Compound Libraries

Ingenol-3-angelate shows anticancer activity, and P-gp-mediated absorptive transport, dermal penetration, and vascular damage contribute to the anticancer activity of ingenol-3-angelate in vivo; it activates a broad range of PKC isoforms and induces apoptosis in acute myeloid leukemia cells by activating the PKC isoform PKCdelta. Ingenol-3-angelate suppresses HIV infection of primary CD4+ T cells through down-modulation of cell surface expression of HIV co-receptors. Ingenol-3-angelate emerges as a unique local chemotherapeutic immunostimulatory debulking agent that could be used in conjunction with immunotherapies to promote regression of metastases.

20(R)-Ginsenoside Rg3 has shown multiple pharmacological activities and been considered as one of the most promising approaches for fatigue treatment, however, 20(R)-Ginsenoside Rg3 has a low bioavailability after oral administration in human, so, 20(R)-Rg3 can be by intranasal administration, the mechanism was related to the increase of the storage of hepatic glycogen, and the decrease of the accumulation of metabolite such as lactic acid and serum urea nitrogen.

Panaxadiol , a ginseng saponin with a dammarane skeleton, selectively interferes with the cell cycle in human cancer cell lines, it inhibits DNA synthesis in a dose-dependent manner with IC50 values ranging from 0.8 to 1.2 μM in SK-HEP-1 cells and HeLa cells, it selectively elevates p21WAF1/CIP1 levels and thereby arrests the cell cycle at G1/S phase by down-regulating Cyclin A–Cdk2 activity.

Ginkgetin is a good STAT3 inhibitor , which has anti-inflammatory, neuroprotective, anti-influenza virus and anti-fungal activities. Ginkgetin induces apoptosis in PC-3 cells via activation of caspase 3 and inhibition of survival genes as a potent chemotherapeutic agent for prostate cancer treatment.

Ginsenoside Rb3 has anti-myocardial ischemia-reperfusion injury, neuroprotective, antidepressant-like, and antioxidant effects, it also possesses the potential of the clinical use in preventing and treating diabetes. Ginsenoside Rb3 significantly attenuates the changes of creatine kinase activity and lactate dehydrogenase activity, exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines, it also inhibits the induction of COX-2 and iNOS mRNA.

Ginsenoside Rh3 is a bacterial metabolite of Rg5, which is the main constituent of heat-processed ginseng, has anti-inflammatory effect in microglia by modulating AMPK and its downstream signaling pathways.

Ginsenosides, which are active compounds found in ginseng (Panax ginseng), are used as antidiabetic treatments; ginsenoside Rb2 may inhibit palmitate-induced gluconeogenesis via AMPK-induced SHP by relieving ER stress, a cause of gluconeogenesis.

Ginsenoside-Rg3, possess an ability to inhibit the lung metastasis of tumor cells, and the mechanism of their antimetastatic effect is related to inhibition of the adhesion and invasion of tumor cells, and also to anti-angiogenesis activity.

Ginsenoside Rk1, one of the main elements of Sung Ginseng, has been confirmed as a new endothelial barrier enhancer recently and has anti-cancer activity, the mechanism involves coordination between inhibition of telomerase activity and induction of apoptosis.

Ginsenoside Rc (Rc), a protopanaxadiol type ginsenoside, is the active component mainly responsible for the therapeutic and pharmacologic properties of ginseng, which are derived from its suppression of superoxide-induced free radicals, Rc can modulate Forkhead box O (FoxO1)phosphorylation through activation of PI3K/Akt and inhibition of AMPK and FoxO1 acetylation through interaction with CBP and SIRT1, and that this leads to upregulation of catalase under conditions of oxidative stress.

Isoginkgetin is a MMP-9 inhibitor, also a pre-mRNA splicing inhibitor with IC 50 of 30 uM. Isoginkgetin can up-regulate adiponectin secretion with potency comparable to that of rosiglitazone, a known modulator of adiponectin production. Isoginkgetin has anti-tumor activity, it can inhibit tumor cell invasion by regulating phosphatidylinositol 3-kinase/Akt-dependent matrix metalloproteinase-9 expression.

Ginsenoside (G)-F1 is an enzymatic metabolite generated from G-Rg1, it has been reported to suppress platelet aggregation and to reduce gap junction-mediated intercellular communication, also as a novel anti-skin cancer drug with anti-proliferative and anti-migration features.

Ginsenoside F2 has the anti-cancer activity, it induces apoptosis in breast cancer stem cells (CSCs) by activating the intrinsic apoptotic pathway and mitochondrial dysfunction, also induces the formation of acidic vesicular organelles, recruitment of GFP-LC3-II to autophagosomes, and elevation of Atg-7 levels, suggests that F2 initiates an autophagic progression in breast CSCs.

Ginsenosides, a class of ginseng compounds of herbal medicine, have therapeutic potential for the neuroprotection of brain damage after cerebral ischemia because of their anti-oxidant and anti-inflammation activities, ginsenoside Rb1 could represent promising applications as anti-oxidants for the anti-aging treatment of neurological disorders, such as stroke, in elderly patients.

Ginsenoside Rh1 has antiallergic action , may originate from its cell membrane-stabilizing and anti-inflammatory activities, and can improve the inflammation caused by allergies.

Ginsenoside Rg5 plays a novel role as an IGF-1R agonist, promoting therapeutic angiogenesis and improving hypertension without adverse effects in the vasculature, it can ameliorate lung inflammation possibly by inhibiting the binding of LPS to toll-like receptor (TLR)-4 on macrophages. Ginsenoside Rg5 blocks cell cycle of SK-HEP-1 cells at the Gl/S transition phase by down-regulating cyclin E-dependent kinase activity and that the down-regulation of cyclin E-dependent kinase activity is caused mainly by induced CDK2 inhibitor, p21Cip/WAF1 and decreased levels of cyclin E.

(20R)-Ginsenoside Rh1 exhibits various pharmacological activities including vasorelaxation, antioxidation, anti-inflammation, and anticancer.

Ginsenoside Rg1 is the main pharmacologically active compound of ginsenosides and has demonstrated pharmacological effects in the cardiovascular system, central nervous system and immune system; Rg1 has protective effect against Aβ25-35-induced toxicity in PC12 cells,might be through the insulin-like growth factor-I receptor (IGF-IR) and estrogen receptor (ER)signaling pathways.

Ginsenoside Re, a main phytosterol of Panax ginseng, inhibits Ca(2+) accumulation in mitochondria during cardiac ischemia/reperfusion, which is attributable to nitric oxide (NO)-induced Ca(2+) channel inhibition and K(+) channel activation in cardiac myocytes, acts as a specific agonist for the nongenomic pathway of sex steroid receptors, and NO released from activated eNOS underlies cardiac K(+) channel activation and protection against ischemia-reperfusion injury, G-Re also exerts antiischemic effect and induces angiogenic regeneration.[1,2]

Ginsenoside Rg2 suppresses the hepatic glucose production via AMPK-induced phosphorylation of GSK3β and induction of SHP gene expression, suggests that it has therapeutic potential for type 2 diabetic patients.

Ginsenoside Rh2 is one of the most active components of red ginseng, controlling cancer and other metabolic diseases including osteoclast differentiation; ginsenoside Rh2 can suppress RANKL-induced osteoclast differentiation in vitro and in vivo through the regulation of c-Fos and NFATc1 expressions, not excluding the involvement of NF-κB and ERK, it is also suggested to be developed as a therapeutic drug for prevention and treatment of osteoporosis.

Ginsenoside Rh2 is one of the most active components of red ginseng, controlling cancer and other metabolic diseases including osteoclast differentiation; ginsenoside Rh2 can suppress RANKL-induced osteoclast differentiation in vitro and in vivo through the regulation of c-Fos and NFATc1 expressions, not excluding the involvement of NF-κB and ERK, it is also suggested to be developed as a therapeutic drug for prevention and treatment of osteoporosis.

GinsenosideRf, as an effective natural product, induces G2/Mphase cell cycle arrest and apoptosis in human osteosarcoma MG-63 cells through the mitochondrial pathway, suggests that it may have a therapeutic effect on human osteosarcoma.

<p>A unique collection of 2808 approved drugs for high throughput screening (HTS) and high content screening (HCS);</p>

<p><br><br>None</p>

<p>Diversity: Selected from 1,600,000 drug-like compounds, 10000compounds representing 5000 scaffolds selected from a large drug-like chemical source；</p>

<p>The library offers a solution for establishing a foundation in the early stages of constructing a large screening library due to its large-scale supply and high cost-effectiveness. This foundation supports subsequent drug-like screening and cutting-edge research involving multiple targets and pathways.</p>

<p>A unique collection of 1133 compounds with confirmed anti-SARS-CoV-2 activity or potential activity and part of them are broad-spectrum antiviral agents；</p>

<p>The Diversity Core Library Part2 collects 25920 compounds from 1.3 million in-stock compounds. With drug-like properties remained, the library ensures structural diversity to provide a comprehensive compound selection for customers involved in drug discovery projects, optimizing the input-output ratio for discovering lead compounds.</p>

<p>The unparalleled chemical diversity of natural products makes them an ideal choice for screening active small molecules. Natural products is always a significant source in drug discovery. According to authoritative statistics, 79 out of 99 small molecule anticancer drugs have been successfully developed based on natural products since 1981._x000D_<br>_x000D_<br>Natural products have demonstrated successful modulation of isolated but crucial targets, especially in antimicrobial targets and protein interactions. Many researchers consider natural products and their derivatives as unique tools for studying and manipulating protein function._x000D_<br>_x000D_<br>The Drug-like Natural Compound Library comprises 522 novel molecules, serving as a complement to the L6000 Natural Product Library. This library enhances the probability of successful drug screening, making it an excellent tool for lead compound discovery.</p>

<p>With the rapid development of genome sequencing technology and the exploration of biosynthetic gene clusters, more novel compounds from fungi have been discovered.Fungal libraries with a high degree of biodiversity are important for both academic research and industry.</p>

<p>The Diversity Core Library Part 1 comprises over 50,000 compounds selected from a pool of 1.6 million compounds. This collection emphasizes the diversity of compound structures obtained after filtering out PAINS, REOS and MedChem filters.</p>

<p>The library consists of more than 4,000 members belonging 22 scaffolds (average 180 compounds per scaffold).</p>

<p>For your convenience, there are Diversity Sets of 5,000, 10,000, 15,000, and 20,000 compounds with no structure overlap.</p>