Catalog No. |
Product Name |
Target |
Pathway |
Information |
S8944
|
G150
|
Others
|
Others
|
G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with IC50 of 10.2 nM.
|
S8913
|
TH5487
|
Others
|
Others
|
TH5487 is a selective active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM.
|
S8938
|
KGA-2727
|
SGLT
|
GPCR & G Protein
|
KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.
|
S8939
|
Mizagliflozin
|
SGLT
|
GPCR & G Protein
|
Mizagliflozin is a novel, potent, selective sodium glucose co-transporter 1 (SGLT1) inhibitor with Ki of 27 nM for human SGLT1. The selectivity ratio (Ki value for human SGLT2/Ki value for human SGLT1) of mizagliflozin is 303. Mizagliflozin shows the potential use for the amelioration of chronic constipation.
|
S8812
|
CM272
|
DNA Methyltransferase
|
Epigenetics
|
CM-272 is a novel first-in-class dual reversible inhibitor of G9a (GLP) and DNMTs with IC50 of 8 nM, 382 nM, 85 nM, 1200 nM, 2 nM for G9a, DNMT1, DNMT3A, DNMT3B, GLP, respectively. CM-272 prolongs survival in in vivo models of haematological malignancies by at least in part inducing immunogenic cell death.
|
S9729
|
Visomitin (SKQ1)
|
Others
|
Others
|
INT-777 (S-EMCA) is a novel potent and selective TGR5 agonist with EC50 values of 0.18 μM, 3.9 μM and 1.45 μM for WT TGR5, TGR5(N76A) and TGR5(Y89F) respectively.
|
S8500
|
BAY1125976
|
Akt
|
PI3K/Akt/mTOR
|
BAY 1125976 is a selective allosteric AKT1/2 inhibitor,exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models. BAY1125976 inhibits the activity of AKT1 (IC50 = 5.2 nM at 10 µM ATP and 44 nM at 2 mM ATP) and AKT2 (IC50 = 18 nM at 10 µM ATP and 36 nM at 2 mM ATP) very potently.Whereas BAY1125976 is almost inactive on AKT3 (IC50 = 427 nM at 10 µM ATP).
|