Ionizable Lipid Products

ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.

Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonistTirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation. Tirofiban is an antithrombotic used in the treatment of unstable angina.Tirofiban, in a concentration-dependent manner reduced platelet aggregation evoked by ADP (IC50 approximately 70 ng/ml), collagen (IC50 approximately 200 ng/ml), and thrombin (IC50 approximately 5,000 ng/ml).

Telotristat etiprate (LX1606 Hippurate) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

1-EBIO is an Epithelial KCa channel activator. Promotes ESC differentiation into cardiomyocytes.

TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM.IC50 value: 20 nMTarget: p38TA-02 is a novel compound with similar cardiogenic properties asSB203580 and SB202190. TA-02 especially inhibits TGFBR-2.

Thymosin beta 4 is a potent regulator of actin polymerization in living cells. Sequence: Ser-Asp-Lys-Pro-Asp-Met-Ala-Glu-Ile-Glu-Lys-Phe-Asp-Lys-Ser-Lys-Leu-Lys-Lys-Thr-Glu-Thr-Gln-Glu-Lys-Asn-Pro-Leu-Pro-Ser-Lys-Glu-Thr-Ile-Glu-Gln-Glu-Lys-Gln-Ala-Gly-Glu-Ser.

TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.

An aminoglycoside antibiotic similar in structure to gentamicin B1; blocks polypeptide synthesis by inhibiting the elongation step in both prokaryotic and eukaryotic cells.

RU 58841 (PSK-3841) is a specific androgen receptor antagonist or anti-androgen. RU 58841 (PSK-3841) has a dramatic effect on hair regrowth.

Crizotinib is a potent inhibitor of c-Met and ALK with an IC50 of 11 nM and 24 nM in cell-based assays, respectively.

ML365 is a novel selective small molecule inhibitor of TASK1(KCNK3) with IC50 of 4 nM(thallium influx fluorescent assay) and 16 nM(automated electrophysiology assay).ML365 possesses more than 60-fold selectivity for inhibition of TASK1 over a closely-related, two-pore domain potassium channel, TASK3. ML365 displays little or no inhibition at 30 μM of more distantly related potassium channels, Kir2.1, potassium voltage-gated channel, KQT-like subfamily, member 2 (KCNQ2), and human ether-a go-go-related gene (hERG). Based on these criteria, ML365 is a best-in-class probe and is a useful pharmacological probe for in vitro studies of TASK1 function and in further studies aimed at developing therapeutic intervention.

Voriconazole(UK-109496) is a second-generation triazole antifungal used to treat serious fungal infections.IC50 Value: Target: AntifungalVoriconazole displays potent activity against Candida, Cryptococcus and Aspergillus species. Voriconazole inhibits ergosterol synthesis by inhibiting CYP450-dependent 14-α sterol demethylase resulting in a depletion of ergosterol in fungal cell membranes

Cambendazol is an antihelmintic that, at a dose of 50 mg/kg/day in mice, eradicates S. ratti adult worms from intestine and S. stercoralis larva from muscle.It inhibits polymerization of microtubules isolated from bovine brain with an IC50 value of 64.2 µM.Formulations containing cambendazol have been used to treat strongyloidiasis in humans and have been studied as potential chemotherapeutics.

Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM.Target: HIV proteaseLopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats.

Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ∼8.5 μM and ∼5 μM, respectively.

Iberin, a sulfoxide analogue of sulforaphane, is a naturally occurring member of isothiocyanate family. It inhibits cell survival with an IC50 of 2.3 μM in HL60 cell.

Nandrolone Decanoate is a mild form of an anabolic steroid.

AEBSF is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, plasmin, thrombin, and trypsin.

Tri-b-GalNAc-b-Ala-PEG3-MAL contains three terminal beta-N-acetylgalactosamine (GalNAc) sugars arranged in a trivalent configuration, facilitating high-affinity binding to the asialoglycoprotein receptor (ASGPR) expressed on hepatocyte surfaces. The crucial functional group is a terminal maleimide (MAL) moiety, enabling chemoselective bioconjugation with biomolecules harboring thiol (-SH) groups. This strategy allows for site-specific conjugation under mild conditions, valuable for developing targeted conjugates in disciplines like targeted drug delivery and antibody-drug conjugate (ADC) development for hepatocellular carcinoma.

Alsterpaullone (9-Nitropaullone;NSC 705701) is a potent cyclin-dependent kinases (CDK) inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to glycogen synthase kinase-3 alpha/beta (GSK-3alpha/GSK-3beta) with an IC50 of 4 nM, with antitumor activity and potential for the treatment of neurodegenerative and proliferative disorders[1].