DC67306 |
1-Propanethiol, 3-(dimethylamino)-, 4-methylbenzenesulfonate (1:1)
Featured
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DC67307 |
1-Piperazineethanamine, N-(phenylmethyl)-
Featured
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DC67308 |
CbzNH-PEG1-Br
Featured
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DC67309 |
H2N(CH2)3N(tert-butoxycarbonyl)(CH2)4NH2
Featured
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DC67310 |
1,4-Piperazinediethylamine
Featured
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DC67311 |
1-Propanaminium, 2,3-dihydroxy-N,N,N-trimethyl-, chloride (1:1), (2R)-
Featured
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DC67312 |
1-Propanethiol, 3-(diMethylaMino)-, hydrochloride
Featured
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DC67313 |
6-Oxohexyl 2-hexyldecanoate
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DC67315 |
Lipid AA15 |
The AA15 lipid, an amino acid-derived ionizable lipid, integrates a carboxylic acid-containing headgroup and biodegradable branched ester tails (R2) to enhance mRNA delivery. Optimized as AA15V LNP, it exhibits a hydrodynamic diameter of 102.3 ± 4.1 nm, low polydispersity (PDI <0.15), and slightly positive zeta potential (+4–6 mV), enabling efficient tumor-targeted delivery. With a pKa ~6.1–6.4, AA15V ensures protonation in acidic endosomes, promoting mRNA release. It achieves >85% mRNA encapsulation efficiency, critical for stable saRNA delivery. In vitro, AA15V LNP-sSE-SCTs induced sustained SE-SCT expression (69% H-2Kb+β2m+ B16F10 cells at 72 h), outperforming mRNA formulations. In vivo, a single intratumoral dose of AA15V LNP-sSE-SCTs suppressed tumor growth by 22-fold in vaccinated mice, synergizing with checkpoint inhibitors (anti-PD-1/CTLA-4) for complete regression in 28.6% of lymphoma models. Ex vivo, AA15V enabled SE-SCT expression in human glioblastoma (7.1% CD45− cells) and lung cancer samples (5.8–8.7%), underscoring clinical potential. Key data: pKa ~6.3; encapsulation: 85–89%; zeta: +4–6 mV; size: 102.3 ± 4.1 nm. |
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DC60799 |
TDI-015051
Featured
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TDI-015051 is a first-in-class non-covalent inhibitor of the viral guanine-N7 methyltransferase (MTase) NSP14 with Kd of 61 pM and IC50 ≤ 0.15 nM, respectively. |
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DC60801 |
VIP36
Featured
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VIP36 is a peripherally restricted cannabinoid receptor type 1 (CB1) agonist with Ki of 22 nM and exerts analgesic efficacy through peripheral CB1 receptors and shows limited analgesic tolerance. |
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DC60802 |
P6CIT
Featured
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P6CIT is a cationic lipid for targeted mRNA delivery to pancreatic ductal adenocarcinoma (PDAC). Pan-tgt (P6CIT) LNP could specifically deliver mRNA to immune cells in PDAC tissues, including dendritic cells (DCs), macrophages, natural killer (NK) cells, and T cells. |
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DC60803 |
BRINP2-related peptide (BRP)
Featured
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BRINP2-related peptide (BRP) is a 12-mer peptide, as a potent anorexigenic peptide. BRP demonstrates significant appetite-suppressing effects in mice and pigs, and triggers FOS activation in the hypothalamus. |
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DC60804 |
Ferfluor-1
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Ferfluor-1 is a novel 1,3,4-thiadiazole-functionalized druglike ferrostatin analogue as a ferroptosis inhibitor and photoluminescent indicator. Ferfluor-1 shows superior anti-ferroptosis potency, favorable BBB permeability and in vivo activity against stroke and Parkinson's disease. |
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DC60805 |
YK-2168
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YK-2168 is a differentiated selective CDK9 inhibitor with IC50 of 5.9 nM, demonstrating 72.5-fold and 45.2-fold selectivity over CDK1 and CDK2, respectively. YK-2168 achieves superior CDK9 selectivity over AZD4573 and comparable selectivity to BAY1251152. |
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DC60806 |
PF-07265028
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PF-07265028 is a selective inhibitor of hematopoietic progenitor kinase 1 (HPK1) with Ki<0.05 nM and represents >280-fold improvement in biochemical potency while maintaining a comparable lipophilicity. |
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DC60807 |
YB-3−17
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YB-3−17 is a novel bifunctional molecule, robustly inhibits mTOR (IC50 of 0.22 nM) and selectively degrades GSPT1 (DC50 of 5 nM). YB-3−17 degrades GSPT1 selectively without affecting GSPT2 or SNUPN. YB-3−17 shows significant off-target inhibition of kinases like FGR, CSF1R, LCK, or LYN, unlike MLN0128. |
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DC60808 |
503O8,12
Featured
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503O8,12 is a branched-tail ionizable lipidoid mRNA delivery with immune cell specificity. In vivo, 503O8,12 demonstrated spleen-tropism (≈50% signal) with significant lung targeting (≈35%) after IV administration. Flow cytometry revealed preferential transfection of lung lymphoid cells (NK/dendritic cells) over endothelial/epithelial cells. It showed no overt toxicity in histology but induced transient pro-inflammatory cytokines. |
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DC65412 |
Acuitas Lipid III-2
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Acuitas Lipid III-2 is an ionizable amine lipid with two identical ester tails adjacent to C6 position relative to amine from patent:WO2017075531A1 with the similar activity as ALC-0315. The head of lipid is propanolamine which can effectively encapsulate mRNA used in gene therapies which depends on the availability of a safe and efficient delivery vehicle. |
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DC67316 |
S-2238 H-D-Phe-Pip-Arg-pNA acetate
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DC67317 |
S-2222 N-benzoyl-ile-glu-gly-arg P-nitroanilide acetate
Featured
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DC67318 |
S-2366 Pyr-Pro-Arg-pNA hydrochloride
Featured
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DC67319 |
S-2403 PyroGlu-Phe-Lys-pNA hydrochloride
Featured
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DC67320 |
S-2732 Suc-lle-Glu (y-Pip) -Gly-Arg-pNA hydrochloride
Featured
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DC60809 |
6Ac1-C12
Featured
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The 6Ac1-C12 LNPs exhibit a pKa of ~6.0, enabling pH-responsive endosomal escape. They demonstrate high stability (maintaining ~100 nm size for 30 days at 4°C) and efficient mRNA encapsulation. With slightly negative surface charge, these nanoparticles show serum resistance. The liver-targeted formulation (4-component) achieves 98% hepatic mRNA expression, primarily in endothelial (60%) and Kupffer cells. The cholesterol-free 3-component lung-targeted version eliminates hepatic accumulation while enabling 71% transfection in pulmonary endothelial cells. Both formulations maintain structural integrity post-dialysis and show low cytotoxicity, with lung-targeted LNPs exhibiting reduced lipoprotein adsorption for enhanced organ specificity. |
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DC60810 |
Lipid head 503 (1,3-Propanediamine, N,N'-bis(2-aminoethyl)-N,N'-dimethyl-)
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DC60815 |
TH35
Featured
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TH35 is a novel class of CRBN-recruiting cGAS-targeting PROTAC degrader with IC50 of 1.8 and 4.8 μM,in THP1-Lucia ISG and RAW-Lucia ISG cells, respectively. TH35 exhibits strong anti-inflammatory effects in the DSS-induced UC mice model. |
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DC60816 |
UNC9426
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UNC9426 is a novel and potent TYRO3 inhibitor with IC50 of 2.1 nM and Ambit selectivity score (S50 (1.0 μM) = 0.026), respectively. UNC9426 shows favorable pharmacokinetic properties in mice. |
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DC67321 |
1,3,5-Tribromoadamantane
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DC60817 |
AM-9747
Featured
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AM-9747 is an MTA-cooperative PRMT5 inhibitor with IC50 of 9.5 nM in the MTAP-del viability assay and shows outstanding 75-fold selectivity over the corresponding isogenic MTAP-WT cellular viability. AM-9747 also shows a significant oral antitumor effect in mouse models employing PDXs. |
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