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SML1861 J104129 fumarate ≥98% (HPLC) J104129 is a muscarinic M3 receptor antagonist greater than 100-fold selectivity for M3 over M2 receptors. Its Ki for M3 receptors = 4.2 nM compared to a Ki of 490 nM for M2 receptors. J-104129 showed potent bronchodilator activity in animal studies.
 
J4580 Jasplakinolide ≥97% (HPLC) Jasplakinolide is an actin-specific reagent that promotes actin polymerization and stabilizes actin filaments. In vitro, Jasplakinolidet potently induces actin polymerization by stimulating actin filament nucleation and competes with phalloidin for actin binding (Kd = 15 nM). In vivo, Jasplakinolide has been found to disrupt actin filaments and induce polymerization of monomeric actin into amorphous masses, the exact mechanism of which has not been determined yet. Jasplakinolide differs from other actin stabilizers in that it is cell permeable. This peptide has fungicidal, insecticidal and antiproliferative activity, and is useful for investigating cell processes mediated by actin polymerization and depolymerization, such as cell adhesion, locomotion, endocytosis, and vesicle sorting and release.
 
J3705 JB1 trifluoroacetate salt ≥98% (HPLC) JB1 is an IGF-I peptide analog; IGF-1 receptor antagonist. IGF-1, once known as somatomedin C, is involved in a multitude of activites including promoting growth and development, particularly neural development, and involved in the growth and proliferation in a variety of human cancers. JB1 is a 12-amino acid cyclic peptide, an IGF-1 analog, used by researchers in a variety of fields to inhibit IGF activity by inhibiting binding of IGF-1 to its receptor.
 
J4145 Jervine ≥98% (HPLC), powder Jervine is a sonic hedgehog (Shh) pathway inhibitor.
human ... EBP(10682)
SML0405 JF5 hydrochloride ≥98% (HPLC) JF5 is an allosteric inhibitor of PAR1. The molecule binds to helix 8 of the receptor, directly interfering with receptor coupling to Gαq, but not Gα12. JF5 also inhibits α2A-adrenergic receptor and mPAR4 activity, but not hPAR4. JF5 blocks granule secretion from platelets activated with the PAR1 agonist SFLLRN (IC50 4 μM), but does not affect platelet activation by convulxin (GPVI agonist), PMA or A23187.
 
J4829 JFD00244 ≥98% (HPLC), solid JFD00244 is a SIRT (sirtuin, human silent information regulator) inhibitor.
 
SML0193 JFD01307SC ≥95% (HPLC) JFD01307SC is a glutamine synthetase inhibitor and anti-tuberculosis agent. It is believed to act as a mimic of L-Glutamate and thus target enzymes involved in glutamine biosynthesis. JFD01307SC showed activity against M. tuberculosis with MIC in the range of 8 to 16 μg/ml.
 
SML0808   JIB-04 ≥98% (HPLC) JIB-04 is a selective inihibitor of Jumonji demethylases without inhibiting other α-ketoglutarate-dependent hydroxylases or histone-modifying enzymes including amine oxidase LSD1 (also known as KDM1A), which demethylates histone lysines. JIB-04 is a pan-inhibitor of Jumonji demethylases with JARID1A (KDM5A) being the most sensitive (IC50=230 nM) followed by JMJD2D (IC50=290 nM) and JMJD3 (KDM6B) and JMJD2C (KDM4C) more resistant (IC50 855 and 1100 nM, respectively). JIB-04 selectively inhibited viability of several human cancer cell lines with little toxicity towards normal cells, and also diminished tumor growth in two separate xenograft mouse models.
 
SML1830 JJKK-048 ≥98% (HPLC) JJKK-048 is a cell penetrant ultrapotent and highly selective inhibitor of monoacylglycerol lipase (MAGL) that exhibits a low cross-reactivity with other endocannabinoid targets. JJKK-048 is an irreversible inhibitor that binds to the active site S122.
 
SML1800 JK-2 ≥90% (NMR) JK-2 is a phosphorothioate-based hydrogen sulfide (H2S) donor that shows greatly accelerated H2S release upon protonation-induced intramolecular cyclization at acidic pH ([H2S]/time/pH = 94 μM/4.5 min/pH 5.0, 84 μM/4.5 min/pH 6.0, 36 μM/90 min/pH 7.4, 21 μM/90 min/pH 8.0 with JK-2; [JK-2] = 100 μM at time 0) and is superior to GYY4137 in H2S generation both in buffer (<5 μM H2S/90 min/pH 5.0-8.0 with GYY4137) and in cells without cytotoxicity up to 400 μM in H9c2 and HeLa cultures. JK-2 protects H9c2 rat myoblasts from anoxia/reoxygenation (A/R; 1 hr 2% O2, then 6 hr reoxygenation with 400 μM H2O2) treatment (100% vs. 60% viability with or without 25 μM JK-2) and is efficacious in reducing infarct size per area-at-risk (INF/AAR) upon myocardial ischemia-reperfusion (MI/R) injury induction in mice in vivo (55% and 56% INF/AAR redcution with 50 μg/kg and 100 μg/kg, respectively, via intracardiac injection).
 
J4205 JK184 ≥98% (HPLC), powder JK184 is a Hedgehog signaling pathway antagonist. JK184 blocks sonic hedgehog induced Gli transcription with an IC50 of 30 nM, and disrupts hedgehog signalling by inhibition of alcohol dehydrogenase 7 and depolymerization of mirotubules.
 
SML0509 JK-P3 ≥98% (HPLC) JK-P3 is a VEGFR-2 inhibitor.
JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50 = 7.8 μM). JK-P3 inhibits FGFR 1/3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endothelial cell proliferation.
 
SML0522 JM6 ≥97% (HPLC) JM6 is a prodrug inhibitor of kynurenine 3-monooxygenase (KMO) that increases kynurenic acid levels and reduces extracellular glutamate in the brain. JM6 prevents spatial memory deficits, anxiety-related behavior, and synaptic loss in mouse model of Alzheimer disease.
 
J3830 JNJ 10191584 maleate salt ≥98% (HPLC) JNJ 10191584 maleate is a highly selective histamine H4 receptor silent antagonist.
 
J4649 JNJ-10198409 ≥98% (HPLC), solid JNJ-10198409 is a potent ATP-competitive inhibitor of Platelet-Derived Growth Factor receptor tyrosine kinase (PDGF-RTK) with both antiangiogenic and a direct tumor cell antiproliferative activity. It is selective for PDGF-β kinase with IC50 values of 4.2 nM for PDGF-β and 45 nM for PDGF-α kinase.
 
J3205 JNJ-1661010 ≥98% (HPLC) JNJ-1661010 is a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with >100-fold preferentially selective for FAAH-1 over FAAH-2. FAAH in an integral membrane enzyme within the amidase-signature family. It catalyzes the hydrolysis of several endogenous biologically active lipids and involves in a variety of physiological and pathological processes, including synaptic regulation, regulation of sleep and feeding, locomotor activity, pain and inflammation.
 
J3580 JNJ 17203212 ≥98% (HPLC) JNJ 17203212 is a reversible, competitive and potent TRPV1 antagonist that does not inhibit related TRP channels such as TRPV2, TRPV4, or TRPA1. Listed in BJP with IC50= 65 nM. TRPV1 channels are activated by heat, capsaicin and the endocannabinoid anandamide. Interest in TRPV1 antagonists in the transmission and modulation of pain.
 
SML0683   JNJ-40418677 ≥98% (HPLC) JNJ-40418677 is a γ-secretase modulator that selectively blocks γ-site cleavage of the APP without affecting processing of Notch. In human neuroblastoma cells and rat primary neuronal cultures, JNJ-40418677 blocked secretion of Aβb42 (IC50 = 20 nM), with no affects on total Ab concentration, Notch signaling or COX activity. In vivo experiments showed that JNJ-40418677 dose dependently inhibited Aβ42 accumulation in the brain while promoting an increase in Aβ38.
 
SML1708 JNJ-47965567 ≥98% (HPLC) JNJ-47965567 is a potent P2X7 antagonist with high affinity for the rat receptor (pKi = 8.7). It is centrally available after systemic injection with a superior brain:plasma distribution compared to other available P2X7 antagonists. JNJ-47965567 was shown to suppress epileptic seizures in a mouse model of epilepsy. It appears to have a disease modifying effect since spontaneous seizure rates did not increase once treatment with JNJ-477965567 was stopped.
 
SML1747   JNJ-55511118 ≥98% (HPLC) JNJ-55511118 is an orally available, brain penetrant, potent and selective negative modulator of AMPA receptors that requires the presence of the accessory protein CACNG8 (TARP-γ8). JNJ-55511118 exhibit potent inhibition of neurotransmission within hippocampus, and a strong anti-convulsant effect.
 
SML1624   JNJ-63533054 ≥98% (HPLC) JNJ-63533054 is a potent and selective agonist of the orphan receptor hGPR139, a GPCR receptor expressed in the brain in circumventricular regions of the habenula and septum. JNJ-63533054 has an EC50 value of 16 nM, crosses the blood-brain barrier, and is orally available.
 
J3770 JNJ7777120 ≥98% (HPLC) JNJ7777120 is a potent, selective non-imidazole H4 histamine receptor antagonist.
 
SML1246 JNK-IN-8 ≥96% (HPLC) JNK-IN-8 is a potent, selective and irreversible inhibitor of JNK1/2/3 that inhibits phosphorylation of c-Jun. JNK-IN-8 forms covalent bonds with a conserved cysteine residue.
 
SML0974 (+/-)-JQ1 ≥98% (HPLC) The human BET family, which includes BRD2, BRD3, BRD4 and BRDT, play a role in regulation of gene transcription. (+/-)-JQ1 ((+/-)SGCBD01) is a selective BET bromodomain (BRD) inhibitor that inhibits Brd4 (Bromodomain-containing 4). Brd4 forms complexes with chromatin via two tandem bromodomains (BD1 and BD2) that bind to acetylated lysine residues in histones and Brd4 association with acetylated chromatin is believed to regulate the recruitment of elongation factor b and additional transcription factors to specific promoter regions. The nuclear protein in testis (NUT) gene is known to form fusions with Brd4 that create a potent oncogene, leading to rare, but highly lethal tumors referred to as NUT midline carcinomas (NMC). JQ1 inhibits recruitment and binding of Brd4 to TNFα and E-selectin promoter elements, and accelerates recovery time in FRAP (fluorescence recovery after photobleaching) assays using GFP-Brd4. Thus JQ1/SGCBD01 is a useful tool to study the role of Brd4 in transcriptional initiation. For full characterization details, please visit the SGCBD01/JQ1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML1525 (-)-JQ1 ≥95% (HPLC) SGC probe negative control. (-)-JQ1 is an inactive enantiomer of JQ1 that serves as a negative control. (-)-JQ1 shows no significant interaction with BRD1-4 or other bromodomains.
 
SML1524 (+)-JQ1 ≥98% (HPLC) (+)-JQ1 is a high affinity, potent and selective inhibitor of BET bromodomain proteins, including BRD2, BRD3, BRD4 and BRDT. (+)-JQ1 (also known as SGCBD01), the active enantiomer of (+/-)-JQ1 (catalog no. SML0974), inhibits Brd4 (bromodomain-containing 4), which forms complexes with chromatin via two tandem bromodomains (BD1 and BD2) that bind to acetylated lysine residues in histones and Brd4 association with acetylated chromatin is believed to regulate the recruitment of elongation factor b and additional transcription factors to specific promoter regions. The nuclear protein in testis (NUT) gene is known to form fusions with Brd4 that create a potent oncogene, leading to rare, but highly lethal tumors referred to as NUT midline carcinomas (NMC). (+)-JQ1 inhibits recruitment and binding of Brd4 to TNFa and E-selectin promoter elements, and accelerates recovery time in FRAP (fluorescence recovery after photobleaching) assays using GFP-Brd4. Thus (+)-JQ1 is a useful tool to study the role of Brd4 in transcriptional initiation. For characterization details of (+)-JQ1, please visit the JQ-1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
J4137 JS-K ≥97% Nitric oxide donor; antiproliferative.
 
J4455 JSH-23 ≥98% (HPLC), solid JSH-23 is an inhibitor of NF-kB nuclear translocation. It inhibits LPS and cytokine-induced nuclear translocation of the p65 subunit of NF-kB as analyzed by EMSA and western blot. The compound displays modest potency (IC50 7.1 uM in RAW 264.7), but has the unique property that it does not affect IkB degradation or recovery. The compound dose dependently inhibits LPS induced expression of cytokines, COX2 and iNOS, and presumably binds to, or interferes with the NLS of p65.
 
SML1672 JT010 ≥98% (HPLC) JT010 is a non-cytotoxic and highly stable (>90% remains after 2 h in 1 mM DTT or 2-mercaptoethanol) chloroacetamido warhead-carrying thiazole derivative that acts as a potent and TRPA1-selective channel activator via covalent modification of TRPA1 active site Cys621. JT0101 stimulates calcium influx in TRPA1-transfected HEK293 cells in a dose-dependent manner (EC50 = 650 pM) with excellent selectivity over TRPV1, TRPV3, TRPV4, TRPM2, TRPM8, and TRPC5 channels (EC50 >1 μM).
 
J3955 JTC-801 ≥98% (HPLC) JTC-801 is a nociceptin/orphanin FQ peptide (NOP) receptor antagonist.
 
J4080   JTE-013 ≥98% (HPLC) JTE-013 is a selective sphingosine 1-phosphate (S1P) receptor antagonist. JTE-013 is highly selective for S1P2 (EDG-5). It inhibits S1P binding to human S1P2 receptors with an IC50 value of 17.6 nM. At concentrations up to 10 mM, JTE-013 displays 4.2% inhibition of S1P3 and does not antagonise S1P1.
 
J4330   JTE-907 ≥98% (HPLC) JTE-907 is a cannabinoid CB2 ligand (inverse agonist). CB2 cannabanoid receptors are expressed in periferal nerves and other non CNS tissues, but are not expressed in the brain. CB2 is believed to have a role in nociceptive pain, but additional functions pertaining to the immune system have yet to be determined. CB2 selective agonists and antagonists provide a necessary tool for functional analyses.
 
SML0549 JTV-519 hemifumarate ≥98% (HPLC) JTV-519 is a potent inhibitor or the ryanodine receptor 2 (RYR2) blocker. RYR2 is a cardiac calcium channel that regulates calcium levels in the sarcoplasmic reticulum. JTV-519 stabilizes RYR2 in the closed state.
 
SML0792   JW480 ≥98% (HPLC) JW480 is a highly potent and selective inhibitor of KIAA1363. JW480 reduce MAGEs and impair the migration, invasion, survival, and in vivo tumor growth of human prostate cancer cell lines.
 
SML0630   JW55 ≥98% (HPLC) JW55 is a potent and selective inhibitor of Wnt/β-catenin signaling, that functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2) leading to stabilization of AXIN2 followed by increased degradation of β-catenin. JW55 specifically inhibits canonical Wnt signaling that results in reduced cell-cycle progression, proliferation, and colony formation in colon carcinoma cell lines.
 
SML0990 JW651 ≥98% (HPLC) JW651 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). JW651 inhibited mouse MAGL with an IC50 ~38 nM compared to 10,380 for ABHD6, a serine hydrolase that acts as an alternative hydrolase of 2-AG and >100,000 for FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA). JW651 was used as the MAGL inhibitor along with JW912, a fluorescent inihibitor of both MAGL and ABHD6.
 
SML0324 JW67 ≥98% (HPLC) JW67 is an efficient and specific inhibitor of the canonical Wnt signaling in vitro and in vivo. It appears that JW67 affects the multiprotein complex consisting of β-catenin/GSK-3b/AXIN/APC/CK1 that controls the degradation of β-catenin. JW67 reduces growth of SW480 CRC cells in vitro by inhibiting cell-cycle progression at the G1/S phase.
 
SML0227 JW74 ≥98% (HPLC) JW74 is an efficient and specific inhibitor of the canonical Wnt signaling in vitro and in vivo. It appears that JW74 affects the multiprotein complex consisting of b-catenin/GSK-3b/AXIN/APC /CK1 that controls the degradation of b-catenin. JW74 reduces growth of SW480 CRC cells in vitro by inhibiting cell-cycle progression at the G1/S phase. JW74 also inhibits tumor formation and growth in the small intestine and colon of ApcMin mice.
 
J4252 JWH-015 ≥98% (HPLC), powder JWH-015 is a selective CB2 cannabinoid receptor agonist.
human ... CNR2(1269)
rat ... Cnr1(25248)
J3455 JZL 184 hydrate ≥97% (HPLC) JZL184 selectively inhibits MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG). Anandamide and 2-AG are the two endogenous endocannabinoids that activate the cannabinoid receptors CB1 and CB2. Anandamide is predominantly metabolized by fatty acid amide hydrolase (FAAH), whereas monoacylglycerol lipase (MAGL) is thought to be the enzyme primarily responsible for the degradation of 2-AG. It is difficult to separate the activities of the two because most currently available inhibitors of MAGL are not selective, and also inhibit FAAH or other enzymes. JZL 184 is the first selective inhibitor of MAGL with nanomolar portency and over 200-fold selectivity for MAGL vs FAAH. When administered to mice, JZL184 increased levels of 2-arachidonoylglycerol in the brain by about 8-fold, with no effect on levels of anandamide.
 
SML0257 JZL195 ≥98% (HPLC) JZL195 is a potent dual inhibitor of Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), enzymes that degrade the endocannabinoids 2-arachidonoylglycerol (2-AG) and anandamide (AEA), the endogenous ligands for the cannabinoid G-protein coupled receptors CB1 and CB2. IC50 values are 2 nM for MAGL and 4 nM for FAAH. JZL195 has been shown to inhibit endocannabinoid hydrolysis and elevate 2-AG and AEA levels in vivo.