Tautomycetin is a potent and specifical PP1 inhibitor with the potential apoptosis-inducing activity. Tautomycetin inhibits purified PP1 and PP2A enzymes with IC50s of 1.6 nM and 62 nM, respectively. Tautomycetin is an antifungal antibiotic and has immunosuppressive effects in vivo. Tautomycetin can be used as a novel powerful tool to elucidate the physiological roles of PP1 in various biological events[1].
Etofylline is a vasodilator.
Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.
QL-X-138 is a selective and potent BTK/MNK dual kinase inhibitor with IC50 of 8, 107.4, and 26 nM for BTK, MNK1, and MNK2, respectively; exhibits covalent binding to BTK and noncovalent binding to MNK; enhances the antiproliferative efficacies in vitro against a variety of B-cell cancer cell lines, as well as AML and CLL primary patient cells; arrests cell cycle progression and strongly induces apoptosis.
VY-3-135 is an orally active, selective acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC50 value of 44 nM. VY-3-135 displayes no inhibitory activity towards recombinant human ACSS1 or ACSS3. VY-3-135 potently inhibits ACSS2 dependent fatty acid metabolism but has no effect on gene expression in tumors. VY-3-135 inhibits triple negative breast cancer (TNBC) tumor growth in mouse ACSS2high but not ACSS2low tumors models[1].
Alpibectir is an antibacterial agent[1].
12-Oxocalanolide A (compound 6) is a potent inhibitor of reverse transcriptase from human immunodeficiency virus type 1 (HIV-1) with an IC50 and EC50 of 2.8 and 12 μM, respectively. 12-Oxocalanolide A is the analogue of Calanolide[1].
Thiohexam is a rubber cure accelerator. Thiohexam is also a known allergen and dermatological sensitizer[1].
(-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
D-(+)-Glucono-1,5-lactone is a polyhydroxy (PHA) that is capable of metal chelating, moisturizing and antioxidant activity.
Inixaciclib is a potent CDK inhibitor, that can be used to research anticancer.
H-D-Phg(4-Cl)-OH is a Glycine (HY-Y0966) derivative[1].
Escin IIa, isolated from horse chestnut, the seeds of Aesculus hippocastanum L., has positive effects on acute inflammation in animals. Escin IIa has gastroprotections on ethanol-induced gastric mucosal lesions in rats[1][2].
(+)-Sotalol ((S)-Sotalol) is the S-isomer of Sotalol (HY-103196). Sotalol is an orally active, non-selective β-adrenergic receptor blocker. (+)-Sotalol is an antiarrhythmic agent. (+)-Sotalol can prolong action potential duration in isolated cardiac muscle[1][2][3].
CJ-13,610, a nonredox-type 5-LO inhibitor, dose dependently suppresses 5-LO product formation in ionophore A23187-stimulated PMNL in the absence of exogenous AA with an IC50 of about 70 nM[1]. PMNL: polymorphonuclear leukocytes; AA: arachidonic acid
NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 μM for p53-null HCT116 cells.IC50 value: 8.38 μM (EC50, for p53-null HCT116 cells)Target: p53in vitro: NSC59984 specifically restores p53 pathway signaling in mutant p53-expressing human colorectal cancer cells. NSC59984 induces cell death in tumor cells but not normal cells with little or no genotoxicity. NSC59984 induces mutant p53 protein degradation through MDM2-mediated ubiquitination in cancer cells. NSC59984 restores p53 pathway signaling through activation of p73. NSC59984 induces p73-dependent cell apoptosis in cancer.in vivo: NSC59984 synergizes with CPT11 to induce cell death in mutant p53-expressing colorectal cancer cells and inhibits mutant p53-associated colon tumor xenograft growth in a p73-dependent manner.
Fmoc-Hyp(tBu)-OH is a proline derivative[1].
Propargyl-PEG3-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
IBU-DC Phosphoramidite is used for synthesis of oligonucleotides[1].
Sulfaguanidine is a sulfonamide, used as an antibiotic.
Arofylline is a PDE4 inhibitor as a potential treatment for asthma.
Pyrrhocoricin is a biological active peptide. (Antimicrobial activity against Gram-negative bacteria)
JNJ-40355003 is a potent and selective atty acid amide hydrolase (FAAH) inhibitor[1].
AC-Asp(OtBU)-OH is an aspartic acid derivative[1].
3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) IC50 valueTarget: PFKFB3 isozymein vitro: 3PO inhibits recombinant PFKFB3 activity, suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH. 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μM) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. The PFKFB3+/- fibroblasts were more sensitive to compound 3PO treatment (IC50, 26 μM) compared with the wild-type PFKFB3+/+transformed cells (IC50, 49 μM).3PO Causes G2-M Phase Arrest, Which Is Preceded by Decreased Fru-2,6-BP and Glucose Uptake. 3PO slows growth through inhibition of PFK-2 activity, then ectopic expression of the PFKFB3 isozyme may thwart the cytostatic activity of 3PO. [1] 3PO inhibits the glycolytic regulator PFKFB3 in endothelial cells (ECs). 3PO decreases glycolysis in ECs and impairs vessel sprouting. 3PO also suppresses vascular hyperbranching induced by inhibition of Notch or VEGF receptor 1 (VEGFR1) and amplified the antiangiogenic effect of VEGF blockade. [2]in vivo: Compound 3PO treatment significantly reduced Fru-2,6-BP in tumor xenografts compared with vehicle control (vehicle: 13.1 ± 1.9 pmol/mg, 3PO: 8.5 ± 1.7 pmol/mg). [1] 3PO also impairs (pathological) angiogenesis. [2]
(Bromomethyl)cyclohexane-d11 is the deuterium labeled (Bromomethyl)cyclohexane[1].
NVP-BKM120 Hydrochloride is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
Reynoutrin (Quercetin-3-D-xyloside) is a flavonoid from Psidium cattleianum, with antioxidant and radical-scavenging activity[1].
Bemcentinib (R428) is a potent and selective inhibitor of Axl with an IC50 of 14 nM.
Thalidomide-Piperazine-PEG2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].