α-hl

HL271, a derivative of metformin, is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment.

HL-PEG2k is the second near-infrared Ru(II) polypyridyl complex. It demonstrates a red-shifted wavelength, enhanced photothermal conversion efficiency (41.77%), and antitumor effects against gliomas. Due to its excellent biocompatibility, HL-PEG2k has the potential to serve as a diagnostic platform for research on combating tumor growth and recurrence.

HL-2 is a ligand for the target protein PI3K kinase of HL-8 and can be used in the synthesis of PROTAC.

HL-8, a PROTAC molecule, effectively targets and degrades PI3K kinase completely at a concentration of 10 μM within 8 hours, showcasing potential for cancer research [1].

Nitto Phase HL UnyLinker 300 is a linking support.

ABT-737 is a BH3 mimetic and an inhibitor of Bcl-2, Bcl-xL, and Bcl-w (EC50=30.3 nM/78.7 nM/197.8 nM). ABT-737 exhibits antitumor activity and anti-aging activity.

Lycorine (Narcissine) inhibits protein synthesis and may inhibit ascorbic acid biosynthesis, although studies on the latter are controversial and inconclusive.

Ginsenoside F5 is a natural product from Panax ginseng C. A. Mey, remarkably inhibits the growth of HL-60 cells by the apoptosis pathway

Meisoindigo (Natura-α) is a derivative of indigo natural, might induces apoptosis and myeloid differentiation of acute myeloid leukemia (AML).

HL22 is a derivative of harmine. It exhibits significant inhibitory effects on three cancer cell lines: HCT116, MGC803, and MCF7. Moreover, HL22 can impede the migration and colony formation of MGC803 cells. Its anticancer mechanism is associated with multiple metabolic pathways and can be utilized for tumor research.

HL001 is an orally active small molecule inhibitor of cyclophilin A (CypA) and a receptor antagonist of lysophosphatidic acid 1 (LPA1). It induces cell cycle arrest and apoptosis in tumor cells via p53. By downregulating G3BP1, HL001 promotes reactive oxygen species production and DNA damage to stabilize p53. It disrupts the interaction between MDM2 and p53-72R in a CypA-dependent manner. HL001 exhibits antitumor activity and can also be used in research on pulmonary fibrosis.

HL403 is a potent dual inhibitor targeting BRD4 and Src, with an IC50 value of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 demonstrates anticancer activity.

HL389-NHC2-PEG3-C2NH is capable of inhibiting the proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 values of 11.39 μM and 9.66 μM, respectively. It serves as a conjugate of an E3 ligase ligand and linker, employed in the synthesis of the PROTAC degrader HL435.

HL389 inhibits the proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 values of 11.39 μM and 9.66 μM, respectively. It serves as a ligand for E3 ligase and is utilized in the synthesis of [PROTACDegraderHL435].

HL435 is a heterobifunctional molecule that degrades BRD4 by linking with JQ1, with DC50 values of 11.9 nM and 21.9 nM in MDA-MB-231 and MCF-7 cells, respectively. It inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1, and A549 cells, arrests the cell cycle, and induces apoptosis. Additionally, HL435 exhibits antitumor activity in mouse models.

Trequinsin hydrochloride (HL 725) is a potent phosphodiesterase (PDE) inhibitor and inhibitor of platelet aggregation, and is a novel antihypertensive vasodilator for the study of cardiovascular disease.

Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.

IM-156 acetate, an activator of NADH dehydrogenase (IC50=2.2 μM) and AMP-activated protein kinase alpha (AMPKα), is an orally available and bioavailable inhibitor of mitochondrial oxidative phosphorylation (OxPhos).IM-156 acetate increases AMPKα activity and inhibits chlorhexadiene-induced peritoneal fibrosis and inhibit tumor growth in rats .

Tunlametinib is a highly selective, orally bioavailable small molecule inhibitor of MEK1 and MEK2 kinases with a reported IC50 value of 1.9 nM for MEK1. Tunlametinib exerts its antitumor effects by blocking the oncogenic RAS-RAF-MEK-ERK signaling pathway, thereby inducing tumor cell cycle arrest and promoting apoptosis, Tunlametinib demonstrates strong inhibitory activity against various RAS/RAF-mutant cancer cells such as those harboring BRAF V600E or KRAS G12C mutations, shows synergistic effects in combination with BRAF/KRASG12C/SHP2 inhibitors and Docetaxel, and is used in targeted therapy for RAS/RAF-driven cancers including melanoma, colorectal cancer, and non-small cell lung cancer (NSCLC).

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM).

HL23 is a histone deacetylase (HDAC) inhibitor that effectively targets hepatocellular carcinoma (HCC). It promotes acetylation at the TXNIP promoter and increases TXNIP expression, modulating potassium channel activity and inducing TXNIP-dependent potassium deficiency. Additionally, HL23 impedes HCC progression and spread, demonstrating greater potency when combined with Sorafenib than the Sorafenib and Vorinostat duo [1].

SAE-14 is a specific GPR183 antagonist. SAE-14 inhibits GPR183 with an IC50 of 28.5 nM in a calcium mobilization assay[1].

Nordalbergin, a coumarin isolated from the bark of Dalbergia sissoo, significantly induces the differentiation of HL-60 cells.

Evocarpine shows antimycobacterial, and vasorelaxant effects, it can inhibit Ca2+ influx through voltage-dependent calcium channels.