sp 5

Sp-Adenosine-5'-O-(1-thiodiphosphate) (Sp-ADP-α-S), an isomer of the sulfur-containing nucleotide derivative ADP-α-S, functions as an inhibitor of phosphorylase kinase with an inhibition constant (Ki) of 0.53 µM. This compound also promotes aggregation of isolated human platelets with an effective concentration (EC50) of 20 µM and induces relaxation in carbamoylcholine-precontracted guinea pig taenia coli with an EC50 of 58.9 µM.

Sp-Adenosine-5'-O-(1-thiotriphosphate) (Sp-ATP-α-S), an isomer of the ATP-α-S sulfur-containing nucleotide derivative and a purinergic P2Y1 receptor agonist, effectively increases calcium mobilization in HEK293 cells harboring the P2Y1 receptor with an EC50 of 9.4 nM for the human receptor. It also inhibits ADP-induced human isolated platelet aggregation with a Ki value of 4 μM and prompts relaxation in carbamoylcholine-tightened guinea pig taenia coli, achieving an EC50 of 426 nM.

Sp-Uridine-5'-O-(1-thiotriphosphate) (Sp-UTP-α-S) acts as a nucleotide agonist for purinergic Y2 (P2Y2) and P2Y4 receptors, efficiently inducing inositol phosphate accumulation in 1321N1 astrocytoma cells that express these receptors, with half-maximal effective concentrations (EC50s) of 14 µM and 81 µM, respectively.

Sp-2'-Deoxycytidine-5'-O-(1-thiotriphosphate) (Sp-dCTP-α-S), an isomer of the sulfur-containing nucleotide derivative dCTP-α-S, functions as an inhibitor of the deoxynucleoside triphosphate triphosphohydrolase SAMHD1, with an inhibition constant (Ki) of 6.3 µM.

Sp-2'-Deoxyguanosine-5'-O-(1-thiotriphosphate), a sulfur-containing isomer of 2'-deoxyguanosine-5'-O-triphosphate (dGTP), functions as an inhibitor of the deoxynucleoside triphosphate triphosphohydrolase SAMHD1, with an inhibitory constant (Ki) of 820 nM.

Sp-Guanosine-5'-O-(1-thiotriphosphate) (Sp-GTP-α-S), an isomer of the sulfur-containing nucleotide derivative GTP-α-S, demonstrates the ability to bind tubulin and facilitate microtubule assembly in cell-free assays at a concentration of 20 mM.

Sp-Thymidine-5'-O-(1-thiotriphosphate) (Sp-TTP-α-S), an isomer of the sulfur-containing nucleotide derivative TTP-α-S, exhibits affinity for HIV-1 reverse transcriptase with dissociation constants (Kds) of 2.88, 4.23, and 20.21 µM in the presence of magnesium, manganate, and cobalt, respectively. Additionally, Sp-TTP-α-S effectively inhibits the enzyme deoxynucleoside triphosphate triphosphohydrolase SAMHD1 with an inhibition constant (Ki) of 46 nM.

Hymenidin, an alkaloid isolated from the Okinawan sponge Hymeniacidon sp. is a 5-hydroxytryptaminergic receptor antagonist and voltage-gated potassium channel inhibitor with potential antiprotozoal effects.It selectively binds to FOXO1 DNA and reduces depolarization-induced elevation of cellular calcium.

Hymenidin HCl is a natural alkaloid isolated from Hymeniacidon sp. and acts as a serotonin (5-HT) receptor antagonist. Hymenidin HCl inhibits voltage-gated potassium channels (Kv), exhibits selective inhibition of CDK5, affects cellular signaling, and induces apoptosis in cancer cells.

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.

L-5-BromoTryptophan (5-BrW) is an analog of the tryptophan (Trp) effector and inhibits the gelation of hemoglobin S.

Splenopentin diacetate (Splenin pentapeptide (32-36)) is a synthetic immunomodulating peptide and can reproduce the biological activities of splenin and thymic hormone thymopoietin.

Berlopentin is splenopentin analog used to treat HIV-positive patients. It also has immunostimulatory properties.

Splenopentin (SP-5) is a synthetic immunomodulatory peptide that can reproduce the biological activity of TP and SP, respectively.

Xanthoquinodin A1 is a fungal metabolite that has been found inHumicolaand has diverse biological activities.1,2It inhibitsE. tenellaschizont formation in BHK-21 cells with a minimum effective concentration (MEC) value of 0.02 μg/ml.1Xanthoquinodin A1 is active againstB. subtilis,M. luteus,S. aureus,A. laidlawii, andB. fragilisin a disc assay when used at a concentration of 1 mg/ml. It is also active againstB. cereus(MIC = 0.44 μM).2Xanthoquinodin A1 is cytotoxic to KB, MCF-7, and NCI H187 cancer cells. 1.Tabata, N., Suzumura, Y., Tomoda, H., et al.Xanthoquinodins, new anticoccidial agents produced by Humicola sp. Production, isolation and physico-chemical and biological propertiesJ. Antibiot. (Tokyo)46(5)749-755(1993) 2.Tantapakul, C., Promgool, T., Kanokmedhakul, K., et al.Bioactive xanthoquinodins and epipolythiodioxopiperazines from Chaetomium globosum 7s-1, an endophytic fungus isolated from Rhapis cochinchinensis (Lour.) MartNat. Prod. Res.34(4)494-502(2020)

Beauvericin A is a cyclodepsipeptide and derivative of beauvericin originally isolated fromB. bassianathat has diverse biological activities.1,2,3It is active againstM. tuberculosis(MIC = 25 μg/ml) andP. falciparum(IC50= 12 μg/ml).2Beauvericin A is toxic to brine shrimp (LD100= 32 μg/ml).3 1.Gupta, S., Montillor, C., and Hwang, Y.-S.Isolation of Novel Beauvericin Analogues from the Fungus Beauveria bassianaJ. Nat. Prod.58(5)733-738(1995) 2.Nilanonta, C., Isaka, M., Kittakoop, P., et al.Antimycobacterial and antiplasmodial cyclodepsipeptides from the insect pathogenic fungus Paecilomyces tenuipes BCC 1614Planta Med.66(8)756-758(2000) 3.Shi, S., Li, Y., Ming, Y., et al.Biological activity and chemical composition of the endophytic fungus Fusarium sp. TP-G1 obtained from the root of Dendrobium officinale Kimura et MigoRec. Nat. Prod.12(6)549-556(2018)

Benastatin A is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2,3It inhibits glutathione S-transferase (GST; Ki= 5 μM for the rat liver enzyme).2Benastatin A is active against several bacteria, including methicillin-resistantS. aureus(MRSA; MIC = 3.12 μg ml). It induces apoptosis and cell cycle arrest at the G1 G0phase in Colon 26 mouse colon cancer cells when used at concentrations of 20 and 16 μM, respectively.3 1.Xu, Z., Schenk, A., and Hertweck, C.Molecular analysis of the benastatin biosynthetic pathway and genetic engineering of altered fatty acid-polyketide hybridsJ. Am. Chem. Soc.129(18)6022-6030(2007) 2.Aoyagi, T., Aoyama, T., Kojima, F., et al.Benastatins A and B, new inhibitors of glutathione S-transferase, produced by Streptomyces sp. MI384-DF12. I. Taxonomy, production, isolation, physico-chemical properties and biological activitiesJ. Antibiot. (Tokyo)45(9)1385-1390(1992) 3.Kakizaki, I., Ookawa, K., Ishikawa, T., et al.Induction of apoptosis and cell cycle arrest in mouse colon 26 cells by benastatin AJpn. J. Cancer Res.91(11)1161-1168(2000)

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.

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)

Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the production of reactive oxygen species (ROS) in, Hep3B human hepatocellular carcinoma cells. It does not induce cytotoxicity in RBL-2H3 mast cells at concentrations up to 100 μM. Streptochlorin prevents degranulation in antigen-stimulated mast cells, as well as inhibits Syk kinase and the Src family kinases LYN and Fyn and reduces the secretion of TNF-α and IL-4 induced by dinitrophenyl-human serum album (DNP-HSA) in RBL-2H3 mast cells. It also decreases swelling and reduces scratching behavior in a mouse model of allergic dermatitis induced by dinitrofluorobenzene (DNFB).

(SP-4-4)-2-[2-(Amino-KappaN)ethyl]phenyl-KappaC]chloro[dicyclohexyl[2',4',6'-tris(1-methylethyl)[1,1'-biphenyl]-2-yl]phosphine]-Palladium is a useful organic compound for research related to life sciences. The catalog number is T66146 and the CAS number is 1028206-56-5.

BE-16627B is a novel metalloproteinase (MP) inhibitor isolated from Streptomyces sp. BE16627B selectively inhibited MPs such as human stromelysin and 92 kD gelatinase. After the cells were cultured with BE16627B for 5 days, BE16627B inhibited MP activity in the primary culture supernatants from synovial cells in a dose-dependent fashion without showing apparent cytotoxicity or affecting the production and secretion of MPs. Its IC50 for active collagenolysis before activation by trypsin was 25 microM.

Substance P (3-11), an SP fragment peptide capable of crossing the blood-brain barrier (BBB), induces contraction in guinea pig ileum and facilitates chemotaxis in human monocytes [1] [2] [5].

1-(2-hydroxyethyl)thymine (2,4(1H,3H)-Pyrimidinedione, 1-(2-hydroxyethyl)-5-methyl-) is a marine derived natural products found in Zoanthus sp.