543

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 of 2.0 nM and Ki of 3.6 nM.

PF-543 hydrochloride (PF-543) inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.

DMP-543 (XR-543) is a KV7 channel blocker that enhances neurotransmitter release.

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a selective and potent inhibitor of sphingosine kinase 1 (SPHK1) and is an efficient inhibitor of 1-phosphate sphingosine (S1P) formation. It possesses anticancer, antifibrotic, and anti-inflammatory activities and can be used in research on colorectal cancer.

VHF 543, Amine is a potent ligand for the WD40 repeat domain (WDR) of DCAF1 (Kd = 31 nM measured by surface plasmon resonance). VHF 543, Amine carries a primary amine functional group handle that allows for rapid binding to linker target protein ligands.

YM-543, a sodium-glucose transporter 2 (SGLT-2) inhibitor, is used potentially for the treatment of type 2 diabetes.

YM-543, also known as ASP-543, is a selective SGLT2 inhibitor. Sodium-glucose cotransporter 2 (SGLT2) is a specifically expressed transporter in the kidney that plays an important role in renal glucose reabsorption, and its inhibition may present a novel therapeutic strategy for treating diabetes. YM543 potently and selectively inhibited mouse and human SGLT2 activities at nanomolar ranges. In vivo single oral administration of YM543 dose-dependently and significantly reduced blood glucose levels and improved glucose tolerance with a concomitant increase in urinary glucose excretion in KK Ay type 2 diabetic mice, effects that were sustained even after 12 h.

GAD65 (524-543) is a biologically active peptide comprising amino acids 524 to 543 of glutamic acid decarboxylase 65 (GAD65). It represents an early islet antigen fragment that elicits proliferative T cell responses in the non-obese diabetic (NOD) mouse model, instrumental in spontaneous autoimmune diabetes research. The peptide serves as a specific, possibly low-affinity stimulant for the diabetogenic T cell clone BDC2.5. Notably, immunization with GAD65 (524-543) heightens NOD mice's vulnerability to type 1 diabetes when subjected to the adoptive transfer of BDC2.5 T cells.

Collagen type IV alpha1 (531-543) is a protein that in humans is encoded by the COL4A1 gene on chromosome 13. It is ubiquitously expressed in many tissues and cell types. COL4A1 is a subunit of type IV collagen and plays a role in angiogenesis.

CGS 15435 is a potent thromboxen (TxA2) synthetase inhibitor (IC50: 1 nM). CGS 15435 acts on PGI2 synthase, cyclooxygenase and liposynthase with much less selectivity than on thromboxin synthase.

PHA 543613 is a specific agonist of α7 nAChR (Ki = 8.8 nM) and can be used in studies about the cognitive deficits of Alzheimer's disease and schizophrenia.

Org 25543 hydrochloride is a potent and selective glycine transporter type 2 (GlyT2) inhibitor (IC50 = 16 nM for hGlyT2). Displays no activity at GlyT1 or 56 other common biological targets (≥ 100 μM), in a glycine uptake assay in CHO cells.

BAY 41-8543 is a nitric oxide (NO)-independent stimulator of soluble guanylyl cyclase (sGC).

INCB054329, a structurally distinct bromodomain and extraterminal domain (BET) inhibitor, inhibits BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2 with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM respectively.

Org 25543 is the development of an N-Acyl amino acid that selectively inhibits the glycine transporter 2 to produce analgesia in a rat model of chronic pain.

GW 284543 hydrochloride is a selective inhibitor of MEK5 .

YM543 free base, a potent and orally active sodium-glucose cotransporter (SGLT) 2 inhibitor, effectively reduces blood glucose levels and is suitable for diabetes research.

Gln-AMS(TFA) inhibits glutaminyl-tRNA synthetase (GlnRS) with a Ki of 1.32 μM. Gln-AMS (TFA) is a type Ia aminoacyl-tRNA synthetase (AARS) inhibitor.

INCB054329 Racemate is an inhibitor of BET protein.

LY285434 is an angiotensin II receptor antagonist [suitable].

TMU 35435 is an inhibitor of histone deacetylases (HDAC). It enhances radiosensitivity by inducing the accumulation of misfolded proteins and autophagy (autophagy) in TNBC, and inhibits the NHEJ pathway through ubiquitination of the catalytic subunit of DNA-dependent protein kinase (DNA-PKcs).

BI1543673 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). It can diminish inflammatory responses in human lung tissue stimulated by TLR4 and TLR7 8. Additionally, BI1543673 reduces inflammatory signaling in a mouse lung inflammation model induced by LPS.

NSC635437 acts as an inhibitor of the EWS-FLI1 oncoprotein in Ewing's sarcoma.

ICI-125436 is a prodrug with anti-inflammatory properties.