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product name
Okadaic Acid, Prorocentrum sp., Okadaic Acid, CAS 78111-17-8, is a highly potent inhibitor of protein phosphatase 1 (IC₅₀ = 10-15 nM) and 2A (IC₅₀ = 0.1 nM).
品質等級
化驗
≥95% (HPLC)
形狀
solid (glassy)
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
colorless
溶解度
DMF: soluble
chloroform: soluble
ethanol: soluble
methanol: soluble
運輸包裝
ambient
儲存溫度
−20°C
InChI
1S/C44H68O13/c1-25-21-34(55-44(23-25)35(46)12-11-31(54-44)24-41(6,50)40(48)49)26(2)9-10-30-14-18-43(53-30)19-15-33-39(57-43)36(47)29(5)38(52-33)32(45)22-28(4)37-27(3)13-17-42(56-37)16-7-8-20-51-42/h9-10,23,26-28,30-39,45-47,50H,5,7-8,11-22,24H2,1-4,6H3,(H,48,49)/b10-9+/t26-,27-,28+,30+,31+,32+,33-,34+,35-,36-,37?,38+,39?,41-,42+,43-,44-/m1/s1
InChI 密鑰
QNDVLZJODHBUFM-AAWJMCDUSA-N
一般說明
An ionophore-like polyether derivative of a C38 fatty acid compound isolated from the dinoflagellates that have fed on the marine sponge Halinchrondria okadai. It is a potent non-comepetitive, reversible inhibitor of serine/threonine-specific protein phosphatases 1 (PP1, IC50 = 10-15 nM, rabbit skeletal muscle, catalytic subunit) and 2A (PP2A, IC50 = 0.1 nM, rabbit skeletal muscle, catalytic subunit). It has only a trivial effect on protein phosphatase 2B (IC50 = 5 µM), a Ca2+/calmodulin-dependent enzyme, while PP2C, a Mg2+ dependent enzyme, is unaffected. Okadaic acid has no significant effect on the activities of tyrosine phosphatases, alkaline phosphatase, acid phosphatase, and inositol trisphosphatase. It is also a non-phorbol ester-type tumor promoter on mouse skin. Useful for the study of protein phosphatases and of PP1/PP2A in cell extracts, as well as in intact cells. Induces apoptosis in human breast carcinoma (MB-231 and MCF-7) and in myeloid cells, but inhibits glucocorticoid-induced apoptosis in T-cell hybridomas. Has marked contractile effect on smooth muscles and heart muscles. Implicated as a causative agent of diarrhetic shellfish poisoning.
An ionophore-like polyether derivative of a C38 fatty acid compound that has tumor promoting properties. Potent inhibitor of protein phosphatase 1 (IC50 = 10-15 nM) and protein phosphatase 2A (IC50 = 0.1 nM). Does not affect the activity of tyrosine phosphatases, alkaline phosphatases, or acid phosphatases. Useful for the study of protein phosphatases in cell extracts as well as in intact cells. Induces apoptosis in human breast carcinoma cells (MB-231 and MCF7) and in myeloid cells but inhibits glucocorticoid-induced apoptosis in T cell hybridomas. Has marked contractile effects on smooth muscle and heart muscle. Implicated as causative agent of diarrhetic shellfish poisoning. A 250 µM (25 µg/124 µl) solution of Okadaic Acid, (Cat. No. 495609) in DMSO is also available.
生化／生理作用
Cell permeable: no
Primary Target
Protein phosphatase
Protein phosphatase
Product does not compete with ATP.
Reversible: no
Target IC50: 10-15 nM and 0.1 nM against protein phosphatase 1 and protein phosphatase 2A, respectively
包裝
Packaged under inert gas
警告
Toxicity: Toxic (F)
重構
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
其他說明
Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
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Kiguchi, K., et al. 1994. Cell Growth Differentiation5, 995.
Ohaka, Y., et al. 1993. Biochem. Biophys. Res. Commun. 197, 916.
Gopalakrishna, R., et al. 1992. Biochem. Biophys. Res. Commun. 189, 950.
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Haystead, T.A., et al. 1989. Nature337, 78.
Kiguchi, K., et al. 1994. Cell Growth Differentiation5, 995.
Ohaka, Y., et al. 1993. Biochem. Biophys. Res. Commun. 197, 916.
Gopalakrishna, R., et al. 1992. Biochem. Biophys. Res. Commun. 189, 950.
Kreienbuhl, P., et al. 1992. Blood80, 2911.
Nomura, M., et al. 1992. Biochemistry31, 11915.
Song, Q., et al. 1992. J. Cell Physiol.153, 550.
Tada, Y., et al. 1992. Immunopharmacol.24, 17.
Cohen, P., et al. 1990. Trends Biochem. Sci.15, 98.
Cohen, P. 1989. Annu. Rev. Biochem.58, 453.
Cohen, P., and Cohen, P.T. 1989. J. Biol. Chem.264, 21435.
Haystead, T.A., et al. 1989. Nature337, 78.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
訊號詞
Danger
危險分類
Acute Tox. 3 Dermal - Acute Tox. 3 Inhalation - Acute Tox. 3 Oral - Skin Irrit. 2
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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The term M-phase supershift denotes the phosphorylation-dependent substantial increase in the apparent molecular weight of numerous proteins of varied biological functions during M-phase induction. Although the M-phase supershift of multiple key mitotic regulators has been attributed to the multisite phosphorylation
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CK1s are acidophilic serine/threonine kinases with multiple critical cellular functions; their misregulation contributes to cancer, neurodegenerative diseases, and sleep phase disorders. Here, we describe an evolutionarily conserved mechanism of CK1 activity: autophosphorylation of a threonine (T220 in human CK1δ) located
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