| DC74237 |
NYX-PCSK9i |
NYX-PCSK9i is an orally bioavailable small-molecule inhibitor of PCSK9, inhibits PCSK9-LDLR interaction with IC50 of 323 nM in in vitro biochemical binding assays. |
|
| DC74238 |
BPN15477 |
BPN-15477 (BPN15477) is a potent splicing modulator compound that restores correct splicing of ELP1 exon 20, increases full-length ELP1 mRNA by increasing exon 20 inclusion with EC50 of 1.9 uM in luciferase splicing assays. |
|
| DC74239 |
CD33 splicing modulator 1 |
CD33 splicing modulator 1 is a small-molecule CD33 pre-mRNA splicing modulator with EC50 of 7.8 uM, enhances the exclusion of CD33 exon 2, reduces full-length V-domain containing CD33 protein. |
|
| DC74240 |
HTT splicing modulator 27 |
HTT splicing modulator 27 is a potent, orally bioavailable, and brain-penetrant small-molecule HTT pre-mRNA splicing modulator with mHTT protein EC50 of 66 nM. |
|
| DC74241 |
Rebecsinib
Featured
|
Rebecsinib (17S-FD-895) is a selective small-molecule inhibitor of splicing-mediated ADAR1 activation, prevents leukemia stem cell generation. |
|
| DC74242 |
Thailanstatin C |
Thailanstatin C (TST-C) is a potent antiproliferative natural product, a pre-mRNA splicing inhibitor and antiproliferative agent.. |
|
| DC74244 |
SRI-42127 |
SRI-42127 is a small molecule, BBB-permeable inhibitor of the RNA regulator HuR, inhibits HuR dimerization with IC50 of 1.2 uM in cell-based assays, prevents HuR oligomerization. |
|
| DC74245 |
STK018404 |
STK018404 is a small molecule inhibitor of RNA-binding protein human antigen R (HuR), decreases the binding of HuR to its target RNA motif. |
|
| DC74246 |
AA132 |
AA132 (AA-132) is a small molecule activator of UPR signaling, covalently modifies a subset of ER protein disulfide isomerases (PDIs), activates global UPR signaling through a mechanism analogous to that of AA147. |
|
| DC74247 |
AG-946
Featured
|
AG-946 (AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively. |
|
| DC74248 |
HA344 |
HA344 (HA 344) is a dual covalent inhibitor of pyruvate kinase M2 (PKM2) and inosine monophosphate dehydrogenase (IMPDH), efficiently inhibits cutaneous metastatic melanoma (CMM). |
|
| DC74526 |
AdipoAI |
AdipoAI is a novel small molecule APN receptor (AdipoR, adiponectin receptor) agonist. |
|
| DC74527 |
ALY688 |
ALY688 (ADP 355) is an adiponectin mimetic adiponectin receptor (AdipoR) agonist, inhibits the growth of AdipoR1/AdipoR2-positive cancer cell lines (MCF-7 cell, 0.1-10 uM). |
|
| DC74528 |
K284
Featured
|
K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals. |
|
| DC74529 |
Wyeth-1 |
Wyeth-1 (hAMCase inhibitor 1) is a potent, selective inhibitor of human acidic mammalian chitinase (hAMCase) with IC50 of 210 nM, 20-fold selectivity over hCHIT1. |
|
| DC74530 |
DL5050 |
DL5050 (DL 5050) is a potent selective agonist of human constitutive androstane receptor (CAR) with EC50 of 0.37 uM in cell-based luciferase reporter assays (Emax=3.8). |
|
| DC74531 |
DL7076 |
DL7076 (CN06) is a small molecule dual activator of the constitutive androstane receptor (CAR, NR1I3) and nuclear factor erythroid 2-related factor 2 (Nrf2) with EC50 of 8.85 and 0.72 uM, respectively. |
|
| DC74532 |
BVT173187 |
BVT173187 is a potent, selective, non-peptide inhibitor of formyl peptide receptor 1 (FPR1), inhibits fMLF and WKYMVM induced oxidase activity. |
|
| DC74533 |
ICT12035 |
ICT12035 (AZ2158) is a potent, selective formylpeptide receptor-1 (FPR1) antagonist with IC50 of 30 nM in calcium mobilisation assays (100 nM fMLF). |
|
| DC74534 |
MD102 |
MD102 is a potent transglutaminase 2 (TGase 2; TG2) inhibitor with IC50 of 0.35 uM, shows p53 stabilization effect and anticancer activity at RCC cell lines. |
|
| DC74535 |
ZED1227 |
ZED1227 is a potent, selective, covalent, and orally active transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 45 nM. |
|
| DC74536 |
LJ4827 |
LJ4827 (LJ-4827) is a potent, specific inhibitor of HASPIN, a mitotic kinase for Histone H3, with Ki value of 0.46 nM, enzyme IC50 of 0.155 nM in HASPIN kinase assay performed with Histone H3 peptide. |
|
| DC74537 |
AG-120-X |
AG-120-X is a first-in-class small molecule inhibitor of ICOS/ICOSL interaction with IC50 of 4.68 uM in TR-FRET assay, dose-dependently blocks ICOS/ICOSL interaction in cellular assay based on co-culturing Jurkat T cells expressing ICOS and CHO-K1 cells e |
|
| DC74538 |
C-5401331 |
C-5401331 is a small molecule T-cell immunoglobulin and mucin domain-containing protein 3 (Tim-3) inhibitor, suppresses acute myeloid leukemia (AML) cell proliferation. |
|
| DC74539 |
L557-0155
Featured
|
L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth. |
|
| DC74540 |
MTX-3937
Featured
|
MTX-3937 is a small-molecule inhibitor targeting Siglec-9 (Sialic acid-binding immunoglobulin-type lectin-9), a member of the Siglec family of immunomodulatory receptors. Siglec-9 is primarily expressed on immune cells, such as myeloid cells and natural killer (NK) cells, and plays a role in regulating immune responses by transmitting inhibitory signals through its intracellular immunoreceptor tyrosine-based inhibitory motifs (ITIMs). |
|
| DC74541 |
ARUK3001185 |
ARUK3001185 is a potent, selective, brain-penetrant inhibitor of Wnt-deactivating enzyme Notum carboxylesterase activity with IC50 of 6.7 nM in OPTS biochemical assay. |
|
| DC74542 |
LP-914822 |
LP-914822 (LP914822) is a potent, selective and orally-active NOTUM with IC50 of 2 nM for human, mouse and rat Notum. |
|
| DC74543 |
LP-935001 |
LP-935001 (LP935001) is a potent, selective and orally-active NOTUM with enzyme IC50 of 0.4 nM for both of human and mouse Notum. |
|
| DC74544 |
AS-48 |
AS-48 is a specific, small-molecule measles virus (MeV) entry inhibitor with IC50 of 0.6 uM agianst MV-KS. |
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