected and analyzed. The results demonstrated that the growth, volume, and weight of tumors were significantly suppressed in the baicalein-treated group compared with the control group (Figure 5A–C, P<0.05). Additionally, the anti-tumor efficacy of baicalein in vivo was assessed by immunohistochemistry staining methods. As presented in Figure 5D, baicalein remarkably reduced the expression of p-AKT, while increasing the expression of Bax and LC3 at the protein level. These results illustrated that baicalein can significantly induce apoptosis and autophagy through negative modulation of the PI3K/AKT pathway in vivo. Reference: Drug Des Devel Ther. 2018 Nov 16;12:3961-3972. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6248272/
Solvent mg/mL mM
Solubility
DMF 52.0 192.42
DMSO 48.9 180.88
Ethanol 1.2 4.26
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 270.24 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Yan W, Ma X, Zhao X, Zhang S. Baicalein induces apoptosis and autophagy of breast cancer cells via inhibiting PI3K/AKT pathway in vivo and vitro. Drug Des Devel Ther. 2018 Nov 16;12:3961-3972. doi: 10.2147/DDDT.S181939. PMID: 30510404; PMCID: PMC6248272. 2. Guo J, You H, Li D. Baicalein Exerts Anticancer Effect in Nasopharyngeal Carcinoma In Vitro and In Vivo. Oncol Res. 2019 May 7;27(5):601-611. doi: 10.3727/096504018X15399945637736. PMID: 31053182; PMCID: PMC7848276.
In vitro protocol:
1. Yan W, Ma X, Zhao X, Zhang S. Baicalein induces apoptosis and autophagy of breast cancer cells via inhibiting PI3K/AKT pathway in vivo and vitro. Drug Des Devel Ther. 2018 Nov 16;12:3961-3972. doi: 10.2147/DDDT.S181939. PMID: 30510404; PMCID: PMC6248272. 2. Guo J, You H, Li D. Baicalein Exerts Anticancer Effect in Nasopharyngeal Carcinoma In Vitro and In Vivo. Oncol Res. 2019 May 7;27(5):601-611. doi: 10.3727/096504018X15399945637736. PMID: 31053182; PMCID: PMC7848276.
In vivo protocol:
1. Yan W, Ma X, Zhao X, Zhang S. Baicalein induces apoptosis and autophagy of breast cancer cells via inhibiting PI3K/AKT pathway in vivo and vitro. Drug Des Devel Ther. 2018 Nov 16;12:3961-3972. doi: 10.2147/DDDT.S181939. PMID: 30510404; PMCID: PMC6248272. 2. Guo J, You H, Li D. Baicalein Exerts Anticancer Effect in Nasopharyngeal Carcinoma In Vitro and In Vivo. Oncol Res. 2019 May 7;27(5):601-611. doi: 10.3727/096504018X15399945637736. PMID: 31053182; PMCID: PMC7848276.
1: Bie B, Sun J, Guo Y, Li J, Jiang W, Yang J, Huang C, Li Z. Baicalein: A review of its anti-cancer effects and mechanisms in Hepatocellular Carcinoma. Biomed Pharmacother. 2017 Sep;93:1285-1291. doi: 10.1016/j.biopha.2017.07.068. Review. PubMed PMID: 28747003. 2: Gong D, Hong Y, Sun G, Zhang J. Novel strategy for quality consistency evaluation of Chinese medicine "YIQING" tablet that combines the simultaneous quantification and screening of ten bioactive constituents. J Sep Sci. 2017 Aug;40(15):3064-3073. doi: 10.1002/jssc.201700291. Epub 2017 Jun 28. Review. PubMed PMID: 28590083. 3: Davatgaran-Taghipour Y, Masoomzadeh S, Farzaei MH, Bahramsoltani R, Karimi-Soureh Z, Rahimi R, Abdollahi M. Polyphenol nanoformulations for cancer therapy: experimental evidence and clinical perspective. Int J Nanomedicine. 2017 Apr 4;12:2689-2702. doi: 10.2147/IJN.S131973. eCollection 2017. Review. PubMed PMID: 28435252; PubMed Central PMCID: PMC5388197. 4: Dinda B, Dinda S, DasSharma S, Banik R, Chakraborty A, Dinda M. Therapeutic potentials of baicalin and its aglycone, baicalein against inflammatory disorders. Eur J Med Chem. 2017 May 5;131:68-80. doi: 10.1016/j.ejmech.2017.03.004. Epub 2017 Mar 6. Review. PubMed PMID: 28288320. 5: Li LC, Kan LD. Traditional Chinese medicine for pulmonary fibrosis therapy: Progress and future prospects. J Ethnopharmacol. 2017 Feb 23;198:45-63. doi: 10.1016/j.jep.2016.12.042. Epub 2016 Dec 28. Review. PubMed PMID: 28038955. 6: Wu J, Hu Y, Xiang L, Li S, Yuan Y, Chen X, Zhang Y, Huang W, Meng X, Wang P. San-Huang-Xie-Xin-Tang Constituents Exert Drug-Drug Interaction of Mutual Reinforcement at Both Pharmacodynamics and Pharmacokinetic Level: A Review. Front Pharmacol. 2016 Nov 28;7:448. eCollection 2016. Review. PubMed PMID: 27965575; PubMed Central PMCID: PMC5124576. 7: Gong WY, Zhao ZX, Liu BJ, Lu LW, Dong JC. Exploring the chemopreventive properties and perspectives of baicalin and its aglycone baicalein in solid tumors. Eur J Med Chem. 2017 Jan 27;126:844-852. doi: 10.1016/j.ejmech.2016.11.058. Epub 2016 Dec 1. Review. PubMed PMID: 27960146. 8: Park S. Cyclic Glucans Enhance Solubility of Bioavailable Flavonoids. Molecules. 2016 Nov 16;21(11). pii: E1556. Review. PubMed PMID: 27854350. 9: Liu H, Dong Y, Gao Y, Du Z, Wang Y, Cheng P, Chen A, Huang H. The Fascinating Effects of Baicalein on Cancer: A Review. Int J Mol Sci. 2016 Oct 9;17(10). pii: E1681. Review. PubMed PMID: 27735841; PubMed Central PMCID: PMC5085714. 10: Noh K, Kang Y, Nepal MR, Jeong KS, Oh DG, Kang MJ, Lee S, Kang W, Jeong HG, Jeong TC. Role of Intestinal Microbiota in Baicalin-Induced Drug Interaction and Its Pharmacokinetics. Molecules. 2016 Mar 10;21(3):337. doi: 10.3390/molecules21030337. Review. PubMed PMID: 26978333. 11: Liu-Smith F, Meyskens FL. Molecular mechanisms of flavonoids in melanin synthesis and the potential for the prevention and treatment of melanoma. Mol Nutr Food Res. 2016 Jun;60(6):1264-74. doi: 10.1002/mnfr.201500822. Epub 2016 Mar 21. Review. PubMed PMID: 26865001; PubMed Central PMCID: PMC4900912. 12: Yarla NS, Bishayee A, Sethi G, Reddanna P, Kalle AM, Dhananjaya BL, Dowluru KS, Chintala R, Duddukuri GR. Targeting arachidonic acid pathway by natural products for cancer prevention and therapy. Semin Cancer Biol. 2016 Oct;40-41:48-81. doi: 10.1016/j.semcancer.2016.02.001. Epub 2016 Feb 4. Review. PubMed PMID: 26853158. 13: Moosavi F, Hosseini R, Saso L, Firuzi O. Modulation of neurotrophic signaling pathways by polyphenols. Drug Des Devel Ther. 2015 Dec 21;10:23-42. doi: 10.2147/DDDT.S96936. eCollection 2016. Review. PubMed PMID: 26730179; PubMed Central PMCID: PMC4694682. 14: de Oliveira MR, Nabavi SF, Habtemariam S, Erdogan Orhan I, Daglia M, Nabavi SM. The effects of baicalein and baicalin on mitochondrial function and dynamics: A review. Pharmacol Res. 2015 Oct;100:296-308. doi: 10.1016/j.phrs.2015.08.021. Epub 2015 Aug 28. Review. PubMed PMID: 26318266. 15: Zhang H, Zhai J, Zhang L, Li C, Zhao Y, Chen Y, Li Q, Hu XP. In Vitro Inhibition of Glyoxalase І by Flavonoids: New Insights from Crystallographic Analysis. Curr Top Med Chem. 2016;16(4):460-6. Review. PubMed PMID: 26268338. 16: Fajardo AM, Piazza GA. Chemoprevention in gastrointestinal physiology and disease. Anti-inflammatory approaches for colorectal cancer chemoprevention. Am J Physiol Gastrointest Liver Physiol. 2015 Jul 15;309(2):G59-70. doi: 10.1152/ajpgi.00101.2014. Epub 2015 May 28. Review. PubMed PMID: 26021807; PubMed Central PMCID: PMC4504955. 17: Dinda B, SilSarma I, Dinda M, Rudrapaul P. Oroxylum indicum (L.) Kurz, an important Asian traditional medicine: from traditional uses to scientific data for its commercial exploitation. J Ethnopharmacol. 2015 Feb 23;161:255-78. doi: 10.1016/j.jep.2014.12.027. Epub 2014 Dec 25. Review. PubMed PMID: 25543018. 18: Kim DH, Sung B, Chung HY, Kim ND. Modulation of Colitis-associated Colon Tumorigenesis by Baicalein and Betaine. J Cancer Prev. 2014 Sep;19(3):153-60. doi: 10.15430/JCP.2014.19.3.153. Review. PubMed PMID: 25337584; PubMed Central PMCID: PMC4189507. 19: Xiao JR, Do CW, To CH. Potential therapeutic effects of baicalein, baicalin, and wogonin in ocular disorders. J Ocul Pharmacol Ther. 2014 Oct;30(8):605-14. doi: 10.1089/jop.2014.0074. Review. PubMed PMID: 25280175. 20: Chen H, Gao Y, Wu J, Chen Y, Chen B, Hu J, Zhou J. Exploring therapeutic potentials of baicalin and its aglycone baicalein for hematological malignancies. Cancer Lett. 2014 Nov 1;354(1):5-11. doi: 10.1016/j.canlet.2014.08.003. Epub 2014 Aug 13. Review. PubMed PMID: 25128647; PubMed Central PMCID: PMC4179973.

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N-(Hydroxy-PEG3)-N-Boc-PEG4-Boc

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