Ionizable Lipid Products

AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.

PF-06282999 is a potent and selective myeloperoxidase inhibitor which is potential useful for the treatment of cardiovascular diseases.

LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.

Taladegib (LY2940680) is an antagonist of the smoothened receptor.

BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC50=280 nM).

Ibiglustat (Venglustat) is an inhibitor of glucosylceramide synthase extracted from patent WO 2015089067 A1, compound example 64.

NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding oligomerization domain (NOD)-like receptors, NOD1 and NOD2, with IC50 of 5.74 μM and 6.45 μM, respectively.

Devazepide is a potent, and orally active CCK1 (CCK-A) receptor antagonist that displays appetite-stimulant effects. It blocks the anorectic response to CCK-8 and increases food intake in rats following systemic and i.c.v administration.

TGN-020 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.

TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor.

SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC50 of 7.9 nM.

GI254023X is a potent MMP9 and ADAM10 inhibitor with IC50s of 2.5 and 5.3 nM, respectively.

Bleomycin sulfate is a DNA synthesis inhibitor with potent antitumor activity.

Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.

Deguelin, a naturally occurring rotenoid, is known to be an Akt inhibitor and to have an anti-tumor effect on several cancers; decrease levels of phosphorylated Akt. in vitro: Deguelin in a dose and time dependent manner inhibited the growth of MDA-MB-231, MDA-MB-468, BT-549 and BT-20 cells. Deguelin administration causes a significant HNSCC cell death. Deguelin induces both cell apoptosis and autophagy by modulating multiple signaling pathways in cultured HNSCC cells. Deguelin inhibits Akt signaling, and down-regulates survivin and cyclin-dependent kinase 4 (Cdk4) expressions, by disrupting their association with heat shock protein-90 (Hsp-90). Deguelin induces ceramide production through de novo synthase pathway to promote HNSCC cell death. Importantly, increased ceramide level activates AMP-activated protein kinase (AMPK), which then directly phosphorylates Ulk1 and eventually leads to cell autophagy. Deguelin inhibited the proliferation of MPC-11 cells in a concentration- and time-dependent manner and caused the apoptotic death of MPC-11 cells. Following exposure to deguelin, the phosphorylation of Akt was decreased. The inhibition of cell growth may be associated with decreased levels of phosphorylated Akt. Deguelin-induced apoptosis was characterized by the upregulation of Bax, downregulation of Bcl-2 and activation of caspase-3. in vivo: Deguelin (2 or 4 mg/kg body weight), when injected intraperitoneally, reduced the in vivo tumor growth of MDA-MB-231 cells transplanted subcutaneously in athymic mice. Moreover it was nontoxic as evident from daily observations on mobility, food and water consumption and comparison of bodyweight and other visceral organ weights with those in control animals at the termination of the study. In the colon cancer xenograft model, the volume of the tumor treated withdeguelin was significantly lower than that of the control, and the apoptotic index for deguelin-treated mice was much higher.

KU-60019 is an improved ATM kinase-specific inhibitor with IC50 of 6.3 nM.

Dynasore is a cell-permeable dynamin inhibitor with an IC50 of 15 μM.

UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively. It has > 6-fold selectivity over other HDACs.IC50 value: 0.06 μM (HDAC3), 0.1 μM (HDAC2), 0.5 μM (HDAC1), 1.5 μM(HDAC 8)Target: HDACin vitro: UF010 is a competitive inhibitor with a fast-on/slow-off HDAC-binding mechanism. UF010 induces accumulation of acetylated histones in HCT116 cells in vitro, arrests cells at G1/S transition. It inhibits proliferation of a range of cancer cell lines. UF010 activates tumor suppression mechanisms while inhibiting oncogenic pathways.

Tyrphostin 23 (Tyrphostin A23) is an EGFR inhibitor with an IC50 and Kiof 35 and 11 μM, respectively.