Secalciferol is a metabolite of Vitamin D, a possibly anti-inflammatory steroid which is involved in bone ossification. IC50 value:Target: In addition, it is known that Secalciferol mediates calcium and phosphorus homeostasis. Also Secalciferol inhibits calcium channels in osteosarcoma cells via suppressing the effects of 1α, 25-dihydroxyvitamin D3 and testosterone. Alternate studies indicate that Secalciferol can decrease the abundance of p53 and Pi-induced cytochrome c translocation. Furthermore, Secalciferol can increase cell proliferation in resting zone (RC) chondrocytes and inhibits matrix enzymes by possibly inhibiting the degradation of the matrix.
Angelol H is a natural tcompound isolated from Angelica pubescens MAXIM. (Umbelliferae)[1].
L-R4W2 is a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), with an IC50 of 0.1 μM. L-R4W2 may act as a potent analgesic[1][2].
Pyruvic acid is an intermediate metabolite in the metabolism of carbohydrates, proteins, and fats.
ENPP1-IN-2 is a potent Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) inhibitor with an IC50 value of 32.38 nM for recombinant human ENPP-1. ENPP1-IN-2 has anti-tumor activity[1].
Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
ICT5040 is a small molecule CXCR4 antagonist (IC50=3.8 μM). ICT5040 inhibits CXCL12-mediated proliferation and migration, and suppresses CXCL12-induced intracellular calcium mobilisation in U87 glioma cells[1].
Tempol-d17 is the deuterium labeled Tempol[1]. Tempol is a general superoxide dismutase (SOD)-mimetic drug that efficiently neutralizes reactive oxygen species (ROS)[2][3].
GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).
Isoastilbin is a dihydroflavonol glycoside compound in Rhizoma Smilacis glabrae and Astragalus membranaceus. Isoastilbin inhibits glucosyltransferase (GTase) with an IC50 value of 54.3 μg/mL, and also inhibits tyrosinase activity. Isoastilbin shows neuroprotective, antioxidation, antimicrobial and anti-apoptotic properties and has the potential for Alzheimer’s disease research[1][21][3].
CDK7-IN-15 is a potent inhibitor of CDK7. CDK7-IN-15 is a pyrimidinyl derivative compound. CDK7-IN-15 has the potential for the research of various cancers, especially the cancer with transcriptional dysregulation (extracted from patent CN114249712A, compound 8)[1].
16-Methoxystrychnine is a alkaloid[1].
H-DL-Abu-OH-d6 is the deuterium labeled H-DL-Abu-OH[1].
IDO1-IN-22 (Compound 3) is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM). IDO1-IN-22 has excellent antitumor efficacy in LLC xenograft model, as well as desirable pharmacokinetic (PK) profile[1].
Sevasemten is an allosteric inhibitor of skeletal muscle myosin. Sevasemten exhibits selectively myosin inhibition with IC50s of ≤10 μM (skeletal), >100 μM (cardiac), respectively[1][2].
Ceftizoxime is a bacterial inhibitor which acts by interfering with bacterial cell wall synthesis and inhibiting cross-linking of the peptidoglycan.
3,4,6-Tri-O-acetyl-D-glucal-13C is the 13C labeled 3,4,6-Tri-O-acetyl-D-glucal[1].
Tolmetin is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin is a non-steroidal anti-inflammatory drug (NSAID)[1][2].
2-Methylpiperazine-d10 is the deuterium labeled 2-Methylpiperazine[1].
AZ1729 is a novel direct, positive allosteric modulator of fatty acid receptor FFA2 (pEC50=6.9), selectively activates Gi signaling but lacks the capacity to activate FFA2 Gq/G11-mediated signaling pathways; produces stimulation of [35S]GTPγS binding with pEC50 7.23, inhibits β-adrenoreceptor agonist-promoted lipolysis in primary mouse adipocytes and promotes chemotaxis of isolated human neutrophils.
D-64131 is a novel inhibitor of Tubulin polymerization that competitively binds with [(3)H]colchicine to αβ-Tubulin. IC50 Value: N/ATarget: Microtubule/Tubulinin vitro: D-64131 is cytotoxic and inhibits tumor cell proliferation in vitro (IC50 = 74 nM). D-64131 prevents growth of tumor models in mice following oral administration in vivo. D-64131 has significant potential in cancer treatment. The proliferation of tumor cells from 12 of 14 different organs and tissues was inhibited with mean IC(50)s of 62 nM by D-64131.in vivo: In animal studies, no signs of systemic toxicity were observed after p.o. dosages of up to 400 mg/kg of D-64131. In xenograft experiments with the human amelanoic melanoma MEXF 989, D-64131 was highly active with treatment resulting in a growth delay of 23.4 days at 400 mg/kg. Therefore, D-64131 and analogues have the potential to be developed for cancer therapy, replacing or supplementing standard therapy regimens with tubulin-targeting drugs from natural sources.
Mefox is a degradation product of folic acid (HY-16637)[1].
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties[1][2][3].
Azomycin is an antibiotic which can be active against aerobic Gram-positive and Gram-negative bacteria.
JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.
DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. DIF-3 exerts a strong antiproliferative effect on the human cervical cancer cell line HeLa by inducing cyclin D1 degradation and inhibiting cyclin D1 mRNA expression[1].
Cyclo(D-Ala-L-Pro) is a cyclodipeptide[1].
Isolupalbigenin is an inhibitor of NO. Isolupalbigenin has anti-proliferative activity on HL-60 cells with an IC50 of 5.1 μM[1].
D-(+)-Trehalose-d14 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi[1][2].
VU0364770 is an allosteric of metabotropic glutamate receptor 4 (mGlu4) modulator, which exhibits a EC50 of 1.1±0.2 μM at human mGlu4.