| DC49943 |
Spermine Prodrug-1 |
Spermine Prodrug-1 (Compound 1) is a redox-sensitive spermine prodrug for the potential treatment of snyder robinson syndrome. Spermine Prodrug-1 inhibits wild-type (CMS-24949) and spermine synthase gene (SMS) mutant (CMS-26559, and CMS-6233) fibroblast cells with IC50s of 326.7, 198.5, and 244.1 μM, respectively. |
|
| DC49944 |
XT2 |
XT2 is a potent, orally active, and selective inhibitor of NF-κB-inducing kinase (NIK) with an IC50 of 9.1 nM. XT2 suppresses CCl4-induced upregulation of ALT, a key biomarker of acute liver injury. XT2 also decreases immune cell infiltration into the injured liver tissue. XT2 has the potential for the research of liver inflammatory diseases. |
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| DC49945 |
RBN013209
Featured
|
RBN013209 is a potent CD38 inhibitor and is useful in the treatment of cancer. |
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| DC49946 |
CD38 inhibitor 2 |
CD38 inhibitor 2 is a potent CD38 inhibitor (IC50 = 0.01 ~ 0.1 μΜ). |
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| DC49947 |
Glucosylceramide synthase-IN-2
Featured
|
Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively. |
|
| DC49948 |
Remdesivir de(ethylbutyl 2-aminopropanoate) |
Remdesivir de(ethylbutyl 2-aminopropanoate) is an impurity of Remdesivir. Remdesivir, a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro. |
|
| DC49949 |
TEPC466 |
TEPC466 is a novel TEPP-46-based aggregation-induced emission (AIE) probe. TEPC466 shows a high degree of selectivity and sensitivity for the detection of PKM2 protein via the AIE effect. EPC466 can be used for the detection of PKM2. TEPC466 is successfully applied in imaging the PKM2 protein in colorectal cancer cells with low toxicity. TEPC466 is a useful tool for cancer diagnosis and research. |
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| DC49950 |
Glutathione synthesis-IN-1
Featured
|
Glutathione synthesis-IN-1 (DC-1) is a glutathione synthesis inhibitor. |
|
| DC49951 |
(±)9,10-DiHOME |
(±)9,10-DiHOME is the racemate of 9,10-DiHOME. 9,10-DiHOME is a leukotoxin derivative of linoleic acid diol that has been reported to be toxic in human's tissue preparations, and is produced by inflammatory leukocytes such as neutrophils and macrophages. |
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| DC49952 |
246C10
Featured
|
246C10 is a synthesized ionizable lipid. 246C10 can be formulated into lipid nanoparticles (LNPs) with dioleoylphosphatidylethanolamine (DOPE), cholesterol, and C16-PEG2000 ceramide (PEG-lipid) as well as mRNA. The lipid nanoparticle formulations can be used for mRNA delivery. To obtain iLNPs that could specifically target liver sinusoidal
endothelial cells (LSECs), six different ionizable lipids (241C10
to 246C10) were synthesized by an epoxide ring-opening
reaction with piperazine- or piperidine-containing amines.
Biodistribution and gene regulation of various iLNPs were
assessed in vivo, and the results showed that the 246C10
iLNPs (containing piperazine amine) had the highest luciferase
expression in the liver. When further analyzing the
246C10 iLNPs transfection efficiency in different types of liver
cells, it was found that tdTomato fluorescence was mainly concentrated
in hepatocytes, not in LSECs. Figure 6f shows that 80%
of hepatocytes are fluorescent, 40% of LSECs are fluorescent, and
20% of Kupffer cells are fluorescent. Due to the mannose receptor
on LSECs, mannose-PEG lipid was introduced into 246C10
iLNPs to alter the distribution of iLNPs in different liver cells. As
shown in Figure 6g, tdTomato fluorescence distribution was 15%
of hepatocytes, 70% of LSECs, and 15% of Kupffer cells, significantly
improved the ability of iLNPs to actively target LSECs.
In contrast, this work indirectly shows that the iLNPs with piperazine
head lipid are more able to deliver mRNA to the liver and
translate the target protein than the iLNPs with piperidine
head lipid. It is worth mentioning that the preparation buffer of 246C10
iLNPs could influence the encapsulation efficiency of mRNA.
With the addition of sodium chloride in the citrate buffer, the
encapsulation efficiency of CRISPR-Cas9 mRNA and sgRNA
was increased. These iLNPs were able to treat hemophilia safely,
without causing hepatotoxicity, the immune response induced by
Cas9 and off-target editing. |
|
| DC49953 |
OncoFAP |
OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential. |
|
| DC49954 |
SSAO/VAP-1 inhibitor 1 |
SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3). |
|
| DC49955 |
THRβ Agonist 1 |
THRβ Agonist 1 is a potent and selective agonist of THRβ. Thyroid hormone receptor mediates the physiological activity of thyroid hormones which plays a key role in normal growth and development of the body and in maintaining metabolic balance. THRβ Agonist 1 has the potential for the research of thyroid hormone receptor-related diseases (extracted from patent WO2021104288A1, compound 2). |
|
| DC49956 |
THR-β agonist 3 |
THR-β agonist 3 is a potent agonist of THR-β. THR-β agonist 3 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021129827A1, compound 6). |
|
| DC49957 |
BuChE-IN-1
Featured
|
BuChE-IN-1 (Compound 23) is a potent inhibitor of butyrylcholinesterase (BuChE). Butyrylcholinesterase (BuChE) is recently regarded as a biomarker in progressed Alzheimer’s disease (AD). |
|
| DC49958 |
THR-β agonist 4 |
THR-β agonist 4 is a potent agonist of THR-β. THR-β agonist 4 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021143706A1, compound 72). |
|
| DC49959 |
GRK6-IN-2 |
GRK6-IN-2 (compound 10a) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM. GRK6 is a critical kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-2 has the potential for the research of multiple myeloma. |
|
| DC49962 |
ADAMTS-5-IN-3 |
ADAMTS-5-IN-3 (Example 37-2) is a potent inhibitor of ADAMTS-5 and ADAMTS-4 with IC50s of 8 and 12 nM, respectively. ADAMTS-5-IN-3 can be used for the research of diseases involving degradation of cartilage or disruption of cartilage homeostasis, in particular osteoarthrosis and/or rheumatoid arthritis. |
|
| DC49963 |
Antimalarial agent 8 |
Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria. |
|
| DC49964 |
CSF1R-IN-6 |
CSF1R-IN-6 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-6 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-6 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 5). |
|
| DC49965 |
CHD1Li 6.11
Featured
|
CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties. |
|
| DC49966 |
RECQL5-IN-1 |
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer. |
|
| DC49967 |
(Rac)-RP-6306
Featured
|
Myt1-IN-4 (compound 181) is a potent Myt1 inhibitor with an IC50 of <10 nM. Myt1-IN-4 has anticancer effects. |
|
| DC49969 |
5-C-heptyl-DNJ |
5-heptyl-DNJ is a potent GAA agonist with a Ki of 0.0047 μM. 5-C-heptyl-DNJ increases GAA activities by chaperrone effects. |
|
| DC49970 |
ZYS-1
Featured
|
ZYS-1 has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or treating cancer or tumor-related diseases. |
|
| DC49971 |
SGC agonist 2 |
SGC agonist 2 is a potent agonist of soluble guanylate cyclase (SGC). Soluble guanylate cyclase is a key signal transduction enzyme in the NO-sGC-cGMP signaling pathway. SGC agonist 2 has the potential for the research of cardiovascular disease (heart failure, pulmonary hypertension, angina, myocardial infarction) and fibrotic diseases (renal fibrosis, systemic sclerosis) (extracted from patent WO2021219088A1, compound 031). |
|
| DC49972 |
SSTR4 agonist 3 |
SSTR4 agonist 3 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 3 has the potential for the research of pain (extracted from patent WO2021233427A1, compound 14). |
|
| DC49973 |
SSTR4 agonist 4 |
SSTR4 agonist 4 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 4 has the potential for the research of pain (extracted from patent WO2021233428A1, compound 14). |
|
| DC49974 |
Chalcones A-N-5 |
Chalcones A-N-5 is a trihydroxy chalcone derivative compound. Chalcones A-N-5 doesn’t show cytotoxicity at the concentration lower than 100 µM (with IC50 > 1 mM), but has a significant effect on promoting cell proliferation. Chalcones A-N-5 potentially promotes neuronal cell growth in the damaged brain tissue. Chalcones A-N-5 also inhibits ferroptosis induced by RSL or erastin and reduces the lipid peroxidation levels induced by Aβ1-42 protein aggregation. Chalcones A-N-5 is a promising molecular skeleton candidate for further development of lead compound for in vivo test to research AD. |
|
| DC49975 |
ABAI-30 |
ABAI-30 is a potent and orally active anti-inflammatory agent. ABAI-30 effectively inhibits NO production in lipopolysaccharide (LPS) induced RAW264.7 cells. |
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