Cuspidiol (compound 3) is a CH2Cl2 extract of Fagara zanthoxyloides Lam. Cuspidiol has antifungal and antioxidative activity[1].
SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia[1].
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM[1].
Tri(Amino-PEG5-amide)-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ikarisoside F is a flavonol glycoside from Vancouveria hexandra; could bind to AdoHcy hydrolase.
BTA-2, a benzothiazole dye, is structurally similar to thioflavin T (ThT), which exhibits an enhanced fluorescence signal when bound to amyloid fibrils. BTA-2 has distinct absorption and emission characteristics in solution and when bound to amyloid fibrils, which makes it can used for identifying amyloid fibrils using spectroscopy[1].
L-Tryptophanylglycine (Trp-gly) is a dipeptide that can inhibit Ceronapril uptake by Caco-2 cells, with a Ki of 7.19 mM[1].
Sivelestat sodium(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.IC50 value: 44 nM [1]Target: neutrophil elastaseONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase [1]. Sivelestat sodium hydrate is an anti-neutrophil elastase inhibitor and may be one of the treatment options for acute respiratory failure due to pneumocystis pneumonia in AIDS patients [2].
Coronaridine, an iboga type alkaloid, inhibits the wnt signaling pathway by decreasing β-catenin expression[1].
Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.IC50 value:Target: 3 β-HSDTrilostane is an inhibitor of 3 β-hydroxysteroid dehydrogenase (3-β-HSD or delta 5-delta 4-isomerase), an essential enzyme for the biosynthesis of all classes of hormonal steroids. It has been used in the treatment of Cushing′s syndrome for stopping the production of cortisol, and is currently approved for dogs in the US, but is still a human drug in the UK and other countries. It is being investigated as a possible treatment for both breast cancer and prostate cancer to prevent the synthesis of estrogens and androgens from endogenous precursors. It has also been used to inhibit endogenous production of progesterone in research studies.
TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9.
Peraquinsin is a MK2 activator. Peraquinsin can be used for the research of vascular disorder or endothelial barrier disorder. Peraquinsin also is an antihypertensive agent[1].
MC-Val-Ala-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
NLRP3 modulators 1 is the potent modulator of NLRP3. NLRP3 modulators 1 agonizes or partially agonizes NLRP3 that are useful for researching a condition, disease or disorder in which a decrease in LRP3 activity contributes to the pathology (extracted from patent WO2017184746A1, compound 107)[1].
MK-2206 free base is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206 free base. MK-2206 free base has anticancer activities[1][2].
Karounidiol is a triterpenoid that can be found in Trichosanthes kirilowii. [1].
KC01 is a potent and selective inhibitor of ABHD16A with IC50 of 90 nM for hABHD16A, 520 nM for mABHD16A; shows significant reductions in all detected cellular lyso-PSs, no activity in other lipids, including PSs, PCs, PEs, lyso-PCs, lyso-PEs, or monoacylglycerols (MAGs); decreases both lyso-PSs and lipopolysaccharide-induced cytokine production in mouse macrophages.
Mtb-cyt-bd oxidase-IN-2 is an inhibitor of Mycobacterium tuberculosis cytochrome bd oxidase (Mtb cyt-bd oxidase) with an IC50 value of 0.67 μM. Mtb-cyt-bd oxidase-IN-2 inhibits the growth of Mycobacterium tuberculosis with a MIC value of 256 μM. Mtb-cyt-bd oxidase-IN-2 can be used for the research of infection[1].
Cauloside C is a triterpene glycoside isolated from Caulophyllum robustum Max. Cauloside C exerts anti-inflammatory effects through the inhibition of expression of iNOS and proinflammatory cytokines[1].
Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity[1].
N-Phenylacrylamide is a special polymer showing high affinity with Ochratoxin A, a colorless and crystalline mycotoxin compound. N-Phenylacrylamide can be applied in the field of mycotoxin extraction, and be used for the security research of agricultural commodities and foods made from cereals and grapes[1].
3-Hydroxycarbofuran, a major metabolite of Carbofuran, is a reversible acetylcholinesterase (AChE) inhibitor[1].
Adarotene is an effective apoptosis inducer, which surprisingly produces DNA damage and exhibites a potent antiproliferative activity on a large panel of human tumor cells.
Echinocystic acid a pentacyclic triterpene isolated from the fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory and anti-tumor properties. In vitro: Echinocystic acid (EA) inhibit the formation of osteoclast. EA inhibit RANKL-induced NF-κB activation and ERK phosphorylation in BMMs. [1] EA inhibit IL-1β-induced inflammation in chondrocytes. [2]In vivo: Echinocystic acid reduces reserpine-induced pain/depression dyad in mice. [3]
PROTAC KRAS G12C degrader-3 (Comp 283) is a potent KRAS G12C degrader for cancer research[1].
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells[1].
Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal is a glucocorticoid receptor agonist. Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used in anti-CD40 antibody drug conjugate (ADC). Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Mal can be used for the research of inflammation and immune regulation[1].
Nitric oxide production-IN-1（Compound 1） is a inhibitor of NO Production which isolated from Tupistra chinensis. Nitric oxide production-IN-1（Compound 1） inhibits NO production in rat abdomen macrophages induced by lipopolysaccharide[1]
EGFR-IN-51 (Compound 6) is a potent EGFR inhibitor with IC50 values of 0.493, 102.60 and 461.63 µM against EGFR, EGFR L858R-TK and EGFR T790M-TK, respectively. EGFR-IN-51 shows cytotoxic activity against cancer cell lines and induces apoptosis[1].
HP210 is a selective glucocorticoid receptor modulator (SGRM). HP210 can inhibit the mRNA expression of IL-1β and IL-6. HP210 has the potential to study inflammation-related diseases[1].