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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.
4μ8C is a salicylaldehyde derivative and its inhibitory action targets the K907 lysine residue in RNase (ribonuclease) domain and affects IRE1α (endoplasmic reticulum to nucleus signaling 1) RNase activity. In vitro analysis proved that 4μ8C was able to inhibit the release of insulin at high glucose levels.
 
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.
 
SML2247 1G244 ≥98% (HPLC) 1G244 is a cell penetrant, highly potent and specific inhibitor of dipeptidyl peptidase 8 (DPP8) and DPP9. 1G244 is a slow-tight binding competitive inhibitor of DPP8, but it is a competitive and reversible inhibitor of DPP9.
 
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.
 
SML2083   [Ala13]-Apelin-13 trifluoroacetate salt ≥96% (HPLC) (Ala13)-Apelin-13 corresponds to Apelin-13 with a Phe-to-Ala substitution at the C-terminus (F13A) and functions as an antagonist against apelin-dependent APJ functions both in cultures and in animal studies in vivo.
 
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.).
 
SML2058 5,7-Dihydroxytryptamine hydrobromide ≥94% (HPLC) 5,7-Dihydroxytryptamine is a neurotoxin that selectively kills serotonergic neurons.
 
SML1814 3,6-DMAD hydrochloride ≥98% (HPLC) 3,6-DMAD is also called as N9-(3-(dimethylamino)propyl)-N3,N3,N6,N6-tetramethylacridine-3,6,9-triamine. It prevents the development of multiple myeloma (MM) tumor xenografts.
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.).
 
SML2070 23-Hydroxybetulinic acid ≥98% (HPLC) 23-Hydroxybetulinic acid is a cytotoxic agent from rizoma of Pulsatilla chinensis (Bunge) Regel. Anticancer activity of 23-Hydroxybetulinic acid is associated with depolarizations of the mitochondrial membrane potential and subsequent cell apoptosis. Additionally it induces autophagic cell death in HL-60 cells via the up regulation of Beclin-1.
 
SML2042 27-hydroxycholesterol ≥98% (HPLC) 27-hydroxycholesterol is a peripherally derived oxysterol that that is produced by the enzyme CYP27A1. There has beeen increasing interest in the oxysterols, especially in the brain. Impairment of brain cholesterol metabolism has been associated with several neurodegenerative diseases. 27-hydroxycholesterol crosses the blood brain barrier and have been associated with Alzheimer′s disease. It is an activator of LXRα and LXRβ in vitro with EC50 values of 85 and 71 nM and an inhibitor of cholesterol synthesis. 27-hydroxycholesterol has also been shown to bind to estrogen receptor-α (ERα) and Erβ, acting as an endogenous selective estrogen receptor modulator (SERM). In murine models of breast cancer 27-hydroxycholesterol significantly increased tumor growth and metastasis.
 
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  
SML2338 4-Octyl itaconate ≥98% (HPLC) The endogenous metabolite itaconate has recently emerged as a regulator of macrophage function. 4-Octyl itaconate is a cell-permeable itaconate derivative that decreases cytokine production and is protective against lipopolysaccharide-induced lethality in vivo. Esterases in mouse myoblast cells and macrophages hydrolyze it to itaconate, which alkylates cysteine residues on KEAP1, allowing the transcription factor Nrf2 to increase the expression of anti-oxidant and anti-inflammatory downstream genes.
 
SML2084   [Pyr1]-Apelin-13 trifluoroacetate salt ≥96% (HPLC) (Pyr1)-Apelin-13, the major apelin form in human plasma and heart, corresponds to Apelin-13 with posttranslationally modified pyroglutamyl (pGlu, pE) at the N-terminus instead of glutamine (Gln, Q). (Pyr1)-Apelin-13 exhibits higher APJ agonist potency than Apelin-13 (EC50 = 0.30 vs. 0.37 nM, respectively; acidification induction in human APJ-expresing CHO cell cultures). (Pyr1)-Apelin-13 is reactive toward human, murine, rat, and bovine species, and widely used for studyinhg APJ-mediated cellular and physiological functions both in cultures and in animals in vivo (via intraperitoneal, intravenous, intrathecal injection).
 
SML2234 1S,3R-RSL 3 ≥98% (HPLC) RSL3 is an inducer of ferroptosis. It acts by a different method than erastin to induce ferroptosis by inhibiting glutathione peroxidase 4 (GPX4).
 
SML2232 α-Spinasterol ≥98% (HPLC) α-Spinasterol is a blood-brain barrier-permeable and orally active plant phytosterol with antioxidant, anticonvulsant (0.1-1 mg/kg i.p. in mice), antidepressant (1-2 mg/kg i.p. in mice) and anti-inflammatory (0.001-1 mg/kg, i.p. or 1-10 mg/kg, i.g. in mice) properties, as well as antinociceptive efficacy via dual actions against transient receptor potential vanilloid 1 (TrpV1; IC50/Emax = 1.4 μM/67% against 2 nM RTX for binding mouse spinal cord membranes; IC50/Emax = 40 μM/62% against 20 μM capsaicin-induced mouse spinal cord synaptosomes Ca2+ influx) and cyclooxygenases (IC50 = 16.17 μM/COX1 and 7.76μM/COX2). a-spinasterol can directly affect membrane structure and packing in a manner similar to cholesterol, both a-spinasterol and stitosterol are reported to lower plasma/liver cholesterol levels and increase fecal cholesterol excretion when supplemented in daily diet (1%) in mice in vivo.
α-Spinasterol is a constituent of argan oil. It regulates nuclear receptors expression and modulates mitochondrial function. It mimics natural cholesterol and its functionality. α-Spinastero lelicits cytoprotective and antiulcerogenic functionality. It has therapeutic potential towards diabetic nephropathy.