Small Molecules
Showing 49–72 of 108 results
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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.
1mg
Cat. No.: 56-L54
$299.00
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Iniparib
Iniparib is a potent inhibitor of poly (ADP-ribose) polymerase-1 (PARP1). PARP1 has been shown to play an important role in the repair of naturally occurring DNA damage in cells and in DNA that has been damaged by chemotherapy. Iniparib has demonstrated activity in multiple types of solid tumors, with prolonged inhibition of its target.
10 mg
Cat. No.: 63-T21
$99.00
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IPA3
IPA3 is a selective inhibitor of P21-activated kinase (PAK1). It functions by targeting the autoregulatroy mechanism, inhibiting the activators from binding to the active sites on the enzyme, producing the inactive conformation of PAKs. The autoinhibitory regions suppress the catalytic activity of its kinase domain, which are removed once activators have bound to the protein. IPA2 does not inhibit PAK1 if activators are already bound to the enzyme. PAK1 is implicated in tumorigenisis and metastasis.
5mg
Cat. No.: 51-N19
$75.00
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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.
2 mg
Cat. No.: 57-G89
$99.00
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IWR-1 endo
Wnt signaling proteins are small secreted proteins active in embryonic development, tumorigenesis and tissue homeostasis. IWR-1 endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 of 180nM. IWR-1 endo inhibits Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein through a destruction complex which consists of Apc, Axin2, Ck1, and Gsk3β. IWR-1-endo stabilizes the destruction complex, increasing the level of Axin2 protein without changing the levels of Apc or Gsk3β. In in vivo tests , IWR-1 endo has been shown to inhibit zebrafish tail fin regeneration at a minimum inhibitory concentration of 0.5 µM.
5 mg
Cat. No.: 35-H18
$79.00
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LBH589
LBH589 (Panobinostat) is a novel HDAC inhibitor that has been shown to induce acetylation of histone H3 and H4, increase p21 levels and disrupt the chaperone function of hsp90. LBH589 induces G(2) M Cell cycle arrest and inhibits HUVEC proliferation and viability. At noncytotoxic concentrations. LBH589 inhibits AKT activity, endothelial tube formation and Matrigel invasion.
10 mg
Cat. No.: 16-K74
$99.00
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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.
2 mg
Cat. No.: 43-X52
$139.00
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LDN193189
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.
Sale!2 mg
Cat. No.: 36-F52
Original price was: $219.00.$119.00Current price is: $119.00.
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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.
5 mg
Cat. No.: 89-Y31
$79.00
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Masitinib (AB1010)
Masitinib (AB1010) is a protein tyrosine kinase inhibitor. It targets c-KIT, PDGFR and FGFR3. It also potently inhibits human and murine KIT with activating mutations in the juxtamembrane domain. In vivo, Masitinib has been shown to block tumor growth in mice with subcutaneous grafts of Ba/F3 cells expressing a juxtamembrane KIT mutant.
10 mg
Cat. No.: 26-A39
$99.00
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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.
5mg
Cat. No.: 15-G73
$60.00
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MS-275
MS-275 is a potent HDAC inhibitor with an IC50 of 0.3 and 8µM for HDAC1 and HDAC3. It has been shown to inhibit tumor growth by inducing tumor suppressors p21WAF1/CIP1 and gelsolin through the acetylation of histones and changing cell cycle distribution. MS-275 has been shown to exert dose-dependent effects in human leukemia cells at low concentrations in human prostate cancer lines. MS-275 inhibits proliferation of various human tumor cell lines and inhibits the growth of human tumor xenographs in the nude mouse.
10 mg
Cat. No.: 92-Y43
$69.00
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Neratinib
Neratinib, also known as HKI-272, is a second-generation inhibitor of the ErbB family of receptor kinases. Neratinib is an irreversible inhibitor of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER-2) tyrosine kinases by targeting a cysteine residue in the ATP-binding site of the receptor. Neratinib has been shown to inhibit the proliferation of HER-2 overexpressing human breast cancer cell lines and EGFR-dependent cells in vitro. In vivo, Neratinib has been shown to be active against HER-2- and EGFR-dependent tumor xenograft models .
5 mg
Cat. No.: 50-P44
$149.00
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Nilotinib
Nilotinib, also known as AMN107 or Tasigna, is a tyrosine kinase inhibitor. It is an analog of imatinib with similar multiple kinase targets, but without inhibition of the Src gene. This gene regulates tyrosine kinase proteins that in turn affect whether cells multiply or die. Tyrosine kinase inhibitors interfere with cell communication and growth. Nilotinib is a selective BCR-ABL inhibitor that fits into the ATP-binding site of the BCR-ABL protein. It has a higher affinity for the BCR-ABl protein than imatinib. It is not only more potent than imatinib against wild-type BCR-ABL (IC50 < 30 nM), but also significantly active against 32/33 imatinib-resistant BCR-ABL mutants. Nilotinib was as potent as imatinib in inducing apoptosis (IC50 = 0.54 nM) and inhibiting proliferation (IC50 = 0.20 nM) of EOL-1 cells.
Cat. No.: 66-J40-500
$640.00
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NKH477
NKH477 is a water-soluble analog of forskolin. Like forskolin, NKH477 activates adenylyl cyclases without altering the activity of phosphodiesterases or sodium/potassium ATPases. This compound stimulates cardiac (type V) adenylyl cyclase more potently than other isoforms. It dose dependently increases cAMP and blocks potassium-induced contraction concetrations in smooth muscle strips (IC50 = 80 nM). NKH 477 causes relaxation of histamine treated guinea pig smooth muscle (IC50 = 32 nM).
5mg
Cat. No.: 50-M87
$79.00
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NSC74589
NSC74859, also known as S3I-201, binds the Stat3-SH2 domain and prevents Stat3 phosphorylation/activation, dimerization, DNA-binding, and Stat3-dependent transcription, therefore, inhibiting growth and inducing apoptosis preferentially in tumor cells that contain persistently activated Stat3. Moreover, NSC74859 also inhibits the expression of the Stat3-regulated genes encoding cyclin D1, Bcl-xL, and survivin.
5mg
Cat. No.: 18-N27
$65.00
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Nutlin-3
Nutlin-3 is a MDM2 antagonist, a p53 activator and an apoptosis inducer. MDM2 works by binding the p53 tumor suppressor protein and negatively regulating its transcriptional activity and stability. Inhibition of the MDM-p53 interaction results in the stabilization of p53, cell cycle arrest and apoptosis.
2 mg
Cat. No.: 75-D58
$69.00
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Olaparib
Olaparib is a potent small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP). It acts by binding to PARP, inhibiting PARP-mediaed repair of single strand DNA breaks. PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins and can be activated by single-stranded DNA breaks.
10 mg
Cat. No.: 54-S12
$74.00
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PD0325901
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.
Sale!2 mg
Cat. No.: 39-C68
Original price was: $219.00.$89.00Current price is: $89.00.
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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.
2 mg
Cat. No.: 14-Z32
$79.00
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PD98059
PD98059 is a highly selective noncompetitive inhibitor of MEK1 and MEK2. It prevents the activation of MAPKK1 by Raf or MEK kinase with an IC50 of 2-7µM, but does not inhibit Raf-activated MAPKK1. At concentrations up to 100µM, PD98059 does not inhibit activation of MKK3 or SEK as determined by measuring phosphorylation at its activation site. PD98059 has been shown to inhibit cell growth and proliferation in acute myelogenous leukemia (AML) cell lines and causes G1 arrest by blocking p53-dependent p21 induction.
Sale!2 mg
Cat. No.: 77-I42
Original price was: $49.00.$39.00Current price is: $39.00.
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PLX-4032
PLX-4032 (AKA Vemurafenib) is a highly selective inhibitor of BRAF kinase activity with an IC₅₀ of 44 nmol/L against V600E-mutant BRAF. BRAFV600E cancer-causing mutation occurs in most melanomas and about eight percent of all solid tumors. PLX-4032 has been shown to selectively inhibit the RAF/MEK/ERK pathway in BRAF mutant cells and induce regression of BRAF mutant xenographs. PLX4032 has also been shown to cause programmed cell death in melanoma cell lines and may be a potential anti-tumor agent.
5 mg
Cat. No.: 34-S51
$99.00
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Ponatinib
Ponatinib, also known as AP24534, is considered to be a pan-BCR-ABL inhibitor. It was specifically designed to bind BCR-ABL with very high potency and to inhibit the entire spectrum of mutants conferring resistance against other tyrosine kinase inhibitors (TKIs), such as VEGFR2, FGFR1, PDGFRα, mutant FLT3 phosporylation and LYN among others, including the T315I mutant that is resistant to all current therapies. It has been shown to suppress BCR-ALB(T315I)-driven tumor growth in mice.
10mg
Cat. No.: 37-N29
$119.00
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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.
5 mg
Cat. No.: 26-Q09
$69.00
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Showing 49–72 of 108 results