Ionizable Lipid Products

Necrostatin-1 is a potent, selective and cell-permeable necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. It acts by inhibiting the death domain kinase RIP (RIP1) in the necroptosis pathway.

NSC260594 (NSC 260594) is a specific inhibitor of HIV-1 RNA packaging, which involves preventing the interaction of Gag with SL3 by stabilizing this small RNA stem-loop which then leads to stabilization of the global packaging signal region (psi or ψ); specifically blocks HIV-1 RNA encapsidation, binds to HIV-1 gRNA and exhibits potent antiviral activity; NSC260594 also is a small molecule inhibitor of the Escherichia coli condensin MukBEF, affects MukB directly.

Solithromycin is a novel fluoroketolide with improved antimicrobial effectiveness.Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis. The mean 50% inhibitory concentrations (IC50s) for Solithromycin inhibition of cell viability, protein synthesis, and growth rate were 7.5, 40, and 125 ng/ml for Streptococcus pneumoniae,Staphylococcus aureus, and Haemophilus influenzae, respectively.

Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.

SCH772984 potently inhibits ERK1 and ERK2 activity with IC50s of 4 and 1 nM, respectively.

GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.

ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.

PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].

Diphenylterazine is a bioluminescence agent.

Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.

GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.

Benitrobenrazide is a novel selective hexokinase 2 (HK2) inhibitor, blocking cancer cells growth by targeting glycolysis.

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.

ML382 is a potent, selective, positive allosteric modulator of Mas-related G protein-coupled receptor X1 (MrgprX1) with EC50 of 190 nM in cell based Ca2+ imaging assay; displays >100-fold selectivity versus MrgX2; enhances the ability of BAM8-22 to inhibit high-voltage-activated Ca2+ channels and attenuates spinal nociceptive transmission; effectively attenuated evoked, persistent, and spontaneous pain without causing obvious side effects; attenuates both evoked pain hypersensitivity and spontaneous pain in MrgprX1 mice; an invaluable research tool to study the role of MrgprX1 in chronic pain.

BUN79398(MRGPRX1 agonist 1) is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1), with an EC50 of 50 nM, and is inactive on MRGPRC11. Analgesic effect[1].

In Vitro Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 of 5.9±0.3 μM for PAD4 and Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1.min-1 for PAD4). Cl-amidine induces apoptosis (identified as annexin V-positive/propidium iodide-negative cells) in such cells in a dose-dependent manner, indicating that Cl-amidine induces apoptosis of WBCs in vitro. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine. In Vivo Significantly higher levels of colon inflammation in the 2% DSS than the 2% DSS+Cl-amidine mice are showed. The mean histology scores are 24.2±1.7 (SE) and 13.9±1.6, respectively. Most of the damage in the DSS-only group is in the distal colon, and this damage is suppressed with DSS+Cl-amidine. For the DSS-treated group, the mean colon length is 7.2±0.2 cm. In contrast, the average colon length of the DSS+Cl-amidine group is 8.4±0.2 cm, which is comparable to the mean colon lengths obtained for the wateralone and water+Cl-amidine groups (8.4±0.3 and 7.9±0.2 cm, respectively). The total distance and average speed of mice over a 96-h period are also measured. The results of these analyses demonstrate that the total distance is 5,072±381 and 3,190±401 m for the water-treated and DSS+Cl-amidine mice, but only 800±163 m for the DSS-only group. Similarly, the average speed on the wheel over the 4-day period is 6.2±0.63 and 5.3±0.58 m/min for the water-treated and DSS+Cl-amidine groups, but only 1.8±0.51 m/min for the DSS group.

A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation[1].

BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.

ZB716 is a steroidal, orally bioavailable SERD (selective estrogen receptor downregulator) that binds to ER with high affinity and exerts its antiestrogenic effect on ER-expressing breast cancer cells.