Hematein

Names

[ CAS No. ]:
475-25-2

[ Name ]:
Hematein

[Synonym ]:
hydroxybrazilein
Haematein
EINECS 207-492-8

Biological Activity

[Description]:

Hematein is a oxidation product of hematoxylin acted as a dye[1]. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells[2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Stem Cell/Wnt >> Wnt

Signaling Pathways >> PI3K/Akt/mTOR >> Akt

[Target]

CKII:0.74 μM (IC50)

Akt

Wnt

[In Vitro]

Hematein (10-100 μM; 14 days) inhibits cells growth in A427 lung cancer cells[1]. Hematein (50 and 100 μM; 48 hours) induces apoptosis in A427 lung cancer cells[1]. Hematein (50 and 100 μM; 48 hours) inhibits CK2-specific Akt phosphorylation[1]. Cell Viability Assay[1] Cell Line: A427 (HTB-53) cell line Concentration: 10-100 μM Incubation Time: 14 days Result: Inhibited cells growth. Apoptosis Analysis[1] Cell Line: A427 (HTB-53) cell line Concentration: 50 and 100 μM Incubation Time: 48 hours Result: Induced apoptosis in A427 lung cancer cells. Western Blot Analysis[1] Cell Line: A427 (HTB-53) cell line Concentration: 50 and 100 μM Incubation Time: 48 hours Result: Inhibited CK2-specific Akt phosphorylation.

[In Vivo]

Hematein (intraperitoneal injections; 50 mg/kg; twice a week for 6 weeks) inhibits tumor growth in A427 lung cancer cell xenografts[1]. Animal Model: Female athymic BALB/c nude mice (6-week-old) [1] Dosage: 50 mg/kg Administration: Intraperitoneal injections; twice a week for 6 weeks Result: Inhibited tumor growth in A427 lung cancer cell xenografts.

[References]

[1]. Shirai, K., & Matsuoka, M. (1996). Structure and properties of hematein derivatives. Dyes and Pigments, 32(3), 159–169.

[2]. Hung MS, et al. Hematein, a casein kinase II inhibitor, inhibits lung cancer tumor growth in a murine xenograftmodel.Int J Oncol. 2013 Nov;43(5):1517-22.

Chemical & Physical Properties

[ Density]:
1.77g/cm3

[ Boiling Point ]:
753.1ºC at 760mmHg

[ Melting Point ]:
180ºC

[ Molecular Formula ]:
C₁₆H₁₂O₆

[ Molecular Weight ]:
300.26300

[ Flash Point ]:
289ºC

[ Exact Mass ]:
300.06300

[ PSA ]:
107.22000

[ LogP ]:
1.32960

[ Vapour Pressure ]:
1.32E-17mmHg at 25°C

[ Index of Refraction ]:
1.765

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DE3120000

CHEMICAL NAME :: Benz(b)indeno(1,2-d)pyran-9(6H)-one, 6a,7-dihydro-3,4,6a,10-tetrahydroxy-

CAS REGISTRY NUMBER :: 475-25-2

BEILSTEIN REFERENCE NO. :: 0093039

LAST UPDATED :: 199701

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C16-H12-O6

MOLECULAR WEIGHT :: 300.28

WISWESSER LINE NOTATION :: T C6 B566 FV LO GH&TT&J EQ JQ NQ OQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 20 umol/L/5H (Continuous)

REFERENCE :: ENMUDM Environmental Mutagenesis. (New York, NY) V.1-9, 1979-87. For publisher information, see EMMUEG. Volume(issue)/page/year: 1,27,1979 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X6653 No. of Facilities: 25 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 760 (estimated) No. of Female Employees: 615 (estimated)

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi

[ Safety Phrases ]:
S24/25

[ RIDADR ]:
NONH for all modes of transport

Articles

The CAP1/Prss8 catalytic triad is not involved in PAR2 activation and protease nexin-1 (PN-1) inhibition.

FASEB J. 28(11) , 4792-805, (2014)

Serine proteases, serine protease inhibitors, and protease-activated receptors (PARs) are responsible for several human skin disorders characterized by impaired epidermal permeability barrier function...

Necrosis- and apoptosis-related Met cleavages have divergent functional consequences.

Cell Death Dis. 6 , e1769, (2015)

Upon activation by its ligand hepatocyte growth factor/scatter factor, the receptor tyrosine kinase Met promotes survival, proliferation, and migration of epithelial cells during embryogenesis. Deregu...

The Effects of a Selective CK2 Inhibitor on Anti-glomerular Basement Membrane Glomerulonephritis in Rats.

Biol. Pharm. Bull. 38 , 1345-51, (2015)

Protein kinase CK2 ("casein kinase II") is a protein serine/threonine kinase that plays critical roles in biological processes such as cell growth, cell cycle progression, and apoptosis. So far, we ha...

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.