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SML2236 L-012 sodium salt ≥98% (HPLC) L-012 is a luminol analog and a widely used reactive oxygen and nitrogen species (RONS; ROS & RNS) chemiluminescence (CL) probe both in cultures and in animals in vivo. L-012 displays significantly higher CL yield and sensitivity than luminol, lucigenin and MCLA. Instead of reacting with superoxide anion (O2) directly, L-012 (LumH2) is converted via a one-electron oxidation (catalyzed by peroxidase in the presence of H2O2) to the LumH· radical form, which then reacts with oxygen (O2) to yield O2 and L-012 quinone (q-Lum). The O2 in turn reacts with the LumH· radical, leading eventually to an endoperoxide that decomposes to emit luminescence. To a less extend, H2O2 can also react with q-Lum to yield luminescence. Although not specific to NADPH oxidase-derived RONS, L-012 is also commonly used for screening NADPH oxidase inhibitors.
SML0891   L-152,804 ≥98% (HPLC) L-152,804 is a potent and selective non-peptide neuropeptide Y Y5 receptor antagonist. L-152,804 induces a potent reduction of food intake in rodents.
SML0690   L-161,982 ≥98% (HPLC) L-161,982 is a potent EP4 receptor antagonist that is selective over all other members of the prostanoid receptor family (Ki values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μM for human EP4, TP, EP3, DP, FP, IP, EP1 and EP2 receptors respectively.
SML1010 L-742001 hydrochloride ≥98% (HPLC) L-742,001 is an inhibitor of the influenza virus RNA polymerase PA subunit, implicated in several roles, including endonuclease and protease activities as well as viral RNA/complementary RNA promoter binding. L-742,001 inhibits the influenza endonuclease-dependent polymerase activity with an IC50 of 430 nM.
L-742001 is useful in the treatment of influenza viral infection.
SML1338 L-779450 ≥98% (HPLC) L-779450 is a potent inhibitor in Raf-induced proliferation of Raf-1 and A-Raf-1 kinases. Raf inhibition is a target for anti-cancer therapy. Raf exists in three isoforms: Raf-1, A-Raf, and B-Raf, which are expressed at different levels in different cell types, tissues, and cancer states. L-779450 compound′s pharmacology found it to inhibit proliferation in Raf-1 and A-Raf, but not B-Raf responsive cells. L-779450 has been used as a reference Raf inhibitor to discover other compounds.
L4545 L-798106 ≥98% (HPLC) L-798106 was among the first prostanoid receptor EP3-selective antagonists. It has been used in multiple studies to tease out EP3 agonist activity, both in vitro and in vivo. It successfully blocks the actions of sulprostone, an EP3-selective agonist, and it helped show that the vascular contraction effect of PGE2 is due to its prostanoid EP3 agonist activity.
SML2199 L-F001 ≥98% (HPLC) L-F001 is a multifunctional, brain penetrant and potent Rho-associated protein kinase (ROCK) inhibitor that protects the PC12 cells from paraquat induced cytotoxicity. L-F001 suppresses neuroinflammation in vitro and in vivo.
SML2645 L-Homocitrulline ≥95% (HPLC) L-Homocitrulline is a natural amino acid amino acid found in milk of mammalian.
SML0759   L002 ≥98% (HPLC) L002 (NSC764414) is an inhibitor of acetyltransferase p300, a lysine acetyltransferase that catalyzes acetyl group attachment to lysine residues of a variety of proteins including histones and p53, and acts as a critical coactivator of several oncogenic transcription factors involved in cancer cell survival and proliferation including STAT3, NF-kB, and hypoxia-inducible factor-1α (HIF-1α). L002 (NSC764414) was discovered from compounds assayed for cytotoxicity to the triple-negative breast cancer (TNBC) cell line MDA-MB-231 but not to the human mammary epithelial cells, then further screened for inhibition of p300. L002 has an in vitro IC50 of 1.98 μM for p300 with lesser inhibition of the GNAT (GCN5-related N-acetyltransferase) family, and no inhibition against the MYST family of histone acetyltransferases (HATs), histone deacetylases (HDACs), or histone methyltransferases (HMTs). L002 potently suppressed tumor growth and histone acetylation of MDA-MB-468 xenografts and leukemia and lymphoma cell lines.
L2167 L-165,041 ≥98% (HPLC), powder PPARβ (PPARδ) selective agonist.
human ... PPARD(5467)
SML0134   L2-b ≥98% (HPLC) L2-b is a bifunctional Aβ-interacting, metal-chelating molecule that modulates ROS production in, and improves survival of neuroblastoma cells incubated in the presence of Aβ along with Copper or Zinc. In cell-free aggregation studies, L2-b inhibits metal-induced Aβ aggregation, and also promotes the dissociation of Ab aggregates in homogenates of human AD brain samples.
L2540 L-368,899 ≥98% (HPLC), powder L-368,899 is a non-peptide oxytocin receptor (OTR) antagonist.
human ... OXTR(5021)
SML1443 L48H37 ≥98% (HPLC) L48H37 is a potent and chemically stable anti-inflammatory curcumin analog that inhibits LPS-induced inflammation through the myeloid differentiation 2 (MD-2) and toll-like receptor 4 (TLR4) complex. L48H37 is a potent MD2 inhibitor that binds to the hydrophobic region of MD-2 and blocks the interaction between MD2 and LPS. L48H37 significantly improves survival and protected lung injury in LPS-induced septic mice.
L9787 L-655,708 ≥98% (HPLC), powder L-655,708 is an inverse agonist of the α5 γ-Aminobutyric acid type A (GABAA) receptor. It has an ability to increase cognition in rats.
Novel ligand selective for the benzodiazepine site of GABAA receptors which contain the α5 subunit.
human ... GABRA5(2558)
SML1797 L67 ≥98% (HPLC) L67 is a potent and specific inhibitor of DNA ligase IIIα (LigIIIα) that preferentially targets mitochondrial LigIIIα resulting in mitochondrial dysfunction. L67 preferentially targets cancer cell mitochondria resulting in enhanced ROS production and caspase 1-dependent apoptosis. L67 in combination with PARP inhibitors decreases survival rate of therapy resistant breast cancer and leukemia cells.
L1790 L-685,458 >96% (HPLC), solid L-685,458 is a potent, selective, structurally novel γ-secretase inhibitor; equipotent inhibitor of both Aβ1-42 and Aβ1-40 production.
L-685,458 mimics the transition state in aspartyl protease. It possesses an IC50 of 17nM with respect to inhibition of Aβ synthesis. It is known to block Notch (neurogenic locus notch homolog protein) signaling, which in turn reduces ERK (extracellular signal regulated kinase) phosphorylation by EGF (epidermal growth factor). L-685,458 targets the active site and substrate binding site of the enzyme.
human ... APH1A(51107), APH1B(83464), NCSTN(23385), NOTCH1(4851), NOTCH2(4853), NOTCH3(4854), NOTCH4(4855), PSEN1(5663), PSEN2(5664), PSENEN(55851)
mouse ... Aph1a(226548), Aph1b(208117), Ncstn(59287), Notch1(18128), Notch2(18129), Notch3(18131), Notch4(18132), Psen1(19164), Psen2(19165), Psenen(66340)
rat ... Aph1a(365872), Aph1b(300802), Ncstn(289231), Notch1(25496), Notch2(29492), Notch3(56761), Notch4(406162), Psen1(29192), Psen2(81751), Psenen(292788)
L8539 L-687,384 hydrochloride ≥98% (HPLC), powder σ1 receptor agonist.
human ... OPRS1(10280)
L0258 L-701,324 ≥98% (HPLC), solid L-701,324 is a high affinity, selective antagonist at the glycine site of the NMDA glutamate receptor. L-701,324 is a potent, active anticonvulsant with a reduced propensity to activate mesolimbic dopaminergic systems in rodents.
human ... GRIN1(2902)
rat ... Grin1(24408), Grin2a(24409)
L119 L-703,606 oxalate salt hydrate solid Potent and selective non-peptide NK-1 tachykinin receptor antagonist.
human ... TACR1(6869)
L135 L-741,626 ≥98% (HPLC) Selective D2 dopamine receptor antagonist.
human ... DRD2(1813), DRD3(1814), DRD4(1815)
L131 L-745,870 hydrochloride Selective D4 dopamine receptor antagonist.
human ... DRD4(1815)
SML1362 L755507 ≥98% (HPLC) L755507 is a potent β3-adrenergic receptor partial agonist with an EC50 value of 0.43 nM for β3 receptors with over 440-fold selectivity for β3 compared to β1 and β2-adrenergic receptor binding. L755507 has been shown to enhance CRISPR-mediated homology-directed repair (HDR) efficiency in human induced pluripotent stem cells (iPSCs), increasing the efficiency of GFP insertion by 3-fold compared to control cells.
L755507 is a potent β3-adrenergic receptor partial agonist.
L755507 is found to stimulate the breakdown of lipids in human adipose tissues. L755507 also promotes urinary bladder relaxation.
L1011 Labetalol hydrochloride >98% (TLC), powder Competitive β-adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152), ADRB1(153), ADRB2(154), ADRB3(155)
SML0946   Lacidipine ≥98% (HPLC) Lacidipine is a long-acting calcium antagonist that is used in the management of hypertension. Lacidipine is a L-type Ca(2+) channel blocker belonging to 1,4-dihydropyridine class. Also, Lacidipine inhibits ryanodine receptors on the ER membrane that enhances folding, trafficking and lysosomal activity of ERAD (ER-associated degradation) misfolded lysosomal glucocerebrosidase (GS).
L6785 Lactacystin ≥90% (HPLC) Lactacystin can block the development of cell cycle and stimulate differentiation in a murine neuroblastoma cell line. It can serve as a precursor for clasto-lactacystin β-lactone. Cell-permeable and irreversible proteasome inhibitor (Ki = 4nM). Inhibits NF-kB activation (IC50 = 10mM). Induces neurite outgrowth in neuro2A mouse neuroblastoma cells.
SML2263 Ladostigil tartrate ≥98% (HPLC) Multifunctional drug designed to treat Alzhemier′s disease by combining in a single molecule the neuroprotective/neurorestorative effects of the (MAO)-B inhibitor rasagiline with the cholinesterase (ChE) inhibitory activity of rivastigmine.
SML1611 Lafutidine ≥98% (HPLC) Lafutidine is a second generation H2 histamine receptor antagonist. Lafutidine has been used clinically to treat ulcers and gastro-esophageal reflux disease (GERD). Lafutidine has also been investigated as a treatment against peripheral neuropathy and for its protective stomach effects during cancer chemotherapies and long term ibuprofen use.
SML2053 Lalistat 2 ≥98% (HPLC) Lalistat-2 is a potent and specific competitive inhibitor of the lysosomal acid lipase (LAL/Lipa). Lalistat-2 affects lipid droplets morphology and localization.
L1295 Lamivudine ≥98% (HPLC), powder Lamivudine is a potent nucleoside analog reverse transcriptase inhibitor (nRTI). It is an analogue of cytidine, and can inhibit both types (1 and 2) of HIV reverse transcriptase as well as the reverse transcriptase of hepatitis B. It needs to be phosphorylated to its triphosphate form before it is active. 3TC-triphosphate also inhibits cellular DNA polymerase.
L3791 Lamotrigine ≥98%, powder Anticonvulsant.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
rat ... Scn2a1(24766), Scnn1a(25122)
SML1082 Lamotrigine isethionate ≥98% (HPLC) Lamotrigine isethionate is an anticonvulsant, water soluble salt of Lamotrigine (Catalog No. L3791).
SML1785 Landiolol hydrochloride ≥98% (HPLC) Landiolol is an ultra-short acting cardioselective β-adrenoceptor antagonist the exhibit β1-selectivity. New data shows that landiolol lacks pharmacochaperoning activity.
L5768 Lanosterol ≥93%, powder Cholesterol precursor sterol.
Lanosterol serves as an endogenous selective modulator of macrophage immunity.
SML0132 Lanreotide acetate ≥98% (HPLC) Lanreotide acetate is a somatostatin analog, a selective agonist for the SRIF-1 sst2 subtype of somatostatin receptor with a binding affinity of 0.8 nM for sst2 compared to 5.2 nM for sst5, 100 nM for sst3 and more than 1000 nM for the SRIF-2 subtypes, sst1 and sst4 receptors. It is used clinically in the management of acromegaly and symptoms caused by neuroendocrine tumors, and in recent studies can also inhibit tumor growth and has shown activity against non-endocrine tumors.
L8533 Lansoprazole ≥98% (TLC), powder Gastric proton pump inhibitor.
human ... ATP4A(495), ATP4B(496)
L2037 β-Lapachone ≥98% (TLC) β-Lapachone is a naturally occurring quinone obtained from the bark of the lapacho tree (Tabebuia avellanedae) with cancer chemopreventive properties. Induces apoptosis in HL-60 and human prostate cancer cells.
SML2259 Lapatinib ≥98% (HPLC) Lapatinib is a dual ErbB-1(EGFR) and ErbB-2 (HER2neu) tyrosine kinase inhibitor with very slow off-rate.
human ... EGFR(1956), ERBB2(2064)
SML2504 Laquinimod ≥98% (HPLC) Laquinimod is an immunomodulator being investigated as a treatment for relapsing-remitting multiple sclerosis (RRMS).
SML2475 Larazotide acetate salt ≥95% (HPLC) Larazotide acetate (AT1001) is a Zonulin receptor antagonist, a tight junction modulator. Larazotide inhibition of zonulin results in reducing trafficking across epithelial cells in the intestines and reducing intestinal permeability and "leaky gut," thought to be a gateway to multiple autoimmune diseases, including celiac disease, irritable bowel syndrome (IBS), inflammatory bowel diseases (IBD, Crohn′s and ulcerative colitis), type 1 diabetes mellitus (T1DM), nonalcoholic steatohepatitis (NASH), chronic kidney disease (CKD) and several others. It has been shown to inhibit the effect of inflammatory cytokines such as tumor necrosis factor (TNF-alpha) and interleukin (IL-4), blocking their increase of intestinal epithelial permeability.
SML1026 Lasofoxifene tartrate ≥98% (HPLC) Lasofoxifene is a third-generation selective estrogen receptor modulator (SERM).
Lasofoxifene possesses strong resistance to intestinal wall glucuronidation and thus promotes oral bioavailability. In postmenopausal women, it reduces bone resorption, bone loss and low density lipoprotein (LDL) cholesterol. Selective and regular dose of Lasofoxifene is known to reduce the risk of fractures, breast cancer, major coronary heart disease, and stroke.
L1167 Latanoprost ≥98% (HPLC) Latanoprost is a potent, selective prostaglandin F2α analog receptor agonist. It is hydrolyzed by esterases into its biologically active form latanoprost acid in the cornea. Latanoprostplays a role in reducing the intraocular pressure (IOP) due to which it has therapeutic effects in treating glaucoma.
human ... PTGFR(5737)
L1417 15(S)-Latanoprost solution ≥95%    
L1292 Latanoprost acid ≥98% (HPLC) Potent, selective FP prostanoid receptor agonist, F-series prostaglandin analog. 200 times as potent as isopropyl ester form.
mouse ... Ptgfr(19220)
L5163 Latrunculin A from sea sponge, ≥85% (HPLC), waxy solid Latrunculin A inhibits actin polymerization by a different mechanism than cytochalasins. Latrunculin A disrupts microfilament-mediated processes.
L5288 Latrunculin B from Latruncula magnifica ≥80% (HPLC), solid Latrunculin B inhibits actin polymerization in vitro. Latrunculin B disrupts microfilament-mediated processes.
SML0042 Lazabemide hydrate ≥97% (HPLC) Lazabemide is a selective and reversible monoamine oxidase B (MAO-B) inhibitor and Anti-Parkinson. Also it inhibits monoamine uptake at high concentrations (IC50 values are 86, 123 and > 500 μM for noradrenalin, serotonin and dopamine uptake respectively).
Lazabemide is effective in treatment of Alzheimer′s disease and in combination with nicotine replacement therapy aids in smoking cessation.
SML2064 LBQ657 ≥97% (HPLC) LBQ657 is the active metabolite of sacubitril. It is an inhibitor of the enkephalinase neprilysin (neutral endopeptidase, NEP) formed by the action of esterases on its prodrug sacubitril (AHU377), which is half of the heart failure combination drug Entresto, along with the angiotensin-receptor blocker Valsartan. LBQ657 prevents neprilysin′s degradation of atrial and brain natriuretic peptide, two blood pressure lowering peptides.
SML2052 LCAT activator compound A ≥98% (HPLC) LCAT activator compound A is an activator of Lecithin:cholesterol acyltransferase (LCAT) including some mutant LCATs found in Familial LCAT Deficiency (FLD). LCAT activator compound A forms a covalent hydrophobic adduct with LCAT Cys 31. The chronic treatment with LCAT activator compound A results in a significant increase in HDLc, HDL particle, size, plasma apolipoprotein A-I level, plasma cholesteryl ester to free cholesterol ratio, and a significant reduction in very low-density lipoprotein cholesterol in hamsters.
SML0466 LCS-1 ≥98% (HPLC) LCS-1 is an inhibitor of superoxide dismutase (SOD1). LCS-1 inhibits the proliferation of lung adendocarcinoma cell lines.
SML2179 LDC000067 hydrochloride ≥98% (HPLC) LDC000067 (LDC067) is an ATP-competitive, potent and selective cyclin-dependent kinase 9 (CDK9) inhibitor (IC50 = 44 nM/CDK9-CycT1 vs. 5.51 μM/CDK1-CycB1, 2.44 μM/CDK2-CycA, 9.24 μM/CDK4-CycD1, >10 μM/CDK6-CycD3 & CDK7-CycH-MAT1; Kd = 32.7 nM/CDK9-CycT1 vs. 1.01 μM/CDK2-CycA, 16.0 μM/CDK7-CycH-MAT1) with much reduced or little potency against a panel of 28 non-CDK kinases. LDC067 selectively inhibits cellular RNA polymerase II CTD Ser2 phosphorylation (by 40% in HeLa; 60-min, 10 μM LDC067), but not CDK9-independent pSer5 or pSer7, causing apoptosis induction (by 239% and 200% of untreated control in A549 and MCF7 cultures) as a result of blocking RNAPII-mediated mRNA synthesis.
SML2582 LDK1305 ≥98% (HPLC) LDK1305 is a selective positive allosteric modulator of CB1 that promote the binding of the agonist CP55940 and inhibits binding of orthosteric inverse agonist SR141716A. LDK1305 is a beta-arrestin-biased ligand that induces cellular internalization of the receptor and recruitment of β-arrestin 2 in HEK293 cells. It stimulates also β-arrestin 1-dependent phosphorylation of the downstream kinases, ERK1/2, MEK, and Src.
SML0755   LDN-192960 dihydrochloride ≥98% (HPLC) LDN-192960 is a potent and selective inhibitor of haspin (Haploid Germ Cell-Specific Nuclear Protein Kinase).
SML0559 LDN193189 hydrochloride ≥98% (HPLC) Although LDN193189 is a structural analog of dorsomorphin, these two drugs are found to establish different cellular responses. In vitro analysis reveals that LDN193189 inhibits a number of intracellular kinases such as, mitogen activated protein kinase 14 and 8 ( p38and c-Jun N-terminal kinase respectively), as well as those associated with AKT (serine/threonine kinase) and mTOR (mammalian target of rapamycin) signaling mechanisms. LDN193189 is known to elevate the levels hemoglobin and thus helps to prevent the onset of anemia of inflammation.
LDN193189 is a derivative of dorsomorphin that is a highly selective antagonist of BMP receptor isotypes ALK2 and ALK3 (IC50 of: 5 and 30 nM). The selectivity of LDN193189 for ALK2/3 is 200 fold over the TGF-B type receptors ALK4,-5 and -7. In murine smooth muscle cells, the compound inhibits BMP-4 induced phosphorylation of SMAD 1/5/8 with an IC50 of 5 nM.
SML0965   LDN-212854 ≥98% (HPLC) LDN-212854 is a selective and potent inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases with over 5,000-fold selectivity for BMP versus the closely related TGF-β and activin type I receptors. LDN-212854 has some selectivity for ALK2 with an IC50 of 1.3 nM in preference to other BMP type I receptors, ALK1 (IC50=2.4 nM) and ALK3 (IC50=85.8 nM). LDN-212854 shows better selectivity than LDN193189 in cell-based assays of BMP signaling. LDN-212854 inhibited BMP6-induced osteogenic differentiation, which functions primarily via ALK2, more potently than BMP4, which functions primarily with ALK3 (IC50s of 10 nM versus 40.5 nM), whereas LDN-193189 inhibited both equally. The only off target effects found against a panel of 198 kinases were for RIPK2, ABL1, and PDGFR-β with IC50 values < 100 nM.
LDN-212854 is also known as 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline. LDN-212854 prevents heterotopic ossification in an inducible mutant ALK2 (activin receptor-like kinase 2).
SML1119 LDN-214117 ≥98% (HPLC) LDN-214117 is a selective inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases with high selectivity for BMP versus TGF-β signaling, and low cytotoxicity. LDN-214117 inhibited ALK2 most, with a biochemical IC50 of 24 nM, followed by TNIK, RIPK2, and ABL1. LDN-214117 has a cell-based IC50 for BMP6 of approximately 100 nM and 164-fold selectivity for BMP6 versus TGF-β1. Fibrodysplasia ossificans progressiva (FOP) is a debilitating and progressive heterotopic ossification disease caused by activating mutations of ACVR1 encoding the BMP type I receptor kinase ALK2. LDN-214117 had nearly identical binding affinity for wild-type ALK2 and each of the FOP-causing mutants tested.
SML0744   LDN-27219 ≥98% (HPLC) LDN-27219 is a revesible inhibitor of transglutaminase 2 (TG2) that binds to the GTP binidng site of the enzyme and inhbits activity with and IC50 of 600 nM.
L4170 LDN-57444 ≥98% (HPLC) LDN-57444 is a potent, reversible, competitive and active site-directed inhibitor of UCHL1
L4295   LDN-91946 ≥98% (HPLC) LDN-91946 is a potent, selective and uncompetitive UCH-L1 inhibitor that targets the enzyme-substrate complex, but not the free enzyme. Ubiquitin C-terminal hydrolase L1 (UCH-L1) is a deubiquitinating enzyme. It is one of the most abundant proteins in the brain. UCKL1 plays a key role in processing polyubiquitin and ubiquitylated proteolytic peptides. The enzyme has been linked to Parkinson disease and lung cancer. LDN-91946 inhibits UCH-L1-catalyzed substrate hydrolysis in an uncompetitive manner by targeting the enzyme-substrate complex, but not the free enzyme. The compound is quite specific and is exhibiting little activity against UCH-L3, TGase 2, Papain, or Caspase-3 even at concentrations as high as 20 μM. Compound was recently launched by Calbiochem. LDN-57444 is acts as competitive inhibitor.
SML0809   LE 135 ≥98% (HPLC) LE135 is a retinoic acid receptor (RAR) antagonist with selectivity for RARβ (Ki = 220 nM) over RARα (Ki = 1.4 μM). LE135 inhibits retinoic acid-induced transcriptional activation of RARβ (>70% inhibition at 10 μM), but not RARα, RARγ or retinoid X receptor α (RXRα). There is high interest in retinoic acid receptors for cancer and for differentiation studies. LE135 has been shown to inhibit retinoid Am80-induced differentiation of human promyelocytic leukemia HL-60 cells with an IC50 value of 0.2 μM. LE135 has been used to study the role of a retinoic acid receptor-β (RARβ) on the differentiation of mesenchymal stem cells, and was found to inhibit the neuronal differentiation promoting effects of all-trans retinoic acid (ATRA) on mesenchymal stem cells.
SML1841   Lecirelin trifluoroacetate salt ≥98% (HPLC) Lecirelin is synthetic hypothalamic gonadotropin releasing hormone (GnRH) analogue. Lecirelin is a potent and longer lasting agonist of gonadotropin-releasing hormone receptor (GnRHR).
SML2283 Lenalidomide ≥98% (HPLC) Lenalidomide, a derivative of thalidomide, is an immunomodulatory agent that is approved drug for treatment of multiple myeloma. Apparently Lenalidomide is a ligand of ubiquitin E3 ligase cereblon that induces the enzyme to degrade the Ikaros transcription factors IKAROS family zinc finger 1 (IKZF1) and IKZF3. Lenalidomide possess pleiotropic antitumor effects. It is used in the treatment of 5q-deletion associated myelodysplastic syndrome (del(5q)-MDS).
SML0670 Leonurine ≥98% (HPLC) Leonurine (SCM-198) is a natural product with antioxidant, anti-inflammatory, and cardioprotective activity being investigated for the treatment of cardiovascular disease and stroke. Leonurine suppresses inflammation and oxidative stress, decreasing a number of inflammatory factors, reducing cardiac Nox4 expression, ROS production, NF-KB activation, and plasma MMP-2 activity and increasing superoxide dismutase (SOD).
L6417 Leptomycin A from Streptomyces sp., ~95% (HPLC), methanol solution Leptomycins are antifungal antibiotics with unique unsaturated, branched-chain fatty acid structures. The physiochemical and biological properties of Leptomycins A and B are very similar. Both are considered to be specific inhibitors of nuclear export. The suggested inhibition mechanism involves the direct binding of leptomycins to CRM1 (Exportin-1), which is the main nuclear export protein. This blocks the binding of CRM1 to proteins containing a nuclear export signal (NES), and therefore prevents their export from the nucleus. Although more research on nuclear export inhibition has been performed using Leptomycin B, it has been shown that Leptomycin A has similar effects and can induce, for example, nuclear accumulation of wild-type ERK5.
Leptomycin A is also active against Schizosaccaromyces pombe and Mucor rouxianus.
L2913 Leptomycin B solution from Streptomyces sp. ≥95% (HPLC), Supplied in methanol: water (7:3) Leptomycin B is an unsaturated, branched-chain fatty acid, and is an important tool in the study of nuclear export. Leptomycin B is a specific inhibitor of proteins containing nuclear export signal. Leptomycin B inhibits nucleo-cytoplasmic translocation of molecules such as the HIV-1 Rev protein and Rev-dependent export of mRNA. The addition of very small amounts to fibroblasts causes accumulation of MEK in the nucleus. Other proteins that are influenced by leptomycin B are actin, c-Abl, cyclin B1, MDM2/p53, IκB, MPF, and PKA. The suggested inhibition mechanism involves the direct binding of leptomycin B to CRM1, which blocks the binding of CRM1 to proteins containing the nuclear export signal, via the interaction with cysteine residue in CRM1 control conserved region.
L6668 Lercanidipine hydrochloride ≥98% (HPLC) Lercanidipine hydrochloride is a L-type (Cav1.2b) vascular channel antagonist; L-type (Cav1.2a) cardiac channel agonist voltage-dependent and highly lipophylic compound, which exhibits a slower onset and longer duration of action than other calcium channel antagonists; an antihypertensive agent in patients with mild-to-moderate hypertension; more vasoselective than lacidipine and amlodipine.
SML1607 Lesinurad ≥98% (HPLC) Lesinurad is a selective inhibitor of Urate transporter 1 (URAT1), a urate-anion exchanger which is responsible for the majority of uric acid reabsorption from the renal tubular lumen. Lesinurad thus reduces serum uric acid levels. Lesinurad has been approved for use in combination with a xanthine oxidase inhibitor to treat hyperuricemia associated with gout.
human ... SLC22A12(116085)
L6545 Letrozole ≥98% (HPLC) Letrozole acts as an adjuvant agent and is used to treat breast cancer.
Letrozole is a third generation nonsteroidal aromatase inhibitor. It is a competitive inhibitor of the aromatase enzyme system and thus inhibits the conversion of androgens to estrogens. Letrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues.
human ... CYP19A1(1588)
SML0886   Leukadherin-1 ≥98% (HPLC) Leukadherin-1 is an agonist of integrin CD11b/CD18 that can increase the extent of CD11b/CD18-dependent cell adhesion of transfected cells and of primary human and mouse neutrophils. Also, Leukadherin-1 decreases leukocyte recruitment and reduced arterial narrowing after injury in rats.
L0517 Leukotriene B4 ~100 μg/mL in ethanol, ≥97% Proinflammatory agent. Stimulates c-Fos and c-Jun proto-oncogene transcription in human monocytes. Stimulates chemotaxis, aggregation, and degranulation of polymorphonuclear leukocytes.
human ... LTB4R(1241)
rat ... Ltb4r(59264)
L5011 Leukotriene D4 ~50 μg/mL (in methanol/ammonium acetate buffer, 70:30, pH 5.6), ≥97% Slow reacting substance of anaphylaxis (SRS-A). Potent bronchoconstrictor and mediator of asthmatic and inflammatory processes. Increases cytosolic free Ca2+ in epithelial cells.
SML0138 Levalbuterol hydrochloride ≥98% (HPLC) Levalbuterol (levosalbutamol) is the more active isomer of albuterol. Levalbuterol is a β-adrenergic agonist; a bronchodilator used clinically to treat asthma and COPD..
Levalbuterol is (R)-albuterol that exhibits bronchodilator effect and is more effective than racemic albuterol for the treatment of exacerbation of asthma in pediatric populations.
human ... ADRB2(154)
L121 Levallorphan tartrate salt ≥98% (HPLC), powder Partial agonist (antagonist) at μ and δ opioid receptors.
human ... OPRD1(4985), OPRM1(4988)
L8668 Levetiracetam ≥98% (HPLC) Levetiracetam is a pyrrolidine with antiepileptic activity. Stereoselective binding of levetiracetam was confined to synaptic plasma membranes in the central nervous system with no binding occurring in peripheral tissue. Levetiracetam inhibits burst firing without affecting normal neuronal excitability, which suggests that it may selectively prevent hyper-synchronization of epileptiform burst firing and propagation of seizure activity.
human ... CACNA1B(774), SV2A(9900)
SML1092   Levobupivacaine hydrochloride ≥98% (HPLC) Levobupivacaine hydrochloride is a sodium channel blocker used as a long-acting local anaesthetic for epidural anesthesia. Levobupivacaine is the (S)-isomer of bupivacaine, with efficacy similar to that of bupivacaine with a reduced risk of cardiotoxicity.
Levobupivacaine mediates its action by blocking the action potential and sodium passage in neuronal membrane.
human ... SCN4A(6329)
L3042 Levocabastine hydrochloride ≥99% (HPLC), solid Non-peptide histamine H1 receptor antagonist; neurotensin NTS2 receptor ligand.
human ... HRH1(3269)
L7795 Levocetirizine dihydrochloride ≥98% (HPLC) Levocetirizine hydrochloride is a nonsedating antihistamine. It is a histamine H1-receptor antagonist, the active isomer of cetirizine. Levocetirizine has high bioavailability, high affinity for and occupancy of the H1 receptor.
human ... HRH1(3269)
L5143 Levorphanol (+)-tartrate salt dihydrate white powder, ≥98% (HPLC) Synthetic morphine analog that is a narcotic analgesic and μ opioid receptor agonist.
L5545 Levosimendan ≥98% (HPLC) Levosimendan has a potential to inhibit both acute human immunodeficiency virus type 1 (HIV-1) replication and the reactivation of latent HIV-1 proviruses. Therefore, it is considered to be a promising anti-HIV-1 agent.
Levosimendan is a calcium sensitiser. The compound increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan binds to cardiac troponin C in a calcium-dependent manner and stabilizes troponin C. This is followed by actin-myosin cross-bridges, without increasing myocardial consumption of ATP. Additionally the compound acts as vasodilator by opening an ATP-sensitive potassium channels. Levosimendan is a drug used for treatment of congestive heart failure. Also it can be used to treat calcium channel blocker overdose.
human ... PDE3A(5139), PDE3B(5140), TNNC1(7134), TNNI3(7137), TNNT2(7139)
SML1752 LF3 ≥98% (HPLC) LF3 is a potent inhibitor of Wnt/β-catenin signaling that suppresses cancer cells motility, cell-cycle progression, and the overexpression of Wnt target genes. LF3 is a potent and specific antagonist of the interaction between β-catenin and the transcription factor TCF4. LF3 blocks self-renewal of cancer stem cells.
L6920 LFM-A13 ≥98% (HPLC), powder LFM-A13 is an inhibitor of the nonreceptor tyrosine kinase Bruton′s tyrosine kinase (Btk), a new molecular target for treatment of B-cell lymphoma and autoimmune disorders. LFMA13 inhibited recombinant BTK with an IC50 value of 2.5microM with 100-fold lower inhibitory activity against a number of other protein kinases including JAK1, JAK2, EGFR, IRK, IKK, and CDK1, 2 and 3, as well as several other related kinases
SML0279 LG100268 ≥98% (HPLC) LG100268 (LG268) is a potent and selective rexinoid and retinoid-X receptor (RXR) agonist. LG100268 binds to the α, β and γ RXR receptors with an IC50 = 3-4 nM and has no activity at the RAR retinoic acid receptors.
SML0771   LG100754 ≥98% (HPLC) LG100754 is a unique RXR ligand that acts as an antagonist against RXR homodimers, but is a strong agonist for RXR:PPARα and RXR:PPARγ heterodimers. The compound does not have agonist activities for other RXR heterodimers containing LXR or GAR/FXR receptors. LG100754 initiates adipocyte differentiation, inhibits TNFα-induced insulin receptor hypophosphorylation and improves insulin resistance in db/db mice.
SML0695   LH846 ≥98% (HPLC) LH846 is a potent and selective inhibitor of the known clock regulatory kinase Casein Kinase CK1δ, with an IC50 of 290 nm, compared to an IC50 of 2.5 μm for CKIα , 1.3 μm for CKIε, and minimal effect on CK2 and 50 other kinases tested. Circadian rhythym has been studied for a long time for things such as jet lag rhythym related disorders, but more recently it has beencome apparent that clock dysfunction can contribute to a variety of pathologies including circadian sleep disorders, cardiovascular disease, cancer, and metabolic disease, so studies of clock regulating enzymes have increased. LH846 increased circadian period by 10 hours in human U2OS cells.
L7757 Lidocaine powder Lidocaine, a neuroprotective agent, mediates blockage of sodium (Na+) channels. It prevents the influx of sodium ions leading to depolarization of sodium channels and metabolically inactivated in liver. Lidocaine has positive effect on cerebral ischemia. It is also used in the treatment of ventricular tachycardia. Lidocaine is an efficient anesthetic agent in ophthalmic surgeries as it is highly potent and has good tissue penetrability.
Na+ channel blocker; class IB antiarrhythmic that is rapidly absorbed after parenteral administration.
human ... CYP1A2(1544), SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
rat ... Scnn1a(25122)
L1026 Lidocaine analytical standard Na+ channel blocker; class IB antiarrhythmic that is rapidly absorbed after parenteral administration.
human ... CYP1A2(1544), SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
rat ... Scnn1a(25122)
L5647 Lidocaine hydrochloride monohydrate solid Na+ channel blocker; class IB antiarrhythmic that is rapidly absorbed after parenteral administration
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
L1663 Lidocaine N-ethyl chloride Lidocaine N-ethyl chloride is an intracellular voltage-gated sodium channel blocker.
L9668 Lidoflazine ≥98% (HPLC), powder Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia. It prolongs QT interval by blocking HERG channel. IC50 < 0.1 μM
L6538 Limaprost ≥99%, crystalline    
PZ0014 Linezolid ≥98% (HPLC) Linezolid is an oxazolidinone antimicrobial. It binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex, thus inhibiting bacterial mRNA translation. Linezolid is also a weak, reversible, nonselective inhibitor of monoamine oxidase.
SML1969 Linoleamide ≥98% (HPLC) Linoleamide is an endogenous lipid, that stimulates sleep in cats, rats and humans.
Linoleamide is an endogenous primary fatty acid amide (PFAM) signaling lipid that modulates intracellular Ca2+ homeostasis. It has been shown to inhibit of SPCA2, a Golgi secretory pathway Ca(2+)-ATPase that transports ions of Ca2+ and Mn2+ and also to inhibit SPCA1a and the Ca2+-ATPase activity of three sarco(endo)plasmic reticulum Ca2+-ATPase (SERCA) pump isoforms. It is thought to be involved in a variety of biological activities including regulation of sleep.
O5507 Linoleic acid, conjugated Potent inhibitor of breast, skin, and colon carcinogenesis and tumor cell proliferation; inhibits bFGF-induced endothelial cell proliferation; potent antioxidant.
L2376 Linolenic acid ≥99% An ω-3 fatty acid that serves as a precursor to eicosapentaenoic acid (EPA) but not docosahexaenoic acid. Conversion is greater in women than men, and conversely, β-oxidation metabolism is greater in men than women.
Linolenic acid is involved in the formation of highly unsaturated fatty acid. It is essential for the development of skin, blood and neural cells. Linolenic acid is also associated with the organization of lipid membranes of neural synapses, pigment epithelial cells of retina and myocardial cells. It plays an important role in brain development and prostaglandin synthesis. Deficiency of essential fatty acid is related to skin disorders and growth retardation.
L1164 Linoleyl ethanolamide ≥98%, ethanol solution A structural analogue of the endogenous cannabinoid receptor ligand anandamide.
T5625 (±)-α-Lipoic acid synthetic, ≥99% (titration), powder Antioxidant and coenzyme needed for the activity of enzyme complexes such as those of pyruvate dehydrogenase and glycine decarboxylase. Exogenous thioctic acid is reduced intracellularly by two or more enzymes. The reduced form then influences a number of cell processes by direct radical scavenging, recycling of other antioxidants, increasing glutathione synthesis, and modulating transcription factor activity particularly that of NF-κB. Decreases the phagocytosis of myelin by macrophages.
human ... ACHE(43), BCHE(590)
rat ... Adra1a(29412), Adra1b(24173), Adra1d(29413)
L0521 Lipoxin A4 ethanol solution Lipoxin A4 (LXA4) is synthesized from arachidonic acid and is an endogenous lipoxygenase-derived eicosanoid mediator. It is a potent human protein kinase C activator. It inhibits cytotoxicity of natural killer cells. LXA4 regulates the immune system and inflammation. In the brain, it modulates neuronal signaling and slow wave sleep. LXA4 binds to cannabinoid receptors. LXA4 plays a key role in the maintenance of endometrium and reproductive function. Depletion of LXA4 contributes to the pathophysiology of cystic fibrosis (CF).
SML1414 Liproxstatin-1 >98% (HPLC) Liproxstatin-1 is a potent inhibitor of ferroptosis, a non-apoptotic form of cell death characterized by iron-dependent accumulation of lethal lipid reactive oxygen species (ROS). Liproxstatin-1 suppressed ferroptosis in human cells and in an ischaemia/reperfusion-induced tissue injury model in mice. Knockout of glutathione peroxidase 4 (Gpx4) Has been shown to cause cell death by ferroptosis. Liproxstatin-1 was able to suppress ferroptosis in Gpx4 knock-out mice.
SML2893 LIT-927 ≥98% (HPLC) LIT-927 is an orally active CXCL12 (SDF1) neutraligand (Kd = 267) that selectively neutralizes CXCL12, but not CCL17, CCL22, CCL5, or CCL2 activity in cultures (10 μM LIT-927 against 5 nM chemokine-induced calcium mobilization). LIT-927 reduces eosinophil recruitment in a murine allergic airway hypereosinophilia model in vivo (330 nmol/kg intranasal, 350 nmol/kg ip. or 1400 μmol/kg po.), offering greatly improved oral activity and solubility than Chalcone-4, and exhibiting little side-effects when compared with dexamethasone or CXCR4 antagonist AMD3100.
L1040   Livin β/ML-IAP human >95% (SDS-PAGE), recombinant, expressed in E. coli, buffered aqueous solution Livin β/ML-IAP, a member of the inhibitor of apoptosis (IAP) protein family, inhibits the activation of caspase 9 in cell extracts incubated with cytochrome c and dATP.
human ... BIRC7(79444)
SML2836   Lixisenatide ≥95% (HPLC) Lixisenatide (AVE0010, ZP10A) is a C-terminal amidated synthetic glucagon-like peptide-1 receptor (GLP-1R) agonist peptide whose sequence corresponds to Pro38 deleted exendin-4 with a C-terminal extension by six Lys residues. Lixisenatide exhibits 4-times higher human GLP-1R affinity than GLP-1(7-36) amide and dispalys in vivo therapeutic efficacy in murine and rat models of type 2 diabetes, as well as rat models of dox-induced renal fibrosis, global cerebral I/R injury, abdominal aortic aneurysm (AAA) and Aβ25-35 toxicity.
SML0603   Lixivaptan ≥96% (HPLC) Arginine vasopressin (AVP) plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). Lixivaptan is an AVP V2-receptor selective antagonist that increases water excretion and normalizes serum sodium levels. Lixivaptan has been in clinical trials for hyponatremia associated with heart failure.
SML1788 LJI308 ≥98% (HPLC) LJI308 is potent pan-RSK inhibitor that targets RSK N-terminal kinase domain (NTKD) ATP-binding site (IC50/[ATP] = 6 nM/5 μM/RSK1, 4 nM/20 μM/RSK2, 13 nM/10 μM/RSK3), exhibiting similary binding affinity toward RSK1-4, but much reduced inhibitory potency against S6K1 (IC50 = 0.8 μM), MEK4 (IC50 >10 μM), and HIP kinase 1 (IC50 >1 μM). LJI308 effectivelfy reduces cellular Y-box binding protein-1 (YB1) Ser102 (EC50 = 0.2-0.3 μM; MDA-MB-231 and H358 cells), but not ribosomal S6 protein (S6RP) S235/236, phosphorylation level and selectively inhibits the growth of YB1-overpressing HTRY-LT triple-negative breast cancer (TNBC) cells, but not the parental non-tumorigenic human mammary epithelial cell (HMEC) line HTRZ (% inhibition = 6.8%/HTRZ, 88%/HTRY-LT1, 66%/HTRY-LT2 in 8 days; 5 μM at 0 and 96 hr).
SML0991   LLP-3 ≥98% (HPLC) LLP-3 is a cell-permeable Survivin inhibitor. LLP-3 is an inhibitor of Survivin-Ran complex formation that induces apoptosis in tumor slice cultures, including resistant tumors.
SML1972 LLY-283 ≥98% (HPLC) LLY-283 is a potent and selective SAM-competitive PRMT5 inhibitor (IC50 = 20 nM against PRMT5-catalyzed methylation of an H4R3-derived peptide substrate) with greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. LLY-283 inhibits Smith (Sm) antigen SmBB’ methylation in MCF7 cells (IC50 = 25 nM; 3 days) and affects MDM4 splicing in A375 cells (IC50 = 40 nM; 3 days). The diastereomer LLY-284 is less potent in the biochemical assay and is an ideal control compound for cellular studies. For characterization details of LLY-283, please visit the LLY-283 probe summary on the Structural Genomics Consortium (SGC) website.

LLY-284 is the negative control for the active probe, LLY-283. LLY-284 is available from Sigma. To learn more about and purchase LLY-284, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1971 LLY-284 ≥98% (HPLC) LLY-284 is the less potent diastereomer of the potent SAM-competitive PRMT5 inhibitor LLY-283 (IC50 = 20 nM against PRMT5-catalyzed methylation of an H4R3-derived peptide substrate) and an ideal control compound for cellular studies. For characterization details of the active probe, LLY-283, please visit the LLY-283 probe summary on the Structural Genomics Consortium (SGC) website.

LLY-283, the active probe, is available from Sigma. To learn more about and purchase LLY-283, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1279 LLY-507 ≥97% (HPLC) LLY-507 is a potent and selective inhibitor of SMYD2 protein lysine methyltransferase (PKMT) with an in vitro IC50 <15 nM and >100-fold selectivity over other methyltransferases and other non-epigenetic targets. LY-507 has been shown to inhibit p53K370 monomethylation in cells with an IC50 ~600 nM. For full characterization details, please visit the LLY-507 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML0664 LM11A-31 dihydrochloride ≥95% (HPLC) LM11A-31 is a non-peptide ligand of the p75 neurotrophin receptor (p75NTR). LM11A-31 blocks pro-NGF induced cell death in neuronal cultures, and protects neuronal cells from the the cytotoxic effects of cisplatin or methotrexate. Oral administration of LM11A-31 promotes the survival of oligodendrocytes and myelinated axons in a mouse spinal cord injury model and improves function in both weight-bearing and non-weight bearing tests.
SML0848   LM22A-4 ≥98% (HPLC) LM22A-4 is a non-peptide and shares similarity with brain-derived neurotrophic factor (BDNF), especially in the loop2 region. It improves oligodendroglia density and favors myelin repair. LM22A-4 elevates the expression of protein kinase B (PKB or Akt) and extracellular signal-regulated kinases (ERKs). LM22A-4 elicits neuroprotection in spinal cord injury (SCI) by deregulating the cleaved-caspase-3 and favoring B-cell lymphoma 2(Bcl-2) expression.
LM22A-4 is a partial agonist of TrkB, a brain-derived neurotrophic factor (BDNF) receptor. In binding assays, LM22A-4 displaces BDNF with an IC50 of 47 nM. The compound restores TrkB phosphorylation and respiratory function in a mouse model of Rett syndrome.
SML2461 LM22B-10 ≥98% (HPLC) LM22B-10 is a brain penetrant, potent and selective TrkB and TrkC neurotrophin receptors agonist that improves cell survival and potently accelerated neurite outgrowth. LM22B-10 inhibits binding of BDNF to TrkB-expressing cells and NT-3 to TrkC-expressing cells.
SML1053   LMK235 ≥98% (HPLC) LMK-235 induces the differentiation of odontoblasts in dental pulp cells. It plays an important role in the regeneration of dental tissue.
LMK235 is a histone deacetylase (HDAC) inhibitor with greater potency against HDAC4 and HDAC5 (IC50 = 11.9 and 4.2 nM, respectively) than other HDAC family members (IC50 values = HDAC1 320 nM, HDAC2 881 nM, HDAC6 55.7 nM, and HDAC8 1278 nM). LMK235 potentiates the cytotoxic effects of cisplatin, and sensitizes platinum-drug resistant tumor cell lines to cisplatin toxicity.
SML1628 LMT-28 ≥98% (HPLC) LMT-28 is a derivative of oxazolidinone. It has the ability to repress the activation of signal transducer and activator of transcription 3 (STAT3) stimulated by interleukin 6 (IL-6). Orally administered LMT-28 reduced arthritis and acute pancreatitis stimulated by collagen in mice pathologic models.
LMT-28 is an IL-6 antagonist that targets the IL-6 Receptor β subunit, Glycoprotein 130 (gp130). Its binding to gp130) results in inhibition of IL-6 activation, and downregulation of levels of p-STAT3. LMT-28 was shown to stimulate phosphorylation of STAT3 and JAK2 protein. IL-6 dysregulation is involved in inflammation and cancers. LMT-28 had inhbitory activity against IL-6–dependent TF-1 cell proliferation and also had therapeutic effect against pancreatitis.
L5670 Locostatin ≥98% (HPLC) Locostatin is a cell permeable, potent inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction and an inhibitor of cell migration.
SML2307 Lodoxamide ≥98% (HPLC) Lodoxamide Tromethamine is a potent agonist of GPR35 in both human and rat, and an antiallergic mast cell stabilizer used clinically in the UK for treatment of allergic conjunctivitis.
SML1019   Lofexidine hydrochloride ≥98% (HPLC) Lofexidine, a derivative of clonidine, is a very potent agonist of α2 adrenoceptors. Lofexidine is used as a treatment for withdrawl from heroin and other opiates, and as a short-activg anti-hypertensive agent.
SML0586 Lomeguatrib ≥98% (HPLC) Lomeguatrib is a highly potent inactivator of O(6)-methylguanine-DNA methyltransferase (MGMT), a DNA repair protein which can confer resistance to some cancer chemotherapeutics, in particular the DNA alkylating agents such as Temozolomide, DTIC, Carmustine, etc. Lomeguatrib is a highly potent inactivator of MGMT and can be used to further investigate mechanisms of resistance. It is a potent irreversible inactivator of all mammalian O6-alkylguanine-DNA-alkyltransferases, so far tested with nanomolar activity in vitro and in vivo.
L6295 Lomerizine dihydrochloride ≥98% (HPLC), powder Lomerizine dihydrochloride is a voltage-dependent calcium channel blocker and selective cerebral vasodilator. It is one of the most selective calcium channel blockers for the CNS and cerebral arteries. It has been reported to inhibit both T-type and L-type Ca2+ currents in rat hippocampal CA1 pyramidal neurons, to prevent glutamate-induced neurotoxicity in rat hippocampal primary cell cultures, and to exhibit protective effects in animal models of migraine, ischemia and hypoxia. In Japan, lomerizine has been used as the first-line prophylactic drug for migraines.
SML0040 Lometrexol hydrate ≥95% (HPLC) Glycinamide Ribonucleotide Formyltransferase (GARFTase) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexate is a potent inhibitor of GARFTase, but does not interfere with enzymes involved in the synthesis of folate. Lometrexerol has been tested clinically for the treatment of various cancers as an anti-folate like agent, similar to methotrexate. Treatment with lometrexol rapidly decreases ATP and GTP levels, cell cycle arrest and induces apoptosis. Although depletion of nucleotide pools induces p53 expression, lometrexol is cytotoxic in both wild-type and mutant p53 expressing tumor cells. Lometrexol is cytotoxic in CCRF-CEm leukemia cells with an IC50 of 2.9 nM.
SML2648 Lomibuvir ≥98% (HPLC) Lomibuvir (VX-222; VCH-222) is a non-cytotoxic, orally active non-nucleoside inhibitor (NNI) against hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (genotype 1a/1b IC50 = 0.94/1.2 μM). Lomibuvir exhibits HCV genotype-selective antiviral activity in vitro (genotype 1a//1b EC50 = 23.3 nM/12 nM; ineffective against 2a & 2b) and in vivo by targeting HCV NS5B thumb II allosteric pocket, exhibiting no inhibitory potency against human DNA polymerase (α, β, γ IC50 ≥56 μM), respiratory syncytial virus, Influenza A and B, and West Nile virus.
SML1385 Lomitapide ≥98% (HPLC) Lomitapide can lower the secretion of very-low-density lipoproteins (VLDL) and chylomicrons.
Lomitapide is an inhibitor of microsomal triglyceride transfer protein (MTP). Lomitapide has been shown to be highly effective in reducing LDL-cholesterol and triglycerides, and has been aproved for treatment of homozygous familial hypercholesterolemia.
human ... MTTP(4547), P4HB(5034)
SML1457 Lonafarnib ≥98% (HPLC) Lonafarnib is a potent inhibitor of farnesyltransferase, an enzyme responsible for a post-translational modification of proteins (including Ras) that gives a protein sufficient hydrophobicity to translocate to the plasma membrane. Farnesylation regulates signaling cascades controlling cell survival, proliferation and differentiation, so variety of possible uses is not surprising a post-translational modification of proteins (including Ras) that gives a protein sufficient hydrophobicity to translocate to the plasma membrane. Lonafarnib has been studies for possible treatment of progeria, various cancers, and hepatitis D.
Lonafarnib prevents the post-translational lipid modification of H-Ras and other farnesylated proteins. Lonafarnib treatment results in microtubule bundling, increased microtubule acetylation and stabilization and suppression of microtubule dynamics.
human ... FNTA(2339), FNTB(2342)
SML0127 Longdaysin ≥98% (HPLC) Longdaysin inhibits CK1, ERK2, and CDK7 kinases in low mM concentrations. The activity of longdaysin results in a lengthening of circadian periods in cell based and in vivo systems. Transgenic zebrafish harboring a per3-luc reporter gene displayed a 10 hour lengthening of circadian period when treated with longdaysin. Longdaysin reduces the phosphorylation of PER1 the regulator of molecular clock function and manipulates the circadian clock.
LO1280   LOPAC®1280    
LO3300   LOPAC®1280 (International Version)    
LO4200   LOPAC®1280 - Small Scale International Version    
LO4100   LOPAC®1280 - Small Scale    
L4762 Loperamide hydrochloride Loperamide hydrochloride (HCl) is a non-selective Ca2+ channel blocker. At nanomolar concentrations, it binds to μ-opioid receptors. Loperamide HCl does not cross the blood-brain barrier.
human ... OPRM1(4988)
SML1222   Lopinavir ≥98% (HPLC) Lopinavir is an antiviral HIV Protease Inhibitor. Lopinavir has insufficient bioavailability alone, so it is used in therapy in combination with Ritonavir, a HIV protease inhibitor, which inhibits cytochrome P450-3A4 (CYP3A4), a liver enzyme that normally metabolizes protease inhibitors. Lopinavir also has an ability to inhibit ZMPSTE24 (zinc metallopeptidase STE24).
L9664 Loratadine ≥98% (HPLC), powder Loratadine is a non-sedating histamine H1-receptor antagonist. Shown to inhibit the two-pore domain potassium channel K2P18.1 (also called TRESK or KCNK18).
Non-sedating histamine H1-receptor antagonist.
human ... CYP3A4(1576), HRH1(3269), KCNH1(3756), KCNH2(3757), PTAFR(5724)
rat ... Hrh1(24448)
L1764 (±)-Lorazepam Anxiolytic; ligand for the GABAA receptor benzodiazepine modulatory site.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
SML1025   Lorcainide hydrochloride ≥98% (HPLC) Lorcainide is a Class 1c antiarrhythmic agent that blocks open fast acting voltage-gated sodium channels (subtype Nav1.5). Data shows that Lorcainide is a potent, selective antagonists/inverse agonists of human and rat H3 histamine receptors.
JN0002 Loreclezole ≥98% (HPLC) Loreclezole (R72063) is a sedative and anticonvulsant that exerts subtype-selective positive allosteric modulator (PAM) potency toward beta2 (β2)- or β3-containing GABAA gamma-aminobutyric acid (GABA) receptors (% potentiation by 1 μM Loreclezole of GABA EC20-stimulated current/human α1βγ2 = 100/α1β2γ2, 120/α1β3γ2, 13/α1β1γ2; α1β2γ2 EC50 = 1 μM) with >300-fold lower β1 affinity, while acting as a negative allosteric modulator (NAM) against the homomeric rho1 (ρ1) GABAA-rho receptor (rat GABAC IC50 = 0.5 μM against GABA EC10-induced current).
PZ0039 Lorlatinib ≥98% (HPLC) Lorlatinib (PF-06463922) is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against most known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. It is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).
SML0338 Lornoxicam ≥98% (HPLC) Lornoxicam is an oxicam-class NSAID with strong analgesic properties.
SML0547 Loteprednol Etabonate ≥98% (HPLC) Loteprednol Etabonate is a "soft" steroid, typically used in topical applications for inflammatory conditions of the eye. Loteprednol Etabonate is an agonist of both glucocorticoid and mineralcorticoid receptors.
Loteprednol Etabonate is an anti-inflammatory corticosteroid (ophthalmology).
Loteprednol etabonate (LE) is a key site-active corticosteroid. It is produced by structural modifications of prednisolone-related compounds to form an inactive metabolite. Double-masked study states that loteprednol etabonate is used to treat giant papillary conjunctivitis, seasonal allergic conjunctivitis, postoperative inflammation and uveitis. LE has good ocular permeation properties.
human ... NR3C1(2908)
L106 Loxapine succinate salt solid D2/D4 dopamine receptor antagonist; 5-HT2A/2B, 5-H7 serotonin receptor antagonist; dibenzoxazepine antipsychotic agent.
human ... DRD2(1813), DRD3(1814), DRD4(1815), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR7(3363)
SML0130 Loxiglumide ≥97% (HPLC) Loxiglumide is a small-molecule antagonist of the cholecystokinin receptor CCKA. Loxiglumide inhibits pancreatic secretion of digestive enzymes, and also blocks CCK-induced gastric secretions and emptying.
L0664   Loxoprofen solid   human ... PTGS1(5742), PTGS2(5743)
L3169 LP 12 hydrochloride hydrate ≥98% (HPLC), solid LP 12 dihydrochloride is a 5-HT7 receptor agonist displaying selectivity over D2, 5-HT1A and 5-HT2A receptors (Ki values are 0.13, 224, 60.9 and 1464 nM, respectively. It also displays selectivity over D2, 1723; over 5-HT1A, 468; over 5-HT2A, 11261; and high potency. Sigma has added LP 44 (L9793) which shows significantly lower D2 selectivity (7.3 nM/0.22 nM for 33-fold), lower selectivity over 5-HT1A, 240; and over 5-HT2A, 1482. LP 12 and LP 44 seem to share a common intermediate.
SML1730 LP117 ≥98% (HPLC) LP117 is a pirinixic acid derivative that interferes with ATP-binding cassette (ABC) transporter ABCB1-mediated substrates transport, including vincristine, vinorelbine, paclitaxel, and actinomycin D, but not doxorubicin, rhodamine 123, or JC-1. LP117 effectively reduces drug-resistance in ABCB1-expressing neuroblastoma cultures while exhibiting no efficacy toward non-ABCB1 substrate cisplatin or in non-ABCB1-expressing cancer cultures.
SML1561 LP-211 ≥98% (HPLC) LP-211 is a brain penetrant selective agonist for the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor. The 5-HT7 receptor is involved in a variety of central nervous system functions including circadian rhythm, sleep, thermoregulation, nociception, and memory, and appears to be involved in cognitive disorders, anxiety, and depression. LP-211 has been used as a selective 5-HT7 receptor agonist in multiple models including studies as a potential therapeutic agent in models of Rett syndrome and Fragile X Syndrome.
L9793 LP44 ≥98% (HPLC), solid LP44 is a high affinity 5-HT7 receptor agonist. Ki = 0.22 nM. LP44 displays selectivity over 5-HT1A and 5-HT2A receptors (200- and >1000-fold, respectively). LP44 induces relaxation of substance P-stimulated guinea pig ileum (EC50 = 2.56 μM).
SML2902 LP-922056 ≥98% (HPLC) New LP-922056 is an orally active, potent and selective NOTUM pectinacetylesterase inhibitor that activates Wnt signaling. LP-922056 stimulates endocortical bone formation in rodents and in humanized NOTUM mouse line.
SML1557 LP99 ≥98% (HPLC) LP99 is a potent and selective bromodomain BRD9 and BRD7 inhibitor with a higher potency for BRD9 (Kd = 99 nM) than for BRD7 (Kd = 909 nM), and no inhibition for any of the 48 other BRDs tested. LP99 was shown to disrupt BRD7 and BRD9 binding to chromatin in cells. LP99 also inhibited interleukin 6 (IL-6) secretion, suggesting that BRD7/9 plays a role in the regulation of pro-inflammatory cytokine secretion. LP99 is not cell cytotoxic up to 25 μM. For full characterization details, please visit the LP99 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
L3669 LPK-26 ≥98% (HPLC), powder LPK-26 is an analog of ICI-199441 and (-)U50,488H (classic kappa agonists). It has extremely high kappa affinity (0.64 nM) and low mu and delta receptor affnities (1170 and 10,000nM). LPK-26 produces an antinocicpetive effect with much higher potency in vivo than morphine or U50488. LPK-26 does not produce physical dependence in mice, but it does suppress naloxone-induced behavioral effects in mice treated with morphine.
SML0600   LPSF/GQ-02 ≥98% (HPLC) LPSF/GQ-02 is a new thiazolidinedione that shows improved insulin resistance, reduces the area of atherosclerotic lesions, and offers a protective effect for the endothelium in LDL receptor-deficient mice. LPSF/GQ-02 induced an overexpression of eNOS and significantly inhibited the expression of metalloproteinases, both of which can result in anti-inflammatory effects.
SML1857 LRE1 ≥98% (HPLC) LRE1 is a selective allosteric inhibitor of soluble adenylyl cyclase (sAC), a ubiquitously expressed, essential component of cAMP-signaling. In contrast to G-protein-regulated transmembrane adenylyl cyclase, soluble adenylyl cyclase is directly activated by calcium and carbonate, and is dispersed throughout the cell cytoplasm. LRE1 was found to bind to the bicarbonate activator binding site. It inhibited cAMP accumulation in 4-4 cells with an IC50 of 11 μM, similar to that of KH7 and without its cellular toxicity.
SML0721   LSN2463359 ≥98% (HPLC) LSN2463359 is a selactive brain penetrant mGluR5 positive allosteric modulator. LSN2463359 is a potentiator of mGluR5-mediated Ca2+ influx in vitro, giving curve shifts 2 to 3 fold over agonist alone. In vivo, the compound exerts wake-promoting, cognitive and motor effects.
SML2249 LSN3154567 ≥98% (HPLC) LSN3154567 is an orally available, potent and highly selective inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). LSN3154567 exhibits broad spectrum and potent anticancer activities without causing retinopathy in the rat. LSN3154567co-administration with nicotinic acid (NA) produces potent anti-tumor activity in tumor xenograft models without retinal and hematological toxicities.
SML1201   LT175 ≥98% (HPLC) LT175 is a dual PPARα/γ agonist that exhibit partial agonist profile at PPARγ. LT175 modulates lipid and glucose metabolism with reduced adipogenic activity. Also, LT175 significantly reduces plasma glucose, insulin, non-esterified fatty acids, triglycerides and cholesterol. LT175 decreases body weight, adipocyte size and white adipose tissue mass in mice on high fat diet. It appears that LT175 binds to different region of PPARγ than rosiglitazone (and other glitazones).
SML0824   Lubeluzole dihydrochloride ≥98% (HPLC) Lubeluzole is an NMDA antagonist. Lubeluzole blocks glutamate release, as well as sodium and calcium gated ion channels. Lubeluzole displays neuroprotective properties in ischemia models.
SML1173   Lubiprostone ≥98% (HPLC) Lubiprostone helps to enhance intestinal permeability in humans. Hence it may inhibit leaky gut syndrome.
Lubiprostone is a bicyclic fatty acid that activates ClC-2 and CFTR chloride channels. Some reports suggest that lubiprostone opens CFTR or both CFTR and ClC-2 through interactions with the prostaglandin receptor EP4. Lubiprostone is used clinically to treat idiopathic chronic constipation and irritible bowel syndrome.
L0144 Lucifer Yellow CH dipotassium salt powder    
SML1722 LUF5834 ≥98% (HPLC) LUF5834 is a potent A2A and A2B adenosine receptor partial agonist with an EC50 value of 12 nM and 45-fold selectivity over the adenosine A3 receptor.
SML0441 LUF6283 ≥95% (HPLC) LUF6283 is a partial agonist of the hydroxy-carboxylic acid receptor 2 (HCA2; GPR109A). LUF6283 binds HCA2 with a Ki value of 0.55 mM, and an intrinsic efficacy for agonist activity of 76% of the full agonist effect of niacin. The EC50 values for niacin and LUF6283 are 0.41 and 3.1 mM, respectively. LUF6283 effectively lowers plasma lipid levels, but does not induce cutaneous flushing as observed with niacin treatment.
SML1927 LUF7346 ≥98% (HPLC) LUF7346 has the ability to enhance the potassium current (IKr) in a heterologous system. It is found to be highly effective than other human ether-a-go-go-related gene (hERG) activators, such as Rottlerin and NS1643.
LUF7346 is a Kv11.1 (hERG) allosteric modulator that prevents proarrhythmic effects caused by hERG blockers in rat ventricular myocyte cultures. LUF7346 reduces Kv11.1 (ERG) affinity toward known Kv11.1 channel blockers dofetilide (Ki for hERG = 4.8 nM without and 12 nM with 10 μM LUF7346) and astemizole (Ki for for hERG = 1.3 nM without and 5.3 nM with 10 μM LUF7346) and effectively suppresses astemizole-induced arrhythmogenic events in a dose-dependent manner among Long-QT syndrome/LQTS (LQT1, JLNS, LQT2) and control isogenic human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). LUF7346 is shown to slow IKr deactivation and positively shifts IKr inactivation among LQTS and control isogenic hiPSC-CMs without affecting KCNQ1/KCNE1-dependent IKs or L-type calcium current ICaL.
SML1595 Luliconazole ≥98% (HPLC) Luliconazole is an imidazole antifungal. Its mechanism of action involves inhibition of ergosterol biosynthesis by inhibition of sterol 14α-demethylase.
SML2866 Lumateperone tosylate ≥98% (HPLC) Lumateperone tosylate (ITI-007) is an orally active, potent 5-HT2A antagonist, postsynaptic D2 antagonist, and serotonin transporter SERT inhibitor (Ki = 0.5, 32, 62 nM, respectively) with in vivo antipsychotic efficacy and no effect toward receptors associated with cognitive and metabolic side effects of antipsychotic drugs (e.g., H1, 5-HT2C, muscarinic). ITI-007 blocks DOI-induced headtwitch (ID50 = 0.09 mg/kg, po.) and D-AMPH-induced hyperlocomotion in mice (ID50 = 0.95 mg/kg, po.), while also acting as a partial agonist at presynaptic striatal D2 receptors.
L5420 Lumefantrine Lumefantrine is is an antimalarial for the treatment of multi-drug resistant strains of falciparum malaria.
SML2928 Lumiracoxib ≥98% (HPLC) Lumiracoxib (COX189) is an orally active, potent and selective cyclooxygenase-2 inhibitor (Ki = 60 nM/COX-2 vs. 3.2 μM/COX-1) that inhibits COX-2-mediated PGE2 production in human whole blood (IC50 = 130 nM; stimulation = 50 μM A23187), but not COX-1-dependent TxB2 production (IC50 = 67 μM; stimulation = 10 μg/mL LPS). Lumiracoxib shows in vivo anti-inflammatory efficacy against carrageenan-induced paw oedema (ED30 = 0.35 mg/kg p.o.), CFA-induced hyperalgesia (ED30 = 5.1 mg/kg p.o.), as well as adjuvant-induced arthritis (ED50 = 3 mg/kg/day p.o.) in rats in vivo.
SML2069 Lurasidone hydrochloride ≥98% (HPLC) Lurasidone is an atypical antipsychotic, used clinically for treatment of schizophrenia and bi-polar disorder. It has nanomolar activity as an antagonist at dopamine D2, serotonin 5-HT2A, 5-HT7, and α2C-adrenergic receptors and as an agonist at 5-HT1A receptors.
human ... DRD2(1813), HTR2A(3356)
L9283 Luteolin ≥98% (TLC), powder Hydroxylated flavone derivative, a strong antioxidant and radical scavenger. Suggested to play a role in prevention of cancer, possibly via the inhibition of fatty acid synthase activity.
human ... CDC2(983), CDK5(1020), CDK6(1021), CYP1A2(1544), GSK3A(2931)
mouse ... Hexa(15211)
rat ... Il4(287287), Tnf(24835)
L2407 Luzindole ≥90% Luzindole is a melatonin (mel) receptor antagonist. It has higher affinity towards the Mel 1b receptor than the Mel 1a receptor subtype.
human ... MTNR1A(4543), MTNR1B(4544)
SML2400 LW106 >97% (HPLC) LW106 is an indoleamine 2,3-dioxygenase 1 (IDO; IDO1) inhibitor (IC50 = 13 nM) that effectively inhibits kynurenine production upon cellular IDO1 upregulation by IFNγ induction (50 ng/mL, 48 h) in HeLa cultures (IC50 = 1.57 μM) and prevents the antiproliferation activity of IDO1-positive DCs against co-cultured CD8+ T-cells (proliferation suppression = 67% with vehicle vs. 33% with 20 μM LW106). LW106 exhibits antitumor activity only in immunocompetent, but not athymic or IDO1-/-, mice, displaying better in vivo efficacy than Epacadostat (Lewis lung carcinoma/B16-F10 tumor suppression = 68%/65% with LW106 vs. 51%/50% with Epacadostat; 80 mg/kg/day i.p.).
SML1499 LW479 ≥98% (HPLC) LW479 is a potent histone deacetylase inhibitor (HDACI) that down-regulates EGFR expression. Apparently, LW479 blocks the binding of the transcription factor Sp1 and HDAC1 to the EGFR promoter region. LW479 potently induces cell cycle arrest and apoptosis breast cancer cell lines. Also LW479 suppressed breast tumor growth and pulmonary metastasis in nude mice.
L9167 LWH-63 hydrochloride ≥98% (HPLC), solid Non-peptide CRF1 corticotrophin-releasing factor antagonist. Ki = 0.68 nM; blocks ethanol-induced effects as well as CRF effects in mice, suggesting a possible therapeutic target for the treatment of stress-induced alcohol drinking.
SML2360 LX-4 ≥98% (HPLC) LX-4 is a cell penetrant, potent and selective activator of p38 mitogen-activated protein kinase (MAPK) pathway that derepress a subset of endogenous genes repressed by DNA methylation.
S009 LY-165,163 solid Selective 5-HT1A serotonin receptor agonist and 5-HT1D serotonin receptor antagonist.
human ... HTR1A(3350), HTR1D(3352)
L9919 LY2033298 ≥98% (HPLC) LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 potentiates ACh-M4 binding, with no effect at M1/3/5 receptors. LY2033298 can also bind to the M ACh receptor, and mediate either positive or negative allosteric effects depending on the ligand used to probe receptor activity.
SML0870   LY 2087101 ≥98% (HPLC) LY 2087101 is a selective positive allosteric potentiator of α7 and α4β2 nicotinic acetylcholine receptors (nAChRs). LY 2087101 was shown to not enhance the activity of α3β4 subtype nAChRs.
SML1438 LY2090314 ≥98% (HPLC) LY2090314 can decrease the development of human MYCN amplified and non-amplified neuroblastoma (NB) cell lines in vitro. It has the ability to prevent the multiplication, colony formation and cell confluency of neuroblastoma.
LY2090314 is a potent and selective ATP-competitive inhibitor of Glycogen synthase kinase-3 (GSK-3) currently in clinical trials for cancer therapy. LY2090314 has IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
human ... GSK3A(2931), GSK3B(2932)
SML2051 LY2109761 ≥98% (HPLC) LY2109761 is a potent and orally active TGF-β receptor (TGFβR) type I & II dual inhibitor (IC50 = 70 and 322 nM against TGFβRI/ALK5 and TGFβRII autophosphorylation, respectively, with 4 μM ATP), inhibiting Fyn/JNK3/Lck/MKK6/SAPK2α only at much higher concentrations (58-89% inhibition at 20 μM) and exhibiting little or no potency against 37 other kinases (IC50 >20 μM). LY2109761 inhibits 0.25 ng/mL TGFβ-induced NIH/3T3 proliferation in cultures (IC50 = 210 nM; 2-hr pretreatment prior to TGFβ for 24 hrs) and suppresses human MX1 breast carcinoma xenograft tumor growth in mice in vivo (by ∼80% on day 37; 75 mg/kg p.o. bid from day 7 to 20). When administered in combination with gemcitabine (25 mg/kg/day i.p.), LY2109761 (50 mg/kg p.o. bid) is shown to significantly reduce tumor burden and spontaneous abdominal metastases in a murine model of metastatic pancreatic cancer.
SML2949   LY2112688 trifluoroacetate ≥95% (HPLC) New LY2112688 is a beta-melanocyte-stimulating hormone (&beta;-MSH)-derived peptide that acts as a high-affinity, potent and selective melanocortin receptor 4 (MC-4, MC-4R, MC4-R, MC4R) agonist (human/rat MC-4 Ki = 0.55/0.39 nM; human MC-1/3/5 Ki = 16.78/56.79/&gt;500 nM). LY2112688 selectively induces MC-4-mediated cAMP release (MC-4/3 EC50 = 0.25 nM/1.61 nM, MC-4/3 Emax = 94.5%/84.1% of NDP-&alpha;-MSH Emax using HEK293 expressing respective human receptors) and exhibits in vivo efficacy in reducing daily food intake and promoting weight loss among diet-induced obese rats (75 & 299 nmol/kg/day s.c.).
L2545 LY225910 ≥98% (HPLC) Cholecystokinin is expressed in the gastrointestinal tract and the central nervous system. Cholecystokinin receptor type 2 (CCK2) is a GPCR that is highly expressed in brain and spinal cord. CCK2 is implicated in many brain processes, including mood, anxiety, and pain, through its modulation of GABA neurotransmission.

LY225910 is a potent, selective CCK2 antagonist. LY225910 blocks agonism of CCK2 by CCK-8S, the peptide agonist. LY225910 has been measured in multiple systems, including GABA efflux from cortical cultures, depolarization of spinal cord neurons (via potassium conductance), modulation of excitatory postsynaptic potentials (EPSPs) in nucleus accumbens slices, and enhancement of morphine analgesia.
SML2943 LY2409881 hydrochloride ≥98% (HPLC) New LY2409881 is a potent IκΒ kinase β (IKK2, IKKβ, IKKbeta) inhibitor (IC50 = 30 nM) that effectively inhibits 10 ng/mL TNFα-induced IκB phosphorylation in LY10 DLBCL cells (by >95%; 10 μM) and exhibits good selectivity by kinase profiling among more than 300 kinases (>10-fold selectivity). LY2409881 enhances TNFα cytotoxicity in SKOV3 ovarian cancer cultures (~20% survival with 316 nM LY2409881 & 10 ng/mL TNFα in 72 hrs; 100% survival with LY2409881 or TNFα alone) by blocking NF-κB antiapoptotic signal activation without affecting TRADD & FADD proapoptotic pathway induction. When administered in vivo, LY2409881 is shown to suppress LY10 xenograft-derived tumor growth in mice (50-200 mg/kg, twice weekly ip.).
SML2452 LY2444296 ≥98% (HPLC) LY2444296 is a brain-penetrant, orally active, short-acting, high-affinity, potent and selective κ (kappa) opioid receptor (KOR) antagonist (human κ/μ/δ Ki = 0.565/35.8/211 nM against diprenorphine binding; GTP-γ-S binding IC50/agonist/subtype transfectant = 1.57 nM/300 nM U69593/κ, 21.3 nM/1 μM DAMGO/μ 293 nM/30 nM DPDPE/d). LY2444296 reverses κ agonist antinociceptive efficacy in vivo (ED50 = 0.24 mg/kg p.o. against 1 mg/kg U69593 sc. by rat formalin test), decreases immobility time (10 or 30 mg/kg sc.) and prevents enhanced alcohol consumption (5 mg/kg i.p.) among mice subjected to stress by forced swimming.
L1920 LY255283 ≥98% (HPLC), powder LY255283 is a competitive leukotriene B4 receptor antagonist, with an IC50 of about 100 nM. It is somewhat selective for the BLT2 receptor, since IC50 values at the BLT1 receptor are >10 μM. LY255283 reduces airway obstruction in animal models of asthma.
SML0225 LY255582 ≥98% (HPLC) LY255582 inhibits the diet-associated increases in mesolimbic dopamine levels and reduces the consumption of highly-palatable food intake.
LY255582 is a centrally active opioid receptor antagonist (defined as an inverse agonist in 2011 JPET paper) that inhibited weight gain in obese Zucker rats over 30 days. It is more that 5-fold selective for mu opioid receptor compared to kappa opioid receptors and 13-fold selective over delta opioid receptors.
SML2892 LY2584702 tosylate ≥98% (HPLC) New LY2584702 is an orally active, ATP-competitive, potent and selective ribosomal protein S6 kinase (p70 S6 kinase, p70S6K, S6K1) inhibitor (IC50 = 4 nM; selective over 83 other kinases and 45 cell surface markers). LY2584702 inhibits HCT116 cellular S6 phosphorylation (IC50 0.1-0.24 μM) and shows anti-tumor efficacy in U87MG glioblastoma and HCT116 colon carcinoma xenograft models in vivo (2.5 mg/kg bid. po.).
SML2855 LY2603618 ≥98% (HPLC) LY2603618 (LCI-1) is a potent and selective checkpoint kinase 1 (Chk1) inhibitor (IC50 = 7 nM) that produces a cellular phenotype identical to that reported upon Chk1 depletion by RNAi. LY2603618 prevents doxorubicin-induced Chk1 autophosphorylation (IC50 = 52 nM; HeLa), allowing cells to traverse the G2/M checkpoint and proceed into mitosis with unresolved replicated chromosomes. LY2603618 renders mutant p53, but not wild-type, HT-29 colon cancer cells more sensitive to gemcitabine both in vitro and in mice in vivo.
L6670 LY266097 ≥98% (HPLC), powder LY266097 is a selective 5HT-2B antagonist with a pKI of 9.7 for the human cloned 5-HT2B receptor and a 100-fold greater selectivity for 5-HT2B than the human 5-HT2C and 5-HT2A.
SML2567 LY2784544 ≥98% (HPLC) LY2784544 is an orally active, ATP-competitive, potent and JAK2-selective janus tyrosine kinase inhibitor (IC50/[ATP] = 2.52 nM/5 μM/JAK2, 19.8 nM/20 μM/JAK1, 48.0 nM/2 μM/JAK3) with little activity toward 79 other kinases. LY2784544 selectively inhibits signaling/proliferation driven by oncogenic JAK2V617F (IC50 = 20/55 nM) over those mediated by wt JAK2 upon IL-3 induction (IC50 = 1183/1309 nM) in Ba/F3 cultures and displays in vivo efficacious in a JAK2V617F-induced murine MPN model (10-80 mg/kg bid po.). LY2784544 is also reported to display Zn-dependent (optimal [Zn+2] = 100 μM) GPR39 agonist activity, but not 11 other GPRs.
L9908 LY-294,002 hydrochloride solid, ≥98% (HPLC) Specific cell permeable phosphatidylinositol 3-kinase inhibitor.
SML2183 LY2955303 ≥98% (HPLC) LY2955303 is a potent and selective RARγ antagonist (Ki = 1.09 nM/RARγ, >1.70 μM/RARα, >2.98 μM/RARβ) that effectively inhibits RARγ-, but not RARα- or RARβ-, dependent reporter activity upon 15 nM all-trans retinoic acid stimulation in respective HEK293 transfectants (KB = 7.11 nM/RARγ, 1.51 μM/RARβ, 4.44 μM/RARα; 10 nM ATRA for RARβ transfectant). LY2955303 exhibits therapeutic efficacy in a rat model of osteoarthritis-like joint pain (ED50 = 0.72 mg/kg; single p.o. dosage 9 days post OA pain induction by MIA intra-articular injection) with good pharmacokinetic properties, aqueous solubility (>1.0 mg/mL in simulated intestinal fluid), oral availability (F = 26%; 10 mg/kg p.o. over 2 mg/kg i.v.), and no RARα antagonism-associated adverse effects (no testicular degeneration up to 10 mg/kg) seen with BMS-189453 treatment or in RARα-knockout mice.
L6795 LY311727 ≥98% (HPLC), powder LY311727 is an orally active; potent secretory Phospholipase A2 (sPLA2; Group IIa) inhibitor.
L5295 LY 320135 ≥98% (HPLC) LY320135 is a potent CB1 receptor antagonist/inverse agonist (Ki = 141 nM) with greater than 70-fold selectivity over CB2 receptors (Ki > 10 μM). Structurally dissimilar from SR 141716A and AM 251. Shows weak binding to both 5-HT2 (Ki = 6.4 μM) and muscarinic receptors (Ki = 2.1 μM)
SML0693   LY-333531 hydrochloride ≥98% (HPLC) LY333531 is a potent inhibitor of protein kinase Cβ (PKCβ; 4.7 and 5.9 nM IC50 values for PKCβ1 and PKCβ2, respectively). PKCβ isoforms are overexpressed in states of oxidative stress, especially in association with diabetes. In diabetic rats, LY333531 improves blood flow and leukocyte entrapment in the retina, and protects against myocardial hypertrophy and cardiac dysfunction.
SML0010 LY-334370 hydrochloride hydrate ≥98% (HPLC), powder LY-334370 hydrochloride is a selective 5-HT1F receptor agonist.
LY-334370 modulates the transmission in the mouse trigeminal system and inhibits the neuronal responses within rat Sp5C by inhibiting c-Fos activation. It shows efficacy in aborting migraine attacks.
SML0556   LY344864 hydrochloride ≥98% (HPLC) LY344864 hydrochloride is a potent and selective 5-HT1F receptor agonist. It has an EC50 of 3 nM, and displays > 80-fold selectivity over other 5-HT receptors
LY344864 might be useful in the treatment approach for migraine. LY344864 is found to prevent the extravasation of dura protein and reduce c-fos like immunoreactions induced by capsaicin.
L1045   LY-354740 hydrate ≥98% (HPLC) LY-354740 is a highly selective and potent agonist of group II mGlu (metabotropic glutamate) receptors. It displays antianxiety and antiaddictive activity in vivo. It?s orally and systemically active. It is anxiolytic and inhibits symptoms of morphine withdrawal in morphine-dependent mice.
L6293 LY-364947 ≥98% (HPLC) LY-364947 is a selective, ATP-competitive inhibitor of Transforming Growth Factor-β Type I receptor kinase (TGF-β RI, ALK5) with IC50 = 59 nM. It is much less potent at related kinases, with IC50 = 400 nM for TGF-β RII and IC50 = 1400 nM for mixed lineage kinase-7 (MLK-7), a kinase in the MAP kinase signal pathway and closely related to TGF-β RII. LY-364947 inhibits TGF-β-dependent cellular growth (IC50 = 81 nM) in NIH 3T3 mouse fibroblasts.
human ... TGFBR1(7046)
L4420 LY-367385 hydrochloride ≥98% (HPLC) LY-367385 hydrochloride has an ability to inhibit induction of long-term potentiation (LTP).
LY-367385 is a selective metabotropic glutamate 1a receptor (mGlu1a) antagonist.
SML2269 LY404039 ≥98% (HPLC) LY404039 is a potent and selective group II metabotropic glutamate receptors mGluR2/3 agonist (Ki = 15 nM against against [3H]LY341495 for binding rat neurons; Ki = 149 nM and 92 nM, respectively, using membrane from human mGluR2- or mGluR3-expressing cells) with >100-fold selectivity over 16 other receptors/transproters, including iGluRs and EAAT1/2/3. LY404039 inhibits forskolin-stimulated c-AMP production in RGT cells expressing human mGluR2 (EC50 = 23 nM) or mGluR3 (EC50 = 48 nM) with little or no potency toward mGluR1a/5a/4a/6/7a/8a-expressing cells (EC50 >10 μM). LY404039 is orally available (Cmax 1528.5 ng/mL, Tmax 2 h; 10 mg/kg p.o. in rats) and exhibits antipsychotic and anxiolytic efficacy in rats (3-30 mg/kg) in vivo.
SML0506 LY-411575 ≥97% (HPLC) LY-411575 is potent, cell permeable and selective γ-secretase inhibitor that reduces Aβ/42 after acute or chronic treatment, and blocks Notch activation. Studies (Cancer Cell) have shown that treatment with LSN-411575 arrests KrasG12V-driven NSCLCs in association with inhibition of HES1 expression and ERK phosphorylation.
SML1938 LY450139 ≥98% (HPLC) LY450139 (Semagacestat) is a notch-sparing, potent and selective gamma-secretase inhibitor. LY450139 lowers plasma and cerebrospinal fluid Aβ in humans.
SML0665   LY-456236 ≥98% (HPLC) LY-456236 is a selective mGlu1 receptor antagonist with an IC50 value of 143 nM for mGlu1 compared to > 10 μM for mGlu5 receptors.
L1170 LY-487379 hydrochloride ≥98% (HPLC) LY-487379 is a positive allosteric modulator of the metabotropic glutamate receptor mGluR2. EC50 = 1.7 μM. LY-487379 shows no intrinsic agonist or antagonist activity at hmGluR2 and has no activity at human mGluR3. LY-487379 markedly potentiates glutamate-stimulated [35S]GTPγS binding in a concentration-dependent manner at hmGluR2, shifting the glutamate dose-response curve leftward by 3-fold and increasing the maximum levels of [35S]GTPγS stimulation. LY-487379 has anxiolytic effects in fear-potentiated startle. This activity profile is useful in all symptom domains of schizophrenia.
SML2921 LYN-1604 hydrochloride ≥98% (HPLC) New LYN-1604 is a potent ULK1 (UNC-51-like kinase 1; Autophagy-related protein 1 homolog) activator (EC50 = 18.94 nM; 1.96-fold activation at 100 nM) that induces ULK complex (ULK1-mATG13-FIP200-ATG101)-dependent death in the triple-negative breast cancer (TNBC) MDA-MB-231 cultures (IC50 = 1.66 μM) involving both autophagy and apoptosis pathway effectors (e.g. ATF3, RAD21, and caspase-3). Intragastric administration is shown to suppress MDA-MB-231 xenograft tumor growth in mice in vivo (EC50 ~50 mg/kg/day on day 14). Mutagenesis and in silico docking studies identify Lys50, Leu53, and Tyr89 as important ULK1 residues that mediate LYN-1604 target site interaction.
SML2097 Lys05 ≥98% (HPLC) Lys05 (Lys01 trihydrochloride) is a dimeric chloroquine (CQ) that deacidifies the lysosome and causes impairment of lysosomal enzymes, exhibiting more than 10-fold higher autophagy inhibitory potency than hydroxychloroquine (HCQ) and CQ (LC3II/LC3I ratio = 15.4 post 4 hr 10 μM treatment in LN229 glioblastoma cells vs. <6.4 with 100 μM CQ or HCQ). Lys05 also shows higher anticancer activity both in vitro (IC50 3.6-6.0 μM vs. 15.6-23.8 μM with HCQ in 1205Lu, c8161, LN229, HT-29 cultures) and in mice in vivo (EC50 in reducing tumor growth rate ∼10 mg/kg/day i.p.; HT29 xenografts) with toxicity observed only at high doses (≥80 mg/kg) as a result of significant lysozyme reduction.
L8542 D-Lys-D-Leu-D-Val-D-Phe-D-Phe-D-Ala trifluoroacetate salt ≥95% (HPLC) Amyloid β40 and β42 fibrillogenesis inhibitor
L1381   L-α-Lysophosphatidylcholine from bovine brain ≥99%, Type V L-α-Lysophosphatidylcholine possess cytotoxic effects and is present at high level in ischemia and atherosclerotic aortas.
Lysophosphatidylcholine is a major component of oxidized low density lipoproteins, and has been implicated in various inflammatory reactions, including atherosclerosis. It is a degradation product of phosphatidylcholine by phospholipase A and has cytolytic properties. The product is used to demyelinate spinal neurons and study the processes underlying remyelination. It activates protein kinase C, p38 MAP kinase, p42 MAP Kinase, and the jun kinase (JNK) pathway, and stimulates transcription of c-jun. Lysophosphatidylcholine accumulates during cardiac ischemia and may induce arrhythmias by uncoupling gap junction communication, and increase ischemic damage by enhancing Na+ loading in cardiac myocytes. It also activates TREK1, TREK2 and TRAAK K+ channels.
SML2189 L-Moses ≥98% (HPLC) L-Moses is a cell penetrant, potent and selective PCAF bromodomain (Brd) inhibitor.
SML2027 L-2-oxothiazolidine-4-carboxylic acid propargyl amide ≥98% (HPLC) L-2-oxothiazolidine-4-carboxylic acid propargyl amide is a cell penetrant, potent and selective competitive inhibitor of cystathionine-γ-lyase that completely abrogated L-cysteine-induced vasorelaxation in tissue.