ac-4

AC-4 is a blocker of photoswitchable TRPV1 channel.

AC-4-130 is a direct STAT5 SH2 domain inhibitor that can disrupt STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription, inducing cell cycle arrest and apoptosis in leukemia cells, and can be used for the study of acute myeloid leukemia (AML).

AC-4-248 is an atypical, noncompetitive inhibitor of the dopamine transporter (DAT) that can reduce the inhibitory potency of cocaine on DAT. Additionally, it is a non-selective inhibitor of SLC6 transporters, with IC50 values of 45.5 μM for hDAT, 96.2 μM for hSERT, and 250 μM for hNET.

Azo-PROTAC-4C-cis is a BCR-ABL PROTAC degrader, exhibiting a lower efficiency in degrading BCR-ABL compared to its trans isomer, Azo-PROTAC-4C-trans. The cis isomer forms as a result of a configurational change of Azo-PROTAC-4C-trans when exposed to ultraviolet light (UV). Under visible light, Azo-PROTAC-4C-cis can be converted back to the highly active Azo-PROTAC-4C-trans, initiating protein degradation. This compound is useful for studying myeloid leukemia.

Azo-PROTAC-4C-trans is a BCR-ABL PROTAC degrader that efficiently targets BCR-ABL fusion proteins and ABL proteins. It exhibits strong, selective antiproliferative activity against K562 cells. The activity of Azo-PROTAC-4C-trans can be precisely and reversibly controlled through UV (for inactivation)/visible light (for activation) irradiation. This compound is applicable for myeloid leukemia research.

AC-45594 is a UPR activator. It induces endoplasmic reticulum stress and activates the unfolded protein response (UPR), promoting the shift from adaptive to terminal stress signaling, ultimately leading to apoptosis (Apoptosis). AC-45594 activates Caspase-3, induces PARP cleavage, and increases DR5 protein levels, selectively inhibiting the growth of Ewing sarcoma cells.

AC-42 is an allosteric agonist of M1 muscarinic receptor.

AC-42 hydrochloride is the hydrochloride salt form of AC-42. It acts as a conformational agonist of the muscarinic M1 receptor (muscarinic M1 receptor), exhibiting EC50 values of 805 nM and 220 nM on human wild-type and Y381A mutant M1 receptors, respectively. Additionally, AC-42 hydrochloride stimulates the accumulation of inositol phosphates (IP) and calcium mobilization in CHO cells.

Ac4ManNAz is an azide-containing metabolic glycoprotein labeling reagent that can selectively modify proteins and can be used for cell labeling, tracking, and proteomic analysis.

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1/2/4/6 (IC50=36/47/510/1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.

Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]

Trichostatin A (TSA), a natural derivative of diene isohydroxamic acids, is a specific and reversible histone deacetylase inhibitor (IC50=1.8 nM) that induces hyperacetylation of core histones to regulate chromatin structure.

Tasquinimod (ABR-215050) is an oral antiangiogenic agent with potential antitumor activity. It is also an S100A9 inhibitor and binds to the HDAC4Zn2+ binding structural domain with Kd values between 10 and 30 nM.

ACY-1083 is a small molecule inhibitor, a highly selective HDAC6 inhibitor (IC50=3 nM), with 260-fold higher selectivity over other classes of HDAC isoforms. It is brain-penetrant and used for research on chemotherapy-induced peripheral neuropathy.

BRD 9757 (N-Hydroxy-1-cyclopentene-1-carboxamide) is a selective inhibitor of HDAC6 (IC50 = 30 nM).

HM90822 is a novel synthetic apoptotic protein (IAP) antagonist that induces apoptosis in human pancreatic cancer cells through proteasome-dependent degradation of IAPs containing the BIR2/3 structural domain.HM90822 inhibits the expression of XIAP and cIAP1/2 proteins in HM822-sensitive Panc-1 and BxPC-3 cells, induces ubiquitylation of IAPs and promotes induces IAP ubiquitination and promotes proteasome-dependent IAP degradation.

MC2590 is a potent and selective histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.

AC 45594 (4-Heptyloxyphenol) is an agonist of steroidogenic factor 1 (SF-1) ( IC50 : 50-100 nM)

Torsemide (AC-4464) is an anilinopyridine sulfonylurea belonging to the class of loop diuretics. Torsemide has a prolonged duration of action compared to other loop diuretics, is extensively protein bound in plasma and has a relatively long half-life.

Butanoic acid is an endogenous human metabolite, an endogenous histone deacetylase (HDAC) inhibitor. The IC50 of HDAC3, HDAC4 and HDAC1 were 2.4 mM, 4.5 mM and 5.3 mM, respectively. 3-Hydroxybutyric acid has the effects of energy metabolism, neuroprotection, anti-inflammatory, and improvement of insulin resistance.

CHDI 00484077 is a highly selective, central nervous system (CNS) permeable Class IIa HDAC inhibitor with inhibitory effects on HDAC4, HDAC5, HDAC7, and HDAC9, which improves neuronal function, and can be used to study Huntington's disease.

N-Ac-4-S-CAP is a compound that exhibits selective cytotoxicity towards melanin-producing cells in mouse hair follicles, causing 98% depigmentation. Within four hours of intraperitoneal injection, visible changes occur in these melanocytes, including the aggregation of melanin granules and nuclear condensation. Electron microscopy reveals progressive destruction of these cells, evidenced by swelling of membranous organelles, nuclear condensation, and cytoplasmic vacuolization, leading ultimately to complete cell death. N-Ac-4-S-CAP selectively targets active melanin-producing melanocytes but does not appear to affect precursor or dormant melanocytes. These properties suggest potential applications for N-Ac-4-S-CAP in melanoma suppression or skin whitening.

CHDI-390576 is a CNS-permeable, selective and potent dibenzoyl isohydroxamic acid class IIa histone deacetylase (HDAC) inhibitor that inhibits class IIa HDAC 4, HDAC 5, HDAC 7, HDAC 9, and can be used in cancer research.

SW-100 is a selective histone deacetylase 6 inhibitor (IC50: 2.3 nM). It also shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays an obviously improved ability to cross the blood-brain-barrier.