| DC70008 |
CLinDMA
Featured
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CLinDMA, a cationic lipid known to potentially trigger inflammatory responses, is utilized in the synthesis of LNP201. This liposome-based assembly is specifically designed for the systemic delivery of siRNA. |
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| DC70009 |
Volanesorsen |
Volanesorsen is an antisense oligonucleotide targeting Apolipoprotein C-III (APOC3)
mRNA to treat patients with the familial chylomicronemia syndrome. |
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| DC70010 |
98N12-5
Featured
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98N12-5 is an ionizable cationic lipid. It has been used in combination with other lipids in the generation of lipid nanoparticles (LNPs). LNPs containing 98N12-5 and encapsulating proprotein convertase subtilisin kexin type 9 (PCSK9) siRNA selectively accumulate in the liver and reduce total serum cholesterol levels in mice and rats and serum LDL levels in cynomolgus monkeys. |
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| DC70011 |
PKN1/2-IN-1 |
PKN1/2-IN-1 is a potent, cell penetrant and selective PKN2 (PRK2) inhibitor (IC50=16 nM; Ki=8 nM). |
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| DC70012 |
BSc5367 |
BSc5367 is a potent Nek1 inhibitor with an IC50 of 11.5 nM. NIMA-related protein kinase Nek1 is crucially involved in cell cycle regulation, DNA repair and microtubule regulation and dysfunctions of Nek1 play key roles in amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD) and several types of radiotherapy resistant cancer. |
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| DC70013 |
17β-HSD1-IN-1 |
17β-HSD1-IN-1 (Compound 1) is a highly selective 17β-HSD1 inhibitor with IC50s of 5.6 and 3155 nM for 17β-HSD1 and 17β-HSD2, respectively. 17β-HSD1-IN-1 can be used for the research of non-small cell lung cancer (NSCLC). |
|
| DC70014 |
ChemR23-IN-3 |
ChemR23-IN-3 is a potent thiazole-based ChemR23 inhibitor with an IC80 value of 12 nM. |
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| DC70015 |
TS010 |
TS010 is a potent inhibitor of GLO-I with IC50 of 0.57 μM. TS010 has the potential for the research of cancer disease. |
|
| DC70017 |
Antitumor agent-49 |
Antitumor agent-49 (Compound 10) is a Harmine derivative-furoxan hybrids containing NO donor, with antitumor activities. Antitumor agent-49 shows cytotoxic activity against HepG2 cells with an IC50 of 1.79 µM. Antitumor agent-49 produces high levels of NO in vitro. |
|
| DC70018 |
Antitumor agent-47 |
Antitumor agent-47 (Compound 3e) is a silibinin derivative with an antitumor activity. Antitumor agent-47 shows cytotoxic activity against NCI-H1299 and HT29 cells with IC50 values of 8.07 µM and 6.27 µM, respectively. |
|
| DC70019 |
BOD-NH-NP |
BOD-NH-NP is an activatable fluorescent probe for imaging endogenous nitric oxide via the eNOS enzymatic pathway. |
|
| DC70020 |
AGL-0182-30 |
AGL-0182-30 is a proprietary microtubule disrupting agent. |
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| DC70021 |
Anticancer agent 33 |
Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM. |
|
| DC70022 |
ZL-Pin13 |
ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells. |
|
| DC70023 |
Anti-inflammatory agent 12 |
Anti-inflammatory agent 12 (Compound 2) is a pentacyclic triterpene compound. Anti-inflammatory agent 12 shows a significant bias in the LPS-induced inflammatory response with an IIC50 value of 2.22 μM. Anti-inflammatory agent 12 has the potential for the research of inflammation disease. |
|
| DC70024 |
GRPR antagonist-1 |
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity. |
|
| DC70025 |
GRPR antagonist-2 |
GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity. |
|
| DC70026 |
PHGDH-IN-2 |
PHGDH-IN-2 is a potent and NAD+ competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells. |
|
| DC70073 |
(Ac)Phe-Lys(Alloc)-PABC-PNP |
A cathepsin cleavable ADC peptide linker. |
|
| DC70113 |
13PCSK9i |
13PCSK9i is a highly potent PCSK9-LDLR disruptor peptide with EC50 of 2 nM, SPR Kd of 6.1 nM and 21 nM for hPCSK9 and mPCSK9.13PCSK9i reduces plasma cholesterol levels and increases hepatic LDLR density in a dose-dependent manner.13PCSK9i functions by a unique, allosteric mechanism and is the smallest molecule identified to date with in vivo PCSK9-LDLR disruptor function. |
|
| DC70123 |
MAL-di-EG-Val-Cit-PAB-MMAE |
A drug-linker conjugate for antibody-drug conjugate by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide SuO-Val-Cit-PAB. |
|
| DC70155 |
BRD5631 |
A small-molecule enhancer of autophagy through an mTOR-independent pathway; significantly reduces the number of eGFP-HDQ74-positive cells, and increases the transcript level of p62 in Atg5+/+ MEFs; significantly reduces levels of endogenous p62 and cell death in NPC1 hiPSC-derived neurons; enhances bacterial clearance and suppresses IL-1β Secretion in an autophagy-dependent manner; a valuable tool for studying the role of autophagy in the context of cellular homeostasis and disease. |
|
| DC70199 |
anle145c |
anle145c is a small molecule inhibitor of amyloid aggregation and formation, inhibits human islet amyloid polypeptide (hIAPP)-induced death of INS-1E cells.anle145c has a special mode of action in which anle145c-stabilized oligomers act as a thermodynamic sink for the preferred aggregation state of hIAPP and anle145c.anle145c prevents hIAPP fibril formation in solution, and converts preformed hIAPP fibrils into non-toxic oligomers.anle145c is a promising candidate to inhibit protein aggregation in case of T2DM. |
|
| DC70209 |
AS105
Featured
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AS105 (AS-105) is a highly potent, ATP-competitive CaMKII inhibitor, inhibits CaMKIIδ with IC50 of 8 nM, Ki of 3 nM.
AS105 is also effective against autophosphorylated CaMKII (in contrast to the commonly used allosteric CaMKII-inhibitor KN-93).
In isolated atrial cardiomyocytes from human donors and ventricular myocytes from CaMKIIδC-overexpressing mice with heart failure, AS105 effectively reduced diastolic SR Ca2+ leak by 38% to 65% as measured by Ca2+-sparks or tetracaine-sensitive shift in [Ca2+]i.
AS105 effectively reduced SR Ca2+-leak, thus improving SR Ca2+-accumulation and reducing cellular arrhythmogenic correlates, without negatively influencing excitation-contraction coupling. |
|
| DC70222 |
Autophagy inducer D61 |
Autophagy inducer D61 is a small molecule autophagy inducer with antibacterial activity, induces LC3II and promotes aggregation of LC3II near Salmonella.D61 (25 uM) reduced the bacterial load (GFP signal in RAW 264.7 macrophages) by 20-fold, with IC50 of 1.3 μM in the SAFIRE assay.D61 antibacterial activity depends on the VPS34 complex and on ATG5.D61 also reduced Salmonella load in the spleens and livers of infected mice.D61 antibacterial activity in macrophages is synergistic with the antibiotic chloramphenicol but that this synergy is largely independent of the known autophagy-stimulating activity of chloramphenicol.Salmonella enterica is a natural bacterial pathogen of humans and animals that causes systemic infection or gastroenteritis. |
|
| DC70223 |
Autophazole |
Autophazole is a novel autophagy inhibitor, promotes cancer cell death via caspase activation.Autophazole was internalized into lysosomes of cells where it induced lysosomal membrane permeabilization (LMP), promoted LMP-mediated apoptosis.LMP induced by Autophazole caused release of cathepsins from lysosomes into the cytosol. Cathepsins in the cytosol cleaved Bid to generate tBid, which subsequently activated Bax to induce mitochondrial outer membrane permeabilization (MOMP).Autophazole is a new chemical probe in efforts aimed at gaining a better understanding of the autophagic process. |
|
| DC70224 |
Autoquin |
Autoquin is a novel autophagy inhibitor (IC50=0.56 uM) by indirect modulation of the activity of the lysosomal enzymes acid sphingomyelinase and acid ceramidase;
Autoquin showed a dose‐dependent inhibition of EGFP‐LC3 puncta after 3 hours upon autophagy induction by amino acid starvation in the primary screening assay.
Autoquin is a lysosomotropic compound that acts as a functional inhibitor of acid sphingomyelinase, increases lysosomal mass and sequesters Fe2+ to the lysosomes in MCF7 cells, causing an increase in lysosomal reactive oxygen species. |
|
| DC70251 |
BI-4916 |
BI-4916 (BI-4916) is the prodrug of BI-4924, which is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM. |
|
| DC70252 |
BI-4924
Featured
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BI-4924 (BI 4924) is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.BI-4924 splays high selectivity against the majority of other dehydrogenase targets. |
|
| DC70275 |
BTX306 |
BTX306 (BTX-306) is a novel protein homeostatic modulator, potently reduces levels of GSPT1, eRF1, CK1α, MCL-1, and c-MYC in myeloma cells, overcomes bortezomib and lenalidomide resistance.BTX306 is much more potently reduced human-derived myeloma cell line viability, with median inhibitory concentrations in the single nanomolar range versus micromolar values for lenalidomide or pomalidomide, and more potently activated caspases 3/8/9.BTX306 did not impact viability of murine hematopoietic cells in an in vivo model, demonstrating its specificity for human cereblon.BTX306 did show some reduced activity in lenalidomide-resistant cell line models but nonetheless retained its nanomolar potency in vitro, overcame bortezomib resistance, and was equipotent against otherwise isogenic cell line models with either wild-type or knockout TP53.BTX306 demonstrated strong activity against primary CD138-positive plasma cells, showed enhanced anti-proliferative activity in combination with bortezomib and dexamethasone.BTX306 was effective in an in vivo systemic model of multiple myeloma. |
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