| DC22862 |
CRT-0105446 |
A novel potent LIMK inhibitor with IC50 of 8 nM and 32 nM for LIMK1 and LIMK2, respectively. |
|
| DC11622 |
MAP3K14-IN-173 |
A novel potent MAP3K14 kinase inhibitor with IC50 of 1.8 nM (NIK autophosphorylation). |
|
| DC11515 |
Azeloprazole |
A novel potent proton pump inhibitor that irreversibly inhibits H+,K+-ATPase activity with IC50 of 0.28 uM. |
|
| DC23393 |
BETi-211 |
A novel potent small-molecule BET bromodomain (BRD) inhibitor that binds to BET proteins with Ki values of <1 nM. |
|
| DC11995 |
BI 703704 |
A novel potent soluble guanylate cyclase (sGC) activator. |
|
| DC11880 |
TH1834 |
A novel potent specific histone acetyltransferaseTip60 inhibitor. |
|
| DC11881 |
TH1834 dihydrochloride |
A novel potent specific histone acetyltransferaseTip60 inhibitor. |
|
| DC22798 |
ADA-07 |
A novel potent TOPK inhibitor that effectively suppresses SUV-induced activation of MAPKs signal transduction resulting in reduced SUV-induced skin carcinogenesis. |
|
| DC11603 |
SR-19871 |
A novel potent ULK1 inhibitor with IC50 of 11 nM.. |
|
| DC11693 |
AJS1669 sodium |
A novel potent, allosteric, orally available muscle glycogen synthase 1 (GYS1) activator with EC50 of 5.2 uM. |
|
| DC11692 |
AJS1669 |
A novel potent, allosteric, orally available muscle glycogen synthase 1 (GYS1) activator with EC50 of 5.2 uM. |
|
| DC21354 |
MT47-100
Featured
|
MT47-100 is a novel compound that exhibits a unique dual functionality as both an allosteric activator and inhibitor of AMP-activated protein kinase (AMPK) complexes, depending on the isoform present. Specifically, MT47-100 acts as a direct activator of AMPK complexes containing the β1 isoform and as a direct inhibitor of AMPK complexes containing the β2 isoform. This isoform-specific modulation of AMPK activity makes MT47-100 a potentially valuable tool for studying the distinct physiological roles of β1- and β2-containing AMPK complexes, as well as a candidate for therapeutic applications targeting AMPK-related pathways. |
|
| DC23525 |
AAT-008 |
A novel potent, and selective prostaglandin EP4 receptor antagonist with binding IC50 of 2.4 nM. |
|
| DC22688 |
AZD 3676 |
A novel potent, combined serotonin 5-HT1A and 5-HT1B receptor antagonist with Ki of 0.13 and 2.4 nM in brain homogenates, respectively. |
|
| DC11986 |
OX03050 |
A novel potent, competitive squalene synthase inhibitor that upregulate the LDLR in mouse and human liver cell lines with EC50 of 26 nM. |
|
| DC20692 |
ASP 8477 |
A novel potent, highly selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 0.99, 1.65 and 57.3 nM for human FAAH-1, FAAH-1 (P129T) and FAAH-2, respectively. |
|
| DC21507 |
PHA-408 |
A novel potent, highly selective, ATP-competitive IKK-2 inhibitor with IC50 of 40 nM, 350-fold selectivity over IKK-1. |
|
| DC23309 |
BCL6 inhibitor 8c |
A novel potent, in vivo-active BCL6 inhibitor with IC50 of 0.1 uM in ELISA assays. |
|
| DC21209 |
KW-2581 |
A novel potent, irreversible and orally active inhibitor of steroid sulfatase (STS) with IC50 of 13 nM in ZR-75-1 cells. |
|
| DC11769 |
MPO-IN-28
Featured
|
A novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM. |
|
| DC21058 |
GNS-1481 |
A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 6.2, 3.4 and 4.2 nM for L858R-T790M, T790M and Del19-T790M, respectively. |
|
| DC21059 |
GNS-1486 |
A novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 8.3, 4.2 and 4.3 nM for L858R-T790M, T790M and Del19-T790M, respectively. |
|
| DC11612 |
KBP-7018 hydrochloride |
A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively. |
|
| DC11611 |
KBP-7018 |
A novel potent, multikinase inhibitor with IC50 of 10, 7.6 and 25 nM for c-Kit, RET and PDGFRβ, respectively. |
|
| DC11751 |
UHC1 |
A novel potent, non-agonist PPARγ ligand that blocks CDK5-mediated PPARγ phosphorylation, without the classical agonism. |
|
| DC11750 |
SR-1664
Featured
|
SR-1664 is a novel potent, non-agonist PPARγ ligand that blocks the Cdk5-mediated phosphorylation in vitro (IC50=80 nM) and in vivo, without the classical agonism. |
|
| DC11968 |
OSU-03013 |
A novel potent, orally active 3-phosphoinositide-dependent kinase-1 (PDK-1) with IC50 of 2 uM. |
|
| DC24024 |
Z-360 |
A novel potent, orally active CCK-2/gastrin receptor antagonist with Ki of 0.47 nM. |
|
| DC11607 |
JTZ-951(Enarodustat)
Featured
|
A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2. |
|
| DC11608 |
JTZ-951 hydrochloride |
A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2. |
|
