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SML0968   Y11 ≥98% (HPLC) Y11 inhibits the activity of focal adhesion kinase (FAK) by binding to the amino-terminal domain of FAK and blocking autophosphorylation of tyrosine residue Y397. Y11 inhibits the viability of SW620 and BT474 cancer cell lines and significantly reduces tumor volume in mouse xenografts.
 
SML0873   Y16 ≥98% (HPLC) Y16 blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM). Y16 specifically inhibits LARG catalyzed activation of RhoA and RhoA signaling pathways. Y16 blocks the growth and migration of MCF7 breast cancer cells.
 
Y0503 Y-27632 dihydrochloride ≥98% (HPLC) Y-27632 is highly potent, cell-permeable, selective ROCK (Rho-associated coiled coil forming protein serine/threonine kinase) inhibitor. Ki = 140 nM for p160ROCK. Y-27632 also inhibits ROCK-II with equal potency. The inhibition is competitive with respect to ATP.
human ... ROCK1(6093), ROCK2(9475)
Y102 YC-1 powder NO (nitric oxide)-independent activator of soluble guanylyl cyclase.
human ... PDE5A(8654)
Y1646 YH439 ≥98% (HPLC) YH439 is an aryl hydrocarbon receptor activator
 
SML1148 YIL-781 hydrochloride ≥98% (HPLC) YIL-781 is a potent antagonist (Ki = 17 nM) of the growth hormone secretagogue receptor (GHS-R1). YIL-781 blocks ghrelin-induced reduction of insulin secretion in rat islets. In vivo, the compound YIL-781 improves glucose tolerance and reduces weight gain.
 
SML1840   YK-3-237 YK-3-237 is an activator of sirtuin-1 (SIRT1). YK-3-237 showed anti-proliferative activity toward triple-negative breast cancer, inducing G2/M cell cycle arrest and apoptosis. In a study on renal fibrosis, YK-3-237 caused enhanced expression of α-SMA and fibronectin, suggesting that long-term use of SIRT1 activators may increase the risk or progression of chronic kidney disease.
 
SML0943   YM-1 YM-1 modulates Hsp70 activity by binding to the nucleotide-binding domain of ADP- but not ATP-bound Hsp70, stabilizing Hsp70 in its ADP-bound conformation. The ADP-bound state has tight affinity for its substrates, promoting their ubiquitination and degradation, and a greatly reduced off rate compared to the ATP-bound state. YM-1 appears to behave in a similar manner to Hip, a Hsp70 co-chaperone that stabilizes Hsp70 in its ADP-bound conformation which favors degradation of misfolded substrates such as those involved in various neurodegenerative diseases.

YM-1 also has anticancer activity, which could be due to enhanced ubiquitination and clearance of Akt, a major survival kinase. In studies with multiple cancer lines, YM-1 was found to selectively target cancer cells over normal cells and to overcome tamoxifen resistance in a tamoxifen-resistant MCF7 cell model. YM-1 had greater efficacy and cytosolic localization than the closely related MKT-077 (M5449).
 
SML0822   YM-08 ≥98% (HPLC) YM-08 is a Heat Shock Protein 70 (Hsp70) inhibitor that is blood-brain barrier permeable. YM-08 is a neutral derivative of the Hsp70 inhibitor MKT-077. MKT-077 reduces tau levels in cellular models, but it doesn′t penetrate the blood brain barrier. Although YM-08 was somewhat less effective than MKT-077 in anti-tau and anticancer assays, it selectively reduced pathogenic tau in brain slices, which MKT-077 did not. Furthermore,YM-08 was not retained in the kidney leading one to speculate that it would not have the nephrotoxicity that was a problem for MKT-077 in clinical trials.
 
SML0220 YM 022 ≥98% (HPLC) YM022 is a very potent, selective antagonist of the gastrin/cholecystokinin (CCK)-B receptor. The Ki value for CCKB is 68 pM vs 63 nM for CCKA. In rats, YM022 inhibits pentagastrin-induced gastric emptying with an ED50 or 7.8 nM/kg.
 
Y1271 YM-202074 sesquifumarate salt hydrate ≥98% (HPLC) YM-202074 is a potent and selective allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist. It bound an allosteric site of rat mGluR1 with a Ki value of 4.8 nM. It also inhibited the mGluR1-mediated inositol phosphates production in rat cerebellar granule cells with an IC50 value of 8.6 nM, while showing selectivity over mGluR(2-7).
 
SML1226 YM-26734 ≥95% (HPLC) YM-26734 is a competitive inhibitor of the secreted (Group II) form of phospholipase A2. The IC50 against rabbit platelet derived sPLA2 is 85 nM. YM-26734 is active against, but less potent for group I (pancreatic) sPLA2 (porcine pancreatic enzyme IC50 = 7 μM), and does not inhibit intracellular PLA2 isoforms.
 
SML0574 YM-298198 hydrochloride ≥98% (HPLC) YM-298198 is an orally active, noncompetitive mGlu1 receptor antagonist. The compound inhibits glutamate-induced inositol phosphate production in NIH3T3 cells (IC50 = 16 nM). YM-298198 displays analgesic and antinociceptive properties in vivo.
 
Y4895 YM-58483 ≥98% (HPLC) YM-58483 is a selective Ca++ release-activated Ca++ (CRAC) [a.k.a. store-operated Ca++ (SOC) channels] that mediate Ca++ influx in T cells and other inflammatory cells. CRAC channel inhibitors have potential clinical applications in autoimmune disease, transplant rejection, allergic airway inflammation and bronchial asthma. YM-58483 is also promoted as a tool for CRAC studies; may be used as a gold standard.
 
Y4877 YM 976 ≥98% (HPLC) Phosphodiesterase type IV (PDE4) inhibitor. Exhibits anti-inflammatory activity without emesis. PDE4 inhibitors are of interest for asthma.
 
SML0815   YMU1 ≥98% (HPLC) YMU1 is a cell-permeable and nontoxic inhibitor of hTMPK (thymidylate kinase) that sensitizes tumor cells to doxorubicin in vitro and in vivo.
 
SML0947   YN1 ≥98% (HPLC) YN1 is a potent inhibitor of PFKFB3 (6-Phosphfructo-2-kinase/fructose-2,6-bisphosphatase: IC50 = 670 nM). PFKFB3 is over expressed in many cancers, and catalyzes the production of fructose-2,6-bisphosphate, which can potentiate PFK1 activity, enhancing glycolysis in tumor cells. YN1 inhibits glycolysis and proliferation in HeLa cells.
 
SML1558   Yoda1 ≥98% (HPLC) Yoda1 is a specific activator of mouse and human cation channel Piezo1, a mechanosensitive channel that mediates Ca2+ influx on mechanical activation and has been linked to a role in blood vessel development. Yoda1 stabilizes the Piezo1 open channel. In red blood cells, this was followed by downstream activation of the KCa3.1 Gardos channel with resultant calcium influx and potassium and water efflux, causing shrinkage of the cells. Yoda1 is the first Piezo1 agonist, giving the first evidence of non-mechanical activation of a Piezo channel.
 
Y3125 Yohimbine hydrochloride ≥98% (TLC), powder α2-adrenoceptor antagonist.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
Y1521 YS-49 monohydrate ≥98% (HPLC) YS-49 protects cells from oxidant injury; anti-inflammatory agent; activator of PI3K/Akt signaling. YS-49, an analog of higenamine, induces heme oxygenase (HO-1) in endothelial cells and protects cells from oxidant injury. The compound was reported to inhibit Ang II-stimulated VSMC proliferation through HO-1 production, which inhibits both the JNK pathway and ROS production. A study (JPET) reported that CKD712 (S-YS-49) confer cardiac protection and anti-inflammatory via activation of the PI3K signal pathway. These effects were antagonized by a PI3K inhibitor, wortmannin.
 
SML1806 YU142670 ≥98% (HPLC) YU142670 is a selective inhibitor against OCRL1/INPP5F (IC50 = 0.71 μM; substrate = PI(4,5)P2) and OCRL2/INPP5B (IC50 = 0.53 and 1.78 μM; substrate = PI3 and INPP5B/PI(4,5)P2, respectively) by targeting OCRL catalytic domain without affecting INPP5A, INPP5E, PTEN, SHP1, shrimp alkaline phosphatase, sphingomyelinase, or SYNJ1. YU142670 causes an increased PI(4,5)P2/PI4P ratio in human skin fibroblasts (by 50%; 50 μM for 1 h) and induces upregulated actin nucleation and ruffle activity at the plasma membrane without obvious cytotoxicity. Consistent with the negative regulatory role of PtdIns(4,5)P2 against the calcium channel mucolipin-1 (MCOLN1) that controls autophagosome-lysosome fusion, ehnahced autophagosome accumulation is observed in human kidney proximal tubule cells (PTCs) upon YU142670 (25 μM for 3 hr) or OCRL shRNA treatment.
 
SML1270   YZ9 ≥98% (HPLC) YZ9 is a potent inhibitor of PFKFB3 (6-phosphfructo-2-kinase/fructose-2,6-bisphosphatase) with an IC50 = 183 nM. PFKFB3 is over expressed in many cancers and catalyzes the production of fructose-2,6-bisphosphate, which can potentiate PFK1 activity, enhancing glycolysis in tumor cells. YZ9 dose dependently inhibits proliferation of HeLa cells.