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1379573-92-8

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1379573-92-8 Usage

Biological Activity

cbb1007 is an inhibitor of histone demethylase lsd1with ic50 values of 5.27μm [1].lsd1 is a member of the fad-dependent amine oxidase family. it converts di-methylated h3k4 to mono- and un-methylated h3k4 and suppresses gene expression. as an inhibitor of lsd1, cbb1007 is developed to understand the function of the enzyme. in the in vitro assay, cbb1007 shows highly potent inhibitory activity with ic50 value of 5.27μm. it is specific against lsd1 and has no effect on other histone demethylases including lsd2 and jarid1a. in the mouse f9 embryonic teratocarcinoma cells, cbb1007 cause a reproducible increase of mono- and di-methylated h3k4 with ic50 value of 1μm-5μm. it also activates the expression of chrm4 and scn3a which are the target genes of lsd1. the inhibition of lsd1 results in the growth inhibition of these cells. furthermore, cbb1007 is found to inhibit the proliferation of other pluripotent cancer cells as well as the embryonic stem cells that express the stem cell markers oct4 and sox2 [1].

references

[1] wang j, lu f, ren q, et al. novel histone demethylase lsd1 inhibitors selectively target cancer cells with pluripotent stem cell properties. cancer research, 2011, 71(23): 7238-7249.

Check Digit Verification of cas no

The CAS Registry Mumber 1379573-92-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,7,9,5,7 and 3 respectively; the second part has 2 digits, 9 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1379573-92:
(9*1)+(8*3)+(7*7)+(6*9)+(5*5)+(4*7)+(3*3)+(2*9)+(1*2)=218
218 % 10 = 8
So 1379573-92-8 is a valid CAS Registry Number.

1379573-92-8Upstream product

1379573-92-8Downstream Products

1379573-92-8Relevant articles and documents

HISTONE DEMETHYLASE INHIBITORS AND USES THEREOF FOR TREATMENT O F CANCER

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Page/Page column 95, (2012/06/15)

A compound of formula I: or a pharmaceutically acceptable salt, Ri is an optionally substituted heterocyclic group; R and R' are independently H, CH3, NO2, SO2N(CH3)2, SO2N((CH3)SO2), COOH, COOCH3, CO(N(CH3)), alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, heteroaryl, heterocycloalkyl, alkoxy, alkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aryloxycarbonyloxy, carboxylate, alkylcarbonyl, alkylaminocarbonyl, aralkylaminocarbonyl, alkenylaminocarbonyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkenylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylthiocarbonyl, trifluoromethyl, pentafluoroethyl, halogen, cyano, thio, amido, ether, ester, hydroxyl, hydroxyalkyl, saturated or unsaturated fatty acids, azido, phosphonamido, sulfonamido, lactam, phosphate, phosphonato, phosphinato, amino, acylamino, amidino, imino, guanidino, sulfhydryl, alkylthio, arylthio, thiocarboxylate, sulfates, alkylsulfinyl, sulfonato, sulfamoyl, sulfonamido, nitro, cyano, or azido; m and n are independently integers from 1 to 4; T, U, V, and Z are independently CH, N, or CR; L is NH, CH2, O, S, or SO2; X is N or CH; Y and Y' are independently O or S; and R3 is an optionally substituted aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group.

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