| DC49945 |
RBN013209
Featured
|
RBN013209 is a potent CD38 inhibitor and is useful in the treatment of cancer. |
|
| 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. |
|
| DC49950 |
Glutathione synthesis-IN-1
Featured
|
Glutathione synthesis-IN-1 (DC-1) is a glutathione synthesis inhibitor. |
|
| 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. |
|
| 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). |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC49987 |
5β-Cholanic acid
Featured
|
5β-Cholanic acid can be used for 5β-Cholanic acid derivatives synthesis. |
|
| DC49991 |
1,2-Dilauroyl-sn-glycerol
Featured
|
1,2-Dilauroyl-sn-glycerol is a saturated diacylglycerol and may play a role in second messenger signal transduction. |
|
| DC49996 |
Coelenteramine 400a
Featured
|
Coelenteramine 400a (Bisdeoxycoelenterazine), a derivative of Coelenterazine, is a Renilla luciferase (RLuc) substrate. In the presence of Coelenteramine 400a, RLuc can emit blue light at 395 nm. |
|
| DC50003 |
MIF-IN-1
Featured
|
MIF-IN-1 (compound 14) is a potent macrophage migration inhibitory factor (MIF) inhibitor (pIC50=6.87). |
|
| DC50009 |
Anisole-piperazine-methanone-benzothiazole-p-methylpiperidine
Featured
|
Anisole-piperazine-methanone-benzothiazole-p-methylpiperidine is an active compound. |
|
| DC50044 |
Edotreotide
Featured
|
Edotreotide is a synthetic somatostatin analogue that is used in nuclear medicine for the diagnosis and research of certain types of cancers, particularly neuroendocrine tumors (NETs). Somatostatin is a peptide hormone that inhibits the release of several other hormones, and many neuroendocrine tumors overexpress somatostatin receptors (SSTRs), making them ideal targets for somatostatin analogues like edotreotide. |
|
| DC50087 |
1,2-Dimyristoyl-sn-glycerol
Featured
|
1,2-Dimyristoyl-sn-glycerol is a saturated diacylglycerol and a weak second messenger for the activation of PKC. |
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|
| DC50088 |
H-7 inhibitor
Featured
|
H-7 is a specific protein kinase C inhibitor, which inhibits superoxide release from human neutrophils (PMN) stimulated with phorbol myristate acetate or synthetic diacylglycerol. |
|
| DC50121 |
GTPL-6019
Featured
|
GTPL6019, also know nas IUN54940, DGFR Tyrosine Kinase Inhibitor III, is a PDGFR inhibitor with potential anticancer activity. |
|
| DC50166 |
Bim-IN-1
Featured
|
Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity. |
|
| DC50173 |
dCeMM4
Featured
|
dCeMM4 (Compound 5) is a glue degrader. dCeMM4 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex. |
|
| DC50184 |
dCeMM3
Featured
|
dCeMM3 (Compound 3) is a glue degrader. dCeMM3 induces ubiquitination and degradation of cyclin K by prompting an interaction of CDK12-cyclin K with a CRL4B ligase complex. |
|
| DC50186 |
5,6-Dichlorobenzimidazole riboside(DBR)
Featured
|
5,6-Dichlorobenzimidazole riboside is a nucleoside analog that inhibits several carboxyl-terminal domain (CTD) kinases including casein kinase II and CDKs. 5,6-Dichlorobenzimidazole riboside trigger p53-dependent apoptosis of human colon adenocarcinoma cells without inducing genotoxic stress to healthy cells. |
|
| DC50205 |
Abiraterone decanoate
Featured
|
Abiraterone decanoate is a potent Abiraterone prodrug. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery. |
|
| DC50245 |
CFT7455
Featured
|
CFT7455 is an orally active zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3) degrader. Cemsidomide is an anti-cancer agent that binds with high affinity to the cereblon E3 ligase (Kd of 0.9 nM) (WO2022032132A1; Compound 1). |
|
| DC50265 |
GDC-1971
Featured
|
GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.
|
|
| DC50275 |
RET-IN-14
Featured
|
RET-IN-14 (compound 49) is a potent RET inhibitor with IC50s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research |
|
| DC50317 |
γ-AA peptide P6 (Cyclic γ-AA Peptide 6)
Featured
|
γ-AA peptide P6 (Cyclic γ-AA P6) is a potent activator of E6 associated protein (E6AP). γ-AA peptide P6 can stimulate the self-ubiquitination of E6AP and E6AP-catalyzed substrate ubiquitination in reconstituted reactions in vitro. γ-AA peptide P6 can also enhance the ubiquitination of E6AP substrates in the cell and accelerate their degradation by the proteasome. |
|
| DC50001 |
UCB-9260
Featured
|
UCB-9260, an orally active compound, inhibits TNF signalling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar Kd of 13 nM. |
|
| DC50002 |
EDP-305
Featured
|
EDP-305 is a novel and potent farnesoid X receptor (FXR) agonist, with no/minimal cross-reactivity to TGR5 or other nuclear receptors. |
|
| DC50004 |
Periplocin
Featured
|
Periplocin is a cardiotonic steroid isolated from Periploca forrestii. Periplocin promotes tumor cell apoptosis and inhibits tumor growth. Periplocin has the potential to facilitate wound healing through the activation of Src/ERK and PI3K/Akt pathways mediated by Na/K-ATPase. |
|
| DC50006 |
Cinobufagin (Cinobufagine)
Featured
|
Cinobufagin, a kind of Chinese materia medica with antitumor effect, is widely used in clinical practice, especially in anti-liver cancer. IC50 value: Target: In vitro: Cinobufagin inhibited proliferation of cancer cells at doses of 0.1, 1, or 10 μM after 2–4 days of culture. Cytotoxicity of cinobufagin on the DU145 and LNCaP cells was dose-dependent. Cinobufagin increased [Ca2+]i and apoptosis in cancer cells after a 24-hr culture as well as caspase 3 activities in DU145 and PC3 cells and caspase 9 activities in LNCaP cells [1]. Cinobufagin suppresses cell proliferation and causees apoptosis in prostate cancer cells via a sequence of apoptotic modulators, including Bax, cytochrome c and caspases [2]. |
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