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SML0962   M-110 ≥98% (HPLC) M-110 is a highly isoform-selective, cell permeable and potent ATP-competitive inhibitor of the PIM kinase family that prefers PIM-3. M-110 is an inhibitor of Wnt/β-catenin signaling that act downstream of the symb-catenin destruction complex to inhibit both Wnt-induced and cancer associated constitutive Wnt signaling via destabilization of β-catenin. The compound chelates iron in vitro and in intact cells. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM, with no activity on normal human peripheral blood mononuclear cells up to 40 μM.
M3324 M100907 ≥98% (HPLC) M100907 is a selective 5-HT2A Antagonist.
SML0128 M30 dihydrochloride ≥98% (HPLC) M30 is a site-activated iron chelator and monoamine oxidase (MAO) inhibitor; with neuroprotective and anti-apoptotic activity. It is a multifunctional non-toxic, brain permeable iron chelator possessing a neuroprotective propargylamine moiety and an antioxidant-iron chelator moiety. M30 is a selective irreversible inhibitor of mitochondrial brain monoamine oxidases A and B (MAO-A and -B), providing for improved levels of neurotransmitters. It reduces oxidative damage and shows neuroprotective and neurorestorative effects in various neurodegenerative models of ALS, Alzheimer′s and Parkinson′s diseases, and is being investigated in other diseases where oxidative stress is a problem.
M5820 M344 ≥98% (HPLC), powder M344 is a HDAC inhibitor; subtype selective for HDAC6 over HDAC1. M344 inhibits HDAC (IC50 = 100 nM) and also inhibits hyperacetylation of histone H4, terminal cell differentiation, transcription (γ-globin), and tumor cell death.
SML0643   M617 trifluoroacetate salt ≥95% (HPLC) M617, galanin(1–13)-Gln14-bradykinin(2–9)amide, is a chimeric peptide that acts as a selective agonist for the Galanin GalR1 receptor. M617 shows 25-fold specificity for GalR1with Ki values of 0.23 for GAL1 and 5.71 nM for GAL2.
SML0893   M8-B hydrochloride ≥98% (HPLC) M8-B is a selective and potent antagonist of the transient receptor potential melastatin-8 (TRPM8) channel. M8-B blocked cold-induced and icilin or methol-induced activation of rat, human, and murine TRPM8 channels with IC50 values in rat ranging from 7.8 nM to 64.3 nM, and it did not block other TRP channels (IC50 values > 20 mM). M8-B decreased deep body temperature in both mice and rats, showing that blockade of TRPM8 receptor might be used to induce therapeutic hypothermia, an effective treatment in cardiac arrest.
SML1519 Macelignan ≥98% (HPLC) Macelignan is a neuroprotective lingan isolated from nutmeg (Myristica fragrans) that protects dopaminergic neurons from inflammatory degeneration. Apparently, the neuroprotective effect of macelignan is mediated by PPARγ activation and arginase-1 expression. Macelignan inhibits LPS induced production of NO as well and inflammatory cytokines including TNF and IL- 1β in primary cultures of microglia.
M8193 MADAM dihydrochloride High affinity ligand for the serotonin transporter SERT
SML1409 Madrasin ≥98% (HPLC) Madrasin is a potent and cell penetrant splicing inhibitor that interferes with the early stages of spliceosome assembly. Madrasin stalls spliceosome assembly at the A complex.
M5757 Maleic acid sodium salt ~99%    
M9651 Maprotiline hydrochloride >99% (HPLC), powder Selective norepinephrine uptake inhibitor.
PZ0002 Maraviroc ≥98% (HPLC) Maraviroc is a CCR5 chemokine receptor antagonist, and antiretroviral entry inhibitor. Maraviroc inhibits HIV entry by blocking interaction of viral coat protein gp120 with the receptor.
M8437   Margatoxin ≥99%, recombinant, expressed in E. coli Voltage-gated (Kv1.3) potassium channel blocker.
M2699 Marimastat ≥98% (HPLC) Marimastat is a broad spectrum matrix metalloprotease (MMP) inhibitor
V2502   Marine venom from Chrysaora quinquecirrha (Sea Nettle) lyophilized powder Sea nettle, Chrysaora quinquecirrha venom (CQV), is toxic to the cardiac, respiratory, renal, and hepatic systems in animal models.
SML1533   (±)-Marinopyrrole A ≥95% (HPLC) Marinopyrrole A (Maritoclax) is a potent and selective inhibitor of Bcl-2 family member Mcl-1, originally isolated from marine streptomycetes for its antimicrobial activity against methicillin-resistant Staphylococcus aureus. Marinopyrrole A directly binds to Mcl-1 and targets it for proteasomal degradation. Marinopyrrole A induced apoptosis in Mcl-1-dependent cancer cells and sensitized cancer cells to ABT-737.
SML1916   Marizomib ≥95% (HPLC), (Salinospora tropica) Marizomib is a second generation proteasome inhibitor with anti-cancer activity. Marizomib binds irreversibly and potently inhibits all three 20S proteasome subunits.
M212 Mastoparan-7 ≥97% (HPLC), lyophilized powder G protein activator via Gαi and Gαo stimulation, similar to G protein-coupled receptors; peptide originally isolated from wasp venom.
M213 Mastoparan 17 ≥96.5%, lyophilized powder Inactive analog of mastoparan; useful as negative control.
M7444   Maurotoxin recombinant, expressed in E. coli, ≥95% (HPLC), lyophilized powder Maurotoxin is a 34 amino acid recombinant toxin, originally isolated from the venom of the scorpion Scorpio Maurus palmatus; a member of the α-KTx6.2 scorpion toxin family. It blocks voltage-gated potassium channels (KV1.1/KCNA1, KV1.2/KCNA2, and KV1.3/KCNA3) and inhibits apamin-sensitive small conductance calcium-activated channels (SK channels), particularly KCa3.1(IKca1, SK4).
SML1683 MAY0132 ≥98% (HPLC) MAY0132 is a selective inhibitor of the cAMP-binding Protein EPAC2 (Exchange Protein directly Activated by Cyclic AMP) subtype 2. MAY0132 has a submicromolar IC50 value at EPAC2, and no activity at EPAC1. MAY0132 is believed to act at an allosteric site, perhaps at the interface of both cAMP binding domains in the EPAC2 protein.
M2017 Mazindol ≥98% (TLC), powder Anorectic agent; inhibits the dopamine, norepinephrine and serotonin transporters with Kis of 27.6 nM, 3.2 nM, and 153 nM, respectively.
human ... SLC6A2(6530), SLC6A3(6531), SLC6A4(6532)
rat ... Htr1a(24473), Htr2a(29595), Slc6a3(24898), Slc6a4(25553)
M2449 MB-3 ≥95% (HPLC) MB-3 is a Gcn5 HAT (Histone Acetyltransferase) inhibitor; anti-inflammatory, anti-carcinogenic.
SML0439 MBCQ ≥98% (HPLC) MBCQ is selective inhibitor of cGMP-specific phosphodiesterase PDE V; IC50=19 nM.
M0571 MBP (85-99) peptide antagonist trifluoroacetate salt 95% (HPLC), lyophilized powder MBP (85-99) peptide antagonist inhibits the binding of MBP 85-99 to HLA-DR2 and IL-2 and is a tool for MS research. The peptide antagonist is a 15-mer peptide that competes with Myelin Basic Protein MBP (85-99), the immunodominant epitope of MBP and major candidate autoantigen in multiple sclerosis (MS).
SML0064   MBX-102 ≥98% (HPLC) MBX-102 has a potent transrepression effect on PPARγ. It is an oral glucose-reducing agent and also has insulin-sensitizing properties. It is useful as treatment for type 2 diabetes. MBX-102 also lowers triglycerides in a PPARα-independent manner.
MBX-102 is a selective PPAR modulator (SPPARM) and has been shown to inhibit phosphorylation of PPARγ. MBX-102 is converted to the active form, MBX-102 acid, in vivo.
M5824 MBX-102 acid ≥98% (HPLC), powder MBX-102 is a selective PPAR modulator (SPPARM) and has been shown to inhibit phosphorylation of PPARγ.
SML2151 MBX2546 ≥98% (HPLC) MBX2546 is a non-cytotoxic (CC50 >100 μM; 283T) molecule that inhibits against influenza hemagglutinin- (HA-) mediated viral entry (IC90 = 5.7 μM against HIV/HA(H5) entry in 293T culture vs. IC90 >100 μM, 98.2 μM, and >85 μM against HIV/LASV-GP, HIV/EBOV-GP, HIV/VSV-G, respectively) by targeting group 1 HA-specific conformational epitope in the HA stem loop region. MBX2546 is shown to inhibit influenza A strains A/PR/8/34 (H1N1) and A/Florida/21/2008 (H1N1-H275Ψ) (oseltamivir-resistant strain), A/California/10/2009/H1N1, as well as high pathogenic avian influenza (HPAI) strain A/Hong Kong/H5N1 (IC50 = 0.3, 5.8, 0.55-1.5, and 3.6 μM, respectively), but not A/Texas/12/2007 (H3N2), A/Perth/16/2009 (H3N2), A/Victoria/3/75 (H3N2), A/Panama/2007/99 (H3N2), A/Sydney/05/97 (H3N2), A/California/7/04 (H3N2), A/Wyoming/03/2003 (H3N2), or influenza B strain B/Florida/4/2006 in MDCK cultures.
M1824 MC1568 ≥97% (HPLC) MC1568 is a selective class II (IIa) histone deacetylas (HDAC II) inhibitor.
SML0213 MC2050 hydrate ≥98% (HPLC) MC2050 is a water-soluble PARP-1 inhibitor. The IC50 for inhibition of PARP-1 activity is 119 nM, compared to 1.8 μM for PARP-2. MC2050 inhibits apoptosis and blocks poly ADP-ribosylation of histone H1 in hydrogen peroxide treated SH-SY5Y neuroblastoma cells.
M3819   MCA-His-Gln-Lys-Leu-Val-Phe-Phe-Ala-Lys(DNP)-NH2 trifluoroacetate salt ≥95% (HPLC), powder α-Secretase substrate I, fluorogenic.
SML1567   MCB-613 ≥98% (HPLC) MCB-613 is a pan-Steroid Receptor Coactivator (SRC) stimulator. There are three steroid receptor coactivators (SRC) that interact with transcription factors and whose overexpression is assciated with a number of cancers, particularly breast cancer. MCB-613 overstimulates SRC activity in cancer cells resulting in excessive generation of reactive oxygen species (ROS), leading to cell stress and death by a process called paraptosis. MCB-613 is a cytotoxic molecule which can kill various human cancer cell lines, like HepG2 (liver), PC-3 (prostate) and MCF-7 (breast) cells.
SML0896   MCC-555 ≥98% (HPLC) MCC-555 is a thiazolidinedione class anti-diabetic compound. In rodent models, MCC-555 attenuates the development of diabetes, maintains B-cell function and improves insulin sensitivity. The compound MCC-555 also inhibits proliferation of several cancer cell lines and reduces tumor growth in xenograft models.
C7041 McN-A-343 ≥98% (TLC) M1 muscarinic acetylcholine receptor agonist.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
rat ... Chrm1(25229)
PZ0159 MCOPPB trihydrochloride hydrate >98% (HPLC) MCOPPB trihydrochloride is a potent non-peptide nociceptin/orphanin FQ peptide (NOP)-receptor full agonist [or opioid-receptor-like-1 (ORL1) receptor agonist]. MCOPPB is the most potent novel non-peptide NOP full agonist in vitro and an orally potent anxiolytic in the mice. It inhibited signaling through the NOP receptor in the mouse brain, suggesting that it penetrated into the brain after it was orally administered. It did not affect locomotor activity or memory, nor did it contribute to ethanol-induced hypnosis.
M0199 Mdivi-1 ≥98% (HPLC), powder Mdivi-1 is a cell-permeable selective inhibitor of mitochondrial division DRP (dynamin-related GTPase) and inhibitor of the mitochondrial division dynamin (Dnm1). Mitochondrial fusion and division play important roles in the regulation of apoptosis. Mdivi-1 is the first selective inhibitor of mitochondrial division dynamins. In principle, Mdivi-1 represents a class of therapeutics for stroke, myocardial infarction, and neurodegenerative diseases.
SML0115 MDL 11939 ≥98% (HPLC) MDL 11,939 is a potent, selective and orally active 5-HT2 receptor antagonist (ASTAR). Ki values values are in the low nanomolar range for 5-HT2A with over 100-fold selectivity over 5-HT2C receptors and low or no affinity for non-5-HT2 receptors or transporters.
M182 MDL-12,330A hydrochloride ≥98% (HPLC), powder Adenylyl cyclase inhibitor.
M6690 MDL 28170 ≥95% (HPLC) MDL 28170 is a potent cell permeable calpain I and II inhibitor; reduces capsaicin-mediated cell death in cultured dorsal root ganglion neurons. Reduced occurrence of apoptosis in H2O2 and A23187 treated PC12 cells. γ-secretase-inhibitor.
human ... CAPN1(823), CAPN2(824)
M2949 MDL 72527 ≥98% (HPLC) MDL 72527is an inhibitor of polyamine oxidase (spermine oxidase SMO). It blocks the production of H2O2 and increases the cells survival. Polyamine catabolism is one of the major causes of the ROS production of prostate cells in general and androgen-induced enhancement of ROS in androgen-dependent CaP cells in particular. Reports suggest that androgen stimulation of prostate cancer results in accumulation of ROS, which lead to progression of cancer, such progression is control by MDL 72527.
SML2139 MDL-860 ≥98% (HPLC) MDL-860 is a 5-nitro-2-phenoxybenzonitrile that exerts broad-spectrum antipicornaviral activity (MIC50 from 0.1-1.5 μg/mL in HeLa cultures) by acting as an irreversible inhibitor against host phosphatidylinositol-4 kinase beta (PI4KB; PtdIns 4-kinase beta; PI4Kbeta; NPIK; PI4K92) via covalent modification of Cys646 located at the bottom of a surface pocket apart from the PI4KB active site. MCL-860 (MIC50 from 0.1-1.5 μg/mL in HeLa cultures). A pleconaril/MDL-860/oxoglaucine consecutive alternating administration (CAA), but not simultaneous daily treatment, is reported to be effective against coxsackievirus B1 infection without the development of drug resistance in newborn mice (75 mg/kg MDL-860 via s.c. every third day on the day following pleconaril and prior to oxoglaucine).
SML0254 4-MDM ≥98% (HPLC) 4-MDM augments the aminopeptidase activity of LTA4 hydrolase without affecting the conversion of LTA4 to LTB4. Treatment with 4-MDM protects mouse lungs from intranasal elastase-induced pulmonary emphysema.
SML0703   MDPPP hydrochloride ≥98% (HPLC) MDPPP hydrochloride is a potential designer drug structurally similar to cathinones, amphetamines, and pyrovalerone.
SML0999   ME0328 ≥98% (HPLC) ME0328 is a selective inhibitor of ADP-ribosyltransferase-3/poly(ADP-ribose) polymerase-3 (ARTD3/PARP3), a PARP family member involved in DNA repair. ME0328 is the most potent isomer of the four ARTD3 ADP-ribosyltransferase inhibitors. ME0328 selectively inhibits ARTD3 (IC50 of 890 nM) with weaker activity against ARTD1 and ARTD2 (IC50 6.3 and 10.8 μM, respectively), and no significant activity (IC50 >30 μM) against any other ARTD enzyme. ME0328 appears to be the first selective inhibitor of ARTD3/PARP3.
M0814 R(−)-Me5 hydriodide solid Potent sodium channel antagonist.
human ... SCN2A(6326)
M9020 Mecamylamine hydrochloride Noncompetitive nicotinic acetylcholine receptor antagonist; preferentially blocks nicotinic receptors at autonomic ganglia; crosses blood-brain barrier.
human ... CHRNA1(1134), CHRNA10(57053), CHRNA2(1135), CHRNA3(1136), CHRNA4(1137), CHRNA5(1138), CHRNA6(8973), CHRNA7(1139), CHRNA9(55584), CHRNB1(1140), CHRNB2(1141), CHRNB3(1142), CHRNB4(1143)
SML0950   Meclizine dihydrochloride ≥97% (HPLC) Meclizine has the ability to increase glycolysis and decrease cellular ATP levels in media that has glucose and galactose. It guards the kidney against ischemia-reperfusion injury. Meclizine is considered as an anti-nausea and anti-dizziness drug, was identified in a ′nutrient-sensitized′ chemical screen. In human, it acts as an agonist of pregnane X receptor (PXR). It enhances the expression of CYP3A4 (cytochrome P450 3A4) mRNA and reduces CYP3A-catalyzed testosterone 6β-hydroxylation in primary cultures of human hepatocytes.
Meclizine is a potent histamine H1 receptor antagonist that is widely used as antiemetic. Recently, meclizine was identified as an inhibitor of hepstin. Also, meclizine is a potent inhibitor of mitochondrial respiration through inhibition of cytosolic CTP:phosphoethanolamine cytidylyltransferase (Pcyt2).
M4531 Meclofenamic acid sodium salt Cyclooxygenase (IC50 = 0.6 μM) and 5-lipoxygenase (IC50 = 46.3 μM) inhibitor.
M5693 MEDICA 16 powder, ≥97% (HPLC) MEDICA 16 is an ATP-citrate lyase inhibitor and potent triacylglycerol-lowering agent. The product is hypolipidemic, antidiabetic, and shows reduced adiposity.
M1629 Medroxyprogesterone 17-acetate ≥97% (HPLC) Medroxyprogesterone 17-acetate (MPA) is a synthetic progestin used as a contraceptive, in hormone replacement therapy and for the treatment of endometriosis. It is a more potent progestin that the nonacetylated form.
human ... AR(367), ESR1(2099), ESRRA(2101), NR3C1(2908), NR3C2(4306), PGR(5241)
rat ... Ar(24208)
M4267 Mefenamic acid    
M2319 Mefloquine hydrochloride ≥98% (HPLC), powder Blocker of gap junction channels Cx36 and Cx50.
SML0087 MEGX ≥95% (HPLC) MEGX is generated by hepatic cytochrome P-450 system upon oxidative de-ethylation. Measurement of MEGX by immunoassay contributes to liver function test. MEGX possesses antiarrhythmic action and therefore extends lidocaine effect.
Monoethylglycinexylidide (MEGX) is an active metabolite of lidocaine.
SML0478   MEL-3 hydrochloride ≥98% (HPLC) MEL-3 is a potent androgen receptor antagonist from a new structural chemical class. MEL-3 has been shown to inhibit the proliferation of both androgen-dependent and androgen-independent AR-positive prostate cancer cell lines. MEL-3 was active against two mutant receptors (AR T877A and ARW741C) that have been found in patients who have become resistant to bicalutamide and hydroxyflutamide, two standard antiandrogens used in prostate cancer therapy.
M5199 Meldonium dihydrate ≥98% (HPLC), powder Meldonium is an Inhibitor of γ-butyrobetaine hydroxylase (BBOX) a key enzyme in the synthesis of carnitine.
M3935 Meloxicam sodium salt hydrate ≥98% (HPLC) Meloxicam, a member of the oxicam family, is a non-steroidal anti-inflammatory drug (NSAID) that shows 300-fold selectivity for cyclooxygenase-2 (COX-2) vs cyclooxygenase-1 (COX-1). Meloxicam has been shown to abolish thymulin-induced increases of cytokines and NGF in the liver of rats. Meloxicam also suppresses tumor growth and may be capable of antagonizing cachexia in vitro.
M9292 Memantine hydrochloride ≥98% (GC) Low-affinity NMDA glutamate receptor antagonist; stimulates dopamine release.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
M5750 Menadione sodium bisulfite ≥95% (TLC) Menadione sodium bisulfite is a water-soluble form of menadione, which belongs to the Vitamin K class of compounds. These are necessary for the biosynthesis of prothrombin and other blood clotting factors. Menadione is a prothrombogenic compound and is used as a model quinone in cell culture and in vivo investigations.

Menadione has been shown to affect gap-junctional intercellular communication by mediation of tyrosine phosphorylation. Menadione has demonstrated cytotoxic activity against a variety of cell lines and can induce apoptosis in cultured cells, such as osteoclasts and osteoblasts, via elevation of peroxide and superoxide radical levels.

An HPLC method for detection of menadione sodium bisulfite in multivitamin formulations has been published. A chemiluminescence assay for menadione sodium bisulfite in pharmaceutical preparations and biological fluids has been reported.
M3196 5-MEO-DIPT hydrochloride hydrate 5-MeO-DIPT is a tryptamine derivative. In animal behavioral studies, 5-MeO-DIPT has been shown to produce behavioral effects that are substantially similar to those of LSD, both schedule I hallucinogens.
M3142 Meperidine hydrochloride Phenylpiperidine analgesic; sedative; μ opioid receptor agonist with greater κ opioid receptor agonist activity than morphine.
M3449 Mephedrone hydrochloride Mephedrone is a synthetic stimulant, an analog of Cathinone and Methamphetamine.
UC175 (S)-(+)-Mephenytoin solid, ≥98% (HPLC) CYP2B6 & CYP2C19 substrate. Methenytoin isomer. Anticonvulsant; antiepileptic.
UC177 (±)-Mephenytoin CYP2B6 and CYP2C19 substrate; anticonvulsive, antiepileptic.
M7945 Mephetyl tetrazole ≥98% (HPLC), oil Mephetyl tetrazole is a potent and selective Kv1.5 potassium channel blocker. IC50 = 330 nM; shows selective atrial prolongation (40%) of effective refractory period (ERP), but no effect on ventricular ERP Kv1.5 channel is a molecular target for the treatment of atrial fibrillation.
SML1444 (±)-Mepivacaine hydrochloride ≥98% (HPLC) (±)-Mepivacaine hydrochloride is a local anesthetic that reversibly blocks transient Na+ inward current, as well as the steady-state K+ outward current. (±)-Mepivacaine blocks tandem pore (TASK) and Kv1.5 potassium channels in model systems.
M2824 Meptazinol hydrochloride Meptazinol entered the human pharmaceutical market as a racemic mixture in the 1980s for use as an analgesic. Its pharmacology is not completely understood; however, its analgesic properties are mostly due to its partial agonism at the mu1 opioid receptor. Due to its partial agonism, Meptazinol antagonizes morphine dependence in vivo. Its advantage over other opiates is its reduced capacity to cause addition and respiratory depression, also due to its intrinsic activity as a partial agonist. Meptazinol has been found to have additional activity as an acetylcholinesterase (AChE) inhibitor, particularly in its (-) enantiomeric form, which may partially explain its analgesic properties. AChE inhibitors are used to treat Alzheimer′s disease, providing additional interest in this compound.
SML2065   Mequitazine ≥98% (HPLC) Mequitazine is a potent, nonsedative, long-acting and selective H1 histamine receptor antagonist. Mequitazine exhibits weak anticholinergic activity.
M2070 Merbarone ≥98% (HPLC), solid Selective topoisomerase II inhibitor. Blocks topo II-mediated DNA cleavage without stabilizing DNA-topo II-cleavable complexes. Induces apoptosis in CEM cells via caspase 3 dependent mechanism.
Thiobarbituric acid with aniline joined by an amide linkage forms merbarone. It is known to prolong cell cycle progression by inducing DNA double strand breaks, retarding S phase and arresting G2 phase. This delays cell entry into mitosis. Merbarone possesses cytotoxic and genotoxic action and promotes endoreduplication. Merbarone has mild antitumor action and is also found to nephrotoxic.
M2574 Meropenem trihydrate ≥98% (HPLC) Meropenem trihydrate is an ultra-broad spectrum beta-lactam antibiotic active against both Gram-positive and Gram-negative bacteria.
SML1488   Metamizole sodium hydrate ≥98% (HPLC) Metamizole (Dipyrone) is a potent analgesic and antipyretic. Metamizole inhibits prostaglandin synthesis in both the periphery and the central nervous system. Metamizole may act as a prodrug. It is rapidly hydrolyzed to N-methyl-4-aminoantipyrine (MAA) and 4-aminoantipyrine (AA) which inhibit cyclo-oxygenase activity and can be further acylated with arachidonic acid forming compounds that bind to central and peripheral cannabinoid (CB1 and CB2) receptors and TRPV1 receptors. It is believed that these metabolites play a major role in metamizole activity. Metamizole has been withdrawn from clinical use in several countries because of a side-effect of agranulocytosis in some patients.
SML0399 D,L-Metanephrine hydrochloride ≥98% (HPLC) Metanephrine is an endogenous metabolite of ephinephrine, formed by catechol-O-methyl transferase activity. It is best known as a biomarker for cancers, as levels of free metanephrine are used to diagnose pheochromocytoma. Metanephrine was previously thought to be biologically inactive, but it is a more potent agonist at Trace amine associated receptor TAAR1 than either epinephrine or norepinephrine. Trace amine associated receptors (TAARs) are recently discovered GPCRs that are activated by endogenous trace amines (tyramine, tryptamine, synephrine, octopamine, β-phenylethylamine), which are chemically similar to monoaminergic neurotransmitters (epinephrine, norepinephrine, dopamine). Trace amines and TAARs are expressed in brain and are implicated in modulation of monoaminergic neurotransmission.
M120 Metaphit methanesulfonate salt ≥98% (HPLC), solid Metaphit methanesulfonate salt is an irreversible, non-competitive antagonist at the phencyclidine site on the NMDA receptor; sigma receptor irreversible, competitive antagonist.
human ... OPRS1(10280)
M2398 Metaproterenol hemisulfate salt β2-adrenoceptor agonist
human ... ADRB2(154)
M4773 Metaraminol (+)-bitartrate salt α-adrenoceptor agonist.
SML0199 Metaxalone ≥98% (HPLC) Metaxalone is a muscle relaxant. The mechanism of action of metaxalone in humans is not fully understood. It was suggested that it acts through general central nervous system depression.
Metaxalone is effective to relieve pain due to acute skeletal muscle pain caused due to musculoskeletal conditions and sprains.
M3668 Metergoline Antagonist at 5-HT1, 5-HT2, and 5-HT7 serotonin receptors; analgesic; antipyretic.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR7(3363)
rat ... Htr7(65032)
M0267 (±)-Methadone hydrochloride powder, ≥98% μ opioid receptor agonist that desensitizes both the μ opioid receptor and the δ opioid receptor on chronic exposure; narcotic analgesic, characterized by a gradual onset of action and prolonged, milder withdrawal; may also block L-type calcium channels independently of its effects on opioid receptors.
M8750 (+)-Methamphetamine hydrochloride Sympathomimetic with more potent central effects than amphetamine. It is transported into terminals via the monoamine transporters and induces release of dopamine, norepinephrine, epinephrine, and serotonin. Dopamine release is important for the addictive properties of methamphetamine while norepinephrine and epinephrine release are important for the cardiovascular effects. Serotonin neurotoxin.
M186 R(+)-Methanandamide 5 mg/mL in absolute ethanol, ≥96% (HPLC) R(+)-Methanandamide is metabolically stable congener of anandamide that has higher affinity for the cannabinoid receptor. Of the analogs tested, (R)-methanandamide exhibited the highest affinity for the cannabinoid receptor with a Ki of 20 +/- 1.6 nM, 4-fold lower than that of anandamide (Ki = 78 +/- 2 nM). (R)-methanandamide exhibits high stability to aminopeptidase hydrolysis. Experiments with mice have demonstrated that (R)-methanandamide also posseses cannabimimetric properties in vivo, as established by the four tests of hypothermia, hypokinesia, ring immobility, and antinociception.
mouse ... Cnr1(12801), Cnr2(12802)
rat ... Cnr1(25248)
SML0720 Methazolamide ≥98% (HPLC) Methazolamide has a plasma half-life of 14 hours in humans. Methazolamide has relatively good lipid solubility and low plasma protein binding ability. Thus, it diffuses into tissues and fluids much more readily than acetazolamide, another carbonic anhydrase inhibitor. Methazolamide has less side effects than acetazolamide.
Methazolamide is a cell-permeable and potent carbonic anhydrase (CA) inhibitor that is used in the treatment of glaucoma. Methazolamide is an insulin sensitizer that reduces hepatic glucose generation in animal models.
M3699   Methedrone hydrochloride ≥98% (HPLC) Methedrone is a synthetic stimulant, an analog of Cathinone and Methamphetamine.
M149 Methiothepin mesylate salt ≥98% (HPLC), solid Methiothepin mesylate salt is a 5-HT1, 5-HT6, 5-HT7 serotonin receptor antagonist, which blocks serotonin autoreceptors.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR6(3362), HTR7(3363)
M6682 Methoprene acid ≥98% (TLC) Demethylation, oxidative cleavage, hydrolysis, photodegradation and degradation of methoprene by microorganism results in methoprene acid and other metabolites. Methoprene acid is an insect growth regulator, and is known to control ecdysteroid signaling during development and metamorphism. It is thus used to control larval growth in insects such as mosquitoes, cigarette beetles, fleas and fire ants.
M6524 Methoxamine hydrochloride α1-adrenoceptor agonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
M1169 7-Methoxycoumarin-4-acetyl-Asp-Glu-Val-Asp-Ala-Pro-(2,4-dinitrophenyl)Lys Fluorogenic substrate for caspase 3 and caspase 3-like enzymes. Cleavage at the P1 Asp residue results in continuous fluorescence at 392 nm.
M6383 2-Methoxyestradiol powder 2-Methoxyestradiol (2-ME) is a potent inhibitor of endothelial cell proliferation and angiogenesis. A major estradiol metabolite, it has little affinity for classical estrogen receptors.
human ... ESR1(2099), ESR2(2100)
SML0699   4′-Methoxyflavone ≥97% (HPLC) 4-methoxyflavone is a neuroprotective agent that inhibits the accumulation of poly (ADP-ribose) and neuronal cell death following chemically-induced DNA damage or NMDA excitation.
UC131 (±)-4´-Methoxymephenytoin Mephenytoin derivative; anticonvulsive derivative.
M2547 8-Methoxymethyl-3-isobutyl-1-methylxanthine ≥98% Selective inhibitor of Ca2+-calmodulin-dependent phosphodiesterase I (PDE1).
human ... PDE1A(5136), PDE1B(5153)
M4251 3-Methoxytyramine hydrochloride ≥95.5%, crystalline Major metabolite of dopamine; product of catechol O-methyltransferase.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
M5644 (±)-Methoxyverapamil hydrochloride ≥98% Blocks L-type Ca2+ channels
M9189 1-N-Methylamino-3,5-dimethyladamantane hydrochloride >98% (HPLC), solid Antagonist of the NMDA receptor-channel complex. Abolishes the PrionSc-induced neuronal injury in vitro, and displays no influence on the synthesis and/or the processing of PrionSc
M5037 2-(Methylamino)propiophenone hydrochloride Potent amphetamine-like stimulant; dimethylpropion metabolite.
M2939 Methyl arachidonyl fluorophosphonate ≥98%, methyl acetate solution (10 mg/mL) MAFP is a selective, irreversible inhibitor of both calcium-dependent and calcium-independent cytosolic phospholipase A2, but not secretory phospholipase A2. MAFP is also a potent acetylcholinesterase inhibitor.
M7033 NG-Methyl-L-arginine acetate salt ≥98% (TLC) NG-Methyl-L-arginine is an inhibitor of nitric oxide synthase in neurons, endothelial cells, and macrophages. It inhibits endothelium-derived relaxing factor and promotes contraction in pulmonary artery and vein. It stereo selectively inhibits the generation of nitric oxide (NO) from arginine. It promotes epinephrine and glucose levels, contributing to hyperglycemia in central nervous system.
human ... NOS1(4842), NOS2(4843), NOS3(4846)
mouse ... Nos2(18126)
rat ... Nos1(24598), Nos2(24599)
M4796 (±)-α-Methyl-(4-carboxyphenyl)glycine Competitive antagonist at Group 1 (mGluR1 and mGluR5) and Group 2 (mGluR2 and mGluR3) metabotropic glutamate receptors.
human ... GRM1(2911), GRM2(2912), GRM3(2913), GRM5(2915)
rat ... Grm1(24414)
M4949 2’-C-Methylcytidine ≥95% (HPLC), powder 2′-C-Methylcytidine is a potent inhibitor of the HCV NS5B RNA polymerase. 2′-C-Methylcytidine was the first nucleoside NS5B inhibitor that showed clinical efficacy. 2′-C-Methylcytidine was found to be effective against the 17D vaccine strain of yellow fever virus YFV in cell culture.
M9440 Methyl-3,4-dephostatin >98% (HPLC), powder Stable analog of dephostatin; selective protein tyrosine phosphatase 1B and SHPTP-1 inhibitor; does not inhibit CD45-associated phosphatases.
human ... PTPN1(5770)
M6517 α,β-Methyleneadenosine 5′-triphosphate lithium salt ≥93% (HPLC), solid P2 purinoceptor agonist that is more potent than ATP at the P2X subtype.
human ... P2RX1(5023)
M7510 β,γ-Methyleneadenosine 5′-triphosphate disodium salt ≥95%, solid Selective P2X purinoceptor agonist that is more potent than ATP, but less potent than α, β-methylene-L-adenosine 5′-triphosphate.
M6267 (±)-3,4-Methylenedioxyamphetamine hydrochloride ≥98% (TLC)    
M1796 (±)-3,4-Methylenedioxy-N-­ethyl­amphetamine hydrochloride ≥98% (TLC) Psychotropic compound causing a reduction in serotonin level and in tryptophan hydroxylase activity in the brain. May cause structural damage to serotonenergic neurons.
M139 S(+)-3,4-Methylenedioxymethamphetamine hydrochloride solid Hallucinogen; releases dopamine and serotonin from nerve terminals; selective serotonergic neurotoxin.
SML0194   3,4-Methylenedioxypyrovalerone hydrochloride ≥98% (HPLC) 3,4-Methylenedioxypyrovalerone is a norepinephrine-dopamine reuptake inhibitor (NDRI) that acts as a CNS stimulant.
3,4-Methylenedioxypyrovalerone is a norepinephrine-dopamine reuptake inhibitor (NDRI); CNS stimulant.
3,4-Methylenedioxypyrovalerone is a derivative of pyrovalerone, a rapidly-absorbed psychostimulant. It belongs to the class of synthetic cathinones often used as performance-enhancing agent by athletes before being banned.
SML0713   2′-C-Methylguanosine ≥98% (HPLC) 2′-C-Methylguanosine (2’-MeG) is a potent and specific RNA dependent RNA polymerase NS5B inhibitor of the hepatitis C virus (HCV).
2′-C-methylguanosine is also known as BMS-986094. This prodrug is used for the treatment of chronic hepatitis C virus infection.
SML0460 Methylhexanamine hydrochloride ≥98% (HPLC) Methylhexanamine induces fat degradation and prevents energy loss during exercise. Thus, it serves as an active ingredient of many dietary supplements.
Methylhexanamine is a naturally substance isolated from Pelargonium graveolen. It is a component of geranium oil. Methylhexanamine is a sympathomimentic that increase levels of norepinephrine in the synaptic cleft.
H128 (R)(−)-α-Methylhistamine dihydrochloride solid, ≥98% (HPLC) Potent, selective H3 histamine receptor agonist which crosses the blood-brain barrier; inhibits histamine synthesis and release.
human ... HRH3(11255)
H5914 Nα-Methylhistamine dihydrochloride solid Production of N-alpha-methyl-histamine (NAMH), a histamine H(3) receptor (H3R) agonist, is promoted in Helicobacter pylori infected human gastric mucosa. NAMH acts directly on histamine H(2) receptors (H2Rs) in animals to stimulate acid secretion and to be a H2R agonist. NAMH dose dependently stimulated cAMP productions in CHO-H2R cells. This production was inhibited by famotidine but not by thioperamide. Control CHO cells were unresponsive to either histamine or NAMH. In addition, the effect of NAMH, in terms of cAMP production in CHO-H2R cells, was more potent than that of histamine-that is, with a lower EC50 concentration and higher maximal cAMP production. Both NAMH and histamine, but not R-alpha-methyl-histamine, effectively inhibited [(3)H] tiotidine binding to CHO-H2R cells. These results confirm that NAMH, which is produced in the gastric mucosa by H pylori, is a potent H2R agonist as well as a H3R agonist.
M8911 Methyl 4-hydroxybenzoate analytical standard   rat ... Ar(24208)
M0388 6α-Methyl-11β-hydroxyprogesterone    
M1514 Nω-Methyl-5-hydroxy­trypt­amine oxalate salt ≥90% (HPLC) Serotonin receptor ligand.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
A5585 5-(N-Methyl-N-isobutyl)­amiloride ≥98% (TLC), powder Potent blocker of the Na+/H+ antiport. Possible antitumor agent.
human ... SCNN1A(6337), SCNN1B(6338), SCNN1D(6339), SCNN1G(6340)
mouse ... Scnn1a(20276), Scnn1b(20277), Scnn1d(140501), Scnn1g(20278)
rat ... Scnn1a(25122), Scnn1b(24767), Scnn1g(24768)
M2689   Methyl γ-linolenyl fluorophosphonate ≥98%, methyl acetate solution An analog of MAFP which has been widely studied as an inhibitor of phospholipases, FAAH, and as a cannabinoid receptor ligand.
M168 Methyllycaconitine citrate salt from Delphinium brownii seeds, ≥96% (HPLC) Potent and specific nicotinic receptor antagonist that binds to neuronal α-bungarotoxin sites.
M200 (±)-N-Methyl-1-(3,4-methylenedioxyphenyl)-2-butanamine hydrochloride solid Non-hallucinogenic; CNS stimulant. Analog of MDMA
M103 1-Methyl-4-(2′-methylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride solid Dopaminergic neurotoxin that is more toxic in mice than MPTP.
SML0277 Methylnaltrexone bromide ≥97% (HPLC) Methylnaltrexone bromide is a narcotic antagonist. It is a peripheral mu-opiod receptor antagonist that cannot cross the blood-brain barrier. It reverses many opioid side-effects without interfering with pain relief.
SML0704   1-Methylnicotinamide chloride ≥98% (HPLC) 1-Methylnicotinamide (MNA) is a primary metabolite of nicotinamide produced mainly by nicotinamide N-methyltransferase (NNMT). 1-Methylnicotinamide (MNA) has been shown to have antithrombotic and anti-inflammatory effects. A recent study indicated that MNA may exert antithrombotic and anti-inflammatory effects through direct action on the endothelium, with a vasorelaxing effect by enhancement of NO bioavailability and reduction of eNOS-dependent oxidative stress. Enhanced NNMT activity is a feature of many types of cancer. How much direct involvement MNA has in the tumorigenesis associated with overexpression of NNMT is under investigation. MNA by itself increased mitochondrial Complex I activity and increased cancer cell viability in SH-SY5Y neuroblastoma cells that do not produce NNMT.
SML0675   α-Methylnorepinephrine ≥95% (HPLC) α-Methylnorepinephrine is a sympathomimetic amine and vasoconstrictor. α-Methylnorepinephrine is used clinically in dentistry in local anesthetic solutions.
M3574 Methylone hydrochloride ≥98% (HPLC) Methylone is a stimulant, an analog of Methamphetamine. Triple reuptake inhibitor; inhibits the re-uptake of dopamine, 5-HT and norepinephrine.
M2892 Methylphenidate hydrochloride CNS stimulant; releases catecholamines; potent inhibitor of dopamine reuptake
M6935 L-threo-Methylphenidate hydrochloride solid Central nervous system stimulant. Less potent enantiomer.
M5435 6-Methyl-2-(phenylethynyl)pyridine hydrochloride ≥98% (HPLC) Highly selective, non-competitive mGluR5 metabotropic glutamate receptor antagonist.
human ... GRIN2B(2904), GRM5(2915)
rat ... Grm5(24418)
M0896 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine hydrochloride powder Dopaminergic neurotoxin.
M0639 6α-Methylprednisolone ≥98%   rat ... Nr3c1(24413)
M3781 6α-Methylprednisolone 21-hemisuccinate sodium salt lyophilized powder Glucocorticoid with slightly longer half-life than that of prednisolone.
M3778 N-Methyl-N-propargyl-3-(2,4-dichlorophenoxy)propylamine hydrochloride ≥97% (GC) MAO-A inhibitor.
human ... MAOA(4128)
rat ... Maoa(29253), Maob(25750)
M110 α-Methylserotonin maleate salt ≥98% (HPLC) 5-HT2 serotonin receptor agonist.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
M6628 O-Methylserotonin hydrochloride crystalline Nonselective serotonin receptor agonist that lacks affinity for the 5-HT3 receptor.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
SML0640 2-Methylserotonin maleate ≥95% (HPLC) 2-Methylserotonin is a selective full agonist at the 5-HT3 receptor.
2-Methylserotonin maleate, a serotonin type 3 (5-HT3) agonist is used as a training drug in drug discrimination studies. Use of 2-methylserotonin in evolving rats shows to reflect the ontogeny of the spinal 5-HT3 receptor system.
S128 N-Methylspiperone hydrochloride solid D2 dopamine receptor antagonist.
SML0343 Methylstat ≥98% (HPLC) Methylstat is an inhibitor of the Jumonji C domain-containing histone trimethyl demethylases (JHDMs). Methylstat inhibits the activity of JMJD2C (IC50 = 4.3 μM), with similar potency against JMJD2E and JMJD3. The compound has poor activity against dimethyl demethylases, and does not inhibit class I or II HDACs. Methylsat blocks proliferation of the esophageal carcinoma cell line KYSE150 with an IC50 value of 5.1 μM.
M7252 17α-Methyltestosterone solid (photosensitive) Methyltestosterone (Mesterone) is an androgen and anabolic steroid.
rat ... Ar(24208)
SML0712   1-Methyl-1,2,3,4-tetrahydroisoquinoline ≥97% (GC) 1-Methyl-1,2,3,4-tetrahydroisoquinoline (1MeTIQ) is an endogenous antidepressant and parkinsonism-preventing substance that demonstrates neuroprotectiveactivity. Following systemic administration in rats, 1-Methyl-1,2,3,4-tetrahydroisoquinoline produces antidepressant-like effect similar to the effect of imipramine. 1MeTIQ is a reversible short-acting moderate inhibitor of MAO A/B.
U101 5-Methylurapidil solid Selective α1A-adrenoceptor antagonist; antihypertensive.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
M137 Methysergide maleate salt solid Nonselective 5-HT1, 5-HT2, and 5-HT7 serotonin receptor antagonist; antimigraine.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR7(3363)
M0763 Metoclopramide hydrochloride solid D2 antagonist; 5-HT3 antagonist; antipsychotic; anti-emetic.
human ... DRD2(1813), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242)
M1195 Metolazone ≥98% (HPLC), solid Inhibitor of thiazide-sensitive Na+-Cl- cotransporter; antihypertensive; moderate "loop" diuretic.
human ... SLC12A1(6557)
M5391 (±)-Metoprolol (+)-tartrate salt ≥98% (titration), powder β1-adrenoceptor antagonist.
human ... ADRB1(153)
M5685 Metrazoline solid Potent and selective imidazoline binding site ligand
M2696 Metyrapone ≥98% (HPLC), solid Metyrapone is a glucocorticoid synthesis inhibitor; a standard in assessing adrenal gland function especially in response to stress, as well as pituitary gland function. In addition to acting as a glucocorticoid synthesis inhibitor, Metyrapone also inhibits cytochrome P450-mediated prostaglandin ω/ω-1 hydroxylase activity and impairs learning and memory. Data shows results in activation of the sleep EEG and a robust decrease in quantitative delta sleep.
M2537 Mevastatin ≥95% (HPLC), powder HMG-CoA reductase inhibitor. Cholesterol lowering drug. Inhibits myoblast formation. An antibiotic shown to cause apoptosis, apparently by inhibiting post-translational prenylation of proteins such as Ras. Similarly, mevastatin increases eNOS mRNA and protein levels by blocking the geranylgeranylation of Rho.
human ... HMGCL(3155), HMGCR(3156)
rat ... Hmgcr(25675)
M2147 Mevinolin from Aspergillus sp. ≥98% (HPLC) Lovastatin is a cholesterol lowering drug and competitive inhibitor of HMG-CoA reductase, a rate limiting enzyme in cholesterol synthesis. Blocks the production of mevalonate, a critical compound in the production of cholesterol and isoprenoids. This product is a substrate of Pgp and CYP3A. It increases cellular resistance to anticancer agents such as doxorubicin and induces apoptosis in myeloma cells. The roles of Pgp and CYP3A, possible connection between drug resistance, regulation of the mevalonate pathway, and iosprenylation of signaling proteins in these observations remain to be resolved. The product induces apoptosis in numerous cancer cell lines perhaps, in part, by inhibiting the isoprenylation of Rho family GTPases. It causes cell cycle arrest in G1 and G2/M phases.
human ... HMGCR(3156)
rat ... Hmgcr(25675)
M2727 Mexiletine hydrochloride powder Class IB antiarrhythmic; sodium channel blocker
SML0658   3-MFA ≥97% (HPLC) 3-MFA is a mefenamic acid analog that blocks the transient receptor potential melastatin 2 (TRPM2) channel. Unlike other TRPM2 blockers such as 2-APB and flufenamic acid, 2-APB does not induce release of calcium from intracellular stores.
M3184 MG 624 ≥98% Nicotinic acetylcholine receptor antagonist; selectively inhibits neuronal nicotinic α-bungarotoxin sensitive receptors that contain the α7 subunit.
human ... CHRNA7(1139)
SML0810   MHY1485 ≥95% (HPLC) MHY1485 is mTOR activator that potently inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
SML0537 MI-1 ≥98% (HPLC) MI-1 is a Menin-MLL interaction inhibitor. The mixed lineage leukemia (MLL) gene encodes MLL, a histone methyltransferase important in regulating gene transcription. MLL rearrangements and formation of fusion oncoproteins can block hematopoietic differentiation and increase proliferation, resulting in acute leukemias. Menin, encoded by the MEN1 gene, is a tumor suppressor associated with multiple endocrine neoplasia type 1. It also acts as an oncogenic co-factor of MLL fusion proteins. MI-1 inhibits Menin-MLL interaction with an IC50 of 1.9 micromolar.
SML1793 MI-4F ≥98% (HPLC) MI-4F is mesoionic compound that exhibits potent anticancer activity against multiple cancer cell lines and in vivo. MI-4F induces apoptosis in HepG2 cells. MI-4F appears to inhibit calcium efflux through inhibition formation of mitochondrial permeability transition pore (MPTP). MI-4F inhibits superoxide dismutase. MI-4F is not susceptible to MDR transporters P-glycoprotein, ABCG2 and MRP1. MI-4F also inhibits ABCG2-mediated efflux of mitoxantrone.
SML1451 MI192 hydrochloride ≥98% (HPLC) MI192 is a potent and selective histone deacetylase 3 (HDAc 3) inhibitor that inhibits IL-6 production in peripheral blood mononuclear cells (PBMCs) from rheumatoid arthritis (RA) but not healthy PBMCs.
M2525 Mianserin hydrochloride Antidepressant; antagonist/inverse agonist at 5-HT2 serotonin receptors; also blocks the H1 histamine receptor and the α2 adrenoceptor.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152), HRH1(3269), HTR2A(3356), HTR2B(3357), HTR2C(3358)
M5441 Mibefradil dihydrochloride hydrate ≥98% (HPLC), powder Ro 40-5967 is a T-type Ca2+ channel blocker; antihypertensive.
SML0438   Mibolerone ≥98% (HPLC) Mibolerone is a synthetic anabolic steroid with a similar profile of activity as R1881 (Metribolone) with a higher affinity (Kd = 1.5 nM) for the androgen receptor in human prostate tissue than R1881 (Kd = 2.3 nM).
The synthetic androgen mibolerone (7α,17α dimethyl-19-nortestosterone) reversibly blocks the multiplication of LNCaP (human prostate carcinoma cell line) cells. In prostate, liver, and cultured cells, it serves as an efficient radioactive ligand for the quantitation and characterization of androgen receptors.
SML2268 Micafungin sodium ≥97% (HPLC) Micafungin is a semisynthetic echinocandin antifungal. Micafungin works by inhibiting the enzyme β(1,3)-D-Glucan synthase and thereby disturbing the integrity of the fungal cell wall. This enzyme does not exist in mammalian systems.
M2419 Midazolam maleate salt Sedative/Hypnotic; ligand for the GABAA receptor benzodiazepine modulatory site; CYP3A4 substrate.
M1323 Midostaurin hydrate ≥98% (HPLC), solid Midostaurin is an inhibitor of tyrosine kinase, protein kinase C, and VEGF. Midostaurin inhibits cell growth and phosphorylation of FLT3, STAT5, and ERK. Midostaurin is a potent inhibitor of a spectrum of FLT3 activation loop mutations.
SML0195 Mifamurtide ≥98% (HPLC) Mifamurtide (Muramyl tripeptide phosphatidylethanolamine; MTP-cephalin; MTP-PE) is a synthetic, lipophilic analog of muramyl dipeptide. It acts as an immunostimulant promoting cancer cell destruction via in vivo macrophage activation.
Mifamurtide is an immunomodulator and regulates the activation of monocytes and macrophages. Mifamurtide upregulates the secretion of pro-inflammatory cytokines such as TNF-α, IL-1, IL-8, nitric oxide and prostaglandins E2 and D2. It has anti-tumor effects in children and young adults with high-grade osteosarcoma.
M8046 Mifepristone ≥98% Mifepristone (RU-486) has activity as both a progesterone receptor antagonist and a glucocorticoid receptor antagonist.
Therefore, mifepristone is considered to be a potent abortifacient. It is also known to inhibit human chorionic gonadotropin. Mifepristone results in decidual necrosis.
human ... AR(367), ESR1(2099), ESR2(2100), HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363), NR3C1(2908), NR3C2(4306), PGR(5241)
mouse ... Nr3c1(14815)
rat ... Nr3c1(24413), Tat(24813)
M1318 Milnacipran hydrochloride ≥98% (HPLC), solid Serotonin and norepinephrine reuptake inhibitor (SNRI)
M4659 Milrinone ≥97% (TLC), powder Phosphodiesterase type III inhibitor; cAMP-specific, cGMP-inhibitable; potent cardiotonic, positive inotropic vasodilator.
human ... PDE3A(5139), PDE3B(5140), PDE4B(5142), PDE5A(8654), PTPRA(5786)
rat ... Pde3a(50678)
M9198 Miltefosine hydrate ≥98% (HPLC) Miltefosine induces apoptosis of triple-negative (TN) breast cancer cells by activation of p38 MAPK pathway and differential down regulation of Akt signaling. Miltefosine is an effective anti-tumor treatment of cutaneous lymphoma, cutaneous metastatic melanoma, squamous cell carcinoma, and cutaneous metastases of breast cancer. It also shows remarkable effectiveness against visceral leishmaniasis. Both the anti-tumor and the antiprotozoal activities appear to be exerted first by insertion of the molecule into the plasma membrane where it interferes with phospholipid metabolism.
Miltefosine or HePC induces death of triple-negative (TN) breast cancer cells. Miltefosine exerts various modes of action leading to different cell death processes, i.e. apoptosis or non-apoptosis, depending on TN breast cancer cell types. These processes involve the activation of p38 MAPK pathway and differential down regulation of Akt signaling. Miltefosine has been used for breast cancer skin metastases, and is an efficient topical anti-tumoral treatment in patients with cutaneous lymphoma, cutaneous metastases of melanoma and squamous cell carcinoma.
SML2021 MIND4-17 ≥98% (HPLC) MIND4-17 is a potent NRF2 (nuclear factor erythroid 2-related factor 2) activator that covalently modifies a critical stress-sensor cysteine (C151) in the BTB domain of the E3 ligase substrate adaptor protein Kelch-like ECH-associated protein 1 (KEAP1), the primary negative regulator of NRF2. MIND4-17 induces NRF2 activation responses in neuronal and non-neuronal cultures (effective conc. 0.1-10 μM) of human, mouse, and rat origins. In addition, MIND4-17 effectively reduces endotoxin-induced IL-6 release from WT as well as YAC128 HD mutant mice-derived primary microglia and astrocytes, however, NRF2 induction by MIND4-17 is shown to be compromised in human Huntington′s diseased (HD) relative to non-disesed neural stem cells due to suppressive influence of the expanded CAG repeat mutation on pathway activation.
M9511 Minocycline hydrochloride powder Minocycline is a broad spectrum antibiotic with bacteriostatic function. Minocycline has anti-inflammatory properties. Minocycline inhibits lipopolysaccharide mediated inflammatory cytokine tumour necrosis factor (TNF-α) secretion by macrophages. Minocycline inhibits macrophage proliferation in a dose dependent manner. Minocycline inhibits neuroinflammation in pre-plaque of Alzheimer′s disease-like amyloid pathology through inhibition of key inflammatory enzymes like inducible nitric oxide synthase (iNOS), matrix metalloproteinase 9 (MMP-9) and 5-lipoxygenase. Minocycline inhibits endothelial cell proliferation and angiogenesis. Minocycline exhibits anti-tumor activity in glioma by inhibiting membrane type 1 matrix metalloproteinase (MT1-MMP). Minocycline increases cognition and neuronal differentiation. zMinocycline effectively reduces neuropathic pain by increasing the functions of nociceptin/orphanin FQ.
SML2159 Minodronic acid monohydrate ≥98% (HPLC) Minodronate is a third-generation bisphosphonate used clinically alone or in combination to treat osteoporosis. It is an inhibitor of farnesyl diphosphate synthase that acts as a bone resorption inhibitor.
M4145 Minoxidil ≥99% (TLC) Activates ATP-activated K+ channels; vasodilator; slow or stop hair loss and promote hair regrowth.
human ... KCNJ1(3758)
M7920 Minoxidil sulfate salt    
M9948 Mirin ≥98% (HPLC), powder Mirin is an inhibitor of the Mre11-Rad50-Nbs1 complex. It disrupts nuclease activity of Mre11 and thus, the ability to repair DNA double strand breaks.
human ... MRE11A(4361)
M0443 Mirtazapine ≥98% (HPLC) Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA). Mirtazapine agonizes selective adrenergic and serotonergic receptors so that both NE release and 5-HT1A mediated serotonergic signaling are increased.
human ... ADRA2A(150), ADRA2C(152), DRD2(1813), DRD3(1814), DRD4(1815), HRH1(3269), HTR1A(3350), HTR2A(3356), HTR2C(3358), HTR7(3363)
mouse ... Slc6a2(20538)
rat ... Adra1a(29412), Drd1a(24316), Drd2(24318), Htr1a(24473), Htr2a(29595), Htr2c(25187), Slc6a3(24898), Slc6a4(25553)
M6891 Mithramycin A from Streptomyces plicatus ≥90% (HPLC) Anticancer antibiotic. Inhibits transcription and protein synthesis. Binds to DNA in native chromatin. Substrate of Pgp in MDR phenotypes.
SML0234 Mitiglinide calcium ≥98% (HPLC) Mitiglinide is a drug for the treatment of type 2 diabetes. It is a highly selective KATP channel antagonist Mitiglinide is a hypoglycemic agent that closes adenosine triphosphate (ATP)–sensitive potassium channels (KATP channel s) in the pancreatic β-islet cells.
SML1300   MitoB ≥98% (HPLC) MitoB is a mitochondria-targeted mass spectrometry probe used to measure hydrogen peroxide (H2O2) levels within mitochondria. MitoB reacts selelectively with H2O2 to form a new product, MitoP. The ratio of MitoP to MitoB can be used to determine mitochondrial H2O2 concentration.
SML0629   Mitochondrial Fusion Promoter M1 ≥95% (HPLC) Mitochondrial Fusion Promoter M1 is a cell permeable hydrazone that enhances mitochondrial fusion. M1 protects cells from mitochondrial fragmentation associated cell death. Mitochondrial Fusion Promoter M1 does not interfere with endoplasmic reticula (ER) and lysosomes morphology.
SML1884 Mitoglitazone ≥98% (HPLC) MSDC-0160 is an mTOT (mitochondrial target of thiazolidinediones) modulator that targets the mitochondrial pyruvate carrier (MPC), which is a key controller of cellular metabolism. MSDC-0160 is reported to enhance the cells’ ability to handle potentially harmful proteins, which leads to reduced inflammation and less nerve cell death. It has already been in clinical trials for diabetes and Alzheimer′s disease and clinical trials for Parkinson′s Disease are planned.
SML2284 Mito A iodide ≥98% (HPLC) MitoA is selective hydrogen sulfide (H2S) probe targeting mithchondria suitable for in vivo use. MitoA accumulates in mitochondria within tissues, where it is converted to MitoN by reaction with H2S. Both compounds are detected sensitively by LC-MS/MS.
SML0734   MitoPY1 ≥95% (HPLC), 1:1 iodide complex MiroPY1 is a cell-permeable fluorescent sensor that is highly selective for detecting the presence of H2O2 within the mitochondria of living cells.
MiroPY1 is an irreversible and bifunctional dye. It employs a triphenylphosphonium targeting group and a boronate-based molecular switch to specifically respond to H2O2 over competing reactive oxygen species (ROS) in the mitochondria. It does not require transfection. MiroPY1 is photostable and limits false positives.
SML1885 Mitotane ≥98% (HPLC) Mitotane is a selective inhibitor of sterol-Oacyl-transferase 1 (SOAT1), also known as ACAT1, (acyl-coenzyme A cholesterol acyltransferase). Mitotane inhibition of SOAT1 in adrenocortical carcinoma cells decreased the formation of cholesteryl esters, which increased free cholesterol levels and caused endoplasmic reticulum (ER) stress, the unfolded protein response, and eventually apoptosis.
SML0737   MitoTEMPO ≥98% (HPLC) MitoTEMPO is a mitochondrially targeted antioxidant, a specific scavenger of mitochondrial superoxide. MitoTEMPO is a combination of the antioxidant piperidine nitroxide TEMPO with the lipophilic cation triphenylphosphonium, giving MitoTEMPO the ability to pass through lipid bilayers with ease and accumulate several hundred-fold in mitochondria. Mitochondrial dysfunction and oxidative stress contribute to a variety of disorders involving cardiovascular, kidney, liver disorders, Parkinson′s and Alzheimer′s disease.
M3047 Mizoribine ≥98% (TLC) Mizoribine is an imidazole nucleoside possessing strong immunosuppressive properties. Selectively blocks T-cell proliferation response to mitogenic and allo-antigenic stimulation. Mizoribine blocks the movement of T cells from G to S phase. In addition, it significantly decreases the number of B cells at the S, G, and M phases. Mizoribine inhibits de novo synthesis of nucleotides by inhibition of inosine monophosphate dehydrogenase. The resulting nucleotide depletion inhibits DNA synthesis.
M3315 MJ33 lithium salt powder, ≥90% (NMR) Novel, active site directed, specific, competitive and reversible inhibitor of phospholipase A2 (PLA2).
SML0347 MJC13 ≥98% (HPLC) MJC13 inhibits the positive regulation of androgen receptor (AR) signaling by the cochaperone protein FKBP52. The molecule inhibits hormone-induced dissociation of the FKBP52, nuclear translocation of AR and AR dependent gene expression. MJC13 inhibits proliferation of the androgen-dependent prostate cancer cell lines LNCaP and LAPC4.
SML0872 MJN110 ≥98% (HPLC) MJN110 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) with >10,000 selectivity over FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA). MJN110 inhibits rat, mouse and human MAGL with IC50 values ranging from < 100 nM in rat to an IC50 of ~1 nM with 10- and 100-fold selectivity over closely related ABHD6, a serine hydrolase that acts as an alternative hydrolase of 2-AG, and LYPLA1/2 in human PC3 cells. MJN110 showed potent anti-hyperalgesic activity in a rat model of diabetic neuropathy, showing a therapeutic potential for treating diabetes chronic pain.
SML0565 MK-0343 ≥98% (HPLC) MK-0343 (MRK-409) is a partial agonist for GABAA receptors with comparable Ki values for α1, α2, α3 and α5 containing receptors (0.2 – 0.4 nM). The compound has the greatest agonist activity against α3 receptors, and is brain penatrant, and displays anxiolytic activity in rodent and primate models.
SML1890 MK204 ≥98% (HPLC) MK204 is a potent and selective inhibitor of aldo-keto reductase family member 1B10 (AKR1B10). AKR1B10 is induced in several cancer types, in particular, hepatocellular carcinoma, and may be involved with drug resistance. MK204 appears to target a distinct AKR1B10 inner specificity pocket not present in the closely related aldose reductase. MK204 had an IC50 value of 80 nM compared to an IC50 value of 21.7 μM for aldose reductase.
M3199 MK-212 hydrochloride ≥98% (HPLC) Selective 5-HT2C serotonin receptor agonist.
M7571 MK-571 sodium salt hydrate ≥95% (HPLC) MK 571 is a potent and selective leukotriene D4 (LTD4) antagonist and ABCC multidrug resistance protein 1(MRP1) inhibitor. The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G-protein coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor. MK 571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. MK 571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors. It potentially inhibits MRP1 and has been shown to overcome acquired arsenic tolerance.
SML1509   MK6-83 ≥98% (HPLC) MK6-83 is a potent activator of wild type and mutant variants F465L and F408D of TRPML1 channel. MK6-83 weakly activates TRPML mutants R403C or V446L. MK6-83 restores channel function and rescue disease associated abnormalities in mucolipidosis type IV (MLIV) patient cells.
SML0993   MK-677 ≥98% (HPLC) It is also known as ibutamoren mesylate. MK-677 is a mimic of growth hormone (GH)-releasing peptide and is orally active.
MK-677 is a potent, non-peptide ghrelin receptor agonist.
M7065 MK-912 hydrochloride hydrate ≥98% (HPLC) Selective α2-adrenoceptor antagonist
human ... ADRB2(154)
SML1038 MKC-733 ≥98% (HPLC) MKC-733 is a 5-HT3 specific agonist.
M5449 MKT-077 ≥98% (HPLC), powder MKT-077 is an inhibitor of mitochondrial hsp70 family member, mortalin (mot-2)n; causes selective death of cancer cells.
I2764 ML-7 powder Selective myosin light chain kinase inhibitor.
human ... MYLK(4638), MYLK2(85366)
C1172 ML-9 ≥99% (TLC), powder ML-9 is myosin light chain kinase inhibitor. It inhibits insulin-induced translocation of glucose transporters GLUT4 and GLUT1 in a dose-dependent manner. ML-9 also inhibits agonist-induced Ca2+ entry into endothelial cells and catecholamine secretion in intact and permeabilized chromaffin cells. ML-9 promotes cell death in cancer cells by triggering accumulation of autophagic vacuoles. ML-9 impacts phosphorylation of myosin light chain kinase and alters trabecular meshwork shape and decreases intraocular pressure in rabbit eyes.
human ... SLC2A1(6513), SLC2A4(6517)
SML1197 ML 00253764 hydrochloride ≥98% (HPLC) ML 00253764 is a brain penetrant and potent MC4 melanocortin receptor antagonist that increases food intake and reduces loss of lean body mass in tumor bearing mice.
SML0901   ML095 hydrochloride ≥98% (HPLC) ML095 is a specific inhibitor of placental alkaline phosphatase, with greater than 25-fold selectivity over tissue non-specific alkaline phosphatase (TNAP) and intestinal alkaline phosphatase (IAP). The IC50 valuess of ML095 against PLAP, TNAP and IAP are 2.1, >100 and 53 μM, respectively.
SML1258 ML099 ≥98% (HPLC) ML099 is a Ras-related GTPase activator. Mutated forms of small GTPases induce proliferation and transformation of a number of cell types as well as differentiation of neuronal cells. The only known activation mechanism of small GTPase is via guanine nucleotide-exchange factors (GEFs). Data suggests that some diseases, including immunodeficienty syndromes result from loss of function mutations in the Rac2 GTPase, and the GEF cdc42. ML099 can activate cdc42, Rac1 and Ras GTPase activity with mid to high nM EC50s. GTPase activatiors could be useful tools for defining the mechanism of GEF activation of GTPases, further understanding of GTPase signaling mechanisms and study of diseases in which loss of function mutants are implicated.
M7319 ML 10302 ≥98%, solid Potent, selective 5-HT4 serotonin receptor agonist
rat ... Htr3a(79246), Htr4(25324)
SML1585   ML116 ≥95% (HPLC) ML116 is a potent and selective inhibitor of STAT3 (signal transducer and activator of transcription 3) phosphorylation. ML116 potently inhibits growth and induces cell death of rodent and human glioma cells. ML116 is inactive against the related STAT1 and NFkB anti-targets.
STAT3 is a transcription factor which is activated by cytokines and growth factors. It is oncogenic and is present in various cancers, such as breast, prostate, renal cell, melanoma, ovarian, lung, leukemia, lymphoma and myelomas. It is associated with cellular growth, survival and malignancy.
SML1174   ML120B ≥98% (HPLC) ML120B is a potent inhibitor of IKK-2 (IC50 = 60 nM). ML120B is orally bioavailable, and inhibits paw swelling, bone and cartilage degradation, and weight loss in rat adjuvant-induced arthritis.
SML0190 ML133 hydrochloride ≥95% (HPLC) ML133 hydrochloride is a selective inhibitor of the Kir2 family of inward rectifier (IRK, KCNJ) potassium channels. ML133 inhibits Kir2.1 with IC50 of 1.8 μM at pH 7.4 and 290 nM at pH8.5. It exhibits little selectivity against other members of Kir2.x family channels, but has no effect on Kir1.1 (IC50 > 300 μM), and displays weak activity for Kir4.1 (76 μM) and Kir7.1 (33 μM), making ML133 the most selective small molecule inhibitor of the Kir family reported to date. It also showed modest selectivity versus hERG and a larger panel of GPCRs, ion channels and transporters.
SML1140 ML138 ≥98% (HPLC) ML138 (CID 44601470) is a highly selective agonist at kappa opioid receptors (KOR) that potently activate G protein coupling but weakly interact with β arrestin2.
SML0407 ML 141 ≥98% (HPLC) ML 141 is a potent, selective inhibitor of the Rho family GTPase cdc42. The IC50 for inhibition of enzymatic activity is 200 nM, with no activity against Rho family members Rac, Ras or Rab. Cdc42 has been implicated in the regulation of actin polymerization through its direct binding to Neural Wiskott-Aldrich syndrome protein (N-WASP), which subsequently activates Arp2/3 complex. This complex mediates the polymerization of actin into branched networks and regulates important functions including cell adhesion, cytoskeletal arrangement, phagocytosis and host-pathogen interactions, motility, migration, and membrane protein trafficking.
SML0418 ML-161 ≥98% (HPLC) ML-161 is an antagonist of the protease-activated receptor 1 (PAR1), that inhibits thrombin and SFLLN-induced platelet activation. ML-161 dose dependently inhibits SFLLN-induced expression of P-selectin with an IC50 of 0.26 μM.
SML0924   ML167 ≥98% (HPLC) ML167 is the first highly selective inhibitor of of Cdc2-like kinase 4 (Clk4) with an IC50 of 136 nM for Clk4, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B, and minimal activity against a panel of other kinases tested. The Cdc2-like kinases (Clk’s) and the dual-specificity tyrosine phosphorylation-regulated kinases (Dyrk’s) are involved in regulation of gene splicing. The Cdc2-like kinases phosphorylate the serine/arginine-rich (SR) proteins, a major component of the spliceosome.
SML0243 ML169 ≥98% (HPLC) ML169 is a positive allosteric modulator (PAM) of the muscurinic acetycholine receptor M1 (CHRM1). ML169 does not cross react with other muscarinic receptors and is able to penetrate the blood brain barrier.
SML1340 ML193 trifluoroacetate ≥98% (HPLC) ML193 is a potent and selective piperadinyloxadiazolone antagonist for G protein-coupled receptor (GPCR) GPR55, a receptor for L-α-lysophosphatidylinosi  
SML0423 ML194 ≥98% (HPLC) ML194 (CID9581011) is an antagonist of GPR35, a GPRC receptor expressed in nervous system tissue, in the GI tract particularly in pancreas and small intestine, followed by colon, spleen, and immune cells, and also expressed in gastric carcinomas. GPR35 is being investigated for potential therapeutic importance in a variety of areas including pain, hypertension, cancer, diabetes and asthma. ML194 is more membrane penetrant and more potent than earlier synthetic antagonists, with an IC50 of 160nM. ML194 was also found to rescue the cell-surface expression of mutant GPR35 receptors, likely acting as a pharmacological chaperone to alter the misfolded receptor structure.
SML0400 ML204 ≥98% (HPLC) ML204 is a potent and selective TRPC4 channel inhibitor.
SML0521 ML 210 ≥98% (HPLC) ML 210 induces non-apoptotic cell death in tumor cells expressing the RAS oncogene.
SML1004   ML211 ML211 is a very potent, dual inhbitor of lysophospholipase 1 (LYPLA1; IC50 = 17 nM) and lysophospholipase 2 (LYPLA2; IC50 = 30 nM).
SML0611   ML213 ≥98% (HPLC) ML213 is a selective opener of the potassium channels KCNQ2 and KCNQ4, with EC50 values of 230 and 510 nM, respectively.
SML0661   ML216 ≥98% (HPLC) ML216 is a 4-F-phenyl analog. It blocks cell proliferation of BLM-proficient fibroblast cells (PSNF5) and shows very less effects on BLM-deficient fibroblast cells (PSNG13).
ML216 is a membrane permeable selective inhibitor of Bloom (BLM) helicase, a member of the RecQ DNA helicase family. Bloom’s syndrome, caused by a mutation in BLM, is associated with susceptibility to cancer, growth retardation, immunodeficiency, sunlight sensitivity, and fertility defects. ML216 is selective for BLM over other members of the RecQ family, especially in vivo, and appears to act at the BLM-nucleic acid substrate binding site, inhibiting DNA binding and blocking BLM′s helicase activity. ML216 could be useful in studies of tumor cells depending on the ALT (alternative lengthening of telomeres) mechanism for telomere maintenance rather than on telomerase, which are proposed to be susceptible to BLM inhibition.
SML0385 ML218 ≥98% (HPLC) ML218 (CID 45115620) is a potent and selective T-Type (Cav3.1, Cav3.2, Cav3.3) calcium channel inhibitor (Cav3.2, IC50 = 150 nM in Ca2+ flux; Cav3.2 IC50 = 310 nM and Cav3.3 IC50 = 270 nM with good Drug metabolism/Pharmacokinetics. In a panel of 68 GPCRs, ion channels and transporters, ML218 was found to bind significantly only two other targets (sodium channel site 2 and sigma 1) and had no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. It showed robust inhibition of calcium current in STN neurons and was orally active in a rodent model of Parkinson’s Disease.
SML0919   ML221 ≥98% (HPLC) ML221 is an antagonist of the apelin receptor (also known as APJ). ML221 blocks Apelin-13 mediated receptor activation (recruitment of β-arrestin) with an IC50 of 1.75 μM.
SML0997   ML 230 ≥98% (HPLC) ML 230 (SID 88095709) is a specific inhibitor of the ABC-binding cassette trasporter BCRP (MRP-1; ABCG2). The compound ML 230 is 36-fold selective for BCRP over MDR-1 (Pgp; ABCB1) with IC50 values of 0.013 and 4.7 mM, respectively.
SML0442 ML239 ≥98% (HPLC) ML239 is an inhibitor of breast cancer stem cells found from a screen using stem cell-like human mammary epithelial cells (HMLE). ML239 inhibited cancer stem cells with an IC50 of 1.16 μM with 24-fold selectivity against the control cell line.
SML1071 ML240 ≥98% (HPLC) ML240 is a selective, ATP-competetive inhibitor of AAA ATPase p97, also called valosine containing protein (VCP). The IC50 for p97 inhibition is 110 nM. ML240 rapidly induces activity of Caspases 3 and 7, leading to apoptosis. ML240 has potent antiproliferative activity towards NCI-60 cancer cell lines.
SML1219   ML243 ≥98% (HPLC) ML243 is a potent and selective inhibitor of cancer stem-like cells (CSCs) that selectively eradicate CSCs in heterogeneous cancer cell populations.
SML0723   ML252 ≥98% (HPLC) ML252 is a potent, brain penetrant potassium channel Kv7.2 (KCNQ2) inhibitor with an IC50 of 69 nM. ML252 is only slightly selective over KCNQ3 and KCNQ4 but is over 40-fold selective for KCNQ2 vs KCNQ1, unlike other KCNQ inbhibitors currently used. ML252 was also selective vs. >68 tested GPCRs, ion channels, and transporters. Potassium channel Kv7.2 has become a new target for Alzheimer′s Disease drug research because inhibiting it enhances acetylcholine release. SAR studies showed a small structural change from ethyl group to hydrogen resulted in a functional shift from antagonist to agonist activity (37, EC50 of 170 nM), suggesting an interaction at a critical site for controlling KCNQ2 channel gating.
SML0831   ML261 ≥98% (HPLC) ML261 blocks lipid droplet formation in murine AML-12 hepatocytes grown in the presence of oleic acid, with an IC50 of 69.7 nM. ML261 appears to be species specific, the compound does not affect lipid droplet formation in HuH7 or primary human hepatocytes.
SML1755 ML264 ≥98% (HPLC) ML264 is a potent and selective inhibitor of Kruppel-like factor 5 (KLF5) expression. ML264 potently inhibits proliferation of colorectal cancer cells in vitro through modifications of the cell-cycle profile.
SML0524 ML277 ≥98% (HPLC) ML277 is a potent activator of KCNQ1 (Kv7.1) channels with >100-fold selectivity versus KCNQ2 and KCNQ4 and no activity against the hERG potassium channel up to 30 μM. KCNQ1 is a voltage-gated potassium channel required for repolarization phase of the cardiac action potential. Mutations in the KCNQ1 gene are associated with long QT syndrome (LQTS), a disorder in which the heart muscles take longer than normal to recover after each heart beat and can lead to dangerous arrhythmias such as atrial fibrillation. Activators of KCNQ1 channels could have potential use in treatments of LQTS. ML277 is the first selective and potent activator found, with an EC50 of 260 nM.
SML0555   ML289 ≥98% (HPLC) ML289 (VU0463597) is a potent, selective and centrally penetrant negative allosteric modifier (NAM) of metabotropic glutamate receptor 3 (mGlu3). ML289 is >15-fold selective vs mGlu2 with an IC50 value of 0.66 μM.
SML0978   ML291 ≥98% (HPLC) ML291 specifically activates the apoptotic arm of the cellular unfolded protein response ( UPR) EC50 = 762 nM) with 105-fold selectivity over activation of the adaptive UPR pathway. ML291 induces apoptosis in wild-type mouse embryonic fibroblasts (MEFs), but not in CHOP KO MEFs.
SML0836   ML297 ≥98% (HPLC) ML297 (VU0456810) is the first potent and selective activator of the GIRK potassium channel. The G protein-coupled inwardly-rectifying potassium channels (GIRKs 1-4) are widely distributed broadly in the central nervous system (GIRKs 1-3) and also found in the heart (GIRK-4). ML297 activates GIRK channels containing a GIRK1 subunit, and does not activate channels without a GIRK1 subunit or the closely related potassium channel Kir2.1 or voltage-gated potassium channels. ML297 has been shown to activate GIRK1/2 with a potency of ~160 nM and also to activate GIRK channels comprising of GIRK1/3 and GIRK1/4 subunit combinations. ML297 was active in two in vivo models of epilepsy, and showed equal or greater efficacy than the anti-seizure medication, sodium valproate.
SML1077   ML298 ≥98% (HPLC) ML298 is a potent, specific inhibitor of Phospholipase D2 (PLD2; IC50 = 355 nM). ML298 does not affect PLD1 activity at concentrations up to 20 μM.
SML1145 ML303 ≥98% (HPLC) ML303 is a potent inhibitor (IC50 = 155 nM) of the influenza viral protien NS1. NS1 enhances virulence by inhibiting host cell immune responses, including the expression of IFN-b, and regulating synthesis, splicing and translation of viral RNA.
SML1298   ML309 hydrochloride ≥98% (HPLC) ML309 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) (R132H and R132C) that binds reversibly the enzyme. ML309 inhibits production of neomorphic 2-hydroxyglutarate in glioblastoma cell line.
SML0926   ML314 maleate ≥98% (HPLC) ML314 is a biased agonist of the Neruotensin 1 (NTR1) receptor. ML314 induces recruitment of β-arrestin to NTR1 with an EC50 of 2 μM, but does not induce G-protein mediated Ca2+ mobilization.
SML1204   ML318 ≥98% (HPLC) ML318 is a biaryl nitrile inhibitor of PvdQ acylase. It decreases the intracellular uptake of iron inside the bacteria.
ML318 is an inhibitor of the siderophore PvdQ (pyoverdine Q), a peptide iron scavenger found in bacteria. ML318 inhibits the biosynthesis of one step in the pyoverdine biosynthesis with an IC50 of 20 nM, and is active in cells.
SML1177   ML323 ≥98% (HPLC) ML323 induces viral replication in vitro and in vivo. It may act as a potential candidate for the intervention of diseases like rheumatoid arthritis and systemic lupus erythematosus.
ML323 is a potent selective inhibitor of the USP1–UAF1 deubiquitinase complex with an IC50 of 76 nM in a ubiquitin-rhodamine (Ub-Rho) assay and excellent selectivity against other human deubiquitinases (DUBs), deSUMOylase, deneddylase and unrelated proteases. Human ubiquitin-specific protease 1 (USP1) associated with UAF1 is involved in the DNA damage response in the DNA translesion synthesis and Fanconi anemia pathways as the DUB responsible for deubiquitinating PCNA, which allows DNA replication past DNA lesions, and FANCD2 and FANCI, which function in interstrand crosslink repair. ML323 was found to potentiate cisplatin cytotoxicity in non-small cell lung cancer and osteosarcoma cells.
SML0741 ML324 ≥98% (HPLC) ML324 is a potent JMJD2 demethylase inhibitor that is highly effective in reducing herpes simplex virus (HSV) IE gene expression. ML324 potently blocks the initiation of viral lytic infection and HSV-1 reactivation in the sensory ganglia of latently infected mice.
SML1185 ML338 ≥98% (HPLC) ML338 is a selective inhibitor of non-replicating Mycobacterium tuberculosis bacilli.
SML1117 ML345 ≥98% (HPLC) ML345 is a cell penetrant, potent and moderately selective insulin degrading enzyme (IDE) inhibitor that targets Cys819 in IDE. IDE is involved in β-chain of insulin degradation and linked to β-amyloid degradation. Recent findings indicate that IDE inhibition is a valid strategy for DMT2 treatment.
SML1273 ML347 ≥98% (HPLC) ML347 is a derivative of dorsomorphin that is a highly selective antagonist of BMP receptor isotypes ALK1 and ALK2 (IC50 values = 46 and 32 nM, respectively). ML347 has little effect on other ALK isoforms, including ALK3 (IC50 = 10 μM).
SML1901 ML348 ≥98% (HPLC) ML348 is a substrate-competitive, reversible and APT1-selective acyl-protein thioesterase (APT) inhibitor (IC50/Ki = 840 nM/300 nM against APT1; IC50 & Ki >10 μM against APT2). ML348 effectively inhibits cellular APT1 activity in cultures (by >95% in HEK293T & mouse T cells; 5 μM for 4 h) and in mice in vivo (by >90% in lung/heart/kidney and by ~50% in brain tissue 4 h post 50 mg/kg i.p. dosing) without affecting more than 15 cellular serine hydrolases and APT2.
SML1918 ML349 ≥98% (HPLC)    
SML1353 ML351 ≥98% (HPLC) ML351 is a cell penetrant, selective and highly potent human lipoxygenase-12/15 (15-Lipoxygenase-1, 12/15-LOX) inhibitor that exhibits protective effects against oxidative glutamate toxicity in mouse neuronal HT22 cells. ML351 reduces infarct size in a mouse model of ischemic stroke.
SML1439 ML354 ≥98% (HPLC) ML354 is a potent and selective PAR4 (protease activated receptor-4) antagonist.
SML1920   ML364 ≥98% (HPLC) ML364 is a potent and specific inhibitor of the deubiquitinase USP2 that induces cellular Cyclin D1 degradation in HCT116 colorectal cancer cells, followed by cell cycle arrest and apoptosis. Also, ML364 inhibits homologous recombination (HR)-mediated DNA repair.
SML1833 ML385 ≥98% (HPLC) ML385 inihbits the activity of the Nrf2 transcription factor by binding to Neh1, a CNC-bZIP domain that allows Nrf2 to heterodimerize with small Maf proteins, blocking NRF2 transcriptional activity. Much research has been done on activating Nrf2 because it induces cytoprotective antioxidant genes. However, some cancer cells may use Nrf2 similarly for their survival. Nrf2 is overexpressed in certain cancers such as non-small cell lung cancer (NSCLC) often due to loss of function mutations in KEAP1, which targets Nrf2 for proteasomal degradation. ML385 was found to have anti-tumor activity with specificity and selectivity for NSCLC cells with KEAP1 mutations.