annexin a

PY-60 can effectively activate YAP transcriptional activity against annexin A2 (ANXA2) (Kd value of 1.4 µM). PY-60 activates a pro-proliferative, YAP-dependent transcriptional program in adult animals that are able to remodel the epidermis through proliferation.

Timonacic (Thioproline) has been used in trials studying the treatment of HIV Infections.

Hydrocortisone 17-butyrate (Cortisol 17-butyrate) is a synthetic glucocorticoid receptor agonist with antiinflammatory, antipruritic and vasoconstrictive effects.

Dexamethasone acetate (NSC 39471) is the acetate salt form of Dexamethasone, a synthetic adrenal corticosteroid with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone also interferes with NF-kB activation and apoptotic pathways. This agent lacks the salt-retaining properties of other related adrenal hormones.

Hydrocortisone acetate (Cortisol 21-acetate) is the synthetic acetate salt form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties.

Amcinonide (CL-34699) is a Corticosteroid. The mechanism of action of amcinonide is as a Corticosteroid Hormone Receptor Agonist.

LCKLSL hydrochloride is a hexapeptide compound and competitive inhibitor of membrane-bound protein A2 (AnxA2) with potential anti-angiogenic activity that inhibits the development of autoimmune encephalomyelitis (EAE) in mice.

LCKLSL acetate is a competitive annexin A2 (AnxA2) inhibitor. LCKLSL acetate potently inhibits the binding of tissue plasminogen activator (tPA) to AnxA2 and the generation of plasmin. LCKLSL acetate has anti-angiogenic roles.

A2ti-1 is a highly selective inhibitor of annexin A2/S100A10 heterotetramer (A2t) (IC50: 24 μM) that inhibits ARV-mediated activation of Src and p38 mitogen-activated protein kinase (MAPK). A2ti-1 can be used to study human papillomavirus type 16 (HPV16) infection.

Ac2-26, an annexin A1 mimetic peptide, was able to attenuate renal inflammatory injury in a diabetic mouse model through inhibition of p38MAPK/NF-κB, as well as sepsis-induced cardiomyocyte apoptosis through the LXA4/PI3K/AKT signalling pathway, and hepatic ischaemia-reperfusion injury in mice by modulating IL-22/IL-22R1/STAT3 signalling pathway.

(R)-SL18 is a degrader of ANXA3 that facilitates its breakdown via ubiquitination. This compound can inhibit the proliferation, migration, invasion, and colony formation of breast cancer cells, while also inducing apoptosis. (R)-SL18 is applicable for research in triple-negative breast cancer.

ANXA3 degrader 1 (Compound 18a5) is a highly selective ANXA3 degrader with activity against cancer cells. It demonstrates significant inhibitory effects in a triple-negative breast cancer (TNBC) tumor xenograft model, with a tumor growth inhibition (TGI) rate of 96%.

CI-936 (MRS-3310) is an orally active A2 agonist with a binding affinity of 25 nM. In preclinical studies, it has demonstrated potent and selective effects, indicating potential antipsychotic efficacy. Additionally, CI-936 inhibits exploratory behavior in mice.

A2ti-2 is a low affinity and selective inhibitor of the membrane-bound protein A2/S100A10 heterotetramer (A2t) (IC50 : 230 μM).A2ti-2 exhibits antiviral activity by selectively disrupting protein interactions between A2 and S100A10, and protects against human papillomavirus type 16 (HPV16) infection.

LCKLSL, an N-terminal hexapeptide, acts as a competitive inhibitor of annexin A2 (AnxA2), effectively preventing the binding of tissue plasminogen activator (tPA) to AnxA2 while also inhibiting the generation of plasmin. In addition, LCKLSL exhibits anti-angiogenic properties.

ABO acts as an annexin A7 modulator, specifically binding to Thr286 to inhibit its phosphorylation on threonine (not on serine or tyrosine) residues within human umbilical vein endothelial cells (HUVECs). This compound furthers the annexin A7 interaction with the EF-hand protein GCA, leading to reduced GCA phosphorylation, lowered intracellular calcium levels, and enhanced autophagy in COS-7 cells. Moreover, ABO lessens phosphorylation of the microtubule-associated protein 1 light chain (LC3) in HUVECs and impedes the upregulation of phosphatidylcholine-specific phospholipase C (PC-PLC) due to oxidized low-density lipoprotein in vascular endothelial cells (VECs). In animal models, specifically apoE-/- mice on a Western diet, administration of ABO (50 or 100 mg/kg per day) has been shown to decrease PC-PLC expression, promote autophagy, and reduce apoptosis, lipid accumulation, and the extent of atherosclerotic plaques in the aortic endothelium.

I194496 is an effective inhibitor of cystathionine γ-lyase (CSE) with an IC50 value of 0.79 mM. It inhibits the growth of human TNBC cells by dual targeting the PI3K/Akt and Ras/Raf/ERK pathways. Additionally, I194496 suppresses the metastasis of human TNBC cells by downregulating the Anxa2/STAT3 and VEGF/FAK/Paxillin signaling pathways.

Linsidomine hydrochloride (SIN-1 chloride) is considered as a metabolite of moxidomine, with vasodilation, inhibition of platelet aggregation, and antiangina activity. In myocardial ischemia-reperfusion models, Linsidomine hydrochloride to reduce myocardial necrosis and reperfusion induced endothelial dysfunction is associated with the cavernosal mechanism of action involved in nitric oxide release.

Lincydomine is a smooth muscle relaxant, beneficial to the treatment of unstable angina pectoris, but also can open the respiratory tract of humans and guinea pigs.

A11 (ANXA1-derived 11 amino acid–long peptide) serves as an inhibitor of the ANXA1-EphA2 interaction, reducing ANXA1 attachment to EphA2 while promoting the association of Cbl (an E3 ubiquitin ligase of EphA2) with EphA2. This peptide also effectively lowers EphA2 levels, greatly enhances EphA2 ubiquitination, and stimulates EphA2 internalization along with the colocalization of EphA2 and Cbl in nasopharyngeal carcinoma (NPC) cells. Moreover, A11 curtails NPC cell proliferation, migration, and invasion, and it suppresses angiogenesis.

AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity, blocking cell proliferation, inducing apoptosis and differentiation, downregulating MLL fusion target genes, and reducing the leukemia burden in vivo[1].

AS-99 TFA is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. It blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1].

AZ-Tak1 is a potent and a relatively selective inhibitor of TAK1 kinase activity, with an IC50 of 0.009 mM. AZ-Tak1 treatment decreased the level of p38 and ERK in mantle cell lymphoma cells, and induced apoptosis in a dose and time dependent manner, with an IC50 of 0.1–0.5 mM. Using the annexin-V and PI staining and FACS analysis, After 48 hours of incubation, AZ-Tak1 (0.1 mM) induced apoptosis in 28%, 34% and 86% of Mino, SP53, and Jeko cells, respectively, which was increased to 32%, 42%, and 86% when 0.5 mM concentration was used.

MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. MHY219 effectively increased the sub-G1 fraction of cells through p21 and p27 dependent pathways in DU145 cells. MHY219 significantly induced a G2/M phase arrest in DU145 and PC3 cells and arrested the cell cycle at G0/G1 phase in LNCaP cells. Furthermore, MHY219 effectively increased apoptosis in DU145 and LNCaP cells, but not PC3 cells, according to Annexin V/PI staining and Western blot analysis. These results indicate that MHY219 is a potent HDAC inhibitor that targets regulating mu......