3-ap

3-AP (Triapine) is a novel inhibitor of the M2 subunit of ribonucleotide reductase (RR).

AP-C2 is a potent small molecule guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) inhibitor with a pIC50 of 5.2 for cGKII.

AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.

T-5224 is a transcription factor c-Fos/AP-1 inhibitor, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors.

CRT0044876 (7-NO2-ICA) is a potent and selective APE1 inhibitor with IC50 of ~3 μM.

AP-C3 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 6.3 and demonstrating only weak inhibition of cGKII-dependent anion secretion [1].

DL-AP3 is a competitive group I metabotropic glutamate receptor antagonist and inhibitor of phosphoserine phosphatase.

20-O-Demethyl-AP3 is a secondary metabolite derived from Ansamitocin P-3, and Ansamitocin P-3 is a macrocyclic antitumor antibiotic exerting its therapeutic effects by inhibiting microtubules.

AP-C6 is a potent inhibitor of guanosine 3',5'-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), exhibiting a pIC50 of 6.5. It inhibits human cGKII activity in vitro in a concentration-dependent manner and potentiates cAMP signaling through phosphodiesterase (PDE) inhibition [1].

AP-C4 is a selective inhibitor targeting guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 5.2. Conversely, AP-C3 does not inhibit cGKII-mediated anion secretion [1].

1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid (Nudifloric Acid) is from Cordyceps bassiana. Nudifloric Acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function.

Aniline-d5 is a deuterated compound of Aniline. Aniline has a CAS number of 62-53-3. Aniline has been reported to be toxic to the spleen via iron overload and induction of oxidative stress via Heme Oxygenase 1 up-regulation. Toxicity of this agent on the spleen is characterized by hyperplasia, fibrosis, and vascular congestion in rats. Studies suggest that this compound causes significant increase in both p-IKKα and p-IKKβ which in-turn increases NF-κB and AP-1 binding activity. In other experiments, Aniline displays a capacity to induce methemoglobinemia, glutathione depletion, membrane cytoskeletal changes, loss of circulating blood cells, and adversely affects blood stability.

Lucidenic acid B (Lucidenicacid B), a natural compound extracted from Ganoderma lucidum, induces activation of caspase-9 and caspase-3 and cleavage of PARP, which can induce apoptosis in human leukemia cells through mitochondrial mediation. Lucidenic acid B inhibits PMA-induced invasion of human hepatocellular carcinoma cells by inactivating the MAPK/ERK signaling pathway and decreasing the binding activity of NF-kappaB and AP-1. Lucidenic acid B had no effect on cell cycle and necrotic cells.

AP-C5 is a compound with selective inhibition of guanosine 3',5' cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII), with a Pic50 value of 7.2 for cGMP, and can be used in the study of diarrheal diseases.

3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) reduces cell proliferation in Caco-2 cells(IC50 = 24.1 μM) more effectively than anthocyanins and may offer protection against colon cancer after its formation in the gut. 3-O-Methylgallic acid inhibits transcription factors NF-κB, AP-1, STAT-1, and OCT-1 which are known to be activated in colorectal cancer.

Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) with antitumor activity. It has the potential to be a first-in-class candidate in AML.

15(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of 15-lipoxygenase (15-LO) on arachidonic acid. It is either metabolized to 14,15-leukotriene A4 [1] or reduced to 15(S)-HETE by peroxidases.[2] [1] 15(S)-HpETE mediates a number of biological functions including the induction of c-fos and c-jun, and activation of AP-1. [3] 15(S)-HpETE inhibits prostacyclin synthesis in porcine aortic microsomes and bovine endothelial cells, and can cause the suicide inactivation of porcine 12-LO.[2][4][5]

L-AP3 is a potent antagonist of metabotropic glutamate receptor (mGluR), demonstrating inhibitory effects on D-phosphoserine and L-phosphoserine with IC50 values of 368 μM and 2087 μM, respectively.