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SML0949   4μ8C ≥98% (HPLC) 4μ8C is a potent inhibitor of the ER transmembrane protein IRE1, which mediates the unfolded protein response. 4μ8C inhibits regulated IRE1-dependent degradation (RIDD) and unconventional spicing of XBP1 mRNA in response to endopasmic reticulum (ER) stress, but has no affect on the kinase activity of IRE1.
 
E1036 116-9e ≥98% (HPLC), powder 116-9e is a blocker of Hsp40-Hsp70 binding thereby inhibiting the chaperone activity of Hsp70-Hsp40. The Hsp40 family of co–chaperones binds to Hsp70 through a conserved J–domain. It is believed that 116-9e inhibits chaperone functions by preventing Hsp70–Hsp40 complex assembly.

The same compound by a different name, MAL2-11B, has been found to inhibit the activity of a viral J-domain protein, large tumor antigen (TAg). MAL2-11B inhibited both TAg’s endogenous ATPase activity and the TAg-mediated activation of Hsp70.
 
SML0114 2002-G12 ≥98% (HPLC) 2002-G12 binds Aβ peptide and was shown to inhibit Aβ42-induced killing of PC12 cells.
 
SML0144 2002-H20 ≥98% (HPLC) 2002-H20 is an Alheimer′s Aβ peptide binder. It inhibits Aβ-induced death of PC12 cells, reducing the amount of toxic oligomer by enhancing fibril formation.
 
SML0983   5F-203 ≥98% (HPLC) 5F-203 is a cytotoxic molecule that forms DNA adducts that lead to cell death. 5F-203 induces aryl hydrocarbon receptor signaling, and elevates expression of CYP1A1. Treatment of cells with 5F-203 also leads to elevation of reactive oxygen species and activation of p38, JNK and ERK.
 
SML0570 21H7 ≥98% (HPLC) 21H7 is an inhibitor of Wnt/β-catenin signaling that act downstream of the symb-catenin destruction complex to inhibit both Wnt-induced and cancer associated constitutive Wnt signaling via destabilization of β-catenin. The compound chelates iron in vitro and in intact cells. 21H7 decrease the viability of mouse B-lymphoma W10 cells, with LD50 values of 0.4 to 1.0 μM, while is significantly less cytotoxic to normal cells.
 
SML0256 2OHOA ≥98% (HPLC) 2OHOA induces cell cycle arrest and apoptosis in several cancer cell lines, including glioma, leukemia, breast and colon cancer lines. 2OHOA increases sphingomyelin (SM) levels in the membranes of tumor cells, which typically display decreased SM membrane content, and remodeled membranes, compared with normal cells. The compound has no effect on SM levels in non-cancer cells.
 
SML0482 3CAI ≥95% (HPLC) 3CAI is an orally active, potent and specific allosteric inhibitor of Akt1 and Akt2 that directly binds to Ak1 and Akt2 in an ATP noncompetitive manner.
 
SML0287 680C91 ≥98% (HPLC) 680C91 is a potent inhibitor of the enzyme tryptophan 2,3-dioxygenase (TDO), which directs the conversion of trypophan to kynurenin. Kynurenin has recently been identified as an endogenous lignd of the arylhydrocarbon receptor (AHR). TDO is highly expressed in glioma cells, and contributes to AHR-mediated glioma cell survival and suppression of anti-tumor immune responses.
 
SML0806   7DG ≥95% (HPLC) 7-Desacetoxy-6,7-dehydrogedunin (7DG) is a selective inhibitor of protein kinase R (PKR). 7DG appears to directly interact with the C-terminal half of PKR, and unlike C16, does not bind the ATP catalytic pocket. 7-Desacetoxy-6,7-dehydrogedunin completely protected macrophages from anthrax lethal toxin (LT)-induced pyroptotic cell death, a model for inflammasome-mediated caspase-1 activation, with an (IC50) of 5 μM, showing a role for PKR in pyroptosis.
 
SML1856 8-Aminoguanine ≥95% (HPLC) 8-Aminoguanine, a guanine derivative, is an orally available and highly efficacious potassium-sparing diuretic/natriuretic that increased sodium excretion by 17.2-fold and decrease potassium excretion by 71.0%. 8-Aminoguanine increases glucose excretion by 12.1-fold. Also, 8-Aminoguanine suppressed deoxycorticosterone/salt-induced hypertension.
 
SML1723 2-Amino-9H-pyrido[2-3-b]indole ≥98% (HPLC) AαC (2-Amino-9H-pyrido[2-3-b]indole) is a potential human carcinogen, which is generated by the combustion of tobacco, or by pyrolysis of protein. AαC potentially contributes to liver or digestive tract cancers. Inside body AαC is metabolized to intermediates (possibly short-lived nitrenium ion of AαC) that react with DNA.
 
SML1798 10-Cl-BBQ ≥98% (HPLC) 10-Cl-BBQ is an orally bioavailable, non-toxic benzimidazoisoquinoline derivative that acts as an aryl hydrocarbon receptor (AhR) agonist via directly binding to AhR (IC50  = 2.6 nM in a competitive binding assay) and induces its nuclear translocation. 10-Cl-BBQ is shown to increase CD4+  T-cells that co-express CD25, CTLA-4 and ICOS, as well as several other genes associated with regulatory T cell (Treg) function in a graft versus host response model (GVH, C57BI/6 T cells injected into B6D2F1 host mice). 10-Cl-BBQ displays good pharmacokinetic profile in mice (t1/2 = 2 h, Cmax = 21.5 μg/L, 10 mg/kg, i.p.). Also shown to prevent insulitis in a NOD T1D mouse model which is independent of Fox3 +  Tregs (60 mg/kg, p.o, q.o.d.).
 
SML1814 3,6-DMAD hydrochloride ≥98% (HPLC) 3,6-DMAD is an acridine derivative that selectively suppresses ER stress- (300 nM Thapsigargin) induced HT1080 cellular XBP1 mRNA splicing (Eff. conc. 500 nM), but not eIF2a phosphorylation, by directly inhibiting IRE1? RNase (endoribonuclease) activity and disrupting IRE1α oligomerization. 3,6-DMAD is shown to exhibit anti-multiple myeloma efficacy in cultures in vitro (%survival/[3,6-DMAD]/cell line/24 h = 13%/4 M/RPMI 8226 and 8%/1 μM/MM1.R) and completely suppress the expansion of established RPMI 8226 tumor in mice in vivo when administered via intraperitoneal injection (10 mg/kg q.o.d.).
 
SML1873 (2R,6R)-Hydroxynorketamine hydrochloride ≥98% (HPLC) (2R,6R)-Hydroxynorketamine is a ketamine metabolite that has rapid antidepressant activity without ketamine-related side effects. The NMDAR antagonist (R,S)-ketamine must be metabolized to (2S,6S;2R,6R)-hydroxynorketamine (HNK) to have antidepressant effects. The (2R,6R)-HNK enantiomer appears to be the enantiomer most responsible for antidepressant effects in a mouse study and unlike (2S,6S)-HNK, (2R,6R)-HNK caused no significant changes in locomotion or coordination. (2R,6R)-HNK does not seem to have the same addiction potential as ketamine, since mice did not self-administer pharmacologically relevant doses of (2R,6R)-HNK under the same conditions where ketamine was readily self-administered. The (2R,6R)-HNK antidepressant appears to involve activation of AMPA glutamate receptors rather than inhibition of NMDA glutamate receptors.
 
SML1875 (2S,6S)-Hydroxynorketamine hydrochloride ≥98% (HPLC) (2S,6S)-Hydroxynorketamin