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m-30

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  • Inhibitors & Agonists
    34
    TargetMol | Inhibitors_Agonists
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    4
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    3
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CBM-301940
CBM301940
T68410902146-11-6
CBM-301940 (compound 5) is a potent and orally active MCD (Malonyl-CoA Decarboxylase) inhibitor with IC50=23 nM that improves cardiac efficiency and function with cardioprotective properties in a rat cardiac ischemia reperfusion model.
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8-10 weeks
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UM-3006
T2018661927013-87-3
UM-3006 is a potent TLR7 8 agonist that enhances immune responses by activating the TLR signaling pathway. This compound holds significant research and application potential in the fields of vaccine adjuvants and immune diseases.
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10-14 weeks
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AFM-30a hydrochloride
T63423
AFM-30a hydrochloride is a potent and highly selective inhibitor of protein arginine deiminase 2 (PAD2). AFM-30a hydrochloride binds to PAD2 (EC50: 9.5 μM) and inhibits H3 guanylation (EC50: 0.4 μM). AFM-30a hydrochloride can be used to study certain cancers and autoimmune diseases such as rheumatoid arthritis (RA), multiple sclerosis, lupus, and ulcerative colitis.
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10-14 weeks
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ZM-306416 hydrochloride
T88548196603-47-1
ZM-306416 (CB 676475) hydrochloride is a potent inhibitor of VEGFR, demonstrating IC50 values of 0.1 µM for KDR and 2 µM for Flt. Additionally, this compound acts as an inhibitor of EGFR with an IC50 value of less than 10 nM.
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10-14 weeks
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HM-30181 mesylate monohydrate
T91732097125-58-9
HM-30181 mesylate monohydrate is an oral P-glycoprotein (P-gp) inhibitor, used to enhance the oral bioavailability of P-gp substrate drugs.
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Fervenulin
T15277483-57-8
Fervenulin is isolated from a nematicidal actinomycete Streptomyces sp. CMU-MH021 with nematicidal activity. It also inhibits egg hatch and J2 mortality of M. incognita (MICs: 30 μg mL and 120 μg mL, respectively).
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6-8 weeks
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TargetMol | Inhibitor Sale
Rigosertib sodium
Rigosertib, Estybon, ON-01910
T5818592542-60-4
Rigosertib sodium (ON-01910), a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.
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TargetMol | Inhibitor Sale
GTP-14564
T7185734823-86-4
GTP-14564 is a novel tyrosine kinase inhibitor that also inhibits wt-FLT3 and ITD-FLT3. GTP-14564 inhibits the growth of interleukin-3-independent Ba F1 expressing ITD-FLT3 at 3 μ m, whereas a 30-fold higher concentration of GTP-14564 is required to inhibit the FLT3 ligand-dependent growth (wt-FLT3) of Ba F3 expressing wild-type FLT3. F3 expressing wild-type FLT3 (wt-FLT3).
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6-8 weeks
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TargetMol | Inhibitor Sale
RIPK2 IN 10W
T2040132789711-40-4
The IC50 value of RIPK2 IN 10W for RIPK2 is 0.6 nM, which is more than 50000 times higher than RIPK1 (IC50>30 μ M). RIPK2 IN 10W has high kinase selectivity, inhibits RIPK2, and prevents NOD induced cytokine production after stimulation with muramyl dipeptide (MDP). RIPK2 as a therapeutic target has shown potential in treating inflammatory bowel disease.
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7-10 days
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7-oxo Staurosporine
T35423125035-83-8
7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits growth of the mycelial, but not yeast form of C. albicans, C. krusei, C. tropicalis, and C. lusitaniae (MICs = 3.1-25 μg/ml). It increases sphingomyelin synthesis in CHO-K1 cells when used at a concentration of 50 nM.
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β-Defensin-2 (human) (trifluoroacetate salt)
T35451
β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes when used at concentrations of 30, 10, and 40 μg/ml, respectively. β-Defensin-2 induces IL-31 production by human peripheral blood-derived mast cellsin vitrowhen used at a concentration of 10 μg/ml and by rat mast cellsin vivofollowing a 500 ng intradermal dose.4Expression of β-defensin-2 is increased in psoriatic skin and chronic wounds.5,6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 3.Niyonsaba, F., Ushio, H., Nakano, N., et al.Antimicrobial peptides human β-defensins stimulate epidermal keratinocyte migration, proliferation and production of proinflammatory cytokines and chemokinesJ. Invest. Dermatol.127(3)594-604(2007) 4.Niyonsaba, F., Ushio, H., Hara, M., et al.Antimicrobial peptides human β-defensins and cathelicidin LL-37 induce the secretion of a pruritogenic cytokine IL-31 by human mast cellsJ. Immunol.184(7)3526-3534(2010) 5.Huh, W.-K., Oono, T., Shirafuji, Y., et al.Dynamic alteration of human β-defensin 2 localization from cytoplasm to intercellular space in psoriatic skinJ. Mol. Med. (Berl.)80(10)678-684(2002) 6.Butmarc, J., Yufit, T., Carson, P., et al.Human β-defensin-2 expression is increased in chronic woundsWound Repair Regen.12(4)439-443(2004)
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6-Prenylindole
T3548523158-16-9
6-Prenylindole is a bacterial metabolite that has been found in Streptomyces and has antifungal and antimalarial properties.1 It is active against A. brassicicola strain TP-F0423 and F. oxysporum f. sp. tulipae TU-4-2 (15 and 30 μg/disc in the paper disc assay), and also drug-resistant P. falciparum strain K1 (IC50 = 21 μg/ml).2 |1. Sasaki, T., Igarashi, Y., Ogawa, M., et al. Identification of 6-prenylindole as an antifungal metabolite of Streptomyces sp. TP-A0595 and synthesis and bioactivity of 6-substituted indoles. J. Antibiot. (Tokyo) 55(11), 1009-1012 (2002).|2. Nkunya, M.H., Makangara, J.J., and Jonker, S.A. Prenylindoles from Tanzanian Monodora and Isolona species. Nat. Prod. Res. 18(3), 253-258 (2004).
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Emestrin
T3577297816-62-1
Emestrin, a mycotoxin originally isolated from *E. striata*, exhibits antimicrobial, immunomodulatory, and cytotoxic activities. It is effective against fungi *C. albicans* and *C. neoformans*, and bacteria *E. coli*, *S. aureus*, and methicillin-resistant *S. aureus* (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg ml, respectively). Emestrin acts as a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes). At 0.1 μg ml, it induces apoptosis in HL-60 cells and causes necrosis in heart, thymus, and liver tissues in mice at doses of 18-30 mg kg.
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Palmitic acid-1,2,3,4-13C4
Palmitic Acid-13C (C1, C2, C3, and C4 labeled)
T35790287100-89-4
Palmitic acid-13C (C1, C2, C3, and C4 labeled) is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a common 16-carbon saturated fat that represents 10-20% of human dietary fat intake and comprises approximately 25 and 65% of human total plasma lipids and saturated fatty acids, respectively.1,2Acylation of palmitic acid to proteins facilitates anchoring of membrane-bound proteins to the lipid bilayer and trafficking of intracellular proteins, promotes protein-vesicle interactions, and regulates various G protein-coupled receptor functions.1Red blood cell palmitic acid levels are increased in patients with metabolic syndrome compared to patients without metabolic syndrome and are also increased in the plasma of patients with type 2 diabetes compared to individuals without diabetes.3,4 1.Fatima, S., Hu, X., Gong, R.-H., et al.Palmitic acid is an intracellular signaling molecule involved in disease developmentCell. Mol. Life Sci.76(13)2547-2557(2019) 2.Santos, M.J., López-Jurado, M., Llopis, J., et al.Influence of dietary supplementation with fish oil on plasma fatty acid composition in coronary heart disease patientsAnn. Nutr. Metab.39(1)52-62(1995) 3.Yi, L.-Z., He, J., Liang, Y.-Z., et al.Plasma fatty acid metabolic profiling and biomarkers of type 2 diabetes mellitus based on GC/MS and PLS-LDAFEBS Lett.580(30)6837-6845(2006) 4.Kabagambe, E.K., Tsai, M.Y., Hopkins, P.N., et al.Erythrocyte fatty acid composition and the metabolic syndrome: A National Heart, Lung, and Blood Institute GOLDN studyClin. Chem.54(1)154-162(2008)
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rac-1,2-bis-Palmitoyl-3-chloropropanediol
T3589351930-97-3
rac-1,2-bis-Palmitoyl-3-chloropropanediol is a 3-monochloropropane-1,2-diol (3-MCPD) ester.1It has been found as a contaminant in edible olive oils, with the lowest and highest concentrations in extra virgin and olive pomace oils, respectively.rac-1,2-bis-Palmitoyl-3-chloropropanediol has also been found in cottonseed and palm oils, as well as in shortening.2It induces renal tubular necrosis and a decrease in spermatids, but no gross pathological changes, in mice.3 1.Hung, W.-C., Peng, G.-J., Tsai, W.-J., et al.Identification of 3-MCPD esters to verify the adulteration of extra virgin olive oilFood Addit. Contam. Part B Surveill.10(3)233-239(2017) 2.MacMahon, S., Begley, T.H., and Diachenko, G.W.Occurrence of 3-MCPD and glycidyl esters in edible oils in the United StatesFood Addit. Contam. Part A. Chem. Anal. Control Expo. Risk Assess.30(12)2081-2092(2013) 3.Liu, M., Gao, B.-Y., Qin, F., et al.Acute oral toxicity of 3-MCPD mono- and di-palmitic esters in Swiss mice and their cytotoxicity in NRK-52E rat kidney cellsFood Chem. Toxicol.50(10)3785-3791(2012)
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PKI-179
T360841197160-28-3
PKI-179 is a potent, orally active compound that functions as a dual PI3K mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].
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6-8 weeks
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Integrin modulator 1
T362912023788-32-9
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1, and increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM[1].
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6-8 weeks
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C6 Urea Ceramide
T36321486991-52-0
C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It inhibits proliferation of, and induces apoptosis and autophagy in HT-29, but not non-cancerous RIE-1, cells when used at concentrations of 5 and 10 μM. C6 urea ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the 20S proteasome in HT-29 and HCT116, but not RIE-1, cells. It reduces tumor growth and increases C16, C18, C20, and C24 ceramide levels in tumor tissue in an HT-29 mouse xenograft model when administered at doses of 1.25, 2.5, and 5 mg/kg for five days. |1. García-Barros, M., Coant, N., Kawamori, T., et al. Role of neutral ceramidase in colon cancer. FASEB J. 30(12), 4159-4171 (2016).
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8-10 weeks
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Suc-AAP-Abu-pNA
T36351108392-27-4
Suc-AAP-Abu-pNA is a specific substrate for pancreatic elastase (Km = 100 μM; Kcat/Km = 35,300 s-1 M-1 for rat pancreatic elastase; Km = 30 μM; Kcat/Km = 351,000 s- 1 M-1 for porcine pancreatic elastase).
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DMU-212
T36674134029-62-2
DMU-212 is a methylated derivative of resveratrol with antimitotic, anti-proliferative, antioxidant, and apoptosis-promoting activities. It induces mitotic arrest, apoptosis, and activation of ERK1 2 protein and has oral activity[1][2]. DMU-212 (0.3125-40 μM) inhibits the growth of human melanoma cells (A375, MeWo, Bro, M5)[1]. At concentrations of 30-50 μM over 24 hours, it upregulates cell cycle inhibitors, induces apoptosis, and activates ERK in A375 cells[1]. DMU-212 also induces G2 M arrest and apoptosis in cancer cells[1]. In a xenograft model of human ovarian cancer with six-week-old SCID female mice (20-24 g), DMU-212 (50 mg kg, administered orally three times a week for 14 days) inhibits tumor growth[2]. [1]. Vasilis Pericles Androutsopoulos, et al. Activation of ERK1 2 is required for the antimitotic activity of the resveratrol analogue 3,4,5,4'-tetramethoxystilbene (DMU-212) in human melanoma cells. Exp Dermatol. 2015 Aug;24(8):632-4. [2]. Hanna Piotrowska, et al. DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer. Biomed Pharmacother. 2014 May;68(4):397-400.
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TAS-103
T36695174634-08-3
TAS-103 is a dual inhibitor of DNA topoisomerase I II, utilized in cancer research.
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RWJ-56110 dihydrochloride
T367172387505-58-8
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 μM), showing no effect on PAR-2, PAR-3, or PAR-4. It inhibits the aggregation of human platelets induced by SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), with high selectivity relative to U46619. RWJ-56110 dihydrochloride also blocks angiogenesis and the formation of new vessels in vivo, and induces cell apoptosis[1][2].
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Pancuronium (bromide hydrate)
T37702
Pancuronium is an aminosteroid antagonist of muscle-type nicotinic acetylcholine receptors (nAChRs) with an IC50value of 14.8 nM using patch clamp electrophysiology in BOSC23 cells expressing mouse nAChRs.1It acts as a non-depolarizing neuromuscular blocking agent.2Pancuronium enhances anesthesia induced by isoflurane , reducing immobilization with an ED50value of 1.62 μg/kg.3 1.Liu, M., and Dilger, J.P.Site selectivity of competitive antagonists for the mouse adult muscle nicotinic acetylcholine receptorMol. Pharmacol.75(1)166-173(2009) 2.Buckett, W.R., Marjoribanks, C.E., Marwick, F.A., et al.The pharmacology of pancuronium bromide (Org.NA97), a new potent steroidal neuromuscular blocking agentBr. J. Pharmacol. Chemother.32(3)671-682(1968) 3.Miyazaki, Y., Sunaga, H., Hobo, S., et al.Pancuronium enhances isoflurane anesthesia in rats via inhibition of cerebral nicotinic acetylcholine receptorsJ. Anesth.30(4)671-676(2016)
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pf-04449613
T378001236858-52-8
PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neuronsin vivo.2It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose. 1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-9068(2012) 2.Lai, B., Li, M., Hu, A., et al.The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learningDev. Neurobiol.78(9)859-872(2018)
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