Novel Nef Protein Inhibitor; Anti-HIV

Novel blocker of AKT1-FAK interaction, reducing the stimulation of FAK phosphorylation in response to extracellular pressure in human SW620 colon cancer cells without affecting basal FAK phosphorylation

Novel Zika virus RNA polymerase inhibitor

Novel CtpF inhibitor, inhibiting Ca -dependent ATPase activity in Mtb membrane vesicles

Novel gp120 of HIV-1 Antagonist

Novel potent and specific inhibitor of the UNC119-Src interaction, binding to UNC119 in cells, and inducing redistribution of Src to endomembranes and reduction of activating Src autophosphorylation on Y419

Novel ASCT2 inhibitor

Cell-permeable fluorometric zinc sensor

Non-competitive AMPA receptor antagonist

Type III progesterone receptor antagonist with enhanced antiproliferative properties

Novel oral multitarget tumour growth inhibitor

Novel potent inhibitor of factor Xa (FXa)

Novel dual mordulator of nNOS-PSD-95 interaction and GABA A receptor

Novel potent and selective BRD4 bromodomain 1 (BD1) inhibitor

Novel potent and selective BRD4 bromodomain 1 (BD1) inhibitor

Novel β-catenin/B-cell lymphoma 9 (BCL9) inhibitor, disrupting the β-catenin/BCL9 protein-protein interaction (PPI) with a Ki of 0.96 μM and without affecting the β-catenin/E-cadherin interaction in living cells, displaying good selectivity for β-catenin/

Novel potent and highly selective inhibitor of wild-type and mutant versions of EZH2

ATP-sensitive potassium channel-blocker; Eukalemic diuretic

Non-steroidal pure antioestrogen

5-Lipoxygenase (5-LO) inhibitor

K-Channel opener (PCO) activating predominantly KATP channels in vitro to relax bladder detrusors

Selective nonpeptide, NK-2 receptor (NK-2R) antagonist

Potassium channel opener

Potent, selective inhibitor of Janus tyrosine kinase 3 (JAK3)

Novel antidiabetic agent for the treatment of type 2 diabetes mellitus (DM)

Inducer of functional angiogenesis through increased H 2 S availability

Potent, selective, and brain penetrating H2 receptor antagonist

Inhibitor of osteoclastogenesis and macrophage recruitment, decreasing bone turnover and stabilizing the bone matrix, exhibiting diverse anti-tumor effects in osteosarcoma

Gastroprotective agent for the treatment of peptic ulcer

Novel zinc sensor with a chloroalkane linker, reacting specifically with the engineered protein HaloTag, binding zinc ions with a threefold fluorescence enhancement

The first potent and selective Mycobacterium tuberculosis Zmp1 inhibitor

Novel potentiator of KCNQ2 potassium channels

Novel COX-2 inhibitor

Antagonist of D1 and D2 dopamine receptors.

Potent, cell-permeable and irreversible caspase-1/5 inhibitor

Natural antibiotic, having diverse biological activities including broad-spectrum antibiosis against Bacteria and lower Eukarya, plant disease suppression, and enhancement of the insecticidal activity of Bacillus thuringiensis toxin against lepidopteran l

Novel multi-target inhibitor, harboring selectivity of inhibiting EGFR T790M sparing wild-type EGFR

Novel Selective Degrader of GSPT1

Novel inhibitor of Cyclophilin J (CyPJ) PPIase, demonstrating remarkable inhibition of tumor cell growth, comparable to CsA but much stronger than 5-fluorouracil

Novel inhibitor of Cyclophilin J (CyPJ) PPIase, demonstrating remarkable inhibition of tumor cell growth, comparable to CsA but much stronger than 5-fluorouracil

Cyclooxygenase-1 inhibitor

Novel next generation orally active DPP-4 inhibitor to treat Type 2 Diabetes

Novel histone deacetylase inhibitor (HDACi) with potent oral antitumor activities

Novel histone deacetylase inhibitor (HDACi) with potent oral antitumor activities

Oral active histone deacetylase inhibitor with potent antitumor activity

Novel slow H2S-NO-releasing hybrid, attenuating cardiac dysfunction after heart failure

Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.

VU0364739 is a selective PLD2 inhibitor (IC50: 22 nM). VU0364739 decreases cancer cell proliferation.

RMC-6236 (Compound A122) is a potent RAS(ON)MULTI inhibitor and can be used for the research of cancer.

DPPE is a derivative of phosphatidylethanolamine with (16:0) palmitoyl acyl chains

DMPE is derivative of phosphatidylethanolamine with (14:0) myristic acid acyl chains.

mPEG-DMG, MW 5,000 is a large PEG lipid containing a DMG group and a methoxy cap. The methoxy cap is inert while the DMG group is a popular ligand for developing PEG-lipids and lipid nanoparticles more broadly. Varying the size of a PEG linker greatly impacts its molecular dynamics, thereby affecting DMPK and ADME properties of a given API.

1-Palmitoyl-sn-glycero-3-phosphocholine is an abundant gonadal LPC (lysophosphatidylcholine).

1-Stearoyl-sn-glycero-3-phosphocholine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

1-Palmitoyl-2-oleoyl-sn-glycero-3-PC (POPC), a phospholipid, is a major component of biological membranes. 1-Palmitoyl-2-oleoyl-sn-glycero-3-PC is used for the preparation of liposomes and studying the properties of lipid bilayers.

DMPG is a phospholipid containing the saturated long-chain (14:0) myristic acid.

DSPA is a form of phosphatidic acid (PA) containing a phosphatidic acid head group and 18:0 fatty acids

DOPG-Na is a phospholipid containing the long-chain (18:1) fatty acid oleic acid inserted at the sn-1 and sn-2 positions. It can be used in the generation of micelles, liposomes, and other artificial membranes. DOPG is an anionic phospholipid derivative. The negatively charged liposomes prepared with DOPG has been found to possess the best loading capacity and encapsulation rate for Peptide Nucleic Acid (PNA) oligomers.

DPhPC is a phospholipid used to synthesize bilayer vesicles. DPhPC bilayers do not permit ions to leak in the absence of a pore/ion channel, which can be used for studies on channel proteins.

DPPA is a form of phosphatidic acid (PA).

2-Oleoyl-1-stearoyl-sn-glycero-3-phosphocholine (1-Stearoyl-2-oleoyl-sn-glycero-3-PC) is an active compound. 2-Oleoyl-1-stearoyl-sn-glycero-3-phosphocholine can be used for various biochemical studies.

18:0-18:2 PE is a lipid for agents delivering. 18:0-18:2 PE is mainly composed of unsaturated fatty acids. 18:0-18:2 is considered important precursors of important odorants (IOs) in Eriocheir sinensis.

1-Stearoyl-2-linoleoyl-sn-glycero-3-phospho-L-serine sodium is a glycerophospholipid.

DIM1 is a sugar-alcohol-derived ionizable lipid with mannitol as the precursor. DIM1T is an optimal LNP formulation for potent mRNA delivery in adipose stem cells (ASCs). Importantly, DIM1T LNPs demonstrated considerably higher mRNA delivery efficiency than MC3, ALC-0315, and SM102. The DIM1T LNP-SEC engineered ASCs (DS-ASCs) prolong expression of hepatocyte growth factor (HGF) and C-X-C motif chemokine ligand 12 (CXCL12), which show superior wound healing efficacy over their wild-type and DIM1T LNP-mRNA counterparts in the diabetic cutaneous wound model.

CBI1 (covalent BAX inhibitor 1) is a compound that selectively derivatizes BAX at C126 with BME50 value of 905 μM. CBI1 inhibits BAX activation by triggering ligands or point mutagenesis.

POPE is a phospholipid, and can be used for drug delivery.

L-Dilinoleoyllecithin is a phosphatidylcholine (PC or GPCho). It is a glycerophospholipid in which a phosphorylcholine moiety occupies a glycerol substitution site. As is the case with diacylglycerols, glycerophosphocholines can have many different combinations of fatty acids of varying lengths and saturation attached at the C-1 and C-2 positions. Fatty acids containing 16, 18 and 20 carbons are the most common. PC(18:2(9Z,12Z)/18:2(9Z,12Z)), in particular, consists of two chains of linoleic acid at the C-1 and C-2 positions. The linoleic acid moieties are derived from seed oils. Phospholipids, are ubiquitous in nature and are key components of the lipid bilayer of cells, as well as being involved in metabolism and signaling.While most phospholipids have a saturated fatty acid on C-1 and an unsaturated fatty acid on C-2 of the glycerol backbone, the fatty acid distribution at the C-1 and C-2 positions of glycerol within phospholipids is continually in flux, owing to phospholipid degradation and the continuous phospholipid remodeling that occurs while these molecules are in membranes. PCs can be synthesized via three different routes. In one route, choline is activated first by phosphorylation and then by coupling to CDP prior to attachment to phosphatidic acid. PCs can also synthesized by the addition of choline to CDP-activated 1,2-diacylglycerol. A third route to PC synthesis involves the conversion of either PS or PE to PC.

DOTAP mesylate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

Trilinolein is an endogenous metabolite.

14:0 PEG2000 PE (DMPE-PEG2000) is a PEG-phospholipid conjugate to prepare nanostructured lipid carrier.

1-Stearoyl-2-myristoyl-sn-glycero-3-PC (1S-2M-PC) belongs to the class of asymmetric phospholipids. 1-Stearoyl-2-myristoyl-sn-glycero-3-PC is abundant in biological membranes.

rac-1,2-Distearoyl-3-chloropropanediol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

1,2-Distearoyl-sn-glycerol (DSG; 1,2-Dioctadecanoyl-sn-glycerol) acts as an internal standard for Separation and identification of molecular species of 1,2-diacyl-sn-glycerol (DAG).

1,2-Dipalmitoyl-rac-glycerol is a diacylglycerol containing palmitic acid at the sn-1 and sn-2 positions. It is found in a variety of vegetable oils, including palm, soybean, canola, and corn. 1 \n 1,2-Dipalmitoyl-rac-glycerol MaxSpec Standard is a quantitative grade standard of 1,2-dipalmitoyl-rac-glycerol prepared for mass spectrometry and related applications requiring quantitative reproducibility . The solution has been prepared gravimetrically and contained in argon-sealed deactivated glass ampoules. Concentrations were verified by comparison to independently prepared calibration standards. This 1,2-dipalmitoyl-rac-glycerol MaxSpec Standard is guaranteed to meet specifications for identity, purity, stability, and concentration and is supplied with a batch-specific Certificate of Analysis. Ongoing stability testing is performed to ensure concentrations remain accurate throughout the shelf life of the product. Note: Add more solution to the vial than listed. Therefore, accurate volume measurements are necessary to prepare calibration standards. Follow recommended storage and handling conditions to maintain product quality.

DLPA is a phosphatidic acid (PA) containing the medium-chain (12:0) lauric acid.

DLPE is a derivative of phosphatidylethanolamine with lauric acid (12:0) acyl chains.

DPyPE is a phosphatidylethanolamine lipid composed of polyisoprene alkyl chains. DPyPE is a co-lipid forvaxfectin mixed with GAP-DMORIE in a 1:1 ratio.

1-Oleoyl-2-hydroxy-sn-glycero-3-phosphoethanolamine is the main degradation product of deltamethrin metabolized by the prokaryotic protein (CYP6A14 and CYP6N6) complexes in vitro.

Also known as 1-Stearoyl-2-Oleoyl-sn-glycero-3-PE. It is is a phospholipid that contains stearic acid and oleic acid

mPEG2000-DSPE is used in COVID 19 mRNA vaccines. It is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-PE . Formulations containing DSPE-MPEG(2000) have been used to prepare liposomes with long circulation time for the delivery of anticancer and antimalarial agents.. mPEG2000-DSPE has also been widely used as hydrophilic surface modifying agent for a variety types of hydrophobic nanoparticles, including recently reported lipid nanoparticle mRNA vaccines.

HUN86681, also known as 1-Hexadecyl-2-acetylphosphatidylcholine, is a lipid Platelet activating factor (PAF). PAF is an ether phospholipid known to exhibit potential biological activities in a variety of cellular phenomena such as platelet aggregation, chemotaxis, hypotension, bronchoconstriction, vascular permeability regulation, inflammation, glycogenesis and in regular cellular breakdown of phosphatidylinositol.

1,2-Dipalmitoyl-sn-glycerol is an endogenous metabolite.

DPPG sodium is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

1-Stearoyl-2-linoleoyl-sn-glycero-3-phosphocholine can be chosen as a model used to investigate the volatile compounds from oxidised phosphatidylcholine molecular species. This method is applied to a real food sample, i.e. soy lecithin.

Diheptanoyllecithin is a non-hydrolyzable analog.

DCAF1-BRD9 PROTAC DBr-1 potently degrades BRD9 with a DC50 of 90 nM but only weakly affected BRD7 protein levels. DBr-1 provides an alternative strategy to tackle intrinsic resistance to VHL-degrader.

Compound 38 (NNMT inhibitor) is a potent uncompetitive inhibitors of nicotinamide n-methyltransferase (NNMT). Compound 38 inhibits NNMT in both in vitro biochemical and cell-based assays with IC50 = 42 nM and 38 nM, respectively. Compound 38 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties.

ARV-393 is an orally active PROTAC that utilizes the ubiquitin-proteasome system to target the degradation of BCL6. ARV-393 consists of ligand conjugates targeting BCL6 and the E3 ligase cereblon, respectively. ARV-393 has DC50 and GI50 values of <1 nM in multiple cell lines of diffuse large B-cell lymphoma (DLBCL) and Burkitt lymphoma (BL). ARV-393 also demonstrated considerable tumor suppressor activity in tumor xenograft models. ARV-393 is being studied to inhibit non-Hodgkin lymphoma.

a LRRK2 degrader for the treatment of PD and PSP

a STAT6 degrader for multiple immune-mediated diseases.

a TYK2 degrader for multiple immune-mediated diseases.

an AR degrader for the treatment of mCRPC.

BMS-986365 (CC-94676) is a highly potent and selective AR degrader that induces rapid and deep degradation of both wildtype and mutant forms of the receptor residing in either the cytoplasmic or nuclear compartments of the cell. BMS-986365 (CC-94676) is about 100-fold more potent than enzalutamide (ENZ) at inhibiting androgen-stimulated transcription of AR target genes, and 10 to 120-fold more potent than ENZ at inhibiting AR-dependent proliferation of multiple prostate cancer cell lines in vitro.

an ER degrader for the treatment of BC.

a BTK degrader for the treatment of B-cell malignancies.

a BTK degrader for the treatment of B-cell malignancies.

a mutant and wild-type NTRK degrader for the treatment of solid tumors.

KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).

a MDM2 degrader for the treatment of r/r high grade myeloid malignancies and solid tumors.

a KRASG12D degrader for the treatment of solid tumors.

a BRD9 degrader for treating synovial sarcoma.

a topical AR degrader for the treatment of acne vulgaris.

20-HETE inhibitor-1 (comp 83) is a 20-HETE formation inhibitor

APG-2575 (lisaftoclax) is a dual Bcl-2 and Bcl-xl inhibitor with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.

Compound 4 (VHL-CDO1 glue degrader) is a molecular glue degrader for cysteine dioxygenase 1 (CDO1) by recruiting it into the Von Hippel-Lindau (VHL) E3 ligase complex and leading to its selective degradation.

CMX990 is a novel covalent SARS-CoV-2 3CL protease inhibitor with EC50 of 10 nM, and shows good oral bioavailability and tolerability in preclinical species. Compared with nirmatrelvir, CMX990 has distinctly differentiated potency (~5-fold more potent in primary cells) and human in vitro clearance (>4-fold better microsomal clearance and >10-fold better hepatocyte clearance), with good in vitro-to-in vivo correlation.

Acetylcholine is stored in vesicles in the presynaptic neuron. These fuse with presynaptic membrane upon stimulation by a nerve signal, thus, generating a pulse of neurotransmitter, which diffuses across the membrane. Acetylcholine may either bind reversibly to one of two different types of acetylcholine receptors on the postsynaptic membrane or be destroyed by the acetylcholine-hydrolyzing enzyme, acetylcholinesterase.

Synucleozid-2.0 is a drug-like small molecule that decreases α-Synuclein (SNCA) levels by inhibiting ribosomes from assembling onto SNCA mRNA. Synucleozid-2.0 dose-dependently inhibits SNCA translation with IC50 of ~2 µM.

Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor with an IC50 of 43 nM, being developed for the treatment of several autoimmune disorders.

Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.

IR-820 is a near infrared dye with its excellent fluorescence penetration, good color rendering and better stability. IR-820 is an infrared blood pool contrast agent to detect and quantify diseased tissue in live animals. IR-820 has maximal excitation and emission wavelengths of 710 and 820 nm, respectively. IR-820 emission is significantly improved in vivo on serum binding to albumin, and elimination occurs predominantly via the gastrointestinal tract. Note: this product has ~80% dye.

PKH 26 is a red fluorescent dye, PKH 26 can stably bind to the lipid region of cell membrane and emit red fluorescence (Ex/Em=551/567 nm), which is mainly used for in vitro cell labeling, in vitro cell proliferation studies and in vivo and in vitro cell tracing studies.

5(6)-Carboxyfluorescein (5(6)-FAM) is an amine-reactive pH-sensitive green fluorescent probe. 5(6)-Carboxyfluorescein (5(6)-FAM) can be used to label proteins, peptides and nucleotides. 5(6)-Carboxyfluorescein can be used for the detection of tumour areas in vivo.

DiR is a long-chain carbocyanine dye. Carbocyanine dyes are widely used as Di to label cells, organelles, liposomes, viruses and lipoproteins.

Tetramethyluric acid (1,3,7,9-Tetramethyluric acid; Theacrine), also known as tetramethyluric acid or theophylline, is a purine alkaloid with a structure similar to caffeine. Tetramethyluric acid is a biomaterial or organic compound that can be used as a research-related biomaterial or organic compound in life sciences.

1-m-PES is an electron mediator which has higher stability of solutions than 1-Methoxy PMS. The stability in neutral to alkali conditions has been extremely improved with 1-Methoxy PES. 1-M-PES is a stable small-molecular compound and it has an equal or higher thermal stability than diaphorase. The 1-Methoxy PES solution can be stored long term.

200Oi10 is an ionizable lipidoid. 200Oi10 formulated LNPs facilitate mRNA delivery to the pancreas.

514O6,10 is an ionizable lipidoid. 514O6,10 formulated LNPs facilitate mRNA delivery to the pancreas.

IBG1 is a PROTAC-like degrader, which comprises JQ1 tethered to E7820. IBG1 selectively degraded BRD2 and BRD4 but not BRD3. IBG1 results in potent BRD4 degradation with DC50 of 0.15 nM and pronounces growth inhibition in various cancer cell lines.

IBG3 is a PROTAC-like degrader. IBG3 shows greater degradation efficiencies over BRD4 and BRD2 than those of IBG1 with DC50 of 6.7 pM and 8.6 pM, respectively.

IBG4 is a PROTAC-like degrader. IBG4 shows high specificity for BRD4 and does not efficiently degrade BRD2.

PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM for human TRPA1.

Precursor of MC1, which is a selective and potent inhibitor for COX-2, used as the radioligands for development as clinically useful PET radioligands.

MC1 is a selective and potent inhibitor for COX-2, and [11C]MC1 detected COX-2 in nonhuman primates after intracerebral injection of an inflammogen.

ZNL-0056 is an ATP-competitive inhibitor that targets both the Cys797 and Cys775 in the ATP binding site of EGFR, which is the first compound capable of targeting a nonconserved and partially buried Cys775.

Compound 181 is a selective and highly potent stabilizer of the 14-3-3σ/ERα complex. Compound 181 shows potency comparable to the natural product Fusicoccin-A.

Mosnodenvir (JNJ-1802) is an orally active pan serotype dengue virus (DENV) inhibitor, with EC50 values ranging from 0.057 to 11 nM for four dengue virus (DENV) serotypes. Mosnodenvir blocks viral replication by inhibiting the formation of complexes between two viral proteins, nonstructural protein 3 (NS3) and NS4B, thereby preventing the formation of new viral RNA. Mosnodenvir exhibits picomolar to nanomolar antiviral activity in vitro and has antiviral efficacy in mice and non-human primates.

Lipid 20b is an ionizable lipid containing a thiophene moiety (Thio-lipid) for mRNA delivery. Lipid 20b enables LNPs to transfect the liver and spleen. Lipid 20b is potent in mRNA delivery to the retina with no acute toxicity.

C14-O2 is an oxidized lipid for mRNA delivery. C14-O2-LNP is capable of potent and selective delivery of mRNA to blood monocytes. C14-O2 LNP is used to deliver a functional CD19-CAR mRNA and is shown to engineer functional CAR monocytes directly in situ.

Lipid 29d is an ionizable lipid containing a thiophene moiety (Thio-lipid) for mRNA delivery. Lipid 29d enables LNPs to transfect the lung and spleen.

1,2-didecanoyl-sn-glycero-3-phosphate is one kind of phosphatidic acid, which is a minor constituent of biological membranes is a simplest glycerophospholipid. It has glycerol backbone with phosphate present at C-3 position. The C-1 and C-2 positions are esterified with fatty acids.It is used as a component in the lipid bilayer to study how lipid geometry acts in coat protein I (COPI) vesicle fission, and maybe used to activate protein kinase C (PKC).

A1-28 is a disulfide bond-containing ionizable cationic lipid.1 It has been used in the generation of lipid nanoparticles (LNPs) for the delivery of CRISPR complementary single-guide RNA (sgRNA) and Cas9 mRNA for genome editing in vitro.

VL422 is an ionizable cationic lipid.1 It has been used in the generation of lipid nanoparticles (LNPs) for the delivery of CRISPR complementary single-guide RNA (sgRNA) and Cas9 mRNA for gene editing in vitro and in vivo. LNPs containing VL422 and encapsulating Cas9 mRNA and sgRNA targeting the gene encoding angiopoietin-related protein 3 (ANGPTL3), a protein whose loss-of-function decreases LDL, HDL, and cholesterol plasma levels, induce a deletion in a premature stop codon in ANGPTL3 in the livers of cynomolgus monkeys.

CL15F6 is an ionizable cationic lipid (pKa = 6.75).1 It has been used in the formation of lipid nanoparticles (LNPs) for the delivery of mRNA and polymer-lipid hybrid nanoparticles for the delivery of plasmid DNA in vitro.1,2

C3-K2-E14 is an ionizable cationic lipid (pKa = 5.5).1 It has been used in the generation of lipid nanoparticles (LNPs) for the delivery of mRNA or siRNA in vitro and in vivo. LNPs containing C3-K2-E14 and encapsulating siRNA targeting the gene encoding colony-stimulating factor 1 (Csf1) reduce the percentage of circulating Ly6Chi monocytes and increase the percentage of circulating Ly6Cint monocytes in mice.

(S)-C12-200 is an ionizable cationic lipid (pKa = 7.12) and an isomer of C12-200 (Item No. 36699).1 It has been used in the formation of lipid nanoparticles (LNPs) for the delivery of mRNA in vivo. Intravenous administration of LNPs containing (S)-C12-200 and encapsulating mRNA encoding Cre recombinase increase the percentage of tdTomato+ hepatocytes, endothelial cells, and Kupffer cells in the livers of Ai14 mice greater than (R)-C12-200-containing and Cre mRNA-encapsulating LNPs.

PPPDA-O16B is a disulfide bond-containing ionizable cationic lipid that has been used in the generation of lipid nanoparticles (LNPs) for plasmid delivery in vitro and in vivo.1 LNPs containing PPPDA-O16B and encapsulating plasmids encoding Ras/Rap1-specific endopeptidase (RRSP) increase RRSP levels and decrease Ras levels in, and reduce the viability of, HeLa cervical cancer cells. LNPs containing PPPDA-O16B and encapsulating plasmids encoding RRSP selectively localize to tumors over the heart, liver, spleen, lungs, and kidneys, as well as decrease tumor volume without reducing body weight, in an HCT116 colorectal cancer mouse xenograft model.

Lipid C3 is an ionizable cationic lipid (pKa = 5.05-5.671).1,2 It has been used in the formation of lipid nanoparticles (LNPs) for the delivery of mRNA in vitro and in vivo.1 Intracerebroventricular administration of LNPs containing lipid C3 and encapsulating mRNA encoding α-L-iduronidase (Idua) to neonates increase midbrain and hippocampal α-L-iduronidase enzyme activity and decrease forebrain, midbrain, and hippocampal glycosaminoglycan levels in an Idua-W392X mouse model of the lysosomal storage disorder mucopolysaccharidosis type I, also known as Hurler syndrome. Intracerebroventricular administration of LNPs containing lipid C3 and encapsulating an mRNA reporter to fetal macaques in utero increase brain GFP expression.

BAmP-O16B is an ionizable cationic amino lipid that has been used in the generation of lipid nanoparticles (LNPs).1 LNPs containing BAmP-O16B and encapsulating NSA-inactivated RNase A reduce the viability of SiHa and HeLa cancer cells, but not non-cancerous NIH3T3 and HEK293T cells, upon intracellular reactivation of RNase A by glutathione (GSH).