Tag: 193.0649

Liu, Yao et al. published their research in Journal of Medicinal Chemistry in 2020 | CAS: 3034-57-9

2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Product Details of 3034-57-9

Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13 was written by Liu, Yao;Hao, Mingfeng;Leggett, Alan L.;Gao, Yang;Ficarro, Scott B.;Che, Jianwei;He, Zhixiang;Olson, Calla M.;Marto, Jarrod A.;Kwiatkowski, Nicholas P.;Zhang, Tinghu;Gray, Nathanael S.. And the article was included in Journal of Medicinal Chemistry in 2020.Product Details of 3034-57-9 This article mentions the following:

Genetic depletion of cyclin-dependent kinase 12 (CDK12) or selective inhibition of an analog-sensitive CDK12 reduces DNA damage repair gene expression, but selective inhibition of endogenous CDK12 is difficult. Here, we report the development of MFH290(I), a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib. In the experiment, the researchers used many compounds, for example, 2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9Product Details of 3034-57-9).

2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Product Details of 3034-57-9

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Lund, Henning et al. published their research in Acta Chemica Scandinavica in 1965 | CAS: 3034-57-9

2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Synthetic Route of C4H5BrN2S

Electroorganic preparations. XVI. Polarography and reduction of quinazoline was written by Lund, Henning. And the article was included in Acta Chemica Scandinavica in 1965.Synthetic Route of C4H5BrN2S This article mentions the following:

The polarographic reduction of quinazoline (I) was observed throughout the pH range 0-12 and in more acid media (acidity function H+ to -2); 2 waves were observed. For the 1st wave the limiting current is diffusion controlled at pH 5 but is kinetically controlled at pH 1. The abnormal pH dependence of the limiting current can be explained by hydration of the protonated I nucleus if it is assumed that only the normal cation and not the hydrated cation is polarographically reducible. The rate constant of the dehydration was determined from polarographic data, and the dehydration was found to be specific acid catalyzed. The second wave of I is a reduction of the 3,4-dihydroquinazoline (II) formed in the first reduction at low concentrations of I. II was reduced in borate buffer to 1,2,3,4-tetrahydroquinazoline. I yields on controlled potential reduction both in acid and alk. solution a dimerized product, which probably is dimerized at C-4. The product can be reoxidized to I with hexacyanoferrate(III) in alk. solution In the experiment, the researchers used many compounds, for example, 2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9Synthetic Route of C4H5BrN2S).

2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Synthetic Route of C4H5BrN2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Liu, Yao et al. published their research in Journal of Medicinal Chemistry in 2020 | CAS: 3034-57-9

2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Product Details of 3034-57-9

Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13 was written by Liu, Yao;Hao, Mingfeng;Leggett, Alan L.;Gao, Yang;Ficarro, Scott B.;Che, Jianwei;He, Zhixiang;Olson, Calla M.;Marto, Jarrod A.;Kwiatkowski, Nicholas P.;Zhang, Tinghu;Gray, Nathanael S.. And the article was included in Journal of Medicinal Chemistry in 2020.Product Details of 3034-57-9 This article mentions the following:

Genetic depletion of cyclin-dependent kinase 12 (CDK12) or selective inhibition of an analog-sensitive CDK12 reduces DNA damage repair gene expression, but selective inhibition of endogenous CDK12 is difficult. Here, we report the development of MFH290(I), a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation and DNA damage repair gene expression. Consistent with its effect on DNA damage repair gene expression, MFH290 augments the antiproliferative effect of the PARP inhibitor olaparib. In the experiment, the researchers used many compounds, for example, 2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9Product Details of 3034-57-9).

2-Amino-5-bromo-4-methylthiazole (cas: 3034-57-9) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Product Details of 3034-57-9

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica