| DC75930 |
NCA029 |
NCA029 is a potent and selective homo sapiens caseinolytic protease P (HsClpP) activator with an EC50 of 0.15 μM. NCA029 acts on HsClpP to activate an ATF3-dependent integrative stress response, leading to colon cancer cell death. |
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| DC75931 |
PXB17 |
PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC. |
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| DC75932 |
Tagtociclib hydrate |
PF-07104091 hydrate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E1-amplified cancers. |
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| DC75933 |
BIX-01294 hydrochloride hydrate |
BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells. |
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| DC60778 |
TH6342
Featured
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TH6342 is a SAMHD1 inhibitor with IC50 of 9.1 μM/11.0 μM/5.8 μM against dGTP/Cl-F-ara-ATP/ara-CTP, respectively. TH6342 engages pre-tetrameric SAMHD1 and deter oligomerization and allosteric activation without occupying nucleotide-binding pockets. |
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| DC60779 |
TH7127
Featured
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TH7127 is a SAMHD1 inhibitor with IC50 of 4.9 μM/4.5 μM/4.0 μM against dGTP/Cl-F-ara-ATP/ara-CTP, respectively. |
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| DC60780 |
TH7126
Featured
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TH7126 is an inactive control of TH6342. TH7126 does not disrupt SAMHD1 dimerization. |
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| DC67275 |
VU0364739
Featured
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VU0364739 is a selective inhibitor of phospholipase D2 (PLD2) with an IC50 value of 22 nM. Phospholipase D (PLD) enzymes, including PLD1 and PLD2, are involved in various cellular processes, such as signal transduction, membrane trafficking, and cytoskeletal reorganization. PLD2, in particular, has been implicated in cancer cell proliferation, survival, and metastasis, making it a potential target for anticancer therapies. |
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| DC153158 |
ND-O1 (SM-86 Analog-2)
Featured
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ND-O1 (SM-86 Analog-2) is a novel ionizable lipid designed to improve the delivery of siRNA via lipid nanoparticles (LNPs) for treating liver fibrosis. It is derived from SM-86 (structurally similar to SM-102, used in COVID-19 mRNA vaccines) but incorporates an ether bond within its hydrophobic tail, a first-of-its-kind modification aimed at enhancing delivery efficiency. In Vitro Efficiency: ND-O1 LNPs (LNP-O1) showed significantly higher siRNA transfection efficiency in activated fibroblasts compared to Lipid 5 LNPs (LNP-M). In Vivo Efficacy: In a CCl4-induced liver fibrosis mouse model, LNP-O1/siHSP47 (loaded with HSP47-targeting siRNA) reduced HSP47 expression by ~84%, threefold more effective than LNP-M. This led to a dramatic reduction in collagen deposition and marked improvement in liver fibrosis. Safety: The ether bond modification did not introduce additional toxicity, maintaining biocompatibility. ND-O1 represents a breakthrough in ionizable lipid design, demonstrating that strategic placement of ether bonds in hydrophobic tails can enhance LNP performance without compromising safety. Its success highlights its potential for clinical translation in RNA-based therapies for liver fibrosis and other hepatic diseases. |
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| DC13591 |
azido-acetal linker(Acid-degradable liker)
Featured
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Azido-acetal linker is stable at physiological pH (7.4) but rapidly hydrolyzes in the acidic environment of endosomes useful as a fragment of lipid synthesis. |
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| DC67279 |
Rhobo6
Featured
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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
Featured
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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
Featured
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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
Featured
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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)
Featured
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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
Featured
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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)
Featured
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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
Featured
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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
Featured
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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)
Featured
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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
Featured
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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
Featured
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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
Featured
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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
Featured
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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
Featured
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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
Featured
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| DC67282 |
Merck Lipid X (L608, Merck-32)
Featured
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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
Featured
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| DC67285 |
DOTA-Octreotide
Featured
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| DC67286 |
N-Desmethyl Galanthamine
Featured
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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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