functions

MSC2360844 is a potent, orally active and selective inhibitor of PI3Kδ(IC50 of 145 nM).

Acesulfame potassium is a non-nutritive sweetener.

D-(-)-3-Phosphoglyceric acid disodium (3-Phospho-D-glyceric acid disodium) is an intermediate in glycolysis/gluconeogenesis and the biosynthesis of serine, glycine, and threonine, competitively inhibiting yeast enolase. It also functions as an intermediate in biosynthetic pathways in plants, eukaryotes, and prokaryotes.

Prostaglandin E2 (PGE2) is a natural hormone-like substance involved in various physiological functions, including the contraction and relaxation of smooth muscles, dilation and constriction of blood vessels, regulation of blood pressure, and modulation of inflammation. It can be used to induce neuropathic pain models.

Avapritinib (BLU-285) is a selective, highly potent, and orally active inhibitor of KIT and PDGFRA activation loop mutant kinases, targeting KIT D816V (IC50:0.27 nM) and PDGFRA D842V (IC50:0.24 nM), and attenuates the transport functions of ABCB1 and ABCG2. It binds to the active conformation of the kinases and exhibits antitumor activity.

Bleomycin sulfate is a glycopeptide antibiotic with antitumor activity. It is commonly used as a DNA-damaging agent and DNA synthesis inhibitor. It functions by inducing DNA strand breaks without affecting RNA strands. Bleomycin sulfate is widely used in cancer research and for establishing pulmonary fibrosis animal models.

Bleomycin hydrochloride is a glycopeptide antibiotic and a DNA synthesis inhibitor. Bleomycin Sulfate can cause DNA strand breaks but not RNA strand breaks. Bleomycin Sulfate has anti-tumor activity.

D18 is an immune modulator that acts as a dual agonist for TLR7/8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1/PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].

COX-2-IN-2, a selective inducible COX2 inhibitor, exhibits potent inhibition with an IC50 of 0.24 μM. Meanwhile, COX-2-IN-1 functions as an anti-inflammatory agent, demonstrating both anti-inflammatory and analgesic activities.

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

Temiverine hydrochloride is a potential calcium channel antagonist with anticholinergic effects that inhibits some of the functions of atropine.

EMD57033 is a cardiac troponin C (cTnC) activator, a dominant Ca2+ sensitizer, which functions by binding to cardiac/slow skeletal troponin C heterodimers to promote cardiac contraction.

BRD3067 serves as a negative control for Tubacin A (AGCR-13900, TubA, AG-CR13900). BRD3067 is a derivative of Tubacin and functions as a selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 15 nM in cell-free assays. BRD3067 has demonstrated potential anticancer and anti-inflammatory activities, making it a valuable tool for studying HDAC6 inhibition.

(Rac)-RK-682 is a racemic mixture that functions as a protein tyrosine phosphatases (PTPases) inhibitor, specifically targeting protein tyrosine phosphatase 1B (PTP-1B), low molecular weight protein tyrosine phosphatases (LMW-PTP), and cell division cycle 25B (CDC-25B), with inhibitory concentrations (IC50s) of 8.6 μM, 12.4 μM, and 0.7 μM, respectively [1].

5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative that inhibits TRPA1-mediated calcium signaling (IC50: 35 μM). It functions as an inhibitor of the Na+/H+ exchanger (NHE) with Ki values ranging from 0.013 to 2.4 μM for various NHE isoforms. Additionally, 5-HMA blocks ASIC3 channels by 51% at 20 μM.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

SPOP-IN-6lc is a potent SPOP inhibitor with multiple roles in cancer, oncostatic in a variety of tumors, but functions as an oncogene in renal cancer.SPOP-IN-6lc can be used to study cell signaling and apoptosis.

Triciferol acts as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR ( IC 50 =87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Triciferol also exhibits efficacious antiproliferative and cytotoxic activities in cancer cell models in vitro [1].

Bexlosteride (LY300502), a benzoquinolinone derivative, functions as a human type I 5α-reductase inhibitor. It demonstrates metabolic inhibition, antiproliferative, and antisecretory activities specifically in LNCaP human prostatic adenocarcinoma cell cultures, positioning it as a potent agent for prostate cancer research [1] [2].

SETDB1-TTD-IN-1 is a potent and selective inhibitor of SET domain bifurcated protein 1 tandem tudor domain (SETDB1-TTD, Kd = 88 nM), and also an endogenous binder competitive inhibitor with a KD of 0.106±0.002 μM for TTD. It can be used to study the biological functions and disease associations of SETDB1-TTD.

Octodrine (2-Amino-6-methylheptane) is primarily used as a pharmaceutical intermediate for Octamylamine; it also functions as a local anesthetic and vasoconstrictor.

Diltiazem hydrochloride (RG 83606 HCl) is a benzothiazepine calcium channel blocking agent with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.

Nebivolol hydrochloride (R 065824 hydrochloride) is a cardioselective ADRENERGIC BETA-1 RECEPTOR ANTAGONIST (beta-blocker) that functions as a VASODILATOR through the endothelial L-arginine/ NITRIC OXIDE system. It is used to manage HYPERTENSION and chronic HEART FAILURE in elderly patients.