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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

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