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SML1954 X-34 ≥90% (HPLC) Fluorescent, amyloid-specific dye
X-34 (1,4-bis(3-carboxy-4-hydroxyphenylethenyl)-benzene) is one among the small-molecule γ-secretase modulators (GSMs) involved in lowering Aβ42 levels (the 42-residue isoform of the amyloid-β peptide). X-34 has also been used to visualize intracellular immunoreactive deposits with classic amyloid fibrillar ultrastructure in living transgenic Caenorhabditis elegans animals. It is also used as a histochemical stain for determining pathological changes in Alzheimer′s disease (AD).
X-34 is a fluorescent, amyloid-specific dye. It binds at a different site than Pittsburgh Compound B and is a highly fluorescent marker for beta-sheet structures.
X3629 X80 ≥98% (HPLC) X80 is an inhibitor of xeroderma pigmentosum group A protein (XPA protein) required for the removal of all types of DNA lesions repaired by nucleotide excision repair Including both transcription coupled and global genomic nucleotide excision repair.
X4879 Xaliproden hydrochloride ≥97% (HPLC), solid 5-HT1A serotonin receptor agonist; neuroprotectant
human ... HTR1A(3350)
X2754 Xanomeline L-tartrate hydrate ≥98% (HPLC) Xanomeline L-tartate is a M1 muscarinic receptor agonist.
SML1317 XAP044 ≥98% (HPLC) XAP044 is a brain penetrant, potent and selective mGlu7 (metabotropic glutamate receptor subtype 7) antagonist that inhibits lateral amygdala long-term potentiation (LTP) in brain slices from wild type mice. XAP044 binds to a pocket localized in mGlu7’s extracellular Venus flytrap domain (VFTD) close to the binding site of the orthosteric agonist L-glutamate. XAP044 exhibits a wide-spectrum anti-stress, antidepressant- and anxiolytic-like efficacy in rodent behavioral model.
X3004 XAV939 ≥98% (HPLC) XAV939 is a Tankyrase inhibitor (thereby inhibiting Wnt / β-catenin signaling)
XAV939 is a cell-permeable dihydrothiopyranopyrimidinol, which elicits anti-tumor functionality against colon, lung, breast and liver cancer. It binds to catalytic poly-ADP-ribose polymerase (PARP) domain of the tankyrase enzyme resulting in β-catenin destruction. It also inhibits tankyrase in neuroblastoma promoting apoptosis in tumor cells.
SML1223 XBD173 ≥98% (HPLC) XBD173 (emapunil, AC-5216) is a potent and selective translocator protein 18 kDa (TSPO) ligand with a Ki value of 0.297 nM. XBD173 acts at the TSPO translocator protein, formerly called the peripheral benzodiazepine receptor, which is involved in production of neuroactive steroids such as allopregnanolone in the brain. TSPO carries cholesterol from the outer to the inner mitochondrial membrane, which is the rate-limiting step of steroidogenesis. XBD173 enhances GABA-mediated neurotransmission via induction of neurosteroidogenesis and exhibits anti-anxiety and antidepressant-like effects.
X4753 XCT790 ≥98% (HPLC), solid XCT 790 is a 5′adenosine monophosphate-activated protein kinase (AMPK) activator. It also acts as a proton ionophore and an uncoupler of oxidative phosphorylation in mitochondria. XCT790 impairs vascular endothelial growth factor (VEGF) and angiopoietin 2 (Ang-2) expression and exhibits suppression of endometrial tumor via estrogen-related receptor (ERRα) inhibition. XCT790 mediates cell cycle arrest and favors apoptosis in triple-negative breast cancer (TNBC).
XCT790 is a potent and specific inverse agonist of ERRα. XCT790 is selective; showing no significant antagonist activity on related nuclear receptors, such as ERRγ or ERα at concentrations below 10 μM. XCT790 inhibits the constitutive activity of ERRα in both biochemical and cell-based assays. The IC50 value is 300-500 nM in transient transfection assays using GAL4-ERR LBD or full-length ERR with the mSHP promoter.
X2254 XE-991 ≥98% (HPLC) XE-991 is a KCNQ channel blocker; which is more potent than linopiridine (Cat. No. L-134).
SML1324   XEN445 ≥98% (HPLC) XEN445 is a potent and selective inhibitor of endothelial lipase with an IC50 of 237 nM and high selectivity over hepatic and lipoprotein lipases. In experiments with wild-type mice, XEN445 raised plasma HDL-cholesterol levels by 16% after 3 days and by 30% after 9 days dosing.
X2628 Xestospongin C film Xestospongin C is a selective, reversible and membrane-permeable inhibitor of IP3 receptor. Reversibly blocks bradykinin- and carbamylcholine- Ca2+ efflux from the endoplasmic reticulum stores.
SML1159 XIB4035 ≥98% (HPLC) XIB4035 is a reported agonist of the glial cell-line derived neurotrophic factor (GDNF) receptor GFRα1. XIB4035 induces GFRα1/RET phosphorylation in Neuro2A cells.
SML2638 XIE62-1004 ≥98% (HPLC) XIE62-1004 is a synthetic sequestosome-1 (p62, SQSTM1) ZZ domain ligand that induces disulfide bond-linked and PB1 domain-dependent p62 self-aggregation, leading to interaction with LC3 on autophagic membranes and p62/cargoes delivery (2.5-10 μM for 6-24 hrs in p62-expressing HeLa cultures). XIE62-1004 treatment (10 μM, 18 hrs) effectively reduces insoluble aggregates of transiently expressed mutant huntingtin (mHTT) constructs in HeLa (GFP-HDQ103) and PC12 (EGFP-HDQ74) trransfectants, as well as in wild-type, but not autophagy defective Atg5-/- MEFs (GFP-HDQ103).
SML1768 Ximelagatran ≥98% (HPLC) It inhibits both clot-bound and free thrombin. It is quickly absorbed by the small intestine and converted to its active dipeptide drug form, Melagatran. Melagatran associates with the arginine side pocket in thrombin and inactivates it. Ximelagatran has a half-life of 4-5 hours. It is administered orally twice a day.
Ximelagatran is orally active, selective and potent direct thrombin inhibitor. Ximelagatran is a prodrug of thrombin inhibitor melagatran.
SML0915   Xipamide ≥98% (HPLC) Xipamide is a sulfonamide diuretic that blocks sodium reabsorption in the distal tubules of the kidney, resulting in increased urine output. Xiopamide also blocks the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel.
X3628 XK469 ≥98% (HPLC), solid XK469 is a topoisomerase IIβ inhibitor; apoptosis inducer.
human ... TOP2B(7155)
SML2393 XL019 ≥98% (HPLC) XL019 is an ATP-binding site-targeting, orally active JAK2 subtype-selective Janus kinase inhibitor (IC50 in nM = 2.2/JAK2 vs. 134.3/JAK1, 214.2/JAK3, 348.3/TYK2) with much reduced or little activity against 116 other kinases (IC50 in nM = 125.4/PDGFRB, 139.7/FLT3, 225.8/c-KIT, 313.8/p70S6K, 370/MLK1, 375.4/IKKbeta, 483.6/KDR, 546.7/PDGFRA, 554.5/FLT4, 910.5/FLT; IC50 >1 μM toward remaining 106 kinases), CYP (1A2, 2C9, 2D6, 3A4 IC50 ≥20 μM), hERG (IC50 = 16 μM), and P-glycoprotein (IC50 >20 μM). XL019 effectively inhibits cellular STAT1/STAT3 phosphorylation both in HEL92.1.7 cultures (IC50 in nM = 386.4/pStat1 and 695/pStat3) and in HEL92.1.7 xenograft-derived tumor in mice in vivo (oral ED50 in mg/kg = 42/pStat1 and 210/pStat3) with significant HEL92.1.7 tumor suppression efficacy in mice (by 60% and 70% on day 14, respectively, with 200 and 300 mg/kg bid p.o. dosage).
SML1239   XL388 ≥98% (HPLC) XL388 is a potent, selective, orally bioavailable ATP-competitive inhibitor of mammalian target of rapamycin (mTOR) with an IC50 of 9.9 nM for mTOR, 8 nM for mTORC1, 166 nM for mTORC2, and 1000-fold selectivity for mTOR over the closely related PI3K kinases and a panel of 141 protein kinases tested. XL388 blocked mTORC1 phosphorylation of p70S6K (T389) with an IC50 value of 94 nM and blocked mTORC2 phosphorylationof AKT (S473) with an IC50 value of 350 nM. XL388 showed complete tumor growth inhibition in mice bearing MCF-7 xenograft tumors.
SML1401 XL413 hydrochloride ≥98% (HPLC) XL413 is a selective inhibitor of the serine-threonine kinase CDC7 (cell division cycle 7 homolog), a regulator of cell cycle checkpoint control that has been implicated in protecting tumor cells from apoptotic cell death during replication stress. XL413 has an IC50 of 3.4 nM for CDC7, compared to 215 nM, 42 nM and 18 nM for CK2, PIM1 and pMCM2, respectively. XL413 caused significant tumor growth regression in rodent models, causing cell cycle arrest in the late S to G2 phase.
SML1753   XMD17-109 ≥98% (HPLC) XMD17-109 is a cell-permeable, non-cytotoxic ATP site-targeting pyrimido-diazepinone derivative that acts as potent inhibitor against ERK5 (MAPK7, BMK1) kinase activity in cell-free assay (IC50 = 162 nM; [ATP] = 50 μM) and EGF-induced ERK5 autophosphorylation in HeLa cells (IC50  = 90 nM). XMD17-109 displayed excellent target selectivity on a 442-kinase panel. XMD17-109 effectively inhibits inflammatory stimuli-induced IL-6 and IL-8 production from human endothelial cells in vitro and protects mice from LPS-induced mortality and systemic inflammation & coagulopathy in vivo with good pharmacokinetics.
SML2568 XMD8-87 ≥98% (HPLC) XMD8-87 is a potent and selective inhibitor of Ack1 (Activated CDC42 kinase 1, TNK2), a kinase that regulates cellular attachment and migration and whose over-expression correlates with a more invasive phenotype of cancer cells and predisposition of primary tumor cells to metastasis. XMD8-87 had a Kd of 15 nM against ACK1 and was also found to inhibit murine Ba/F3 tumor cells having leukemia-associated TNK2 mutations. It inhibited TNK2 D163E cells with an IC50 value of 38 nM and TNK2 R806Q cells with an IC50 value of 113 nM.
SML1382 XMD8-92 ≥98% (HPLC) XMD8-92 is a potent and selective inhibitor of BMK1/ERK5/MAPK7 and DCAMKL1 (DCLK1), kinases implicated in tumorigenesis. XMD8-92 has a Kd of 80 nM for ERK5 and a Kd of 97 nM for DCAMKL1. The next closest targets are DCAMKL2 (190 nM), TNK1 (890 nM), and PLK4 (600 nM). Through inhibition of BMK1 activity, XMD8-92 blocked tumor cell proliferation in vitro in a wide variety of cancer cell lines and significantly inhibited tumor growth in vivo by 95% in mouse studies. XMD8-92 inhibited AsPC-1 human pancreatic cancer cell proliferation and pancreatic tumor xenograft growth via a DCLK1-dependent mechanism.
SML2233 XMU-MP-1 hydrochloride ≥98% (HPLC) XMU-MP-1 inhibits MST kinase activity (IC50 = 9.8 nM/MST1, 18.2 nM/MST2, 44.8 nM/MST3, 27.3 nM/MST4) in a reversible and ATP-competitive manner (MST1 IC50/[ATP] = 164 nM/10 μM and 4036 nM/300 μM; MST2 IC50/[ATP] = 34 nM/10 μM and 1498 nM/300 μM), exhibiting significant affinity and/or inhibitory potency toward only 17 other kinases among a panel of 468 (401 unique kinases). XMU-MP-1 selectively inhibits H2O2-stimulated MST autophosphorylation and phosphorylation of endogenous MST1/2 substrates (MOB1, LATS, YAP), but not JNK, in human and murine cells (Effective conc. 1 μM), effectively upregulating YAP nuclear localization and protecting HepG2 cells (3 μM) against MST2 overexpression-induced cell death. XMU-MP-1 exhibits in vivo efficacy toward liver and intestinal repair and regeneration in various murine models (1-3 mg/kg/day i.p.) and oral availability in rats (t1/2 = 5.18 h, Tmax = 3 h, AUC = 993 ng•h/mL, F = 39.48%; 10 mg/mL p.o.).
SML1230   XW4.4 ≥98% (HPLC) XW4.4 can generate insulin-producing cells from rat mesenchymal stem cells. XW4.4 induced pancreatic differentiation of rat bone marrow derived mesenchymal stem cells into insulin-producing cells shown to release C-peptide and insulin in response to physiological or high glucose levels, which could lead to a possible treatment for Type 1 diabetes. Its mechanism of action is postulated to be through increasing expression of hepatocyte nuclear factor 3β (HNF3β), a member of the forkhead box transcription factor family that regulates expression of several genes in the pancreas during early embryogenesis.
X1126 Xylazine ≥99% α2-adrenoceptor agonist, sedative, muscle relaxant.
Xylazine when used along with ketamine is considered to be a potent and safe anaesthetic in experimental animal. It is known to elevate the hepatic release of glucose, which aggravates to hyperglycemia.
X1251 Xylazine hydrochloride ≥99.0% (HPLC) α2-Adrenergic receptor agonist, sedative, muscle relaxant.
Xylazine is used as a sedative in goats as it is safe, active and a cheap drug. It is a centrally acting drug, which exhibits muscle relaxant and analgesic properties.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
X6000 Xylometazoline hydrochloride α-adrenoceptor agonist; imidazoline binding site ligand.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)