Featured Products 2015

Highlighted products added to the Tocris Bioscience range during 2015

December 2015

H-Ras-cRaf1 interaction inhibitor; inhibits Raf signaling
5475 | Kobe 0065

Inhibits Raf signaling. Selectively attenuates proliferation and induces apoptosis of cancer cells harboring Ras oncogenes. Reduces growth of K-Ras mutant SW480 colon carcinoma cell xenografts in mice. Orally active.

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Highly potent and selective renin inhibitor
5563 | VTP 27999

EC50 = 0.47 nM. Displays >1000-fold selectivity over related and unrelated off-targets. Blocks renin-stimulated ERK1/2 phosphorylation in vascular smooth muscle cells. Exhibits a different mode of action to aliskiren (Cat. No. 5491).

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Potent and selective NUAK1 inhibitor
5622 | HTH 01-015

IC50 = 100 nM. Exhibits no significant inhibition against a panel of 139 kinases, including ten AMPK family members. Inhibits NUAK1-mediated MYPT1 phosphorylation. Also inhibits cell proliferation in U2OS cells in vitro, to a similar extent as NUAK1 knockdown models.

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PDK1 inhibitor; inhibits Akt signaling
5682 | OSU 03012

Induces apoptosis of PC-3 and medulloblastoma cells, and inhibits growth of a number of tumor cell lines. Sensitizes radiotherapy-induced cell death and enhances cytotoxic effects of chemotherapeutic agents in vitro. Attenuates tumor growth of medulloblastoma xenografts in mice.

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High affinity and selective PLK4 inhibitor
5690 | Centrinone B

Ki = 0.6 nM. Exhibits >2000-fold selectivity for PLK4 over Aurora A and Aurora B. Depletes centriole and centrosome levels in vitro. Induces cell cycle arrest in normal human cell lines in a p53-dependent manner.

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November 2015

Enhances HDR efficiency
5342 | SCR7 pyrazine

Enhances CRISPR-Cas9-mediated homology-directed repair (HDR) efficiency in vitro. Inhibits nonhomologous end-joining (NHEJ).

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High affinity C5a receptor antagonist
5455 | W 54011

Ki = 2.2 nM. Inhibits C5a-induced generation of reactive superoxide species, chemotaxis and intracellular Ca2+ mobilization in human neutrophils (IC50 values are 1.6, 2.7 and 3.1 nM, respectively).

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Stat3 inhibitor; blocks cancer stem cell self-renewal
5522 | Napabucasin

Blocks spherogenesis of cancer stem cells (CSC), but not hematopoietic stem cells. Inhibits PaCa-2 xenograft tumor growth in mice, even after cessation of treatment, and decreases population of CSCs in PaCa-2 tumors from treated mice. Also blocks spleen and liver metastases of colon cancer cells in a mouse model.

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Potent hM3Dq DREADD receptor agonist
5548 | DREADD agonist 21

EC50 = 1.7 nM. Highly selective for hM3Dq DREADD receptors over endogenous hM3 receptors.

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Potent and selective LIMK inhibitor; antitumor
5626 | SR 7826

IC50 values are 43, 5536 and 6565 nM for LIMK1, ROCKI and ROCKII, respectively. Inhibits cofilin phosphorylation in A7r5 cells and suppresses migration and invasion of PC-3 cells in vitro. Orally bioavailable.

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October 2015

Selective P2X4 allosteric antagonist
5545 | BX 430

IC50 = 0.54 μM. Exhibits >10-fold selectivity for human P2X4 receptors over P2X1, P2X2, P2X3, P2X5 and P2X7 receptors. Binds noncompetitively at extracellular allosteric site. Effective at human and zebrafish, but not mouse and rat P2X4 receptors.

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PP1 regulatory subunit PPP1R15A inhibitor
5553 | Sephin 1

Inhibitor of the regulatory subunit PPP1R15A of protein phosphatase 1. Does not bind PPP1R15B or have α2 adrenergic agonist activity. Cytoprotective in endoplasmic reticulum stressed cells in vitro. Prevents defects associated with protein misfolding in a mouse Charcot-Marie Tooth-1B model. Orally available.

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Potent and selective BRD9 inhibitor
5591 | I-BRD9

pIC50 = 7.3. Exhibits >70-fold selectivity for BRD9 over a panel of 34 other bromodomains and >700-fold selectivity over the BET family. Downregulates CLEC1, DUSP6, FES and SAMSN1 genes in Kasumi-1 cells.

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Potent and selective PI 4-kinase IIIβ inhibitor
5604 | MI 14

IC50 = 54 nM. Exhibits >1,800-fold selectivity for PI 4-K IIIβ over PI 4-K IIIα and PI 4-K IIα, respectively. Exhibits antiviral activity against single-stranded positive sense RNA viruses in HeLa cell-based assays.

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High affinity ALK and ROS1 inhibitor
5640 | PF 06463922

Ki values are <0.02, <0.07 and 0.7 nM for ROS1, wild-type ALK and ALK-L1196M, respectively. Exhibits >100-fold selectivity for ROS1 over a panel of 204 other kinases. Inhibits proliferation of BaF3 cells containing crizotinib-resistant ROS1 mutation in vitro. Inhibits tumor growth in relevant mouse models. Orally available and brain penetrant.

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September 2015

Potent and selective IRAK4 inhibitor
5430 | AS 2444697

IC50 = 21 nM. Displays 30-fold selectivity for IRAK4 over IRAK1. Inhibits LPS-induced TNFα and IL-6 production in PBMCs in vitro. Renoprotective and anti-inflammatory in a rodent model of chronic kidney disease.

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Potent and highly selective ROCK inhibitor
4961 | TC-S 7001

IC50 values are 0.6 and 1.1 nM for ROCK1 and ROCK2, respectively. Exhibits >200-fold selectivity over TRK and FLT3 receptors, and >900-fold selectivity over a panel of other kinases and cardiovascular relevent enzymes and receptors. Reduces blood pressure in normotensive and hypertensive rats. Orally active.

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Insulin degrading enzyme (IDE) inhibitor
5402 | 6bK

IC50 = 50 nM. Regulates insulin, glucagon and amylin levels, and improves glucose tolerance in a diabetic mouse model.

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Potent kynurenine 3-monooxygenase inhibitor
4926 | UPF 648

IC50 = 20 nM. Increases kynurenic acid levels, and decreases 3-HK and QUIN levels in cerebrum and liver of neonatal rodents. Neuroprotective in a Drosophila model of Huntington's disease.

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Potent and selective JAK2 inhibitor
5617 | AZD 1480

IC50 < 3 nM. Exhibits >50-fold selectivity for JAK2 over JAK3. Exhibits antitumor effects and inhibits formation of lung metastases in a mouse renal cancer model. Also inhibits STAT3 signaling, tumor angiogenesis and myeloid cell migration in vivo.

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August 2015

Potent DYRK1B inhibitor
5232 | AZ 191

IC50 values are 17, 88 and 1890 nM for DYRK1B, DYRK1A and DYRK2 respectively. Inhibits DYRK1B-induced Gi phase cell cycle arrest in Panc-1 cells in vitro.

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Selective TRPM3 agonist
5521 | CIM 0216

Exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. Stimulates insulin release from pancreatic islet cells in vitro. Evokes nocifensive behavior in mice.

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Potent Smo antagonist
5554 | IHR 1

IC50 = 7.6 nM. Selectively inhibits Hedgehog signaling over Wnt and Notch signaling pathways. Blocks Smo accumulation in primary cilium in vitro.

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High affinity, selective KCa2.2 blocker
5571 | Lei-Dab 7

Kd = 3.8 nM. Exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, IK, Kv and Kir2.1. Increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. Convulsive in vivo.

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Potent and selective PI 3-kinase p110α inhibitor
5595 | A66

IC50 = 32 nM. Exhibits >100-fold selectivity for p110α over other PI 3-kinase isoforms. Inhibits Akt signaling and tumor growth in SK-OV-3 xenografts in mice.

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July 2015

Potent PI 3-kinase inhibitor
4702 | ETP 45658

IC50 values are 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively. Also inhibits DNA-PK and mTOR (IC50 values are 70.6 and 152 nM respectively). Inhibits proliferation of multiple cancer cell lines in vitro and reduces Akt phosphorylation levels in vivo.

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Cytokine release inhibitor; anti-inflammatory
5185 | JTE 607

Inhibits production of IL-1β, IL-8, IL-6, IL-10 and TNFα (IC50 values are 5.9, 7.3, 8.8, 9.1 and 11.0 nM, respectively) from LPS-stimulated PBMCs. Reduces proinflammatory cytokine-release and attenuates lung permeability in a rat lung injury model. Induces apoptosis in leukemia cells in vitro and prolongs survival in a mouse leukemia model.

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Potent and selective GPR39 agonist
5355 | TC-G 1008

EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively. Selective over a panel of kinases (IC50s > 10 μM) and displays minimal binding affinity for ghrelin and neurotensin-1 receptors (IC50s > 30 μM). Increases GLP-1 levels in vitro and in vivo. Orally bioavailable.

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Mcl-1 inhibitor; proapoptotic
5368 | Maritoclax

Disrupts Mcl-1-Bim interaction and induces Mcl-1 proteasomal degradation. Exhibits no effect on Bcl-XL-Bim interaction. Selectively induces apoptosis in Mcl-1-dependent K562 leukemia cells. Sensitizes K562 and Raji cells to ABT-737-induced apoptosis.

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High affinity P-gp inhibitor
5456 | Zosuquidar

Kd = 79 nM. Restores doxorubicin (Cat. No. 2252) sensitivity in P-gp-expressing multidrug (MDR) resistant cancer cell lines. Also potentiates antitumor efficacy of taxol (Cat. No. 1097) in a MDR human non-small cell lung carcinoma xenograft mouse model.

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June 2015

Potent TLR7 agonist
4809 | DSR 6434

EC50 = 7.2 nM. Activates several immune effector cells in vitro. Suppresses metastasis in vivo and enhances efficacy of radiation therapy in a model of colorectal carcinoma.

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Potent and selective PDGFR family inhibitor
5013 | AC 710

IC50 values are 1.2, 2, 7.7 and 10.5 nM for KIT, FLT3, PDGFRβ and CSF1R respectively; Kd = 1.3 nM for PDGFRα. Exhibits >30-fold selectivity over a panel of other kinases and exhibits no activity against cytochrome P450. Causes tumor regression of leukemia cell xenografts. Also reduces joint swelling and inflammation in a mouse model of collagen-induced arthritis. Orally active.

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High affinity and selective WDR5 antagonist
5267 | OICR 9429

WD repeat-containing protein 5 (WDR5) antagonist (Kd = 24-52 nM), Disrupts WDR5 interaction with MLL and H3 with >100-fold selectivity over other methyltransferases tested. Also disrupts MLL1-RbBP5 in vitro.

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Potent and selective ERK5 inhibitor
5393 | ERK5-IN-1

Inhibits EGFR-induced ERK5 autophosphorylation (EC50 = 90 nM) and ERK5 enzymatic activity (IC50 = 162 nM). Exhibits at least 30-fold selectivity for ERK5 over LRRK2 in a cell based assay. Also selective for ERK5 over a panel of other kinases. Orally bioavailable.

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Potent C5a receptor antagonist
5473 | PMX 53

IC50 = 20 nM. Also MrgX2 agonist. Stimulates MrgX2-mediated mast cell degranulation. Also inhibits C5a-induced hypernociception in rats.

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May 2015

Potent human fatty acid synthase inhibitor
5303 | GSK 2194069

IC50 = 7.7 nM. Inhibits hFAS β-ketoacyl reductase activity. Also inhibits lipid synthesis and attenuates proliferation of A549 non-small-cell lung cancer cells (EC50 = 15 nM) in vitro.

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IAP antagonist
5330 | AEG 40730

Binds to the BIR3 domain of cIAP1, cIAP2 and XIAP with nanomolar affinity. Reduces cIAP1, cIAP2 and XIAP protein levels in human breast cancer MDA-MB-231 cells. Induces apoptosis in combination with TNF, and potentiates TRAIL-mediated apoptosis in human colorectal carcinoma HCT 116 cells. Cell permeable.

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Potent TASK-3 channel blocker
5338 | PK-THPP

IC50 = 35 and 300 nM for TASK-3 and TASK-1 respectively. Increases breathing rate and induces respiratory alkalosis in rats.

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Potent and selective c-MET kinase inhibitor
5356 | SGX 523

IC50 = 4nM. Exhibits minimal inhibition against a panel of 213 other protein kinases (at 1 μM). Suppresses growth of tumor xenografts derived from human glioblastoma, lung and gastric cancer cells.

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Potent and selective PLK1 inhibitor
5403 | TAK 960

IC50 values are 0.8, 16.9 and 50.2 nM for PLK1, PLK2 and PLK3 respectively. Exhibits >20-fold selectivity for PLK1 over FAK, MLCK and FES, and has minimal activity against a panel of 282 other kinases. Inhibits proliferation of a range of cancer cell lines in vitro and inhibits tumor growth of multiple human cancer cell xenografts in vivo. Orally bioavailable.

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April 2015

Selective allosteric inhibitor of IKK
4806 | BMS 345541

IC50 values are 0.3 and 4.0 μM for IKKβ and IKKα respectively. Exhibits no effect against a panel of 15 other kinases. Attenuates LPS-induced cytokine production in vitro and blocks NFκB dependent transcription in mice. Also suppresses joint destruction in a mouse model of arthritis.

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Potent and selective GlyT1 inhibitor
5308 | ASP 2535

IC50 = 92 nM. Exhibits 50-fold selectivity over GlyT2. Attenuates MK 801-induced working memory deficits and PCP-induced visual learning deficits in mice. Orally available and brain penetrant.

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Potent allosteric inhibitor of PRMT3
5367 | SGC 707

IC50 = 31 nM. Inhibits PRMT3-mediated methyltransferase activity in vitro. Displays >100-fold selectivity against 31 other methyltransferases and 250 other non-epigenetic targets.

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Potent and selective Lck and Src inhibitor
5413 | WH-4-023

IC50 values are 2 and 6 nM respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases. Supports self-renewal of naive hESCs in combination with PD 0325901, CHIR 99021 and SB 590885.

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ATP non-competitive kinesin Eg5 inhibitor
5454 | BRD 9876

ATP non-competitive kinesin Eg5 inhibitor. Selectively inhibits microtubule-bound Eg5. Inhibits multiple myeloma cell growth (IC50 = 2.2 μM).

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March 2015

Potent and selective DGAT-1 inhibitor
4837 | AZD 3988

IC50 = 0.6 nM. Exhibits selectivity for DGAT-1 over DGAT-2, Kv11.1 (hERG) and cytochrome P450 enzymes. Suppresses triacylglyceride (TAG) plasma excursion and adipose tissue TAG synthesis in rats. Reduces body weight of diet-induced obese rats. Cell permeable and orally bioavailable.

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Selective Mps1 kinase inhibitor
5142 | Mps1-IN-1

IC50 = 367 nM. Exhibits >1000 fold-selectivity against a panel of 352 kinases with the exceptions of ALK and Ltk. Disrupts the recruitment of Mad2 to kinetochores. Increases frequency of multipolar mitosis in U2OS cells.

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Potent and selective BRPF1 inhibitor
5385 | GSK 5959

IC50 = 80 nM. Exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains. Inhibits BRPF1 interaction with histone H3.3. Cell permeable.

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Aquaporin 1 (AQP1) channel blocker
5412 | TC AQP1 1

IC50 = 8 μM. Inhibits water flux in Xenopus oocytes.

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Inhibitor of TNF-α receptor 1 signaling
5432 | R 7050

Blocks TNFR1 association with TRADD and RIP1. Inhibits TNF-α-induced NF-κB and MAPK signaling pathway activation. Attenuates intracerebral hemorrhage-induced neurovascular injury in mice.

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February 2015

Potent and selective EZH2/EZH1 inhibitor
4904 | UNC 1999

SAM-competitive EZH2/EZH1 lysine methyltransferase inhibitor (IC50 values are 2 and 45 nM respectively). Selective for EZH2/EZH1 over a panel of other methyltransferases and non-epigenetic targets. Reduces H3K27me3 levels in vitro. Prolongs survival of MLL-AF9 bearing mice. Orally bioavailable.

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Potent and selective ITK inhibitor
5009 | BMS 509744

IC50 = 19 nM. Displays 200-fold selectivity over Tec family kinases and 55-fold selectivity over other kinases tested. Decreases HIV infection of primary CD4+ T cells and attenuates the establishment of HIV infection in vitro. Reduces T cell proliferation and IL-2 production in vitro. Attenuates lung inflammation in a mouse model of ovalbumin-induced allergy/asthma.

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PFKFB3 inhibitor; antiangiogenic
5121 | 3PO

Reduces glycolytic flux and suppresses glucose uptake. Inhibits endothelial cell proliferation and causes G2/M cell cycle arrest in vitro. Suppresses vessel sprouting and tumor growth in vivo. Amplifies the antiangiogenic effect of VEGFR blockers.

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USP10 and USP13 inhibitor
5197 | Spautin 1

IC50 values are 0.6 and 0.7 μM respectively. Inhibitor of autophagy and promotes degradation of Vps34 (class III PI 3-kinase) complexes. Selectively promotes apoptosis of cancer cells under starvation conditions. Prevents the PDGF-induced conversion from the contractile to synthetic phenotype in vascular smooth muscle cells.

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Potent and selective MAGL inhibitor
5206 | JJKK 048

IC50 = 0.4 nM. Exhibits >13,000 and ~630-fold selectivity for MAGL over FAAH and ABHD6 respectively.

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January 2015

Potent Smoothened receptor agonist
4366 | SAG

Kd = 59 nM. Antagonizes cyclopamine action at the Smo receptor. Potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM); induces pathway activation independently of Ptch proteins. Enhances neuronal differentiation of iPSCs into dopaminergic neurons.

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Potent and selective Iks channel blocker
5011 | HMR 1556

IC50 values are 10.5 and 34 nM in canine and guinea pig ventricular myocytes respectively. Selectively inhibits IKs currents over IKr, IKI, Ito and L-type calcium channel currents. Also has little or no effect on Kv11.1 Kv1.5, Kv1.3, Kir2.1 and HCN2 channel currents. Potentiates E-4031 -induced arrhythmias in vivo.

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Potent and selective NUAK1/2 inhibitor
5177 | WZ 4003

IC50 values are 20 and 100 nM respectively. Exhibits no significant inhibition against a panel of 139 kinases, including ten AMPK family members. Inhibits NUAK1-mediated MYPT1 phosphorylation. Also inhibits cell proliferation in U2OS cells.

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Potent and selective Aurora kinase A inhibitor
5286 | TC-S 7010

IC50 = 3.4 nM. Exhibits 1000-fold selectivity for Aurora kinase A over Aurora kinase B. Displays antiproliferative activity in HCT116 and HT29 cells (IC50 values are 0.19 and 2.9 μM respectively).

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High affinity and selective activator of Bax
5314 | SMBA 1

Ki = 43.3 nM. Binds to the S184 binding pocket to block Bax phosphorylation. Does not bind to other Bcl-2 family members, including Bcl-2, Bak and Bid. Induces apoptosis in lung cancer cell lines expressing high levels of Bax. Represses tumor growth of A549 lung cancer xenografts in mice.

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