Thioguanine Inhibitor CAS No. 154-42-7

Cat. No.	Name	Size	Price	Add Cart
KI1357	Thioguanine	500 mg	$272
KI1357	Thioguanine	1 g	$448

Chemical Characteristic

Product Name	Thioguanine
Synonyms	Tioguanine, 6-thioguanine
CAS No.	154-42-7
Molecular Weight	167.19
Formula	C₅H₅N₅S
Chemical Name	2-?amino-?1,?9-?dihydro-6H-?purine-?6-?thione
Smiles	c12c(c(nc(n1)N)S)nc[nH]2
Chemical Structure

Biological activities

Thioguanine is a purine antimetabolite widely used in the treatment of acute lymphoblasic leukemia, ulcerative colitis, and some autoimmune diseases. Thioguanine utilises the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) to be converted to 6-thioguanine monophosphate (TGMP). High concentrations of TGMP may accumulate intracellularly and hamper the synthesis of guanine nucleotides via the enzyme Inosine monophosphate dehydrogenase (IMP dehydrogenase).^[1] In the parental human ovarian cancer cell line 2008 and its DDP-resistant subline 2008/C 13×5.25, the IC50 value for 6-thioguanine is 6.5 and 3.7 µM, respectively.^[2] In human CCRF-CEM cell lines that do and do not overexpress thiopurine S-methyl-transferase (TPMT), the IC50 value for thioguanine is 1.1 and 0.55 µM, respectively.^[3] In mice bearing xenografts derived from BRCA2-deficient V-C8 cells, thioguanine (1.5 mg/kg) causes significant growth delay and three of five complete tumor regressions.^[4]

Protocols

In vivo: 6-thioguanine is dissolved in PBS.^[4]

References

[1] Dubinsky MC, et al. 6-thioguanine can cause serious liver injury in inflammatory bowel disease patients. Gastroenterology. 2003, 125(2): 298-303. [2] Aebi S, et al. Loss of DNA mismatch repair in acquired resistance to cisplatin. Cancer Res. 1996, 56(13): 3087-3090. [3] Dervieux T, et al. Differing contribution of thiopurine methyltransferase to mercaptopurine versus thioguanine effects in human leukemic cells. Cancer Res. 2001, 61(15): 5810-5816. [4] Issaeva N, et al. 6-thioguanine selectively kills BRCA2-defective tumors and overcomes PARP inhibitor resistance. Cancer Res. 2010, 70(15): 6268-6276.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.

KareBay^TM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.

About

KareBay^TM Biochem
Sitemap
Blog

Custom Services

Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services

Biochemical Products

Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR

KareBay^TM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852

Telephone

: 732-823-1545

Fax

: 732-823-1349

product@karebaybio.com
service@karebaybio.com
support@karebaybio.com