| DC72158 |
UCB7362
Featured
|
UCB7362 is an orally active and potent antimalarial plasmepsin X (PMX) inhibitor, with an IC50 of 7 nM. UCB7362 inhibits parasite growth. |
|
| DC72169 |
RP-6685
Featured
|
RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model. |
|
| DC72179 |
UNC1021
Featured
|
UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM. |
|
| DC72210 |
NDI-034858(Zasocitinib)
Featured
|
NDI034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM. |
|
| DC72237 |
BI-0474
Featured
|
BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models. |
|
| DC72265 |
GDC-2394
Featured
|
GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation. |
|
| DC72269 |
Tri-GalNAc(OAc)3 TFA
Featured
|
Tri-GalNAc(OAc)3 TFA is a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera. |
|
| DC82001 |
4A3-SC8
Featured
|
4A3-SC8 is a novel Ionizable amino lipid for RNA delivery.The CRISPR-Cas9 gene editing system has been a hotspot in the
field of gene therapy, especially the gene correction induced by
homology-directed repair (HDR). However, its application has
various obstacles, such as large molecular weight, poor stability,
off-target risk, and the complexity of codeliver multiple genes.
Farbiak et al. established a novel ionizable lipid library consisting
of four distinct amine cores (3A3, 3A5, 4A1, 4A3) and nine
peripheries with different alkyl chain lengths (SC5-SC14), and screened out a class of iLNPs with ability of encapsulating
Cas9 mRNA, sgRNA and donor DNA simultaneously.
The delivery efficiency (quantified by luciferase mRNA expression)
and iLNPs toxicity were evaluated with three different cell
lines (HEK293T, HeLa, and IGROV-1), indicating the formulation
containing 4A3-SC8 was the best. 4A3-SC8 iLNPs successfully
induced HDR in HEK293 cells by one-pot delivery of Cas9
mRNA, sgRNA, and the correct ssDNA template. Confocal
microscopy imaging showed that a portion of blue fluorescence
in cells was corrected to green fluorescence. Furthermore, the
nucleic acid ratios of Cas9: sgRNA: donor DNA loading in
iLNPs at a ratio of 2:1:3 could maximize the HDR efficiency with
the editing efficiency up to 23%, which breaks through the current
bottleneck of HDR efficiency of only 1–5%. This progress is
undoubtedly an important advance in the gene therapy field to
cure diseases caused by genetic mutations. |
|
| DC60315 |
BAY-4931
Featured
|
BAY-4931 is a potent covalent PPARγ inverse-agonist with IC50 of 0.17 nM and could be a novel tool for probing the in vitro biology of PPARγ inverse-agonism. |
|
| DC60316 |
Benzamide, 2-bromo-N-[2-(4-ethylphenyl)-5-benzoxazolyl]-5-nitro-
Featured
|
BAY-0069 is a potent covalent PPARγ inverse-agonist with IC50 of 0.22 nM and could be a novel tool for probing the in vitro biology of PPARγ inverse-agonism. |
|
| DC60318 |
BAY-069
Featured
|
BAY-069 is a potent dual BCAT1/BCAT2 inhibitor with IC50 of 31 nM/153 nM. BAY-069 displays high cellular activity in U-87 MG and MDA-MB-231 cell lines. |
|
| DC81060 |
ATX-001
Featured
|
ATX-001 is a novel ionizable cationic lipid compound for RNA delivery. |
|
| DC82003 |
A12-Iso5-2DC18
Featured
|
A12-Iso5-2DC18 is a novel amine containing lipid can be used for mRNA delivery, activate the stimulator of interferon genes (STING) pathway, and exhibit anti-tumor immunity. |
|
| DC60311 |
Adaptaquin
Featured
|
Adaptaquin is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PHD2), with an IC50 of 2 μM. Adaptaquin can inhibit lipid peroxidation and maintain mitochondrial function[1][2]. |
|
| DC60317 |
(E/Z)-ZINC09659342
Featured
|
(E/Z)-ZINC09659342 is an inhibitor of Lbc-RhoA interaction[1]. |
|
| DC60319 |
sigma-1 Receptor antagonist 1
Featured
|
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain[1]. |
|
| DC60320 |
sigma-1 Receptor antagonist 2
Featured
|
Sigma-1 receptor antagonist 2 is a potent and selective sigma 1 receptor (σ1 R) antagonist with Kis of 3.88 and 1288 nM for σ1 and σ2 receptor, respectively[1]. |
|
| DC60321 |
WAY-352753 (GSK3-IN-1)
Featured
|
GSK3-IN-1 (compound 11) is a GSK-3 inhibitor with an IC50 value of 12 μM. GSK3-IN-1 can be used in the research of diabetes[1]. |
|
| DC60322 |
CYM 50358 hydrochloride
Featured
|
|
|
| DC82030 |
MYF-03-176
Featured
|
MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration[1]. |
|
| DC60323 |
Dopamine D2 receptor agonist-2
Featured
|
Dopamine D2 receptor agonist-2 (compound 36) is a potent dopamine D2 receptor biased agonism ligand with an Ki value of 11.2 nM. Dopamine D2 receptor agonist-2 can be used to research antipsychosis[1]. |
|
| DC60324 |
WAY-622024
Featured
|
WAY-622024(Compound 5j) is a GPCR GPR109b (HM74) agonist, with a pEC50 value of 6.51. GPCR agonist-2 can be used for research of lipid disorders. |
|
| DC60325 |
Olvanil
Featured
|
Olvanil (NE-19550)is an agonist of transient receptor potential vanilloid type 1 (TRPV1) channels with an EC50 of 0.7 nM.Analgesic[1]. |
|
| DC60326 |
PQM130
Featured
|
PQM130, a Feruloyl-Donepezil Hybrid compound with brain penatration, is a multitarget drug candidate against the neurotoxicity induced by Aβ1-42 oligomer (AβO) and shows anti-inflammatory activity. PQM130 acts as a neuroprotective compound for anti-AD drug development[1]. |
|
| DC60327 |
BPTF-IN-BZ1
Featured
|
|
|
| DC60328 |
PKR-IN-C51
Featured
|
PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM. PKR-IN-C51 inhibits intracellular PKR activation in a dose-dependent manner in primary mouse macrophages[1]. |
|
| DC60329 |
c-Fms-IN-13
Featured
|
c-Fms-IN-13 (compound 14) is a potent FMS kinase inhibitor with an IC50 value of 17 nM. c-Fms-IN-13 can be used as an anti-inflammatory agent[1]. |
|
| DC60330 |
RLX-33
Featured
|
RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome[1]. |
|
| DC60331 |
ISR-IN-1
Featured
|
ISR-IN-1 (Compound 48) is an inhibitor of the integrated stress response. |
|
| DC60332 |
ISRIB-A15
Featured
|
ISR-IN-2 (Compound 47) is an inhibitor of the integrated stress response . |
|
