As we update our core systems, key features of the website including ordering and real-time price and availability, may be unavailable from 8:00 PM CDT Friday, June 21st until 9:00 AM CDT Saturday morning June 22nd.


We apologize for any inconvenience this may cause.


Q | R | S

Product #


Product Name

Biochem/physiol Actions

Gene Symbol (ID)

Add to Cart

SML2160 R-568 hydrochloride ≥95% (HPLC) R-568 is a positive allosteric modulator of the calcium-sensing receptor (CaSR), increasing the sensitivity to activation by extracellular Ca2+. In rats, orally administered R-568 decreases plasma levels of PTH and Ca2+ and, at higher doses, increases plasma levels of calcitonin.
SML1377 R-7050 ≥95% (HPLC) R-7050 is a cell-permeable TNF-α receptor antagonist that blocks TNF-α-induced binding of TNF-αRI with TNFαR-associated death domain protein and receptor interacting protein 1, blocking internalization of the TNFα-TNFαR complex. R-7050 was found to reduce neurovascular injury in a mouse model of hemorrhagic stroke.
SML2073 (R)-9bMS ≥98% (HPLC) (R)-9bMS is a potent and selective inhibitor of ACK1 (TNK2) tyrosine kinase that exhibits potent anticancer activity. (R)-9bMS attenuates AR and AR-V7 expression in prostate cancer cells. (R)-9bMS potently inhibits triple negative breast cancer (TNBC) cells proliferation.
SML1614 Rp-8-Br-cGMPS sodium salt ≥98% (HPLC) Rp-8-bromo-cGMPS is a cell permeable cGMP analog that blocks cGMP-dependent protein kinase (cGK, G-kinase, Protein Kinase G, PKG). Rp-8-bromo-cGMPS is resistant to hydrolysis by phosphodiesterases and binds cGK without activating it, resulting in competitive inhibition.
SML2045 R-IMPP hydrochloride ≥98% (HPLC) R-IMPP is a potent and selective inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) secretion that stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. R-IMPP binds selectively to human ribosomes and causes transcript-dependent inhibition of PCSK9 translation.
SML2092 R115866 ≥98% (HPLC) R115866 (Talarozole) is an orally active all-trans retinoic acid (RA) metabolism blocking agent (RAMBA; IC50 = 4 nM against RA metablism in yeast microsomes expressing human CYP26) with much reduced or little potency against CYP19 (aromatase), CYP17 (17,20-lyase), CYP2C11, CYP3A, and CYP2A1 (IC50 from 1.2 to >10 μM). Plasma and tissue RA upregulation via R115866 oral treatment exhibits in vivo efficacy in several retinoid-responsive rodent models, including vaginal keratinization suppression (ED50 = 1.0 mg/kg/day vs. 5.1 mg/kg/day with RA in rats), pinnal hyperplasia induction (ear epidermis thickness = 35.5 μm with 2.5 mg/kg/day R115866 vs. 16.5 μm in control mice), conversion of caudal para- to ortho-keratosis (90% with 1.25 mg/kg/day R115866 vs. 30.3% in control mice). Comparing to liarozole, R115866 is CYP26-selective and does not inhibit CYP-mediated biosynthesis of adrenal and gonadal steroid hormones.
SML1074 R1530 ≥98% (HPLC) R1530 is a multi-kinase inhibitor with activity against several kinases associated with tumor growth and angiogenesis, including VEGFR, FGFR, PDGFR, Chk2 and Cdk2. In tumor cells, R1530 inhibits tubulin polyerization and mitotic checkpoint function, resulting in polyploidy. The compound R1530 inhibits tumor growth and angiogenesis in animal models.
R0908 R1881 ≥98% (HPLC) Androgen receptors (ARs) are nuclear hormone receptors/transcription factors. R1881, also known as methyltrienolone, is a synthetic androgen. It is the gold standard AR agonist.
SML0108 R18 trifluoroacetate ≥98% (HPLC) R18 is a competitive inhibitor of the 14-3-3 scaffolding proteins. It binds to the general binding groove of 14-3-3. R18 blocks 14-3-3 interaction with most or all of its client proteins.
SML2176 R283 ≥98% (HPLC) R283 (NTU283; Rob283) is a cell-permeable 2-[(2-oxopropyl)thio] imidazolium derivative that acts as an irreversible inhibitor against factor XIIIa (FXIIIa) and transglutaminase 2 (TG2, TGase II) by targeting FXIIIa and TG2 active site cysteine (Cys) for acetonylation in a selective manner with little glutathione (GSH) inhibitory potency (app 2nd order rate const = 23000/M/s, 19000/M/s, 0.12/M/s, respectively). A useful tool for investigating TG2-mediated cellular functions (typical conc. range: 25-500 μM).
SML1254 R547 ≥98% (HPLC) R547 is a potent and selective ATP-competitive inhibitor of Cyclin-Dependent Kinases (CDK) 1, 2 and 4 with Ki of 2 nM for CDK1/cyclin B, 3 nM for CDK2/cyclin E, and 1 nM for CDK4/cyclin D1. R547 is less potent for CDK7 and GSK3α/β, and inactive (Ki > 5,000 nmol/L) against a panel of >120 unrelated kinases. R547 was shown to inhibit retinoblastoma protein in tumor cells and xenografts and showed up to 95% tumor growth inhibition in the HCT116 human colorectal tumor xenograft model in nude mice.
R9032 R-715 TFA salt ≥95% (HPLC) Novel, selective, metabolically stable B1 bradykinin receptor antagonist.
SML1676   R9-caPep trifluoroacetate salt ≥95% (HPLC) R9-caPep is an octadecapeptide composed of N-terminal membrane-permeant nona-D-arginine sequence linked via a -Cys-Cys- spacer to a C-terminal proliferating cell nuclear antigen (PCNA) interdomain loop-derived sequence (L126-Y133) that mediates PCNA interaction with its binding partners via their PIP-box domains. R9-caPep selectively kills human neuroblastoma cells (IC50 = 10 - 32 μM vs. IC50 = 98 μM/PBMCs and >100 μM/neural crest stem cells), especially those with MYCN gene amplification, by interfering with PCNA-dependent replication fork extension and DSB HR repair, resulting in exacerbated replication stress. R9-caPep intratumoral injection (3 times a week) is reported to suppress SK-N-BE(2)c xenograft tumor expansion in mice in vivo.
SML1717 RA-2 ≥98% (HPLC) RA-2 is a selective pan-negative-gating modulator of KCa2/3 channels that potently inhibits both ex vivo and in vivo human KCa3.1 and all three human KCa2 channels subtypes. RA-2 right-shifts the KCa3.1 concentration-response curve for Ca2+-activation.
SML1206 RA-9 ≥98% (HPLC) RA-9 is a cell permeable and potent inhibitor of the ubiquitin-proteasome system (UPS) that targets deubiquitinating enzymes (DUB) without affecting 20S proteasome catalytic-core activity. RA-9 directly inhibits activity of following DUB UCH-L1, UCH-L3, USP2, USP5 and USP8 deubiquitinating enzymes, which results in rapid accumulation of poly-ubiquitinated proteins leading to cell cycle checkpoint arrest and tumor cell apoptosis.
SML0476 Rabeprazole sodium ≥98% (HPLC) Rabeprazole sodium is gastric proton pump inhibitor. It suppresses the production of acid in the stomach by inhibiting the gastric H+/K+ATPase (hydrogen-potassium adenosine triphosphatase) at the secretory surface of the gastric parietal cell. Rabeprazole sodium has been used clinically to treat acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevent gastroinetestinal bleeds associated with NSAID use.
SML0043 Racecadotril ≥98% (HPLC) Inhibition of enkephalinase by Racecadotril prevents the breakdown of enkephalins in the gastrointestinal tract. This reduces secretion of water and electrolytes into the gut without affecting the mobility.
Racecadotril is a neutral endopeptidase inhibitor, an antidiarrheal drug which acts as a peripherally acting enkephalinase inhibitor.
R121 S(−)-Raclopride (+)-tartrate salt >97%, solid Selective D2 dopamine receptor antagonist.
human ... DRD2(1813)
SML0364 RAD51 Inhibitor B02 ≥98% (HPLC) B02 is a specific inhibitor of human RAD51 recombinase, a protein crucial for DNA repair processes including the repair of double strand breaks. Rad51 is often overexpressed in cancer cells where it helps to cause resistance, so RAD51 inhibitors are being sought to aid in cancer treatment.
R2146 Radicicol from Diheterospora chlamydosporia solid Green Alternative Antifungal macrolactone antibiotic that inhibits protein tyrosine kinase. Radicicol induces the differentiation of HL-60 cells into macrophages, blocking cell cycle at G1 and G2. It suppresses NIH 3T3 cell transformation by diverse oncogenes such as src, ras and mos and also suppresses the expression of mitogen-inducible cyclooxygenase-2. As a cell differentiation modulator, radicicol has anti-angiogenic activity in vivo, inhibiting the proliferation of and plasminogen activator production by vascular endothelial cells.
human ... HSP90AA1(3320), SRC(6714)
rat ... Src(83805)
SML0378 Ralfinamide mesylate ≥98% (HPLC) Ralfinamide is a mixed sodium and N-type calcium channel blocker. Inhibiton is voltage-dependent, with higher potency against inactivated channels. Ralfinamide is two fold selective for tetrodotoxin (TTX)-resistant sodium channels compared with TTX-sensitive currents.
R1402   Raloxifene hydrochloride solid Raloxifene is a selective estrogen receptor modulator (SERM); acts as an anti-estrogen in both breast and uterine tissue while being estrogenic in bone. May have efficacy against estrogen-sensitive cancers.
R9156 Raltitrexed ≥98% (HPLC), solid Raltitrexed is a folate-based inhibitor of thymidylate synthase (TS) that is rapidly and extensively metabolized to its more potent polyglutamate derivatives. By inhibiting the formation of precursor pyrimidine nucleotides, raltitrexed prevents the formation of DNA and RNA, which are required for the growth and survival of both normal cells and cancer cells.
R0531 Ramatroban ≥98% (HPLC), solid Ramatroban is used for the treatment of allergic rhinitis as an antagonist of the thromboxane receptor. It is also an antagonist of the DP2 receptor with IC50 values of 100-170 nM. It is more potent at the DP2 receptor than the TP receptor by 4-5 fold. It is therefore a useful tool for the elucidation of PGD2/DP2 function in eosinophils, basophils, and other cells of the TH2 cell-type.
SML2262 Ramelteon Ramelteon is a cell penetrant, potent and selective agonist at MT1/MT2 melatonin receptor that exhibits sleep-promoting properties. It is not binding to GABA receptor complex. Ramelteon is an analog of melatonin recently approved to treat insomnia.
R0404 Ramipril ≥98% (HPLC) Angiotensin converting enzyme (ACE) inhibitor.
human ... ACE(1636)
SML0674   Ramosetron hydrochloride ≥98% (HPLC) Ramosetron hydrochloride is a potent serotonin 5-HT3 receptor antagonist with higher afinity for the 5-HT3 receptor than other currently available antagonists. Ramosetron is used clinically both as an antiemetic to treat nausea and vomiting following chemotherapy or after surgery, and in treatment of irritable bowel syndrome.
Ramosetron is a tetra hydrobenzimidazole derivative, containing an indole ring. It inhibits colon contraction mediated by serotonin, competitively.
SML1315 Ranirestat ≥97% (HPLC) Ranirestat (AS-3201) is an aldose reductase (AR) inhibitor. Aldose reductase is a rate-limiting enzyme in the conversion of D-glucose to fructose via D-sorbitol. Ranirestat has been implicated in diabetic complications (cataract formation, retinopathy, neuropathy, nephropathy). Ranirestat prevents sorbitol accumulation and is thus hoped to be effective in the remedy of diabetic neuropathy.
R101 Ranitidine hydrochloride solid H2 histamine receptor antagonist; anti-ulcer agent.
human ... HRH2(3274)
R6152 Ranolazine dihydrochloride ≥98% (HPLC), powder pFOX (partial fatty acid oxidation) inhibitor, a new class of anti-anginal drugs, which inhibit fatty acid beta-oxidation and activates pyruvate dehydrogenase, thereby diverting the heart′s energy source from lipids to glucose, which requires less oxygen and helps maintain myocardiac function at times of ischemia
R8781   Rapamycin Ready Made Solution, 2.5 mg/mL in DMSO (2.74 mM), from Streptomyces hygroscopicus Rapamycin is a macrocyclic triene antibiotic possessing potent immunosuppressant and anticancer activity. It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). mTOR is a member of the phosphoinositide kinase-related kinase (PIKK) family that enhances cellular proliferation via the phosphoinositol 3-kinase/Akt signaling pathway. Inhibition of this pathway by rapamycin blocks downstream elements that result in cell cycle arrest in G1. The effectors of mTOR action include 4EBP1 and S6K1.
R0395 Rapamycin from Streptomyces hygroscopicus ≥95% (HPLC), powder A macrocyclic triene antibiotic that binds to and inhibits the molecular target of rapamycin (mTOR). It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). Rapamycin is a potent immunosuppressant and has anticancer activity.
human ... FKBP1A(2280)
SML1745 Raptinal ≥95% (HPLC) Raptinal is a cell-permeable bifluorene-dicarbaldehyde compound that acts as a rapid activator of mitochondrial pathway-mediated intrinsic apoptosis.
SML0124 Rasagiline mesylate ≥98% (HPLC) Rasagiline mesylate is an effective therapeutic option in early stages of Parkinson′s disease. It improves the motor fluctuations in levodopa-treated patients and may be a useful adjunct to such patients. It has neuroprotective effects and increases the survival of dopaminergic neurons.
Rasagiline mesylate is an irreversible inhibitor of monoamine oxidase selective for MAO type B over type A by a factor of fourteen. It has anti-apoptotic and neuroprotectant activity and has been used as a treatment for Parkinson′s disease.
SML1216   Ravuconazole ≥97% (NMR) Ravuconazole (BMS-207147) is a potent and broad spectrum triazole antifungal. Ravuconazole is an inhibitor of sterol biosynthesis by inhibition of cytochrome P450 14α-demethylase, an enzyme in the sterol biosynthesis pathway that leads from lanosterol to ergosterol.
BM0011 Razaxaban hydrochloride ≥98% (HPLC) Razaxaban is an orally available, potent and specific coagulation factor Xa inhibitor that reduces thrombus and fibrin formation. Razaxaban exhibits potent antithrombotic efficacy in animal models and in patients with deep vein thrombosis.
R8657 Razoxane >98% (HPLC) Razoxane is clinically active against angiogenesis and metastasis. Razoxane specifically inhibits topoisomerase II without inducing DNA strand breaks (topo II catalytic inhibitor). It is an antimitotic agent with immunosuppressive properties. Razoxane inhibits blood-borne and lymphatic metastases in different experimental models. Studies have shown that razoxane inhibits specifically the vasculogenic mimicry of B16F10 melanoma cells.
SML1295 RBC8 ≥98% (HPLC) RBC8 is a selective inhibitor of the Ras-like GTPases RalA and RalB, downstream mediators of Ras signalling, without direct inihibition of Ras or RhoA activity. RBC8 binds to a site on the GDP-bound form of Ral, its inactive state, inhibiting the binding of Ral to its effectors, such as Ral-binding protein 1 (RALBP1; also known as RLIP760, which are involved in proliferation, survival, and metastasis of several human cancers. RBC8 inhibited growth in human luung cancer cell lines with IC50 values of 2.0 μM in H2122 cells and 1.3 μM in H358 cells, and also inihbited tumor xenograft growth..
SML1865 Rbin-2 ≥98% (HPLC) Rbin-2 (ribozinoindole-2) is a cell penetrant, potent, selective and reversible inhibitor of Midasin that inhibits eukaryotic ribosome biogenesis. Rbin-2 directly targets AAA+ ATPase Midasin.
SML0401 RBx-0597 ≥96% (HPLC) RBx-0597 is a potent, competitive inhibitor of DPP-IV (IC50 = 30 nM), that displays selectivity or 150 and 300 fold over DDP-VIII and DDP-IX, respectively.
R9653 RC-3095 ≥95% (HPLC), lyophilized powder RC-3095 is a potent BB2 (GRP-preferring) bombesin receptor antagonist.
SML0228   Rc-Ome ≥98% (HPLC) Rc-OMe is a GABAA PAM that distinguishes α1β2γ2s from α1β2 receptors. The compound has very weak potentiating effects on α1β2, but potentiates GABA-elicited currents of α(123)β2γ2s receptors, all with low μM EC50s. Rc-OMe acts at a binding site that is distinct from BDZ, pentobarbital and loreclezole modulatory sites.
R5655 Rebamipide hydrate ≥98% (HPLC), powder Rebamipide is an anti-ulcer agent with free-radical scavenging and anti-inflammatory effects. It has been used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. It works by enhancing mucosal defense, scavenging free radicals, and temporarily activating COX-2 genes. Rebamipide significantly reduced ulcerogenesis and maintained mucosal superoxide dismutase (SOD) activity. It has also been used for the treatment of Behçet′s disease. Rebamipide may be involved in a noval mechanism to enhance tear secretion and increase mucin levels covering conjunctiva and cornea.
Rebamipide helps to reduce intestinal injury, stimulated by radiation.
R6527 Reboxetine mesylate hydrate >96% (HPLC), solid Reboxetine mesylate hydrate is a selective noradrenaline uptake inhibitor.
SML0561 REDD1 inducer ≥98% (HPLC) 6-(1,3-Dioxo-6-(piperidin-1-yl)-1H-benzo[de]isoquinolin-2(3H)-yl)hexanoic acid is an inhibitor of influenza A virus virulence factor NS1 through activation of host expression of the mTORC1 inhibitor REDD1 ((regulated in development and DNA damage responses. REDD1 induction inhibits mTORC1 by preventing the inactivation of the TSC1–TSC2 complex by AKT1 and, thus, blocks activation of the mTORC1 pathway.
6-(1,3-Dioxo-6-(piperidin-1-yl)-1H-benzo[de]isoquinolin-2(3H)-yl)hexanoic acid is an inhibitor of influenza A virus virulence factor NS1 by activation of host expression REDD1 expression.
Regulated in DNA damage and development 1 (REDD1) induction promotes autophagy-mediated neutrophil extracellular traps (NETs) release from neutrophils in familial mediterranean fever (FMF) patients during remission. Insulin is also one of the known inducers of REDD1 transcription.
SML0335 Remacemide hydrochloride ≥98% (HPLC) Remacemide HCl is a low affinity NMDA antagonist with anticonvulsant properties. Remacemide also been shown to block voltage-dependent sodium channels.
R1908 Remifentanil hydrochloride ≥97% (HPLC), powder Remifentanil hydrochloride is a mu opioid receptor agonist, anesthetic, and analgesic compound. Remifentanil was developed as an ultra-short-acting mu opioid receptor agonist with improved pharmacodynamic properties.
SML1112 Remodelin hydrobromide ≥98% (HPLC) Remodelin is an inhibitor of acetyl-transferase NAT10, a nucleolar N-acetyltransferase involved in stabilization of microtubules. Remodelin was found to correct cell defects associated with progeria, improving nuclear shape and reducing the DNA damage believed to be associated with mutations in the gene for laminin A. Although the mechanism is still being studied, microtubule stability appears to be involved. Remodelin inhibition of NAT10 activity in laminopathic cells appears to result in reduced microtubule anchorage, normalizing the nuclear shape of laminopathic cells. Remodelin should be a useful tool to study how NAT10 affects nuclear architecture and its relationship to and possible treatments for laminopathies and aging and as well as its over-expression found in a variety of soft tissue sarcomas.
R9028 Repaglinide ≥98% (HPLC), solid Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell. It represents a new class of insulin secretagogues, structurally unrelated to sulphonylureas, which were developed for the treatment of type 2 diabetes.
human ... KCNJ1(3758)
R0158 RepSox ≥98% (HPLC) RepSox Inhibits TGF-beta receptor signaling. Retroviral transduction of Sox2, Oct4, and Klf4 genes results in direct reprogramming of somatic cells into induced pluripotent stem cells (iPSCs).
R0875 Reserpine Inhibits vesicular uptake of catecholamines and serotonin.
Reserpine is an alkaloid present in Rauwolfia species. It is useful in treating systemic hypertension, schizophrenia, psychiatric disorders and Raynaud′s syndrome. Reserpine is known to inhibit adrenaline induced-cutaneous blood vessel constriction. It diminishes the effect of hyperthyroidism on cardiovascular and nervous system.
human ... HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358), HTR3A(3359), HTR3B(9177), HTR3C(170572), HTR3D(200909), HTR3E(285242), HTR4(3360), HTR5A(3361), HTR5B(645694), HTR6(3362), HTR7(3363)
83580 Reserpine crystallized, ≥99.0% (HPLC) Inhibits vesicular uptake of catecholamines and serotonin.
R8756 Resiniferatoxin from Euphorbia poisonii, ~95% Potent VR1 vanilloid receptor agonist that has been used to label the vanilloid receptor in sensory ganglia; activates protein kinase C. Diterpene ester that is related to phorbol, but is not tumorigenic.
rat ... Trpv1(83810)
SML0196 Resiquimod ≥98% (HPLC) Resiquimod (R-848) is a potent synthetic agonist of TLR7/TLR8 that possesses antiviral and antitumoral activities.
Resiquimod belongs to the class of imidazoquinolinamines compounds with immunomodulatory effects. Resiquimod increases the levels of cytokines such as TNF-α, IL-6 and IFN-α.
R2625 Retinoic acid ≥98% (HPLC), powder all−trans−Retinoic acid (ATRA) is a ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR). The bound RAR and RXR act as transcription factors that regulate the growth and differentiation of both normal and malignant cells. Cytochromes P450 (CYPs) catalyze the 4-hydroxylation of ATRA. Retinoic acid primes embryonic stem cells to become neurons.
human ... RARA(5914), RARB(5915), RARG(5916), RXRA(6256), RXRB(6257), RXRG(6258)
mouse ... Rara(19401), Rarb(218772), Rarg(19411), Rxrb(20182)
R4643 9-cis-Retinoic acid ≥98% (HPLC) 9-cis-Retinoic acid (9cRA) is an isomer of all-trans-retinoic acid (ATRA), both of which are lipid molecules synthesized from a common precursor, vitamin A. 9cRA is a potent agonist for retinoid X receptor (RXR) and retinoic acid receptor (RAR). It has neurotrophic functionality, promotes neuronal differentiation and may have therapeutic potential in treating stroke. It also regulates cytokine secretion and lymphocyte proliferation. 9cRA favors the dopamine cells survival and induces neuroprotection in neurodegenerative disorder like parkinson′s disease. It elicits anti-inflammatory function and stimulates mast cells and inhibits interleukin 4 and 5 expression levels. 9cRA is in clinical trial phase II for treating refractory cancer.
Ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR) that act as transcription factors to regulate the growth and differentiation of normal and malignant cells.
human ... RARA(5914), RARB(5915), RARG(5916), RXRA(6256), RXRB(6257), RXRG(6258)
R3255 13-cis-Retinoic acid ≥98% (HPLC) 13-cis-Retinoic acid (RA) has anti-inflammatory and anti-tumor action. The action of RA is mediated through RAR-β and RAR-α receptors. RA attenuates iNOS expression and activity in cytokine-stimulated murine mesangial cells. It induces mitochondrial membrane permeability transition, observed as swelling and as a decrease in membrane potential, and stimulates the release of cytochrome c implicating mechanisms through the apoptosis pathway. These activities are reversed by EGTA and cyclosporin A. RA also increases MMP-1 protein expression partially via increased transcription.
human ... NOS2(4843), RARA(5914), RARB(5915)
H7779 Retinoic acid p-hydroxyanilide ≥95% Vitamin A acid analogue with antiproliferative activity in cultured human breast cancer cells; induces apoptosis in malignant hemopoietic cell lines.
R1906 RETRA ≥98% (HPLC), solid RETRA is a mutant p53-dependent activator of p73, an activator of p53-regulated genes, and a suppressor of mutant p53-bearing tumor cells. Greater than 50% of tumors express mutant p53 which is defective for the tumor-suppressor function and contributes to malignancy by blocking a p53 family member p73. Activation of p73 in human cancer produces a cytotoxic effect. RETRA increases expression level of p73 and releases p73 from the inhibitory complex with mutant 53. It thereby produces tumor-supressor effect, in vitro and in vivo, similar to functional reactivation of p53.
SML1085 Retro-2 ≥98% (HPLC) Retro-2 is a non-toxic inhibitor of the endosome-to-Golgi retrograde transport that selectively protect cells from ricin, cholera toxin, and Shiga-like toxins, without affecting compartment morphology, endogenous retrograde cargos, or other trafficking steps.
R0382 Retrorsine ≥90% (HPLC)    
R5523 REV 5901 Leukotriene D4 receptor antagonist.
human ... DRD4(1815)
rat ... Alox5(25290)
SML0173 Reversan ≥98% (HPLC) Reversan increases the efficacy of vincristine and etoposide and increases the sensitivity of murine models of neuroblastoma to conventional chemotherapy.
Reversan is a selective and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp) inhibitor.
R3904 Reversine ≥98% (HPLC), solid Reversine was first described as a synthetic substituted purine with activity as a dedifferentiation agent; it was shown to induces differentiated lineage-committed cells to become multipotent mesenchymal stem cells (MSCs). Reversine has also been show to have activity as a potent, selective human A3 adenosine receptor antagonist (Ki value of 0.66 μM), as an ATP-competitive Aurora kinase inhibitor, and as a Mps1 kinase inhibitor. Additionally, studies have shown reversine to be an anti-cancer agent, inhibiting growth and inducing cell death in various cancer cell types.
human ... ADORA1(134), ADORA2A(135), ADORA2B(136), ADORA3(140)
rat ... Adora3(25370)
SML0626   RFRP-3 human trifluoroacetate salt ≥98% (HPLC) RFRP-3 (RFamide-related peptide-3) is a homolog of avian gonadotropin-inhibitory hormone. RFRP-3 binds to the GPR147 receptor (also known as neuropeptide FF receptor 1). RFRP-3 blocks release of gonadotropin from the pituitary, and inhibits FSH-, LH- and forskolin-stimulated cAMP accumulation and progesterone production in human granulosa-lutein cells.
R8279 RG108 ≥98% (HPLC), powder RG108 is a DNA methyltransferase (DMNT) inhibitor. It reactivates tumor suppressor gene expression (p16, SFRP1, secreted frizzled related protein-1, and TIMP-3) in tumor cells by DNA demethylation. RG108 also inhibits human tumor cell line (HCT116, NALM-6) proliferation and increased doubling time in culture.
R0783 RG-239 hydrate Semisynthetic derivative of betulinic acid (3β-allylbetulinic acid), RG-239 is an agonist at the G-protein coupled receptor TGR5. TGR5 signalling induces glucagon-like peptide-1 (GLP-1) release in brown adipose tissue, enhancing glucose tolerance and attenuating diet-induced obesity.
SML1652 RGFP966 ≥98% (HPLC) RGFP966 changes signal-specific primary auditory cortical plasticity. It is highly effective in cardiomyopathy-associated pathologies.
RGFP966 is a selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 value of 80 nM and no inhibition of any other HDACs at concentrations up to 15 μM. In mouse studies, RGFP966 facilitated extinction of cocaine-seeking behavior and enhanced long-term object memory acquisition and consolidation. In a rat study, RGFP966 ameliorated amyloid-β oligomer-induced synaptic plasticity impairment. RGFP966 was also found to reduce proliferation and inducd differentiation in mouse lymphoid and myeloid malignancies.
R2028 RHC 80267 ≥98% (HPLC), solid RHC 80267 is a diacylglycerol (DAG) lipase inhibitor and an important second messenger in signal transduction pathways. RHC 80267 is generated by the hydrolysis of phosphatidylinositol (PI) and bPC by phospholipase C (PLC). DAG mediates the actions of a large number of hormones and cytokines by activating protein kinase C (PKC). A sustained elevation in intracellular DAG may cause neoplastic transformation.
R7269 Rhein Constituent that is enriched in rhubarb with anti-inflammatory, anti-osteoarthritic, and anti-cancer activity. It reduces IL-1β production and secretion, caspase-3 activity, inducible nitric oxide synthase activity, and phosphorylation of c-Jun and c-Jun NH2-terminal kinase (JNK).
R1533   Rhodblock 3 ≥98% (HPLC), powder Rhodblock 3 is an inhibitor of Rho Kinase pathway. Rhodblock 3 acts upstream of Rok in Drosophila, resulting in the downregulation of Rok and inhibition of myosin phosphorylation. Rhodblock 3 inhibits phospho-MRLC localization as well as furrow localization of the septin Peanut and increased Peanut’s localization on microtubules but did not affect other proteins tested, such as Anillin.
R1283 Rhodblock 6 ≥98% (HPLC) Rhodblock 6 is an inhibitor of the Rho Kinase pathway. Rhodblock 6 directly inhibited Rok and its human ortholog ROCK I in a kinase assay.
R1783 Rhodblock 1a ≥98% (HPLC) Rhodblock 1a is an inhibitor of the Rho Kinase pathway.
SML1274 RI-1 ≥98% (HPLC) RI-1 is a cell-permeable RAD51 inhibitor that binds covalently to the protein surface at Cysteine 319. RI-1 disrupts homologous recombination in human cells.
SML1851 RI(dl)-2 ≥98% (HPLC) RI(dl)-2 is a cell-permeable pyrroloquinoxaline derivative that selectively inhibits Rad51-mediated D-loop formation (IC50 = 11.1 μM) without affecting its ssDNA-binding activity (IC50 >100 μM). RI(dl)-2 is shown to inhibit DSBs-induced cellular homologous recombination (HR) activity (IC50 = 3.0 μM by HEK293-based DR-GFP reporter assay) by stabilizing nucleoprotein filaments in a nonfunctional state without affecting DNA damage-induced RAD51 nuclear loci formation or stimulating single-strand annealing (SSA) activity.
SML1685 Ribocil-C ≥98% (HPLC) Ribocil-C is a potent inhibitor of bacterial riboflavin riboswitches. Riboswitches are cis regulatory elements present in non-coding RNA that specifically bind to natural ligands to regulate gene expression. Ribocil-C blocks the flavin mononucleotide riboswitch-mediated expression of the ribB gene, which is required for riboflavin biosynthesis, with an IC50 value of 23 nM. Ribocil-C inhibited bacterial cell growth of E. coli MB5746 and bacterial burden in a mouse E. coli septicaemia model of infection.
R5030 Ridaifen-B ≥98% (HPLC), white solid Ridaifen-B (RID-B) is a novel tamoxifen (TAM) analog that significantly augments apoptosis-inducing effect of TAM in estrogen receptor (ER)-negatives cells. Ridaifen-B induces mitochondria-involved apoptosis in Jurkat cells, as evidenced by chromatin-condensed cells as well as downstream activation of caspases (caspase-3, -8 and -9) in a dose- and time-dependent manner. At 4 hours of incubation, IC50 for RID-B is 4 muM (30 muM for TAM). And at prolonged treatment of 48 hours, IC50 for RID-B is 0.1 muM. In a related report on the global anti-tumor activity, RID-B strongly inhibits 39 human cancer cells (JFCR 39), both ER-+ or ER-- at concentrations of equal or less than 1muM (e.g., at 0.38muM for SF-539 [central nervous system], at 0.58muM for HT-29 [colon], at 0.20muM for DMS114 [lung], at 0.21muM for LOX-IMVI [melanoma], and at 0.23muM for MKN74 [stomach]. The binding protein of RID-B that exerts the apoptosis events is currently under investigation.
R3530   Rifabutin >98% (HPLC), powder Rifabutin is an antibiotic; antitumor. Rifabutin interferes with HSP-90 molecular chaperone, enhances ubiquitination and protein degradation, and inactivates bacterial RNA polymerase.
R134 Rilmenidine hemifumarate salt solid Selective I1 imidazoline receptor agonist.
human ... NISCH(11188)
R116 Riluzole solid Glutamate release inhibitor; anticonvulsant
rat ... Scnn1g(24768)
SML0800   Rimonabant hydrochloride ≥98% (HPLC) Rimonabant hydrochloride (SR-141716A) is a potent and selective CB1 cannabinoid inverse agonist/antagonist with a Ki of 1.6 nM, minimal affinity for CB2, and and some GPR55 agonist activity. Rimonabant was developed as an anti-obesity drug because of its appetite suppressant activity, but was taken off the market because of side effects of depression and anxiety.
SML1600   Rinvanil ≥98% (HPLC) Rinvanil is a Capsaicin analogue that potently activates transient receptor potential vanilloid 1 (TRPV1) channels. Rinvanil induces neuroprotective mild hypothermia in ischemic brain injured mice through TRPV1 activation. Rinvanil exhibits potent anticancer activity in cancer cell lines including cervical (HeLa, CaSKi, ViBo) and leukemia (P388, J774, WEHI-3) cell lines. Rinvanil is not cytotoxic to normal lymphocytes.
TRPV1 (transient receptor potential vanilloid 1) is a capsaicin receptor. It is strongly expressed in sensory neurons and participates in pain perception. In brain, it regulates neuronal function, motor behaviour and neuroinflammation. Capsaicin plays an important role in the activation of TRPV1.
SML2100   RIPA-56 ≥98% (HPLC) RIPA-56 is a metabolically stable type III kinase inhibitor that targets receptor-interacting protein 1 kinase (RIP1; RIPK1) in a highly potent and selective manner (RIP1 IC50 = 13 nM) by locking RIP1 in its inactive form, exhibiting no inhibitory potency toward RIP3, IDO or a panel of multiple kinases (tested at 10, 200, and 5 μM, respectively). RIPA-56 protects against TNFα-induced necroptosis (necrosis) upon apoptosis/NF-κB pathway blockage (EC50 = 27 nM/murine L929 and 28 nM/human HT-29 cells) in cultures as well as TNFα-induced mortality and multiorgan damage in a murine model of systemic inflammatory response syndrome (SIRS) in vivo (100% survival rate with 3 mg/kg/12 h or single 6 mg/kg i.p.) with good pharmacokinetics and bioavailability (F post 10 mg/kg p.o. or i.p. dosing = 22% and 100%, respectively, of 2 mg/kg i.v.). Long-term daily RIPA-56 supplementation (150 or 300 mg/kg in chow) is reported to prevent aging-associated deterioration of the male reproductive system in mice.
SML0650   Risedronate sodium ≥97% (HPLC) Risedronate sodium is a bisphosphonate bone resorption inhibitor. It has an affinity for hydroxyapatite crystals in bone and acts as an antiresorptive agent and is an inhibitor of farnesyl diphosphate (FPP) synthase, which results in downstream inhibition of osteoclast activity and reduced bone resorption and turnover. Risedronate sodium has been used to treat postmenopausal osteoporosis and Paget′s disease.
R3030 Risperidone ≥98% (HPLC), powder Risperidone is an antipsychotic; serotonin-dopamine antagonist.
R7752 Ristomycin monosulfate ≥90% ristocetin A basis (balance primarily Ristocetin B) Ristocetin activates platelets. Ristocetin-induced platelet agglutination (RIPA) is decreased in patients undergoing chronic hemodialysis. Together with increased plasma glycocalicin levels (a product of enzymatic cleavage of GPIb), RIPA may contribute to diminished platelet adhesion to vascular subendothelium and increased bleeding associated with uremia. Addition of ristocetin and vWf caused specific agglutination of rGPIbα-liposomes suporting the potential use of rGPIbα-liposomes to enhance platelet function in vivo and support hemostasis in thrombocytopenic individuals.
R103 Ritanserin powder Potent 5-HT2A serotonin receptor antagonist/inverse agonist that crosses the blood-brain barrier.
Ritanserin is a potent serotonin 2A receptor (5-HT2A) serotonin receptor antagonist/inverse agonist, which crosses the blood-brain barrier. It modulates 5-HT2A receptors and has been suggested to have antiparkinsonian effect. Ritanserin also impacts schizophrenia by modulating mood, cognition and negative symptoms.
human ... HTR2A(3356)
rat ... Adra1a(29412), Drd2(24318), Htr1a(24473), Htr2a(29595), Htr7(65032)
R0758 Ritodrine hydrochloride β2-adrenoceptor agonist; relaxes uterine muscle contraction.
human ... ADRB2(154)
SML0491 Ritonavir ≥98% (HPLC) Ritonavir is an HIV protease inhibitor now used frequently as a booster of other protease inhbitors. Ritonavir inhibits cytochrome P450-3A4 (CYP3A4), a liver enzyme that normally metabolizes protease inhibitors. It has also been investigated as a possible anti-cancer agent.
SML0881   Rivastigmine tartrate ≥98% (HPLC) Rivastigmine is an orally available, brain penetrant, reversible cholinesterase inhibitor that enhances cognitive function in patients with Alzheimer′s and Parkinson′s diseases. Rivastigmine inhibits both butyrylcholinesterase and acetylcholinesterase.
Rivastigmine tartrate is used to treat Alzheimer′s disease. It helps to improve thinking ability. It helps to increase cholinergic function by inhibiting acetylcholinesterase.
SML0247 Rizatriptan benzoate salt ≥98% (HPLC) Rizatriptan is a serotonin 5HT-1B/1D-receptor agonist used to treat migraine.
R2033 RK-682 ≥98% (HPLC) RK-682 is a specific and noncompetitive inhibitor of protein tyrosine phosphatase; It inhibited dephosphorylation activity of CD45 and VHR with IC50 54 and 2.0 microM and 4.5 microM against PTP1B.
Specific and noncompetitive inhibitor of protein tyrosine phosphatase.
SML2187 RL5a ≥98% (HPLC) RL5a is a potent inhibitor of the replication licensing system in human cells. RL5a blocks the binding of the origin recognition complex (ORC) to origin DNA, which is required interaction for licensing. RL5a appears to act as noncompetitive inhibitor of ORC with respect to ATP.
SML1738 RL648_81 ≥98% (HPLC) Ethyl (2-amino-3-fluoro-4-((4-(trifluoromethyl)benzyl)amino)phenyl)carbamate (RL648_81) is 15 times more effective and more selective than retigabine, an anticonvulsant. RL648_81 helps to treat or inhibit neurologic disorders linked with neuronal hyperexcitability.
RL648_81 is a selective and potent KCNQ2/3 channel activator.
R9407   RM-65 ≥98% (HPLC) RM-65 is an arginine methyltransferase inhibitor and is cell (HepG2) permeable.
R0658 RN-1734 ≥98% (HPLC) RN-1734 is a selective TRPV4 antagonist.
R1033 RN-1747 ≥98% (HPLC) TRPV4, a close relative of the vanilloid receptor TRPV1, is activated by diverse modalities such as endogenous lipid ligands, hypotonicity, protein kinases and, possibly, mechanical inputs. TRPV4 is a nociceptor playing an important role in inflammatory and neuropathic mechanical hyperalgesia in rodent models apparently specifically activated under pathological conditions.
SML1547 RN-9893 ≥98% (HPLC) RN-9893 is a potent and selective antagonist of the Transient Receptor Potential ion channel TRPV4. RN-9893 has IC50 values of 420 nM, 660 nM, and 320 nM for human, rat and mouse TRPV4 receptors, respectively. RN-9893 shows excellent selectivity over related TRP receptors with no inhibition of TRPV1 at a concentration of 10 μM, an IC50 >30 μM against TRPV3, an IC50 of approximately 30 μM against TRPM8, and also good selectivity using 54 binding assays against common biological targets.
R108 Ro 41-0960 solid Specific, reversible, orally-active COMT-inhibitor.
human ... COMT(1312)
SML0639   Ro 11-1464 ≥98% (HPLC) Ro 11-1464 induces the hepatic expression of apoA-1 and leads to increased levels of apoA-1 in the plasma. Treatment of human apoA-1 transgenic mice with Ro 11-1464 resulted in a three-fold increase in hapoA-1 mRNA in the liver, and a two-fold increase in plama apoA-1levels. The compound causes a significant decrease in plama lipids and enhances reverse cholesterol transport.
R7150 Ro 25-6981 hydrochloride hydrate ≥98% (HPLC), powder Potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit.
human ... GRIN2B(2904)
R136 Ro 31-8220 methanesulfonate salt solid Inhibitor of GRK-5 (G protein-coupled receptor kinase); PKC (protein kinase C); MAPKAP kinase 1β and p70 S6 kinase.
R137 Ro 31-0432 solid Protein kinase C (PKC) inhibitor; membrane-derived PKC inhibitor.
R3905 Ro 27-3225 trifluoroacetate salt ≥98% (reversed phase HPLC) Ro 27-3225 is a selective melanocortin MC4 receptor agonist. EC50 = 1 nM. Ro 27-3225 shows some activity at the MC1 receptor. Ro 27-3225 reverses hemorrhagic shock, reduces multiple organ damage, and improves survival. Ro 27-3225 may have a protective role against multiple organ failure following circulatory shock. Ro 27-3225 also reduces food intake in ob/ob mice.
SML2038 RO3280 ≥98% (HPLC) RO3280 is a potent and selective Polo-like kinase 1 (PLK1) inhibitor. RO3280 induces mitotic catastrophe and apoptosis in human bladder cancer cells and leukemia cells.
SML0569 RO-3306 ≥98% (HPLC) CDK1 (cyclin dependent kinase 1) is considered to be the “master switch” in cell division, which maintains the mitotic state of cells.
RO-3306 is a selective ATP-competitive inhibitor of CDK1. It inhibites CDK1 cyclin B1 activity with Ki of 35 nM, nearly 10-fold selectivity relative to CDK2/cyclin E and over 50-fold relative to CDK4/cyclin D. RO-3306 has been used to cause cell cycle arrest at the G2/M boundary.
R8782 Ro4368554 ≥98% (HPLC) Ro4368554 is a 5-HT6 receptor antagonist. RO4368554 acts selectively at 5-HT6 receptors where it binds with a greater than 100-fold selectivity over other monoamine receptor subtypes (-log M pKi = 9.4 at 5-HT6 and 7.1 at 5-HT2A).
R109 Ro 15-4513 solid Benzodiazepine receptor partial inverse agonist; anxiogenic; ethanol antagonist.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA5(2558), GABRA6(2559)
rat ... Gabrg1(140674)
SML1190 Ro 67-4853 ≥98% (HPLC) Ro67-4853 is a positive allosteric modulator of metabotropic glutamate 1 (mGlu1) receptors. Ro67-4853 is active in both human and rat.
SML0573   Ro 41-5253 ≥98% (HPLC) Ro 41-5253 ( GR110) is a potent (IC50 = 16 nM) and selective retinoic acid receptor-α (RARα) antagonist, with some recently discovered activity as a PPARγ agonist at 50-fold higher concentrations (EC50 = 810 nM). Ro 41-5253 inhibited differentiation and prevented the loss of human HSCs that otherwise occurs in short-term culture.
SML1893 RO5256390 ≥98% (HPLC) RO5256390 is an agonist of Trace amine-associated receptor 1 (TAAR1), a GPCR primarily found in the brain, expressed in areas where the major monoamine amine transmitters (DA and NE) are also present. RO5256390 is a selective TAAR1 agonist shown to be a negative regulator of dopamine transmission. It has antipsychotic activity in models of schizophrenia, reduces cocaine′s reinforcng effects, and blocks binge-eating disorder.
SML2225 RO5263397 ≥98% (HPLC) RO5256390 is an orally available partial agonist that targets trace amine-associated receptor 1 (TAAR1) with high affinity (Ki in nM = 0.9/mouse, 4.1/human, 9.1/rat, 24/monkey TARR1), potency (EC50 in nM/relative efficacy with respect to β-phenylethylamine = 1.3/0.59/mouse, 17/0.81/human, 47/0.76/rat, 251/0.85/monkey TARR1-dependent cellular cAMP production), and selectivity (by a 112-receptor/channel/transporter and a 42-enzyme panel), without agonistic activity toward mouse TAAR4-expressing cells even at a high concentration of 30 μM. When applied via oral administration (0.003-1 mg/kg), RO5256390 exhibits similar in vivo efficacy as the full agonist RO5256390 in blocking psychostimulants-induced hyperlocomotion in mice.
SML2133 Ro 65-6570 Hydrochloride ≥98% (HPLC) Ro 65-6570 is a nonpeptidic, high-affinity (Ki = 0.52 against 0.1 nM OFQ for binding human ORL1) nociceptin/orphanin FQ (N/OFQ) receptor ORL-1 (KOR-3, NOP) agonist (EC50 = 40 nM by GTPγS binding assay; IC50 = 0.28 nM against 1 μM forskolin-stimulated cellular cAMP accumulation) with good selectivity over opioid receptors μ, k, δ (Ki = 5.9, 26, 250 nM against 1.5 nM naloxone, 3 nM naloxone, 0.3 nM [Ile5,6]-deltorphin II for binding respective receptors), dopamine and serotonin receptors (Ki = 520 nM/D2, 1210 nM/D3,350 nM/D4.4; Ki ≥1 μM for 5HT 1Dα, 2A, 2C, 6, 7). Ro 65-6570 elicits ORL1-dependent anxiolytic-like effects in rats in vivo (0.32-3.2 mg/kg i.p.; elevated plus maze) without affecting spontaneous locomotion. Unlike OFQ, Ro 65-6570 does not affect cocaine-induced conditioned place preference (CPP) in rats.
R140 Ro 04-6790 dihydrochloride solid Selective 5-HT6 serotonin receptor antagonist.
human ... HTR6(3362)
SML0495 Ro 25-6981 maleate salt ≥98% (HPLC) Ro 25-6981 maleate salt is a potent and selective antagonist of NMDA glutamate receptors containing the NR2B subunit with IC50 values of .009 μM for NR2B vs. 52 μM for NR2A subunits. Ro 25-6981 has been shown to have neuroprotectant effects and to reduce inflammatory and neuropathic pain in rodent models.
R0529 Ro 90-7501 ≥98% (HPLC) Inhibitor of Aß42 fibril formation
SML0233 Ro 61-8048 ≥98% (HPLC) Inhibition of kynurenine 3-hydroxylase by Ro 61-8048 reduces the episodes of dystonia and dyskinesias induced by decreased levels of kynurenic acid.
Ro 61-8048 is an inhibitor of kynurenine 3-monooxygenase (KMO) that increases kynurenic acid levels and reduces extracellular glutamate in the brain.
SML1200   RO8191 ≥98% (HPLC) RO8191 is an orally available, potent and specific type I interferon receptor agonist that directly binds to IFN-α receptor 2 (IFNAR2). RO8191 suppresses HCV replication without inducing host cell toxicity.
R8900 Ro 8-4304 solid NR2B-selective, noncompetitive NMDA glutamate receptor antagonist
human ... GRIN2B(2904)
R0279 Ro 23-9358 ≥97% (HPLC), solid Diacylglycerol lipase inhibitor. Target for anti-obesity drugs.
SML0656   Rocaglamide ≥96% (HPLC) Rocaglamide is a potent anticancer agent isolated from the genus Aglaia. Rocaglamides inhibit protein synthesis without affecting DNA or RNA synthesis. Recent study shows that Rocaglamide binds to prohibitin (PHB) 1 and 2, which prevents interaction between PHB and CRaf and inhibits CRaf activation and subsequently CRaf-MEK-ERK signaling. Also, Rocaglamide is an immunosuppressant that inhibits activation of NF-kB and NF-AT.
Rocaglamide is associated with osteoblast differentiation. In rheumatoid arthritis, rocaglamide might suppress inflammation, by preventing the expression of cytokines involved in it.
SML0613   Rofecoxib ≥98% (HPLC) Rofecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor with >800-fold COX-2 selectivity in CHO cells expressing human COX-1 and COX-2.
Rofecoxib is derived from furanone and has the ability to cross human placenta. Along with anti-inflammatory action, it possesses analgesic and antipyretic properties. Cytosolic hepatic enzymes are responsible for the metabolism of rofecoxib. It is known to cause oligohydramnios and ductus arteriosus constrictions. Rofecoxib inhibits the action of CYP1A2 (cytochrome P450 family 1 subfamily A member 2). It might be associated with aseptic meningitis. Rofecoxib is known to ameliorate the risk of colorectal adenoma, but might contribute to toxicity.
SML1099 Roflumilast ≥98% (HPLC) Roflumilast is a highly potent, orally active, and selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 0.8 nM. Roflumilast has anti-inflammatory properties and is used clinically to treat COPD.
SML2106 Roflupram ≥98% (HPLC) Roflupram (FFPM) is a potent anti-inflammatory phosphodiesterase 4 (PDE4) inhibitor that was found to suppress inflammasome activation in microglial cells by enhancing autophagy. In microglial BV-2 cells roflupram enhanced the level of microtubule-associated protein 1 light chain 3 II (LC3-II) and decreased the autophagy receptor ubiquitin-binding protein p62 (SQSTM1), enhancing autophagy, reducing the activation of inflammasome and suppressing the production of IL-1β. Roflupram (FFPM) was found to reverse learning and memory deficits in APP/PS1 transgenic mice.
R6520 Rolipram solid, ≥98% (HPLC) Selective cAMP-specific phosphodiesterase (PDE4) inhibitor.
human ... LITAF(9516), PDE3A(5139), PDE4A(5141), PDE4B(5142), PDE4C(5143), PDE4D(5144), PDE5A(8654), PDE7A(5150)
mouse ... Pde4a(18577)
rat ... Adora1(29290), Pde1b(29691), Pde2a(81743), Pde3a(50678), Pde4a(25638), Pde4b(24626), Pde4c(290646), Pde5a(171115)
SML1175 Romidepsin ≥98% (HPLC) Romidepsin is a very potent natural prodrug inhibitor of HDAC1 and HDAC2 that is converted to active form by glutathione. Romidepsin has IC50 values of 36 nM and 47 nM for HDAC1 and HDAC2, respectively. Romidepsin kills lymphoma cell lines overexpressing Bcl-2 and Bcl-XL, and has been approved for the treatment for cutaneous T-cell lymphoma (CTCL) and peripheral T-cell lymphoma, and a variety of other cancers.
Romidepsin promotes apoptosis, while hindering tumor growth in glioma models.
R2530 Ropinirole hydrochloride powder, ≥98% (HPLC) An agonist at the D2 and D3 dopamine receptor subtypes, binding with higher affinity to D3 than to D2 or D4. It has negligible effect on D1-receptors. It has medium in vitro affinity to opioid receptors. Ropinirole is said to have virtually no affinity to 5-HT1, 5-HT2, benzodiazepine, GABA, muscarinic, α1-, α2-, and β-adrenoreceptors. Used as antiparkinsonian drug.
R0283 Ropivacaine hydrochloride monohydrate ≥98% (HPLC) Local anaesthetic with less cardiotoxicity than bupivacaine; causes reversible blockade of impulse propagation along nerve fibres by preventing the inward movement of sodium ions through the cell membrane of the nerve fibers.
SML0406   Roquefortine C ≥98% (HPLC), from Penicillium roqueforti Roquefortine C is a paralytic neurotoxin of a dioxopiperazine structure produced by a diverse range of fungi, most notably Penicillium species. It has been found in blue cheese and in many other food products due to natural occurrence and contamination. Roquefortine C was found to be active on a wide range of organisms. It inhibits the growth of Gram-positive bacteria, and cockerels treated with roquefortine lost their righting reflex and died within 8-12 hours. Mice injected with roquefortine C experienced neurotoxic properties. Roquefortine C was also reported to inhibit cytochrome P450 as well as tubulin polymerization.
SML0738   RORγ Activator 1b ≥98% (HPLC) RORγ Activator 1b binds to the retinoid-related orphan receptor RORγ and induces IL-17 reporter gene expression with an EC50 of 0.1 μM. The compound RORγ Activator 1b enhances differentiation of CD4+ T cells to IL-17-secreting cells with a maximum effect of 220 percent of control at 3 μM.
SML0336 Rosavin ≥98% (HPLC) Rosavin is a well-known glycoside antioxidant from Rhadiola rosea (Golden Root, or Arctic Root) that exhibits antidepressant, anxiolytic and adaptogenic properties.
R7772 Roscovitine ≥98% (TLC) Roscovitine is a potent, selective inhibitor of cyclin-dependent kinases.
Roscovitine is a purine derived inhibitor. It stimulates apoptosis in cancer cells. It has inhibitory action on mitogen activated protein kinase (MAPK) and M-phase promoting factor (MPF) kinase activity. Roscovitine is known to arrest meiosis and thus, prevent embryonic development.
human ... CDK1(983), CDKN1A(1026), CDKN1B(1027), CDKN1C(1028), CDKN2A(1029), CDKN2B(1030), CDKN2C(1031), CDKN2D(1032), CDKN3(1033)
mouse ... CDK1(12534)
rat ... CDK1(54237)
SML1583   Roseoflavin ≥95% (HPLC) Roseoflavin is an analog of flavin mononucleotide (FMN) and riboflavin with antimicrobial activity. Roseoflavin is converted to the flavin mononucleotide (FMN) analog roseoflavin mononucleotide (RoFMN) by flavokinase and to the flavin adenine dinucleotide (FAD) analog roseoflavin adenine dinucleotide (RoFAD) by FAD synthetase, and acts as a riboflavin antagonist. Roseoflavin is an inhibitor of bacterial riboflavin riboswitches, cis regulatory elements present in non-coding RNA that specifically bind to natural ligands to regulate gene expression. Roseoflavin, converted to RoFMN, blocks the flavin mononucleotide riboswitch-mediated expression of the ribB gene, which is required for riboflavin biosynthesis.
R2408 Rosiglitazone ≥98% (HPLC) Rosiglitazone is a potent agonist for PPARγ with an EC50 of 43 nM for the human receptor. It is antidiabetic, working as an insulin sensitizer by binding to the PPARγ receptors in fat cells and making the cells more responsive to insulin.
SML0892   Roslin 2 ≥98% (HPLC) Roslin 2 is a p53 reactivator that disrupts the FAK and p53 interaction, and reactivates transcriptional activity of p53 with p21, Mdm-2 and Bax transcriptional targets. Roslin 2 decreases viability and clonogenicity of cancer cells, and inhibits tumor growth.
SML1139   Rostafuroxin ≥98% (HPLC) Rostafuroxin is a digitoxygenin derivative that selectively antagonizes the effects of endogenous ouabain on the Na+,K+-ATPase, which maintains sodium and potassium ion gradients across plasma membranes. Rostafuroxin lowers blood pressure (BP) in animal models of hypertension.
SML1264   Rosuvastatin calcium ≥98% (HPLC) Rosuvastatin calcium is a competitive inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Rosuvastatin calcium is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
R9281 Rotigotine hydrochloride ≥98% (HPLC) Rotigotine is a dopamine receptor agonist with preference for D3 receptors over D2 and D1. As such, it is an effective anti-Parkinsonian agent. Racemic rotigotine is about 50 times as potent as quinpirole, the gold standard D2 agonist.
R5648 Rottlerin Recently, Rottlerin (mallotoxin) has been shown to be a potent activator of the large conductance voltage and Ca2 activated K+ channel and to potently leftward shift the conductance-voltage relationship of the channel. Mallatoxin tested on hERG channels increased both step and tail hERG current by leftward shifting the voltage dependence of hERG activation and slowing channel deactivation. These actions distinguish Mallatoxin as a novel naturally occurring hERG channel activator.
human ... CDK2(1017)
SML2329 RP22 ≥98% (HPLC) RP22 is a AA147 analog with no ATF6α-activating potency. RP22 is the recommended inactive control for AA147 in probing ATF6α signaling-mediated unfolded protein response (UPR).
R8907 RPI-1 ≥98% (HPLC) RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor. Recently it was discover that the compound also inhibits c-Met. Increased tumorigenicity, motility, and invasiveness have been described as biological consequences of HGF/Met deregulation in tumor cells, thus not surprisingly RPI-1 treatment of H460 cells resulted in a strong reduction of both colony number and size (IC50 = 24.5 + 0.5 microM). Compound is also active at mouse NSCLC H460 xenograft tumor and metastasis model. Mechanistically RPI-1 inhibits Met phosphorylation at Tyr1234/Tyr1235, known to activate the intrinsic kinase activity. It appears that " Ret/ptc1 cross talks with Met at transcriptional and signaling levels and promotes ?-catenin transcriptional activity to drive thyrocyte neoplastic transformation". It appears that we do not have anything specific in Ret area. Handbook lists RPI-1 as Ret inhibitor.
SML1602 RQ-00203078 ≥98% (HPLC) RQ-00203078 is an orally available potent and selective TRPM8 antagonist that potently reduces cation currents induced by menthol and other TRPM8 agonists. RQ-00203078 inhibits HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.
R7532 RRD-251 hydrochloride ≥98% (HPLC) RRD-251 hydrochloride is a reversible, potent, and selective disruptor of Rb/Raf-1 interaction. The retinoblastoma tumor suppressor protein (Rb) controls the G1-S boundary by repressing the transcriptional activity of the E2F family of transcription factors. Raf-1 kinase binds and phosphorylates Rb early in the G1 phase. RRD-251 significantly inhibits angiogenesis and tumor growth in vivo in an Rb-dependent manner. RRD-251 does not inhibit the binding of B-Raf to Rb and Raf-1 to Mek1/2. Also, RRD-251 does not affect the kinase activities associated with cyclin D, cyclin E, or Raf-1.
R9782 RS-1 ≥98% (HPLC) RS-1 (RAD51-stimulatory compound 1) is a stimulator of the human homologous recombination (HR) protein RAD51. RS-1 stimulates binding of hRAD51 to single stranded DNA (ssDNA) and enhances recombinogenic activity by stabilizing the active form of hRAD51 filaments without inhibiting hRAD51 ATPase activity. RS-1 has been shown to enhance CRISPR-Cas9 knock-in efficiency in HEK293A cells and has been shown to enhance both TALEN and Cas9-mediated knock-in efficiency in rabbits.
SML1718   RS09 trifluoroacetate salt ≥98% (HPLC) RS09 is a potent and specific toll like receptor 4 (TLR-4) agonist that mimic LPS by interacting with TLR-4. RS09 causes NF-KB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS09 function as an adjuvant in vivo when administered with X-15-KLH in mice.
R1658 RS-102221 hydrochloride hydrate ≥98% (HPLC) RS-102221 is a selective, high affinity 5-HT2C receptor antagonist.
R2533 RS-127445 hydrochloride ≥98% (HPLC), powder RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi=9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
SML1909   RS 23597-190 ≥98% (HPLC) RS 23597-190 is a high affinity 5-HT4-selective antagonist with in vitro and in vivo efficacy. RS 23597-190 is a 4-amino-5-chloro-2-methoxybenzoate that antagonizes 5-HT-mediated relaxation of carbachol-contracted rat oesphageal muscularis mucosae ex vivo (pA2 = 7.5) and prevents 5-HT-induced tachycardia (tachyarrhythmia) of anaesthetized micropigs in vivo (6 mg/kg RS 23597-190 and 3-10 &amp;mu;/kg 5-HT via i.v.) by targeting 5-HT4 with high affinity (pKB = 7.8) and selectivity, while exhibiting no efficacy against 5-methoxytryptamine-mediated 5-HT3 activation in guinea-pig ileum and displaying much reduced or little affinity toward 5-HT3 (pKi = 5.7/mouse NG108-15 cells and pKB &amp;lt;5/guinea-pig ileum), dopamine receptors (pKi &amp;lt;4/D1 &amp; &lt;3/D2), muscarinic receptors (pKi &lt;4.5 toward M1/2/3/4), 5-HT1A &amp; 5-HT2 (pKi <5.2).
SML0711   RS504393 ≥98% (HPLC) RS504393 is a highly selective CCR2 chemokine receptor antagonist. RS504393 inhibits MCP-1 chemotaxis and ischemia-reperfusion injury in kidneys.
SML1882 RS 67333 hydrochloride ≥98% (HPLC) RS 67333 is a selective, high affinity (pKi = 8.7 for the 5-HT4 binding site in guinea-pig striatum) partial agonist toward 5-HT4 receptor that relaxes carbachol-contracted rat oesphageal muscularis mucosae ex vivo (pEC50/%reversal = 8.7/50 with RS 67333 vs. 8.2/100 with 5-HT) and induces tachycardia (tachyarrhythmia) of anaesthetized micropigs in vivo (ED50 via i.p. in μg/kg over max heart rate increase in beats/min = 4.9/35 with RS 67333 vs. 3.2/95 with 5-HT). RS 67333 is also reported to show high affinity for sigma receptors (pKi = 8.9/σ1 and 8.0/σ2), while exhibiting much reduced affinity toward a panel of other receptors, including 5-HT1A, 5-HT2A, 5-HT2C, 5-HT3 (pKi <6.4), muscarinic receptors (pKi = 5.2/M1 & 5.3/M2), and adrenoceptors (pKi <6.7 for α1A, α1B, α2A, α2B, β1, β2).
SML1113 RSC133 ≥98% (HPLC) RSC133 is an epigenetic modulator that effectively enhances reprogramming of human somatic cells and maintenance of human stem cell pluripotency. Apparently, RSC133 facilitates the reprograming by dual inhibition of histone deacetylase and DNA methyltransferase activities. In hFFs, RSC133 rapidly activates pluripotency-associated genes Nanog, Oct4, and Rex1 up to 2- to 2.5-fold. RSC133 exerts positive effects on cell proliferation and ablates pro-senescence phenotypes.
SML1695 RSV604 ≥98% (HPLC) RSV604 (RSV-604) is a cell-permeable, non-cytotoxic (CC50 >50 μM) benzodiazepine derivative that is reported to target respiratory syncytial virus (RSV) nucleoprotein (N) via affinity interaction (Kd = 134 μM) and display similar antiviral potency against 40 clinical human RSV isolates (Ave. EC50 = 800 nM), including both subtypes A and B. Although RSV604 displays host-dependent potency against RSV cellular replication (EC50 = 2 μM/HeLa, 1.8 μM/HEp-2, >50 μM/BHK-21 based on cellular viral F protein level 72 hrs post RSV A2 infection) and release (by >1,000,000-fold/HeLa vs. no effect/BHK-21 72 hrs post infection; [RSV604] = EC90), complete loss of infectivity of released RSV from RSV604-treated cells is observed in both HeLa and BHK-21 cultures. RSV604 is also active against bovine RSV, but inactive toward mouse pneumonia virus, human metapneumovirus or parainfluenza virus types 1 &3 (PIV1 &PIV3).
SML0779   RSVA314 ≥98% (HPLC) RSVA314 is a resveratrol analog that is a potent indirect activator of AMPK (AMP-activated protein kinase). RSVA314 is a potent inhibitor of adipogenesis in vitro in cultured cells and in vivo in mice. Apparently RSVA314 activates AMPK via a mechanism implicating CaMKKβ and LKB1. Also RSVA314 increases intracellular clearance of the amyloidogenic peptide Aβ, the core component of the amyloid plaques.
SML1725 RTC13 ≥98% (HPLC) RTC13 is a cell-permeable thiazolidinone derivative that promotes ribosomal read-through activity of premature termination codons (PTCs) and effectively restores full-length protein production from transcripts containing nonsense mutations-generated PTCs, including ataxia-telangiectasia (A-T) mutated in A-T lymphoblastoid cell cultures and dystrophin in mdx Duchenne muscular dystrophy (DMD) mice-derived muscle myotubes.
SML2013 RU 24969 hemisuccinate ≥98% (HPLC) RU-24969 is a potent and selective agonist at the 5-HT1A and 5-HT1B receptors.
R2153 RU 26752 ≥98% (HPLC), solid RU 26752 is a mineralocorticoid receptor antagonist.
R1408 RU7 ≥98% (HPLC) RU7 is a selective inhibitor of bacterial β-clamp interaction with DNA polymerase POL III, and an inhibitor of a DNA polymerase sliding clamp. Sliding clamps are proteins which function with diverse DNA polymerases, repair factors, and cell cycle-control proteins. RU7 binds to the peptide-binding pocket of the β-clamp and selectively inhibits Pol III, compared with Pol II and Pol IV.
SML1311   Rubone ≥98% (HPLC) Rubone has strong anticancer activity. Rubone and paclitaxel (PTX) combination therapy retarded cancer cell growth, migration and cancer stem-like cells (CSC) population growth.
Rubone is a miR34a modulator that specifically restores miR34a in hepatocellular carcinoma cells with wild-type or mutated p53. Rubone potently inhibits growth of hepatocellular carcinoma in a mouse xenograft model. Rubone does not effect the growth of nontumorigenic human hepatocytes.
Rubone is a miR34a modulator that specifically restores miR34a in hepatocellular carcinoma cells.
SML1577   Rubrofusarin ≥98% (HPLC) Rubrofusarin is an orange polyketide pigment produced by Fusarium graminearum and other fungal species that exhibit potent anti-cancer and anti-mycobacterial activities. Rubrofusarin is a mycotoxin that inhibits human DNA topoisomerase II-α.. Additionally, Rubrofusarin shows a significant anti-estrogenic activity.
R8404 Rufinamide ≥98% (HPLC), powder Broad-spectrum anticonvulsant.
PZ0315   Rupintrivir ≥98% (HPLC) Rupintrivir (AG7088) is an irreversible human rhinovirus (HRV) 3C protease inhibitor, also found to inhibit enterovirus and norovirus.
SML1000   RU-SKI 43 maleate ≥98% (HPLC) RU-SKI 43 is a potent and selective inhibitor of Hedgehog acyltransferase (Hhat) with an IC50 of 850 nM. RU-SKI 43 is the first small molecule found that inhibits the activity of Hedgehog acyltransferase (Hhat) and inhibits palmitoylation of Shh by endogenous Hhat in vitro and in cells. Most inhibitors of hedgehog signaling act downstream, inhibiting Smo or Gli components of the Shh pathway. The upstream activity of RU-SKI 43 directly on palmitoylation of the Shh ligand is unique.
R9525 RX 821002 hydrochloride solid, ≥98% (HPLC) Selective α2-adrenoceptor antagonist
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
SML0862   RX871024 ≥98% (HPLC) RX871024 is an imidazoline receptor antagonist that stimulates insulin secretion in β-cells and islets at lower concentrations than other imidazoline ligands. 0.1 μM RX871024 enhances glucose-induced insulin secretion under nonpolarizing conditions and at higher concentrations, it enhances secretion through a KATP channel-independent mechanism.
SML0981   RXFP1-Agonist-8 ≥98% (HPLC) RXFP1-Agonist-8 is a potent selective agonist of the G-protein-coupled receptor RXFP1, human relaxin/insulin-like family peptide receptor 1, with an EC50 of 94 nM in HEK293 cells and no activity with RXFP2 or RXFP3, other members of the relaxin family of receptors. RXFP1-Agonist-8 is believed to interact with an allosteric site at the ECL3 loop acting non-competitively with the natural hormone relaxin to activate RXFP1, and is the first bioavailable small-molecule agonist of human RXFP1 with good metabolic stability. Relaxin has long been known as a female hormone secreted by the corpus luteum that helps soften the cervix and relax the pelvic ligaments in childbirth. However, Relaxin also has potent cardiovascular and renal effects, inducing a 20% increase in cardiac output, 30% decrease in systemic vascular resistance, 30% increase in global arterial compliance and 45% increase in renal blood flow during pregnancy, anti-fibrotic, vasodilatory and pro-angiogenic effects that can be reproduced in both women and men with potential for treating various disorders including hypertensive diseases and acute heart failure.