hl 2

HL2-m5 is an inhibitor of the sonic hedgehog/patched (Shh/PTCH1) interaction, with a Kd for Shh of 170 nM. It effectively inhibits the activation of the Hedgehog signaling pathway and the transcription of Gli-controlled genes, with an IC50 of 230 nM.

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

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.

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.

HL271 hydrochloride is a chemical derivative of metformin and a potent AMPK activator that enhances AMPK phosphorylation levels. In animal models, HL271 hydrochloride alleviates age-related cognitive impairment. As an effective inhibitor of oxidative phosphorylation (OXPHOS), HL271 can be used in solid tumor research.

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.

CHL2310 is an inhibitor of CYP46A1 with an IC50 of 0.11 nM and a Kd of 0.37 nM. It is capable of crossing the blood-brain barrier. When labeled with radioactive [18F], CHL2310 can serve as a PET imaging agent.

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 .

IMMU-114 is a humanized antibody targeting HLA-DR, which inhibits human responses to bovine cells, used in malignant tumor research.

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].

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

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.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

2-Methylcyclohexa-2,5-diene-1,4-dione exhibits inhibitory activity against cancer cells such as A2780, HT-29, HL-60, and K562 (IC50 = 2.8–12.1 µM) and antibacterial activity against Bacillus subtilis.

Clofilium tosylate is a potassium channel blocker. It induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3.

SGD-1882 (PBD dimer) is a cytotoxic conjugate that is a target for mouse and human hematopoietic stem cells (HSC) and acute myeloid leukemia cells.

CB2 receptor agonist 8 (Compound 17) is an agonist of the cannabinoid receptor 2 (CB2 receptor). It shows cytotoxicity in U87, RPMI 8226, HL-60, and L929 cells with IC50 values of 91.03, 16.29, 23.51, and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expression of pro-apoptotic genes BAX, BAD, BIM, and the tumor suppressor gene p53, and induces apoptosis in U87 cells. Additionally, it inhibits the migration of U87 cells.

BAY R3401 is an orally active inhibitor of glycogen phosphorylase, leading to irreversible and non-selective inhibition of liver glycogenolysis. It suppresses glycogen breakdown in hepatocytes with IC50 values of 27.06 μM in HL-7702 cells and 52.83 μM in HepG2 cells. BAY R3401 is applicable for research in type 2 diabetes.

PROTACPIN1degrader-2 (1) is a PROTAC degrader of PIN1. The IC50 values of PROTACPIN1degrader-2 (1) against various cancer cells are as follows: 2248 nM for MV-4-11 cells, 3984 nM for MOLM-13 cells, and 3925 nM for HL-60 cells.

Piericidin A is a natural mitochondrial NADH- ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A interferes with the electron transfer chain by inhibiting the activity of NADH- ubiquinone reductase, thus inhibiting mitochondrial respiration, which shows a certain neurotoxic effect. Piericidin A has potential quorum sensing inhibitory activity, antibacterial, antitumor and insecticidal activities.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

1. Crebanine iv 5mg/kg can eonvert BaCl_2-induced arrhythmia into sinus rhythm in rats, and can significantly increase the tolerant dose of aconitine to produce ventrieular fibrillation(VF) and cardiac arrest (CA) in rata. 2. Crebanine can also decrease t