| DC73764 |
CRD733
Featured
|
CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor. |
|
| DC73789 |
K306
Featured
|
K306 is a small molecule agonist that specifically targets SH2-containing 5' inositol phosphatase 1 (SHIP1), an enzyme involved in regulating cellular signaling pathways. SHIP1 is a lipid phosphatase that hydrolyzes the 5' phosphate of phosphatidylinositol-3,4,5-trisphosphate (PIP3), converting it to phosphatidylinositol-3,4-bisphosphate (PI(3,4)P2). This activity modulates the PI3K (phosphoinositide 3-kinase) signaling pathway, which is critical for cell survival, proliferation, and immune responses. |
|
| DC73792 |
NSC74429
Featured
|
NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay. |
|
| DC73804 |
MK-0773
Featured
|
MK-0773 is a selective androgen receptor modulators (SARMs) that binds to AR with an IC50 of 6.6 nM. |
|
| DC73809 |
ITE
Featured
|
A endogenous ligand, potent aryl hydrocarbon receptor (AhR) agonist in vitro. |
|
| DC73817 |
ATF3W-aeg peptide
Featured
|
ATF3W-aeg peptide is a selective, peptide inhibitor of activating transcription factor 3 (ATF3) with high affinity (Kd=151 nM), increases CCL4 expression levels in human macrophages. |
|
| DC73820 |
SLU-PP-332
Featured
|
SLU-PP-332 is a potent, selective pan ERRα/β/γ agonist with EC50 of 98, 230 and 430 nM for ERRα, ERRβ and ERRγ, in full-length ERR cell-based cotransfection/reporter assays. |
|
| DC73825 |
MG-002
Featured
|
MG-002 is a second-generation, orally bioavailable inhibitor of eIF4A, a key RNA helicase involved in the initiation of cap-dependent mRNA translation. By targeting eIF4A, MG-002 effectively disrupts the translation of certain mRNAs, particularly those with complex 5' untranslated regions (UTRs) that are highly dependent on eIF4A activity. This mechanism of action makes MG-002 a promising candidate for targeting cancers and other diseases driven by dysregulated translation. |
|
| DC73855 |
BPA-B9
Featured
|
BPA-B9 (Bipyridine amide B9) is a small molecule RXRα-targeted anti-mitotic agent, binds to RXRα (Kd=39 nM) and selectively inhibits the p-RXRα/PLK1 interaction to induce mitotic arrest and catastrophe in cancer cells. |
|
| DC73863 |
ODH-08
Featured
|
ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect.
ODH-08 does not activate other nuclear receptors involved in lipid metabolism such as PPARα, PPARγ, PPARδ, and LXRα.
ODH-08 reduces hepatic collagen deposition and expression levels of fibrogenic markers such as α-smooth muscle actin and collagen type I alpha 1 chain in Western diet-fed mice.
ODH-08 suppresses the expression of fibrogenic proteins in hepatic stellate cells (HSCs).
ODH-08 suppresses the activity of SMAD2 and 3, which are the primary downstream proteins of transforming growth factor β. |
|
| DC73866 |
CS27109
Featured
|
CS27109 is a potent, selective thyroid hormone receptor-β (THR-β) agonist with AC50 value of 1.98 uM, 12.6-fold selectivity over THR-α. |
|
| DC73867 |
EN171
Featured
|
EN171 covalently targets both C38 and C96 on 14−3−3 to enhance 14−3−3 interactions with ERα, YAP, and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity. |
|
| DC73881 |
(R)-SKBG-1
Featured
|
(R)-SKBG-1 is a covalent small molecule ligand of RNA-binding protein NONO, engages NONO Cys145 and suppress an array of cancer-relevant genes and impair cancer cell proliferation. |
|
| DC73882 |
(S)-CKi-1
Featured
|
(S)-CKi-1 is a selective, covalent inhibitor of creatine kinases (CKs), inhibits recombinant creatine kinase B (CKB) phosphotransfer activity with IC50 of 0.6 uM, depletes creatine phosphagen energetics in cells. |
|
| DC73890 |
5M-8OH-Q
Featured
|
5M-8OH-Q is a specific small molecule inhibitor of UDP-glucose glycoprotein glucosyltransferase (UGGT), binds a CtUGGTGT24 “WY” conserved surface motif conserved across UGGTs (Kd=47 uM) but not present in other GT24 family glycosyltransferases. |
|
| DC73898 |
AGI-25696
Featured
|
AGI-25696 (AGI 25696) is a potent and selective inhibitor of methionine adenosyltransferase MAT2A, blocks the growth of MTAP-deleted tumors in vivo. |
|
| DC73909 |
ARUK2001607
Featured
|
ARUK2001607 is a potent, selective and brain penetrant PI5P4Kγ inhibitor with binding KD of 7.1 nM, pIC50 of 7.1 (PI5P4Kγ+). |
|
| DC73933 |
C902
Featured
|
C902 is a small-molecule inhibitor targeting LIN28-let-7 interaction, shows dose-dependent inhibition in an EMSA validation assay with IC50 of 5 uM. |
|
| DC73948 |
CMP05
Featured
|
CMP05 (Endosomolytic compound CMP05) is a novel endosomolytic small-molecule compound that exhibits higher transfection efficiency/ability to induce endosomal escape of oligonucleotides (ONs) than current compounds such as chloroquine. |
|
| DC73949 |
CMP05-7
Featured
|
CMP05-7 (Endosomolytic compound CMP05-7) is a novel endosomolytic small-molecule compound that exhibits higher transfection efficiency/ability to induce endosomal escape of oligonucleotides (ONs) than current compounds such as chloroquine. |
|
| DC73953 |
CPAG-1
Featured
|
CPAG-1 (PGRMC2 activator CPAG-1) is a small-molecule activator of PGRMC2.
CPAG-1 treatment had no effect on weight or food intake but treated mice had reduced fasting glycemia and insulin levels.
CPAG-1 decreased Rev-Erbα protein in BAT of CPAG-1-treated mice.
CPAG-1 also significantly increased labile heme in the nucleus of brown adipocytes from CPAG-1-treated mice within 4 days of treatment. |
|
| DC73963 |
DB2313
Featured
|
DB2313 is a small-molecule transcription factor PU.1 inhibitor abrogating DNA binding by PU.1 with Kd of 29 nM. |
|
| DC73980 |
DS55980254
Featured
|
DS55980254 (DS 55980254) is potent, selective and orally active PTDSS1 (phosphatidylserine synthetase 1) inhibitor, suppresses phosphatidylserine (PS) production activity of PTDSS1 (IC50=100 nM) in cell-free assays, but not that of PTDSS2. |
|
| DC73988 |
EP055
Featured
|
EP055 (EP-055) is a small molecule that targets EPPIN on the surface of sperm and inhibits motility (IC50=199.5 uM, CASA assay using human sperm), binds to the C-terminal domain of EPPIN. |
|
| DC74017 |
HTL0041178
Featured
|
HTL0041178 is a potent GPR52 agonist with EC50 of 27.5 nM (human or rat GPR52). |
|
| DC74022 |
IDE-397
Featured
|
IDE-397 (GSK-4362676, GSK-676) is a potent, selective small molecule methionine adenosyltransferase 2a (MAT2A) inhibitor, displays broad anti-tumor activity across a panel of MTAP-deleted patient-derived xenografts. |
|
| DC74047 |
Kakeimide
Featured
|
Kakeimide is a potent GH3 inhibitor that selectively targets IAA-conjugating GH3 proteins at subnanomolar concentrations in vitro, shows auxin-like activity by inhibiting endogenous IAA catabolism. |
|
| DC74064 |
Macrocyclic peptide D4-2
Featured
|
Macrocyclic peptide D4-2 is a macrocyclic peptide consisting of 15 amino acids that binds to the ectodomain of mouse SIRPα (Kd=10 nM, IgV-B6 SIRPα) and efficiently blocks CD47-SIRPα interaction in an allosteric manner (IC50=0.18 uM). |
|
| DC74090 |
NCGC00378430
Featured
|
NCGC00378430 (Compound 8430) is a novel small molecule compound that reduces the SIX1/EYA2 interaction in vitro with IC50 of 52 uM in the Alphascreen assay. |
|
| DC74093 |
NCP26
Featured
|
NCP26 is a potent, ATP-competitive prolyl-tRNA synthetase (ProRS, PRS) inhibitor, inhibits recombinant human ProRS in the presence of 100 μM proline with KD of 0.35 nM in TR-FRET assays. |
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