Synonym
GSK 137; GSK-137; GSK137
IUPAC/Chemical Name
5-((5S,7R)-3-fluoro-7-(2-methylpyridin-3-yl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-5-yl)quinolin-2-amine
InChi Key
WSRZNMRSHUJOED-RBUKOAKNSA-N
InChi Code
InChI=1S/C21H19FN6/c1-12-13(5-3-9-24-12)19-10-18(27-21-16(22)11-25-28(19)21)14-4-2-6-17-15(14)7-8-20(23)26-17/h2-9,11,18-19,27H,10H2,1H3,(H2,23,26)/t18-,19+/m0/s1
SMILES Code
FC1=C(N[C@H](C2=CC=CC3=C2C=CC(N)=N3)C[C@@H]4C5=C(C)N=CC=C5)N4N=C1
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
B-cell lymphoma 6 (BCL6) is a zinc finger transcriptional repressor possessing a BTB-POZ (BR-C, ttk, and bab for BTB; pox virus and zinc finger for POZ) domain, which is required for homodimerization and association with corepressors. BCL6 has multiple roles in normal immunity, autoimmunity, and some types of lymphoma. Mice bearing disrupted BCL6 loci demonstrate suppressed high-affinity antibody responses to T-dependent antigens. The corepressor binding groove in the BTB-POZ domain is a potential target for small compound-mediated therapy. Several inhibitors targeting this binding groove have been described, but these compounds have limited or absent in vivo activity. Biophysical studies of a novel compound
Preparing Stock Solutions
The following data is based on the
product
molecular weight
374.42
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Pearce AC, Bamford MJ, Barber R, Bridges A, Convery MA, Demetriou C, Evans S, Gobbetti T, Hirst DJ, Holmes DS, Hutchinson JP, Jayne S, Lezina L, McCabe MT, Messenger C, Morley J, Musso MC, Scott-Stevens P, Manso AS, Schofield J, Slocombe T, Somers D, Walker AL, Wyce A, Zhang XP, Wagner SD. GSK137, a potent small-molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice. J Biol Chem. 2021 Aug;297(2):100928. doi: 10.1016/j.jbc.2021.100928. Epub 2021 Jul 15. PMID: 34274316; PMCID: PMC8350397.
