DC67279 |
Rhobo6
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Rhobo6 is a cell-impermeable small-molecule fluorophore designed for labeling the extracellular matrix (ECM) in live tissues. It contains a phenylboronic acid group that binds to diols commonly found in ECM glycans, resulting in a significant increase in fluorescence and a red shift in emission spectra. This property allows Rhobo6 to effectively visualize ECM architecture without perturbing native structures, making it suitable for long-term imaging studies. Additionally, Rhobo6's low affinity for monosaccharides enables reversible binding, which prevents photobleaching and allows for dynamic imaging of ECM components. While Rhobo6 does not specifically target individual ECM components, it provides a holistic view of ECM distribution and is particularly useful for studying ECM-related biological phenomena in samples that are not amenable to genetic manipulation or ex vivo culture. |
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DC60781 |
TRPC6 activator compound 2
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TRPC6 activator compound 2 is selective activator of TRPC6 that does not potentiate TRPC3 and mTRPC7. Comp2 is able to cross BBB. |
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DC60782 |
Lipid A4B4-S3
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A4B4-S3 is a novel biodegradable ionizable lipid that has been meticulously designed through modular platforms and optimized specifically for mRNA delivery. It serves as a critical component of lipid nanoparticles (LNPs) and enhances mRNA delivery efficiency by facilitating endosomal escape. The structural design of A4B4-S3 leverages the Passerini reaction, a highly efficient and modular chemical method that enables the rapid generation of diverse lipid libraries. The design focuses on optimizing the methylene units between lipid headgroups and linkages to strengthen hydrogen bonding interactions with mRNA ribophosphate complexes. This enhanced hydrogen bonding allows for more effective release of mRNA from endosomes, thereby boosting delivery efficiency. Concurrently, the structural optimization improves biodegradability, reducing potential long-term toxicity risks.
In experimental studies, A4B4-S3 has demonstrated superior gene editing efficacy in mouse liver compared to SM-102, a clinically prevalent lipid used in Moderna's COVID-19 vaccine. It also shows potential for repeat-dose protein replacement therapies, suggesting enhanced stability and safety for long-term treatment regimens. Technologically, A4B4-S3 not only provides a more efficient LNP formulation but also deepens the understanding of the relationship between structure and delivery efficiency. This offers new directions for the development of future mRNA therapeutics. In summary, A4B4-S3 represents a next-generation delivery carrier achieved through rational design and high-throughput screening strategies. Its performance enhancements and biodegradable properties position it as a promising candidate for gene therapies and vaccine applications. |
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DC60783 |
LD4172
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LD4172 is a highly potent and specific RIPK1 degrader with Ki of 4.8 nM. LD4172 enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy in female C57BL/6J mice. |
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DC60784 |
IRX5010 (IRX4647F)
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IRX5010 (IRX4647F) is a highly selective RARγ nuclear receptor agonist with EC50 less than 0.1 nM. IRX5010 demonstrates substantial treatment effects on inhibition of growth of murine triple negative breast cancer in vivo. |
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DC60785 |
GS-2278
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GS-2278 is a potent and selective LPAR1 antagonist with EC50 of 12 nM. GS-2278 dose-dependently blocks LPA-induced histamine release and demonstrates efficacy in an interventional model of bleomycin-induced lung fibrosis. |
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DC60786 |
SR-C-107(R)
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SR-C-107(R) is a potent, orally available inhibitor of eleven-nineteen-leukemia YEATS with IC50 of 40 nM.SR-C-107(R) also exhibits superior inhibitory activity against ENL-dependent leukemia in xenografted mice. |
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DC60787 |
UNC10142
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UNC10142 is a first-in-class antagonist of the tandem chromodomains of CHD1 with IC50 of 1.7 μM. UNC10142 treatment results in synthetic lethality in PTEN-deficient prostate cancer cells while sparing PTEN-intact prostate cancer cells. |
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DC60788 |
PT-129
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PT-129 is a potent G3BP1/2 PROTAC degrader and dissolves preformed stress granules (SG). PT-129 disrupts the protective SG environment, making cancer cells more susceptible to stress-induced cell death. |
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DC65387 |
BP Lipid 132(LP01 analog)
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BP Lipid 132 is a well-designed ionizable lipid that combines effective mRNA encapsulation with enhanced biodegradability and tissue clearance, making it a valuable component in LNP-based mRNA delivery systems. |
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DC65390 |
BP Lipid 135
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BP Lipid 135 is a well-designed ionizable lipid optimized for mRNA encapsulation and delivery. Its propanolamine headgroup, ester bonds at the C8 position, and 9-carbon tail contribute to efficient mRNA complexation, stability during delivery, and improved biodegradability. These properties make it a valuable component in LNPs for gene therapy and other mRNA-based therapeutic applications. |
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DC65362 |
BP Lipid 114
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BP Lipid 114 is a well-designed ionizable lipid optimized for mRNA encapsulation and delivery. Its ethanolamine headgroup, ester bonds at the C6 and C8 positions, and 9-carbon tail contribute to efficient mRNA complexation, stability during delivery, and improved biodegradability. These properties make it a valuable component in LNPs for gene therapy and other mRNA-based therapeutic applications. |
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DC60789 |
SM-86 Analog-1
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SM-86 Analog-1 is a novel ionizable lipid designed to improve the delivery of RNA via lipid nanoparticles (LNPs) It is derived from SM-86,with 8 carbon within its hydrophobic tail. |
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DC60790 |
DesMEM AZD4694
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DesMEM AZD4694(AZD4694 Precursor 1)is the precursor of [18F] AZD4694 for the synthesis of [18F] AZD4694, an amyloid-β imaging ligand with high affinity for amyloid-β plaques. |
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DC60791 |
Cholestify Precursor
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Precursor of Cholestify,18F-Cholestify, which binds cytochrome P450 46A1, detected cholesterol breakdown in the mammalian brain. CYP46A1 converts cholesterol to 24-hydroxycholesterol, a form easily eliminated from the brain. |
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DC67281 |
BNT-51
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DC67282 |
Merck Lipid X (L608, Merck-32)
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L-608 is a novel ionizable amino lipid designed for formulating lipid nanoparticles (LNPs) to enable efficient subcutaneous (s.c.) delivery of mRNA therapeutics. Engineered to address inflammation associated with mRNA LNPs, L608 integrates seamlessly with steroid prodrugs, such as budesonide-C16 and budesonide-C18:1, to suppress local and systemic inflammatory responses while prolonging therapeutic protein expression. Preclinical studies demonstrate that L608 LNPs significantly reduce injection-site edema (>80% improvement) and lower systemic inflammatory markers (e.g., haptoglobin), while achieving 2–3× higher plasma AUC for proteins like hFGF21 compared to non-steroid LNPs. |
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DC67284 |
NOTA-NOC
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DC67285 |
DOTA-Octreotide
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DC67286 |
N-Desmethyl Galanthamine
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N-Desmethyl Galanthamine is indeed a metabolite of Galanthamine, a well-known acetylcholinesterase (AChE) inhibitor. Galanthamine is a natural alkaloid originally derived from plants such as Galanthus (snowdrop) and is widely used in the treatment of Alzheimer's disease and other cognitive disorders due to its ability to enhance cholinergic neurotransmission. |
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DC67287 |
3-Methoxy-2',4',6',4-tetrahydroxychalcone
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DC67288 |
Oxypalmatine
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Oxypalmatine is a bioactive alkaloid compound isolated from Phellodendron amurense, a plant commonly known as Amur cork tree. Phellodendron amurense is a traditional medicinal plant widely used in East Asian medicine, particularly in China, Japan, and Korea, for its anti-inflammatory, antimicrobial, and antipyretic properties. Oxypalmatine is one of the many alkaloids found in this plant, contributing to its pharmacological effects. |
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DC67289 |
Hydrangetin
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Hydrangetin is a bioactive compound that has been identified as having antiplatelet aggregation properties, meaning it can help prevent blood clots by inhibiting the clumping together of platelets. This compound can be isolated from Zanthoxylum schinifolium, a plant commonly known as the Sichuan pepper or Korean pepper, which is used in traditional medicine and culinary practices in East Asia. |
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DC60792 |
10-Oxo-12(Z)-octadecenoic acid
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10-oxo-12(Z)-Octadecenoic acid is a metabolite of linoleic acid and an activator of transient receptor potential vanilloid 1 (TRPV1). It is formed from linoleic acid by conjugated linoleic acid dehydrogenase (CLA-DH) via a 10-hydroxy-12(Z)-octadecenoic acid intermediate and can also be produced from linoleic acid by gut microbiota.1 10-oxo-12(Z)-Octadecenoic acid (100 µM) selectively increases calcium levels in HEK293 cells expressing TRPV1 over those expressing TRPV2, TRPV3, TRPV4, and TRP melastatin 8 (TRPM8). It also induces inward currents in HEK293 cells expressing TRPV1, an effect that can be blocked by the TRPV1 antagonist capsazepine (Item No. 10007518). Dietary administration of 10-oxo-12(Z)-octadecenoic acid (0.1% w/w) reduces weight gain and adipose tissue weight and increases the expression of the gene encoding mitochondrial uncoupling protein 1 (Ucp1) in wild-type, but not Trpv1 knockout, mice fed a high-fat diet. It also decreases plasma glucose and triglyceride levels in diabetic KKAy mice fed a high-fat diet. |
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DC60793 |
LUMI6
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The LUMI-6 lipid, autonomously designed via the LUMI-lab platform, is a brominated ionizable lipid optimized for mRNA delivery. Formulated at a molar ratio of 35:28:34.5:2 (LUMI-6:DOTAP:cholesterol:C14-PEG2000), LNPs exhibit uniform physicochemical properties, including a hydrodynamic diameter of ~80 nm, polydispersity index (PDI) <0.2, and robust mRNA encapsulation efficiency. In vitro, LUMI-6 LNPs demonstrated 1.8-fold higher transfection potency in human bronchial epithelial cells compared to its debrominated counterpart (LUMI-6D), with minimal cytotoxicity confirmed by CCK-8 assays. In vivo, pulmonary delivery of CRISPR-Cas9 mRNA via LUMI-6 LNPs achieved 20.3% gene editing efficiency in murine lung epithelial cells, surpassing SM-102 (Moderna’s clinical benchmark) and demonstrating preferential tropism for lung epithelium over endothelial cells—critical for inhaled therapies targeting cystic fibrosis and surfactant disorders. The brominated tail enhances endosomal escape through optimized protonation dynamics, though explicit pKa values remain unmeasured. Synthesized via high-throughput combinatorial chemistry and refined through AI-driven active learning, LUMI-6 combines scalable production with organ-selective delivery, positioning it as a transformative platform for pulmonary nucleic acid therapeutics. |
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DC67293 |
D-Val-Gly-Arg-pNA
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D-Val-Gly-Arg-p-nitroaniline (D-VGR-pNA) is a synthetic chromogenic peptide substrate specifically designed for assessing the enzymatic activity of tissue plasminogen activator (tPA), including its isoforms tPA I and tPA II. Upon cleavage by tPA, the release of p-nitroaniline (pNA) generates a measurable colorimetric signal, enabling precise quantification of amidolytic activity. This substrate is widely utilized in biochemical assays to study tPA’s role in fibrinolysis and to evaluate its enzymatic kinetics in both research and diagnostic applications. |
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DC60794 |
SABA1
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SABA1 is an antibacterial agent effective against Pseudomonas aeruginosa and Escherichia coli. It works by inhibiting biotin carboxylase (BC), an enzyme that catalyzes the first step of the acetyl-CoA carboxylase (ACC) reaction, a process essential for bacterial fatty acid synthesis. What makes SABA1 particularly notable is its atypical inhibition mechanism: it binds to the biotin binding site of BC in the presence of ADP. This unique mode of action distinguishes SABA1 as a promising candidate for the development of new antibiotics, offering a potential solution to the growing challenge of antimicrobial resistance. |
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DC60795 |
Boscalid
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Boscalid is a broad-spectrum fungicide widely used in agriculture to protect crops from fungal diseases. Its bioactivity stems from its ability to inhibit fungal respiration by targeting succinate dehydrogenase (Complex II) in the mitochondrial electron transport chain. By binding to this enzyme, Boscalid blocks electron transfer, disrupting ATP synthesis and energy production in fungal cells, ultimately leading to their death. This mechanism makes Boscalid highly effective against a wide range of fungal pathogens, including Botrytis, Alternaria, Sclerotinia, and powdery mildew species. |
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DC67295 |
Lipid MK16
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MK16 is a specialized lipid designed to traverse the blood-brain barrier (BBB) for effective mRNA delivery. Its formulation, MK16 BLNP, leverages dual mechanisms involving caveolae and γ-secretase to facilitate BBB penetration, ensuring the targeted and efficient transport of functional mRNA to diverse brain cell types. Demonstrating excellent tolerability across a range of dosing regimens, MK16 BLNP represents a promising platform for brain-targeted therapeutic applications. |
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DC60796 |
HIFN
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HIFN (2-fluoro-N-(2-(5-hydroxy-1H-indol-3-yl)ethyl)nicotinamide) is a synthetic small-molecule agonist of the tropomyosin-related kinase B (TrkB) receptor, designed to mimic brain-derived neurotrophic factor (BDNF) signaling. Structurally, HIFN replaces the six-membered lactam ring of its parent compound HIOC with a fluoropyridine moiety, rendering it achiral and configurationally stable. This modification enhances binding affinity and pharmacokinetic properties.
HIFN activates TrkB by inducing receptor dimerization and phosphorylation, triggering downstream survival pathways (PI3K/Akt, MAPK/Erk). In vitro, HIFN outperforms HIOC in TrkB activation (10 nM concentration) in primary neurons and NIH-3T3-TrkB cells. In vivo, systemic administration of HIFN (30–40 mg/kg) mitigates blast-induced retinal ganglion cell (RGC) degeneration and preserves visual function (contrast sensitivity, acuity) in mice for up to 8 weeks post-injury. Its effects are TrkB-dependent, as co-treatment with the TrkB antagonist ANA-12 abolishes neuroprotection.
HIFN exhibits a critical therapeutic window of ≤3 hours post-injury and dose-dependent efficacy, with no toxicity observed at 600 mg/kg (acute) or 40 mg/kg/day (40-day chronic). Safety assessments reveal no histopathological or biochemical abnormalities in vital organs.
By combining potent TrkB activation, blood-retina barrier penetration, and a robust safety profile, HIFN emerges as a promising therapeutic candidate for traumatic optic neuropathy and broader CNS disorders involving TrkB dysregulation. |
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