sp 10

Peptide originally derived from SARS-CoV Spike (S) protein; corresponds to amino acid residues 668 to 679. Highly potent inhibitor of SARS-CoV S protein and ACE2 interaction (IC50 = 1.88 nM in biochemical assay). Inhibits interaction of SARS-CoV S protein and Vero E6 cells in vitro. Please note, this peptide displays 80% sequence identity to homologous site on SARS-CoV-2 S-protein (residues 689-697).

exo-β-1,3-Xylosidase, Streptomyces sp. SWU10 (EC.3.2.1.72), is an endo-xylanase capable of degrading xylan into various xylooligosaccharides.

Guanidine hydrochloride (Aminoformamidine Hydrochloride) is a strong organic base existing primarily as guanidium ions at physiological pH. It is found in the urine as a normal product of protein metabolism. It is also used in laboratory research as a protein denaturant.

Dsp-1053 is a powerful SERT (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonizing activity.

Spautin-1 is an autophagy inhibitor that suppresses the deubiquitination activity of ubiquitin-specific peptidase USP10 and USP13. Spautin-1 inhibits UPR and exhibits preferential cytotoxicity in glucose-starved cancer cells.

USP10-IN-3 (compound D1) is a potent inhibitor of USP10, with an IC50 of 7.2 µM. It can suppress cell proliferation, induce apoptosis, and cause cell cycle arrest in the S phase.

USP10-IN-4 is a potent inhibitor of ubiquitin-specific protease 10 (USP10), with an IC50 of 10.87 μM and a Kd of 365 nM. It effectively inhibits USP10-mediated proteasomal degradation of downstream proteins YAP and p53, leading to the downregulation of CDK4 in the p53 signaling pathway. USP10-IN-4 promotes apoptosis in liver cancer cells (apoptosis) and inhibits the initiation and progression of liver cancer. It is applicable in the study of hepatocellular carcinoma (HCC).

WW-104 is a selective USP10 inhibitor with an IC50 of 16.75 μM and a Kd of 237 nM. It can induce G2 phase arrest and apoptosis (Apoptosis) and exhibits significant antiproliferative effects on cell lines overexpressing USP10. Additionally, WW-104 demonstrates anticancer activity against hepatocellular carcinoma.

KNK437 (Heat Shock Protein Inhibitor I), a pan-HSP inhibitor, suppresses the synthesis of inducible HSPs(HSP105, HSP72, and HSP40).

SP-100030 is a dual inhibitor of NF-κB and activator protein-1 (AP-1), demonstrating potent inhibition with IC50 values of 50 nM for both. It effectively reduces the production of IL-2, IL-8, and TNF-alpha in Jurkat and other T cell lines. Additionally, SP-100030 has been shown to decrease the severity of murine collagen-induced arthritis (CIA).

DSP-1053, a benzylpiperidine derivative, is a potent serotonin transporter (SERT) inhibitor with a dissociation constant (K_i) of 1.02 nM and exhibits partial agonistic activity at the 5-HT_1A receptor with a K_i of 5.05 nM, indicating its potential as an antidepressant.

Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis.

SP100030 analogue 1 (compound 11) is a selective transcription activation (SITA) inhibitor within the SP100030 class, capable of inhibiting XPO1-dependent upregulation of IL2 in a Jurkat-based IL2-Luc reporter assay, with an EC50 of 137 nM.

Procainamide-d4 (Procaine amide-d4) is a deuterium-labeled version of Procainamide, which is a potent and specific inhibitor of DNA methyltransferase 1 (DNMT1). It reactivates tumor suppressor gene expression by demethylating these genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Additionally, it relaxes tracheal smooth muscle by activating the potassium channel and is applicable in research related to cancer and arrhythmia.

Fmoc-Cys-Asp10 (TFA) is a non-releasable oligopeptide linker involved in synthesizing releasable oligopeptide linkers. These releasable linkers are used to deliver drugs to fracture-targeting oligopeptides, thereby reducing the healing time of fractured femurs.

Beauveriolide III, a cyclodepsipeptide found in Beauveria fungi, inhibits lipid droplet formation (at 3-10 μM) and cholesterol synthesis (IC50=0.41 μM). This compound also suppresses acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity (IC50=5.5 μM) and reduces atherosclerotic lesion size in Ldlr-/- and ApoE-/- mouse models (25-50 mg/kg).

COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg/kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.

SP-Chymostatin B is a potent inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases. It weakly inhibits human leucocyte elastase. It is effective at a final concentra

19,20-Epoxycytochalasin D is a fungal metabolite that has been found in the endophytic fungus Nemania sp. UM10M. It is active against the chloroquine-sensitive and -resistant strains of P. falciparum (MIC = 0.4 ng/ml for both) without inducing cytotoxicity in Vero cells. It is cytotoxic to BT-549, LLC-PK11, and P388 cells (IC50s = 7.84, 8.4, and 0.16 µM, respectively) but not SK-MEL, KB, or SKOV3 cells up to a concentration of 10 µM.

Benastatin C is a polyketide synthase-derived benastatin found in [Streptomyces] with diverse biological activities. It inhibits glutathione S-transferase (GST; IC50 = 24 μg/ml for the rat liver enzyme) and the esterase activity of isolated porcine pancreatic lipase (IC50 = 10 μg/ml). Benastatin C also increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner.

Beauveriolide I is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.78 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide I also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 6 μM).2 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Nocardamine is a ferrioxamine siderophore that has been found inStreptomycesand has diverse biological activities.1,2,3,4It chelates iron in a chrome azurol S assay (IC50= 9.9 μM).1Nocardamine inhibitsM. smegmatisandM. bovisbiofilm formation (MIC = 10 μM for both), an effect that can be reversed by iron.2It is cytotoxic to T47D, SK-MEL-5, SK-MEL-28, and RPMI-7951 cancer cells (IC50s = 6, 18, 12, and 14 μM, respectively).3Nocardamine also induces morphological changes in BM-N4 insect cells.4 1.Lopez, J.A.V., Nogawa, T., Futamura, Y., et al.Nocardamin glucuronide, a new member of the ferrioxamine siderophores isolated from the ascamycin-producing strain Streptomyces sp. 80H647J. Antibiot. (Tokyo)72(12)991-995(2019) 2.Ishida, S., Arai, M., Niikawa, H., et al.Inhibitory effect of cyclic trihydroxamate siderophore, desferrioxamine E, on the biofilm formation of Mycobacterium speciesBiol. Pharm. Bull.34(6)917-920(2011) 3.Kalinovskaya, N.I., Romaneko, L.A., Irisawa, T., et al.Marine isolate Citricoccus sp. KMM 3890 as a source of a cyclic siderophore nocardamine with antitumor activityMicrobiol. Res.166(8)654-661(2011) 4.Matsubara, K., Sakuda, S., Tanaka, M., et al.Morphological changes in insect BM-N4 cells induced by nocardamineBiosci. Biotechnol. Biochem.62(10)2049-2051(1998)

Amycolatopsin C is a polyketide macrolide originally isolated fromAmycolatopsisthat has antimycobacterial and anticancer activities.1It is active againstM. bovisandM. tuberculosis(IC50s = 2.7 and 5.7 μM, respectively) but notB. subtilis,S. aureus,E. coli, orP. aeruginosa(IC50s = >30 μM for all). Amycolatopsin C is cytotoxic to SW620 colorectal and NCI H460 lung cancer cells (IC50s = 10 and 5.9 μM, respectively). 1.Khalil, Z.G., Salim, A.A., Vuong, D., et al.Amycolatopsins A-C: Antimycobacterial glycosylated polyketide macrolides from the Australian soil Amycolatopsis sp. MST-108494J. Antibiot. (Tokyo)70(12)1097-1103(2017)

10-Norparvulenone is a fungal metabolite originally isolated fromMicrosphaeropsis.1It decreases viral sialidase activity in, and increases survival of, MDCK cells infected with the mouse-adapted influenza virus A/PR/8/34 when used at a concentration of 1 μg/ml. 1.Fukami, A., Nakamura, T., Kim, Y.P., et al.A new anti-influenza virus antibiotic, 10-norparvulenone from Microsphaeropsis sp. FO-5050J. Antibiot. (Tokyo)53(10)1215-1218(2000)