23056-10-2

Usage

Uses

Used in Chemical Research:
5-Thiocyanato-Thiazol-2-ylamine is used as a research chemical for studying its properties and potential applications in the field of chemistry. Its unique structure and characteristics make it a valuable compound for scientific investigation.
Used in Pharmaceutical Research:
5-Thiocyanato-Thiazol-2-ylamine is used as a starting material or intermediate in the synthesis of pharmaceutical compounds. Given the medicinal properties of related thiazol-2-ylamine derivatives, 5-THIOCYANATO-THIAZOL-2-YLAMINE may contribute to the development of new drugs with therapeutic applications.
Used in Drug Production:
5-Thiocyanato-Thiazol-2-ylamine is used as a component in the production of drugs, particularly those that are based on thiazol-2-ylamine derivatives. Its presence in the final drug product may be attributed to its role in the synthesis process or its direct contribution to the drug's therapeutic effects.

InChI:InChI=1/C4H3N3S2/c5-2-8-3-1-7-4(6)9-3/h1H,(H2,6,7)

Upstream product

• 96-50-4 2-thiazolylamine 
• 1147550-11-5 ammonium thiocyanate 
• 333-20-0 potassium thioacyanate 
• 61296-22-8 5-bromothiazol-2-amine hydrobromide 
• 540-72-7 sodium thiocyanide 
• 163276-49-1 1-thiocyanatopyrrolidine-2,5-dione 
• 3034-22-8 5-bromo-2-aminothiazole 

Downstream Products

• 36016-97-4 2-acetamino-5-thiocyanatothiazole 
• 91059-77-7 N-(5-thiocyanato-thiazol-2-yl)-benzamide 
• 37469-45-7 phenylpropynoic acid 5-thiocyanato-thiazol-2-ylamide 
• 116636-52-3 2-Ethoxycarbonylamino-5-thiocyanato-thiazole 
• 224436-97-9 2-amino-5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-thiazole 
• 745074-48-0 5-(2-amino-thiazol-5-ylsulfanylmethyl)-2,3-dimethyl-benzoic acid methyl ester 
• 1001419-49-3 C₁₃H₁₁N₃OS₂ 
• 859524-83-7 1,1-dicyclohexyl-3-(5-thiocyanatothiazol-2-yl)urea 

Relevant academic research and scientific papers

Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13

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, 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.

Metal-Free One-Pot Chemoselective Thiocyanation of Imidazothiazoles and 2-Aminothiazoles with in situ Generated N-Thiocyanatosuccinimide

A chemoselective thiocyanation of imidazothiazoles and 2-aminothiazoles with use of in situ generated N-thiocyanatosuccinimide (NTS) at room temperature is described. The protocol offers mild reaction conditions and high chemoselectivity for electrophilic substitution in imidazothiazoles over nucleophilic substitution. This method provides metal-free and easy conversion of imidazothiazoles and 2-aminothiazoles into their corresponding C-3 and C-5 thiocyanates, respectively, in good to excellent yield. The present protocol also offers the effective thiocyanation of bifunctional imidazothiazoles containing aliphatic -OH and C(sp 2)-H bond functionalities.

INHIBITORS OF CYCLIN-DEPENDENT KINASES

The present invention provides novel compounds of Formulae (I'), (I), (II'), and (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing proliferative diseases (e.g., cancers (e.g., leukemia, acute lymphoblastic leukemia, lymphoma, Burkitt's lymphoma, melanoma, multiple myeloma, breast cancer, Ewing's sarcoma, osteosarcoma, brain cancer, ovarian cancer, neuroblastoma, lung cancer, colorectal cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., CDK7, CDK12, or CDK13), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

CDK INHIBITORS

The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.

CDK INHIBITORS CONTAINING A ZINC BINDING MOIETY

The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.

UREA GLUCOKINASE ACTIVATORS

This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutic

UREA GLUCOKINASE ACTIVATORS

This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutic

NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME

Compounds are provided which are glucokinase activators and thus are useful in treating diabetes and related diseases and have the structure wherein in the ring represents one or two double bonds; R1 is aryl or heteroaryl; R2 is halogen, cycloalkyl, heterocyclyl, aryl, or heteroaryl; R5 is as defined herein; Z is O, S, S(O), S(O)2, or NR5a; X is S, O, N, NR3, or CR3; Y is NCR4 or N4; R3, R4, and R5 are as defined herein; R8 is aryl or heteroaryl; R6 and R7 are independently H, halogen, or alkyl; m is 0 or 1; and n is 0 to 3, or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

NOVEL GLUCOKINASE ACTIVATORS AND METHODS OF USING SAME

Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring; R4 is —(CH2)n-Z-(CH2)m—PO(OR7)(OR8), —(CH2)nZ-(CH2)m—PO(OR7)Rg, —(CH2)n-Z-(CH2)m—OPO(OR7)Rg, —(CH2)nZ—(CH2)m—OPO(R9)(R10), or —(CH2)nZ—(CH2)m—PO(R9)(R10);R5 and R6 are independently selected from H, alkyl and halogen;Y is R7(CH2)s or is absent; andX, n, Z, m, R4, R5, R6, R7, and s are as defined herein; or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

UREA GLUCOKINASE ACTIVATORS

The invention provides a compound of general formula (I) wherein the substituents are defined futher in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds