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Stem Cell

What's a Small Molecule?

A small molecule is a fast working compound that has an effect on protein function. Small molecules can function across a variety of cell types and species and show great potential for use in therapeutics. Small molecules are unique in that they can inhibit a specific function of a multifunctional protein. They can also disrupt protein-protein interactions. Small molecules are also useful in that they can often be reversed or turned off if needed.

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  1. A-922500

    A-922500 is a diacylglycerol acyltransferase 1 (DGAT-1) inhibitor for both human and mouse. DGATs catalyze the final reaction step in the synthesis of triglyceride. Learn More
  2. A769662

    A769662 is a potent and reversible small molecule that activates AMP-activated protein kinase (AMPK). The activation of AMPK inhibits mTOR (mammalian target of rapamycin) signaling, which is a positive effector of cell growth, proliferation and survival. A769662 has been shown to inhibit the Na⁺K⁺-ATPase at higher concentrations. It also inhibits the differentiation of adipocytes. Learn More
  3. A83-01

    A83-01 is a TGFβ kinase/activin receptor like kinase (ALK5) inhibitor. It blocks the phosphorylation of Smad2 and inhibits TGFβ-induced epithelial-to-mesenchymal transition. A83-01 is more potent than small molecule SB431542, and has been shown to inhibit differentiation of rat induced pluripotent stem cells (iPSCs) and increases clonal expansion efficiency. Small molecule A83-01 helps maintain homogeneity and long-term in vitro self-renewal of human iPSCs.


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  4. Anacardic Acid
    Anacardic Acid

    Anacardic acid is a histone acetyltransferase (HAT) inhibitor. It inhibits the HAT activity of the transcription co-activators p300 and p300/CREB-biding protein associated factor (pCAF) with IC50 values of 8.5 and 5 µM. It has been shown to display a variety of biological activities, including antibacterial, antimicrobial, prostaglandin synthase inhibition, tyrosinase, and lipoxygenase inhibition. Anacardic acid has been shown to decrease expression of NF-κB regulated gene products including, invasion, inflammation, proliferation and cell survival. It has also been linked to be a potent activator of Aurora Kinase A (ARK-1) mediated phosphorylation of histone H3.

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  5. BIO

    BIO is a potent, reversible and ATP-competitive inhibitor of GSK3α/β.  The inhibition of  GSK by BIO has been shown to activate the Wnt signaling pathway  and sustain pluripotency in murine and human embryonic stem cells. BIO is the first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells. It has also been shown to induce the differentiation of neonatal cardiomyocytes.

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  6. BIX01294

    BIX01294 is a histone lysine methyltransferase (HMTase) inhibitor that modulates the epigenetic status of chromatin. It selectively inhibits the G9a HMTase and the generation of histone H3 lysine 9 methylation. BIX01294, when used in combination with HDAC inhibitor Valproic Acid has been used as a replacement for ectopic OCT4 (POU5F1) and cMyc respectively in pluripotent stem cell induction (iPS) recipes. BIX01294 is a useful for the study of histone lysine methylation, differentiation and reprogramming. 


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  7. Brefeldin A
    Brefeldin A

    Brefeldin A (BFA) (IC50 value of 0.2 μM) is an inhibitor of ATPase. ATPase is a chemical enzyme. It is essential in the ADP/ATP exchange providing chemical potential energy. ATP supplies the energy for such physiological activities such as importing metabolites necessary for cell metabolism, exporting toxins, wastes, and solutes that can hinder cellular processes, cell proliferation, ER stress and so forth. When tested with cell line HEK293 cells (stably express wild-type (wt) CRELD2), BFA treatment nearly abolished the secretion of wtCRELD2 completely via inhibiting the transportation of proteins from the ER to the Golgi apparatus [4]. In MCF-7 cells and Hela cells, treatment with BFA induced p53 expression via inhibiting ATP which enhanced ER stress [5]. When treated with colorectal cancer cell line HCT116 cells, BFA treatment induced cells apoprosis by inhibiting ATP which functioned in the process of cellular vesicle trafficking Treatment with BFA could attenuate stimulus-dependent hyperalgesia phenomenon via inhibiting vesicular exocytosis which process is important for ATP release. BFA also is reported as an inhibitor for GTP/GDP exchange in a dose-dependent way, which is important in vesicular trafficking. Learn More
  8. BX-795

    BX-795 is a potent inhibitor of both PDK1 and TBK1 as well as IKKε.  It acts by blocking phosphorylation and is reversible. Learn More
  9. CHIR99021 Structure

    Regular Price: $219.00

    Special Price: $84.00

    CHIR99021 is the most selective inhibitor of glycogen synthase kinase 3β (GSK3β). CHIR99021 does not show cross-reactivity against cyclin-dependent kinases (CDKs) with a 350 fold selectivity toward GSK3β compared to CDKs with a Kᵢ of <10nM in vitro. CHIR99021 has been shown in long term expansion of murine embryonic stem cells in conjunction with MEK/MAPK inhibitor PD184352 and fibroblast growth factor receptor (FGFR) inhibitor SU5402. Learn More
  10. Ciglitazone

    Ciglitazone is an antihyperglycemic agent of the thiazolidinedione structural class, selective agonist at PPARγ (peroxisome proliferator-activated receptor γ). It activates PPARγ with an EC50 value of 3 μM in vitro, and is at least 33-fold selective over PPARα and δ. Antihyperglycemic in vivo. Ciglitazone inhibits HUVEC differentiation and angiogenesis and also stimulates adipogenesis and decreases osteoblastogenesis in human mesenchymal stem cells. Learn More
  11. Cyclopamine

    Cyclopamine is a small molecule inhibitor of the sonic hedgehog pathway (Hh) by binding to the heptahelical bundle of Smoothened. It inhibits the growth of medulloblastoma cells. Hedgehog signaling is involved in embryogenesis as well as cancer progression. It is a steroid alkaloid  and originally identified as a teratogenic agent.


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  12. Daidzin

    Daidzin is a glucoside of the isoflavone daidzein found in soy beans. It demonstrates chemopreventive activities by inhibiting the bioactivation of carcinogenic arylamines. It is also a potent, selective inhibitor of human mitochondrial aldehyde dehydrogenase. Learn More
  13. DAPT

    DAPT is a γ-secretase inhibitor that indirectly inhibits Notch, a γ-secretase substrate. Since Notch is involved in the development of the nervous system and pancreas, DAPT has been suggested to be used in the modulation of Notch activity in embryonic stem cell differentiation. As an inhibitor of γ-secretase, DAPT may also be useful in the study of β-amyloid (Aβ) formation.


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  14. Dexamethasone

    Dexamethasone, a synthetic glucocorticoid with a higher affinity than a natural ligand, cortisol, has a range of effects on cell survival, cell signaling and gene expression. It is know to affect inflammatory responses, cellular proliferation, and differentiation in target tissues. Dexamethasone has been shown to inhibit differentiation of cord blood stem cell derived dendritic cells (DC) precusors into immature DCs. Learn More
  15. Dorsomorphin Chemical Structure

    Regular Price: $99.00

    Special Price: $59.00

    Dorsomorphin (also known as Compound C) is a potent, reversible, AMPK inhibitor with Ki of 109 NM in the absence of AMP. In addition, it has been found to selectively inhibit bone morphogenetic protein (BMP) signaling. Learn More
  16. EHNA Hydrochloride
    EHNA Hydrochloride

    EHNA Hydrochloride is a reversible adenosine deaminase inhibitor that selectively inhibits the cGMP-specific phosphodieterase (PDE2). At a 10µM concentration, EHNA has been shown to effectively and reversibly block the differentiation and maintain the pluripotency of the hES cell line SA121 in feeder- free cultures without exogenously added FGF for up to 30 passages. EHNA has also been used to study the cardioprotective and neuroprotective efforts during ischemia and in the study of cAMP/cGMP signaling.


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  17. Forskolin

    Forskolin is a cell-permeable diterpenoid that possesses anti-hypertensive, positive inotropic, and adenylyl cyclase activating properties. Many of its biological effects are due to its activation of adenylyl cyclase and the resulting increase in intracellular cAMP concentration. Cyclic AMP is a signaling molecule and key regulator of critical enzymes in cellular processes.  Forskolin has also been shown to effect calcium currents and inhibit MAP kinase.


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  18. G418

    Geneticin Sulfate, also known as G418, is an aminoglycoside antibiotic. This compound has been shown to cause a bypass of nonsense mutations during translation. Experiments have shown that G418 inhibits the incorporation of amino acids into protein and can destroy fibroblasts. G418 is toxic to bacteria, yeast, higher plants, mammalian cells, protozoans and helminths. In mammalian cells, selection is commonly performed using 400 mg/L G418, followed by 200 mg/L for culture maintenance. G418 is commonly used for the selection of cells that are genetically engineered with a plasmid containing the neo (neor) gene, which provides resistance to G418. This antibiotic is commonly used during the selection of transfected cell lines. Learn More
  19. HA-1077 (dihydrochloride)
    HA-1077 (dihydrochloride)

    HA-1077 is a potent inhibitor of Rho-associated kinase II (ROCK-II), and also inhibits Protein Kinase C-related kinase 2 (PRK2),  Mitogen- and Stress-Activated Protein Kinase (MSK1), and Mitogen Activated Protein Kinase-Activated Protein Kinase 1b (MAPKAP-K1b). HA-1077 is a novel vasodilator agent which inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist. Through the inhibition of Rho-kinase, HA-1077 has been shown to reduce blood vessel constriction, decrease pulmonary arterial pressure, inhibit tumor angiogenesis, and improve insulin signaling in rodent models.


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  20. Indolactam V
    Indolactam V

    Indolactam V is an activator of protein kinase C (PKC) that works by inhibiting PKC isozymes (alpha, beta-I, beta-II, gamma, delta, epsilon, eta, theta). This inducing differentiation in embryonic stem cells into pancreatic progenitors. It also exhibits tumor promoting activity. Learn More
  21. IWP-2

    IWP-2 is an inhibitor of Wnt production and an inactivator of Porcn function.  The Wnt/b-catenin pathway maintains transcriptional programs that enable stem cells to remain multipotent and hyperactivation of this pathway leads to disease stage. IWP-2 inactivates Porcn function by either directly inhibiting the Porcn active site or by modulating the function of the Porcn regulator.


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  22. LDE225

    LDE225 (NPV-LDE225) is a novel and specific small molecule Smoothened (Smo) inhibitor with an IC₅₀ of 11nM. LDE225 has been shown to potentially inhibit Hh- and Smo-dependent proliferation in vivo. It also induced the regression of preformed basaloid lesions with an IC50 of <150 nmol/l and almost complete regression at 1.5 μmol/l. Topical application of a 1% LDE225 solution to depilated skin of C57/BL6 mice completely inhibited hair growth during anagen phase as well as the expression of the Hh-pathway target genes and partial inhibition was obtained when applying a 0.3% solution.

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  23. LDN193189

    Regular Price: $219.00

    Special Price: $119.00

    LDN193189 is a highly potent small molecule BMP inhibitor. It inhibits BMP type I receptors ALK2, ALK3 and ALK6. LDN193189 was derived from structure-activity relationship studies of Dorsomorphin and functions by preventing phosphorylation of Smad1, Smad5 and Smad8. It shows in vivo clinical utility by reducing ectopic ossification in mouse models. 


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  24. LY294002

    LY294002 is a cell permeable, selective phosphatidylinositol 3-kinase (P13K) inhibitor that acts as a competitor inhibitor of the ATP binding site of the enzyme. LY294002 inhibits cell proliferation of choroidal melanoma OCM-1 cells. In mESC’s LY294002 prevents self-renewal by inhibiting LIF2. LY294002 does not affect the activities of EGF receptor kinase, MAP kinase, PKC, PI 4-kinase, S6 kinase and c-Src even at 50µl. LY294002 has also been shown to be an inhibitor of casein kinase II. Learn More
  25. MG132

    MG132 is a proteasome inhibitor. Proteasome are found at high concentrations in eukaryotic cells, which causes protein degradation. This inhibitor enhances thermotolerance in a variety of cell types. MG132 also activates JNK-1 which may lead to apoptosis under cell stress. It has been shown to be involved with the cell cycle, in controlling inflammatory processes and gene expression. Learn More
  26. PD0325901 Structure

    Regular Price: $219.00

    Special Price: $84.00

    PD0325901 is an organic molecule targeting mitogen– activated protein kinase (MAPK/ERK kinase or MEK). PD0325901 is a derivative of MEK inhibitor CI-1040 and selectively binds to and inhibits MEK which may result in the inhibition of the phosphorylation and activation of MAPK/ERK and the inhibition of tumor cell proliferation.  In combination with CHIR99021, PD0325901 has been shown to prevent cell differentiation and sustain ES cell self-renewal.


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  27. PD173074

    PD173074 is a potent, cell permeable and ATP competitive inhibitor of FGFR and VEGFR. It has been shown to arrest the G0/G1 phase of FGFR3– expressing cells.  PD173074 blocks the FGFR signaling pathway and leads to self-renewal of stem cells via ERK1/2 activation. Treatment of FGF2-expressing human multipotent adipose-derived stem cells with PD173074 has been shown to dramatically decrease their differentiation potential and clonogenicity. 

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  28. Pluripotency Set
    Pluripotency Set

    The Reagents Direct Pluripotency Set is composed of four small molecules that when used in combination, have been shown to help maintain the pluripotency of embryonic stem cells. This set contains four signaling inhibitors; ROCK inhibitor Y27632 (2mg), MEK inhibitor PD0325901 (2mg), ALK5 inhibitor A83-01 (2mg) and GSK-3β inhibitor CHIR99021 (2mg).

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  29. PP242

    PP242 is a potent and selective inhibitor of mTOR, inhibitor, a Ser/Thr kinase  and cell growth controller.  PP242, but not Rapamycin has been shown to induce cell death in mouse and human leukemia cells in vitro.  In vivo, PP242 delayed leukemia onset and enhanced the effects of the front-line tyrosine kinase inhibitors more effectively than rapamycin. PP242 has also been shown to significantly augment histone deacetylase inhibitor-induced apoptosis in hepatocellular carcinoma cells. 


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  30. PS48

    PS48 is an allosteric small molecule activator of phosphoinositide-dependent protein kinase 1 (PDK1) that binds to the HM/PIF binding pocket rather than the ATP-binding site. PS48 is one of the only allosteric compounds that targets a regulatory binding site on a protein kinase catalytic domain that is not adjacent to or overlaps with the ATP binding site. PS48 has been shown to enhance reprogramming of neonatal human epidermal keratinocytes (NHEKs).

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  31. Purmorphamine

    Purmorphamine is a 2,6,9-trisubstituted purine that has been shown to promote the differentiation of both human and mouse mesenchymal progenitor cells into osteoblasts. Purmorphamine has been found to directly bind to and activate the 7-transmembrane Smo receptor of the Hedgehog signaling pathway. It has also been used in studies to replace sonic hedgehog for the generation of motor neurons from human embryonic stem cells.

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  32. Resveratrol

    Resveratrol is a natural polyphelol, found in grapes and red wine, and is a selective inhibitor of cyclooxygenase-1 (COX-1). It inhibits COX and peroxidase activities of COX-1 with essentially no inhibition of the COX activity of COX-2. It has also been used extensively in stem cell studies to enhance self-renewal and multipotency of MSCs. It has anti-tumor, antioxidant, anti-platelet, anti-inflammatory and anti-fungal effects. Learn More
  33. Reversine Structure

    Reversine is a potent, selective A3 adenosine receptor antagonist. It has been shown to induce differentiated myogenic-linage committed cells to become multipotent mesenchymal progenitor cells. Learn More
  34. RG108

    RG108 is a potent and specific DNA methyltransferase (DNMT) inhibitor. It causes demethylation and reactivation of tumor suppressor genes and can be used to enhance reprogramming. RG108 has been found to inhibit human tumor cell line proliferation and increases doubling time in culture. Learn More
  35. RO4929097

    RO4929097 is a small molecule gamma secretase inhibitor with an IC₅₀ of 4nM. It binds to gamma secretase and blocks the activation of Notch receptors, which may inhibit tumor cell proliferation. RO4929097 inhibits Notch processing in tumor cells as measured by the reduction of intracellular Notch expression by Western blot. RO4929097 produces a less transformed and flattened slower-growing phenotype but does not induce apoptosis or block tumor cell proliferation.

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  36. SB202190

    SB202190 is a pyridinyl imidazole that inhibits p38 kinase in vivo through competition with ATP. It binds within the ATP pocket of the active kinase and selectively inhibits p38α and β isoforms. SB202190 induces apoptosis through the activation of cysteine protease (CPP32) like kinases.  SB202190 has been shown to block both lipopolysaccharide (LPS) induced gene expression and nitric oxide (NO) induced stabilization of interleukin (IL) -8 mRNA in monocytes. 


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  37. SB431542

    SB431542 is a selective and potent inhibitor of TGFβ superfamily type I activin receptor-like kinase (ALK) receptor, specifically ALK4, ALK5 and ALK7. It does not affect BMP receptors ALK2, ALK3 or ALK6. SB431542 specifically blocks Smad signaling and suppresses renewal in embryonic and induced pluripotent stem (iPS) cells and promotes differentiation. When used in combination with MEK inhibitor PD0325901, SB431542 has been found to enhance reprogramming efficiency. Learn More
  38. Sodium Butyrate
    Sodium Butyrate

    Sodium Butyrate is a short fatty acid chain that has an effect on the molecular, tissue and cellular levels. Sodium Butyrate has been shown to induce cell growth arrest, differentiation and apoptosis in cancer cells. It inhibits histone deacetylase (HDAC) and decreases Ca²⁺ release from intracellular stores. Sodium butyrate has been used to direct the differentiation of mouse embryonic stem cells into hepatocytes when used in combination with Activin A.

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  39. SP600125

    SP600125 is a selective, reversible ATP competitive inhibitor of c-Jun N-terminal kinase (JNK). It exhibits greater than 300-fold selectivity for JNK against related MAP kinases ERK1 and p38-2, and the serine threonine kinase PKA. In cells, SP600125 causes dose-dependent inhibition of the phosphorylation of c-Jun, the expression of inflammatory genes IL-2, COX-2, TNF-α, IFN-γ, and blocks the activation and differentiation of primary human CD4 cell cultures.


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  40. Thiazovivin

    Regular Price: $219.00

    Special Price: $159.00

    Thiazovivin is a small molecule that has been shown to dramatically improve survival of hESCs upon trypsinization. When used in combination with ALK5 inhibitor SB431542 and MEK inhibitor PD0325091, Thiazovivin has been shown to enhance the efficiency of fibroblast reprogramming. Learn More
  41. Tranylcypromine

    Tranylcypromine hydrochloride , also known as 2-PCPA, is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110), a histone demethylase, and non-hydrazine monoamine oxidases (MAO). Histones contain unstructured N-terminal residues that are the site of numerous post-translational modifications, involving acetylation, ubiquitination, methylation, and sumoylation to produce a specific gene regulatory outcome. Complementary enzymes catalyze the addition and removal of these modifications as needed. The amine oxidase domain-containing enzyme lysine-specific demethylase 1 (LSD1) is a part of one of two classes of histone demethylases capable of demethylating lysine residues. LSD1 shares similar catalytic sites with monoamine oxidases (MAO) A and B. Treatment of P19 embryonal carcinoma cells with tranylcypromine resulted in global increase in H3K4 methylation as well as transcriptional derepression of the pluripotent stem cell marker Oct43. Learn More
  42. Valproic Acid
    Valproic Acid

    Valproic Acid is a small molecule histone deacetylase (HDAC) inhibitor that that exhibits anticancer, anti-inflammatory and neuroprotective effects . It has been shown to inhibit multiple pathways including the ERK, PKC and Wnt/β-Catenin pathways.  Valproic Acid has been shown to regulate the differentiation and proliferation of various cell types, including mesenchymal and hematopoietic stem cells, primary neurons, neuroblastomas and neural progenitor cells. Valproic acid, when used in combination with cytokines differentiate cells into a uniform and homogeneous cell population of hepatic progenitor cells, followed by maturation into functional hepatocytes.


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  43. XAV939

    XAV939 is a cell permeable, small molecule inhibitor of the Wnt/β– catenin pathway. It inhibits tankyrase 1 (IC₅₀= 11nM)and tankyrase 2 (IC₅₀=4nM), stabilizes axin and stimulates β-catenin degradation.  Small molecule XAV939 has also been shown to inhibit proliferation of the µ-catenin-dependent colon carcinoma cell line DLD-1.


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  44. Y27632 Structure

    Y27632 (dihydrochloride) is a highly potent ATP-competitive inhibitor of Rho– associated coiled-coil forming protein serine/threonine kinase (ROCK). It has been shown to prevent dissociation-induced apoptosis in human embryonic stem cells (hES cells). Y27632 enhances the survival and cloning efficiency of dissociated hES cells without affecting their pluripotency. Learn More

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