Endothall

Modify Date: 2024-01-07 18:46:00

Endothall structure	Common Name	Endothall
	CAS Number	145-73-3	Molecular Weight	186.16200
	Density	1.431	Boiling Point	350oC(e)
	Molecular Formula	C8H10O5	Melting Point	144oC
	MSDS	N/A	Flash Point	190.5oC

Purity		Quantity		Budget		Inquiry

Use of Endothall Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 μM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy[1].

• Properties

• Spectrum

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 Names

Name	endothal
Synonym	More Synonyms

 Endothall Biological Activity

Description	Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 μM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy[1].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase
In Vitro	Endothall, an organic acid, is the least toxic structural analogue of Cantharidin that still inhibits PP2A[2]. Endothall inhibits preferentially hepatocellular carcinoma (HCC) growth and these new rat hepatocellular carcinoma lines may be useful for further biochemical and pharmacological studies on PP2A inhibitors, and for testing new forms of treatment of hepatic cell carcinomas. The HR-2, HR-3, HR-4, and Zajdela hepatocellular carcinomas are most sensitive to Endothall (IC50 of 1.7, 1.2, 0.9, and 1.7 μg/mL), whereas newborn rat hepatocytes growing exponentially in primary culture (IC50=6.2 μg/mL), rat DHD/K12 colon carcinoma cells (IC50=3.6 μg/mL), or human HT-29 colon carcinoma cells (IC50=4.9 μg/mL) were less sensitive[2]. Endothall inhibits the growth of HCC lines in culture more than that of normal hepatocytes or colon carcinomas, inducing mitotic arrest, followed by cell death. Endothall causes dose- and time-dependent cytostasis specifically in G2/M[2]. Endothall (3 μg/mL) inhibits the cell cycle at G2/M and subsequent apoptotic cell death[2].
In Vivo	Endothall exhibits acute LD50 of 14 mg/kg in mice[2].
References	[1]. Janetti R Signorelli, et al. Protein phosphatases decrease their activity during capacitation: a new requirement for this event. PLoS One. 2013 Dec 2;8(12):e81286. [2]. J P Thièry, et al. Hepatocellular carcinoma cell lines from diethylnitrosamine phenobarbital-treated rats. Characterization and sensitivity to endothall, a protein serine/threonine phosphatase-2A inhibitor. Hepatology. 1999 May;29(5):1406-17.

 Chemical & Physical Properties

Density	1.431
Boiling Point	350oC(e)
Melting Point	144oC
Molecular Formula	C8H10O5
Molecular Weight	186.16200
Flash Point	190.5oC
Exact Mass	186.05300
PSA	83.83000
Vapour Pressure	2.88E-09mmHg at 25°C
Index of Refraction	1.568

 MSDS

Endothall MSDS(Chinese)

 Toxicological Information

CHEMICAL IDENTIFICATION RTECS NUMBER : RN7875000 CHEMICAL NAME : 7-Oxabicyclo(2.2.1)heptane-2,3-dicarboxylic acid CAS REGISTRY NUMBER : 145-73-3 LAST UPDATED : 199701 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C8-H10-O5 MOLECULAR WEIGHT : 186.18 WISWESSER LINE NOTATION : T55 A AOTJ CVQ DVQ HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Human - man DOSE/DURATION : 571 uL/kg TOXIC EFFECTS : Cardiac - other changes Kidney, Ureter, Bladder - urine volume decreased Nutritional and Gross Metabolic - metabolic acidosis REFERENCE : AJEMEN American Journal of Emergency Medicine. (WB Saunders, Philadelphia, PA) V.1- 1983- Volume(issue)/page/year: 6,509,1988 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 38 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : PCOC** Pesticide Chemicals Official Compendium, Association of the American Pesticide Control Officials, Inc., 1966. (Topeka, KS) Volume(issue)/page/year: -,471,1966 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Administration onto the skin SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >1 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 7,299,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 14 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JAFCAU Journal of Agricultural and Food Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1953- Volume(issue)/page/year: 35,823,1987 *** U.S. STANDARDS AND REGULATIONS *** EPA FIFRA 1988 PESTICIDE SUBJECT TO REGISTRATION OR RE-REGISTRATION FEREAC Federal Register. (U.S. Government Printing Office, Supt. of Documents, Washington, DC 20402) V.1- 1936- Volume(issue)/page/year: 54,7740,1989

 Safety Information

Hazard Codes	T
Risk Phrases	21-25-36/37/38
Safety Phrases	S45;S36/S37/S39
RIDADR	UN 2811 6.1/PG 2
WGK Germany	1
RTECS	RN7875000
Packaging Group	II
Hazard Class	6.1(a)
HS Code	2932190013

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