Featured Products 2016

Highlighted products added to the Tocris Bioscience range during 2016

December 2016

Potent fluorescent Smo antagonist
5561 | IHR-Cy3

IC50 = 100 nM. Non fluorescent analog IHR 1 also available.

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Potent and selective ERK5 inhibitor
5843 | AX 15836

IC50 = 8 nM. Exhibits >1,000-fold selectivity for ERK5 over a panel of over 200 kinases. Also exhibits selectivity over bromodomain BRD4 (Kd = 3,600 nM).

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Potent and selective PARG inhibitor; cell permeable
5952 | PDD 00017273

IC50 = 26 nM. Exhibits >350-fold selectivity for PARG over a panel of ion channels, enzymes and receptors, including PARP1 and ARH3. Maintains PAR chains and induces DNA double stranded breaks in cells following DNA damage. Decreases colony formation of ZR-75-1 BRCA1 WT cells. Cell permeable.

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Potent and selective BRD1 and TAF1 inhibitor
5970 | BAY 299

IC50 values are 6 and 13 nM, respectively. Displays selectivity over other bromodomains (>30-fold over other members of the BRPF family; BRD9 and ATAD2; >300-fold over BRD4). Displays BRD1 and TAF1 inhibition in a NanoBRET cell assay.

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Potent ALK2/3 inhibitor; promotes neural induction of hPSCs
6053 | LDN 193189

IC50 values are 5 and 30 nM, respectively; inhibits BMP4-mediated Smad1/5/8 activation. Exhibits >200-fold selectivity for BMP signaling over TGF-β signaling. Also exhibits selectivity over AMPK, PDGFR and MAPK signaling. Promotes neural induction of hPSCs in combination with SB 431542 (Cat. No. 1614), SU 5402 (Cat. No. 3300), CHIR 99021 (Cat. No. 4423) and DAPT (Cat. No. 2634).

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November 2016

Potent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonist
5701 | AMG 853

IC50 values are 8 and 35 nM, respectively in plasma. Inhibits PGD2-induced down modulation of CRTH2 on CD16- granulocytes in human whole blood and PGD2-induced cAMP response in platelets. Inhibits PGD2-induced airway constriction in vivo. Orally bioavailable.

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Potent and selective PFKFB3 inhibitor
5742 | AZ PFKFB3 67

IC50 values are 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively.

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Potent LPA1 antagonist
5913 | Ro 6842262

IC50 = 25 nM. Exhibits >1,200-fold selectivity for LPA1 over LPA3. Attenuates NHLF human lung fibroblast cell proliferation and contraction in vitro. Also reduces LPA-induced histamine plasma levels in mice. Orally bioavailable.

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Potent and selective PI 3-kinase p110δ inhibitor
5919 | PI 3065

IC50 = 5 nM; Ki = 1.5 nM. Exhibits >100-fold selectivity over p100α, p100γ and p100β isoforms (IC50 values are 600, 910, >10,000 nM, respectively). Attenuates 4TI tumor growth and metastasis in vivo.

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Potent δ-opioid receptor positive allosteric modulator
5983 | BMS 986187

EC50 = 30 nM. Exhibits 100-fold selectivity for δ over μ-opioid receptor. Enhances affinity of [Leu5]-Enkephalin (Cat.No. 1889), SNC 80 (Cat.No. 0764) and TAN 67 (Cat.No. 0921) for the δ-opioid receptor.

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October 2016

Potent Nek2 inhibitor
4546 | rac-CCT 250863

IC50 = 73 nM. Exhibits selectivity for Nek2 over PLK1, MPS1, Cdk2 and Aurora A.

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Negative allosteric modulator at mGlu7; brain penetrant
5715 | (±)-ADX 71743

IC50 = 300 nM. Blocks high frequency-induced LTP at SC-CA1 synapses in hippocampal slices in vitro. Increases evoked excitatory postsynaptic currents (eEPSCs) in mice. Brain penetrant.

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Potent TMEM16A (Anoctamin-1) blocker
5770 | MONNA

IC50 = 80 nM. Exhibits >100-fold selectivity for TMEM16A over bestrophin-1, CLC2 and CFTR. Induces vasorelaxation of rodent resistance arteries in presence or absence of chloride ions.

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Selective noradrenalin and dopamine fluorescent indicator
5905 | Neurosensor 521

Exhibits selectivity over adrenalin, glycine and glutamate. Enables visualization of noradrenalin and dopamine in fixed and live cells. Excitation wavelength 488 nm, emission 521 nm.

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Selective myeloperoxidase (MPO) inhibitor
6004 | PF 06281355

IC50 = 1.5 μM in LPS-stimulated human whole blood. Selective for MPO over a panel of 50 receptors, enzymes, ion channels and transporters, including thyroid peroxidase. Inhibits MPO activity in peritoneal lavage and plasma in a murine peritonitis model. Also reduces lung edema in a murine pulmonary immune complex vasculitis model. Orally bioavailable.

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September 2016

High affinity and selective P2Y14 antagonist
4862 | PPTN

KB = 434 nM. Exhibits >10,000-fold selectivity for P2Y14 over other P2Y receptors. Inhibits UDP-glucose and MRS 2690-induced porcine pancreatic artery contraction ex vivo. Also blocks UDP-glucose-induced chemotaxis of HL-60 leukemia cells in vitro.

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Selective mIDH1 inhibitor; phenotypically lethal
5244 | TC-E 5008

Ki = 120-190 nM. Displays >60-fold selectivity for mIDH1 (found in ~75% of gliomas) over wild type IDH1. Also inhibits D-2-hydroxyglutaric acid in cells expressing mIDH1 (EC50 = 2.4 μM). Does not display cytotoxicity towards non-cancerous human cells. Phenotypically lethal.

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Potent cdk1/2 inhibitor
5654 | BMS 265246

IC50 values are 6, 9 and 230 nM for cdk1, cdk2 and cdk4, respectively. Inhibits proliferation of HCT-116 colon cancer cells in vitro.

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Potent and selective inhibitor of integrins αvβ3 and αvβ5
5870 | Cilengitide

IC50 values are 4.1 and 70 nM for αvβ3 and αvβ5, respectively. Exhibits ~10-fold selectivity over gpIIb/IIIa. Increases endothelial monolayer permeability. Also exhibits antiangiogenic activity.

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ADAM 17 (TACE) and MMP inhibitor; orally bioavailable
5960 | TMI 1

IC50 values are 3, 4.7, 6.6, 8.4, 12, 26 and 26 nM for MMP-13, MMP-2, MMP-1, ADAM 17, MMP-9, MMP-7 and MMP-14, respectively. Suppresses TNF-α production in an acute LPS-mouse model. Reduces severity score in an in vivo model of rheumatoid arthritis. Displays selective cytotoxicity towards tumor cells and cancer stem cells in vitro. Induces tumor apoptosis in a breast cancer in vivo model. Orally bioavailable.

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August 2016

Potent inhibitor of EGFR, ErbB2 and Abl receptor tyrosine kinases
4397 | AV 412

IC50 values are 0.5-2, 19 and 41 nM, respectively. Also weak inhibitor of FLT1 and Src. Inhibits EGFR and ErbB2 autophosphorylation in vitro in NSCLC and T-47D breast cancer cell lines, respectively. Inhibits tumor growth of EGFR-overexpressing A431 and ErbB2 overexpressing BT-474 tumor xenografts in mice.

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Potent P2Y12 antagonist; cell permeable
5650 | SAR 216471

IC50 = 17 nM. Displays antiplatelet and antithrombotic activity in vivo. Orally available.

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Potent and selective type I PRMT inhibitor
5713 | MS 023

IC50 values are 8, 8, 30, 83 and 119 nM for PRMT6, PRMT8, PRMT1, PRMT4 and PRMT3, respectively. Exhibits no significant activity against type II and III PRMTs, PKMTs, DNMTs, KDMs and reader proteins. Reduces global arginine asymmetric dimethylation levels in vitro.

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Selective tryptophan 2,3-dioxygenase (TDO) inhibitor
5794 | LM 10

IC50 values are 0.62 and 2 μM for human and mouse TDO, respectively. Exhibits selectivity for TDO over IDO, MAO-A, MAO-B, and a panel of receptors and transporters. Reduces growth of TDO-expressing P815 mastocytoma tumors in mice. Orally bioavailable.

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Potent microsomal prostaglandin E synthase 1 (mPGES-1) inhibitor
5917 | PF 9184

PIC50 values are 16.5 and 1080 nM for human and rat mPGES-1, respectively. Exhibits >6500-fold selectivity for mPGES-1 over COX-1 and COX-2. Inhibits IL-1β-induced PGE2 synthesis in vitro.

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July 2016

Potent and selective BRD9 and BRD7 inhibitor; orally active
5590 | BI 9564

Kd values are 14 and 239 nM, respectively. Exhibits selectivity for BRD9/7 over 48 other bromodomains, 324 kinases and 55 GPCRs. Inhibits proliferation of AML cell lines in vitro and reduces AML tumor xenograft growth in vivo. Cell permeable and orally active.

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Nrf2 activator; inhibits Nrf2/Keap1 interaction
5707 | RA 839

Kd = 6 μM. Suppresses LPS-induced iNOS and nitric oxide expression in macrophages. Anti-inflammatory.

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Potent and selective S1P5 agonist
5766 | A 971432

EC50 values are 4.1 and 5.7 nM in cAMP and GTPγS assays, respectively. Exhibits 60-fold selectivity over S1P1, and >1,600-fold selectivity over S1P2-4 and a panel of 129 kinases and 79 receptors. Improves blood-brain barrier integrity in vitro and reverses age-related cognitive decline in vivo. Orally available.

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Potent TNKS1/2 inhibitor
5775 | AZ 6102

IC50 values are 1 and 3 nM, respectively. Exhibits >100-fold selectivity for TNKS1/2 over PARP-1, PARP-2 and PARP-6. Inhibits Wnt signaling in DLD-1 cells (IC50 = 5 nM). Exhibits moderate oral bioavailability.

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Selective ASIC1a inhibitor; analgesic
5938 | Mambalgin 1

IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively. Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases latency of tail and paw withdrawal in mouse tail-flick and paw-flick tests. Analgesic.

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June 2016

High affinity and selective EP4 antagonist
5327 | BGC 20-1531

Ki = 3 nM. Exhibits >2500-fold selectivity for EP4 over EP2 and EP3. Also selective over a range of other prostanoid receptors, ion channels, transporters and enzymes. Inhibits PGE2-induced vasodilation of middle cerebral and meningeal arteries in vitro, and carotid blood flow in vivo. Orally bioavailable.

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High affinity and selective HNE1 inhibitor
5651 | ONO 6818

Ki =12 nM. Exhibits >100-fold less activity at other related proteases including trypsin, pancreatic elastase, collagenase and murine macrophage elastase. Inhibits NA-induced lung hemorrhaging and suppresses leukocyte levels in an in vivo model of COPD. Orally active.

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Oct3/4 inducer
5664 | O4I2

Promotes Oct3/4 expression and stabilizes the Oct3/4 protein in HEK293 cells. Induces expression of the pluripotent-associated genes Lin28, Sox2 and Nanog, and suppresses Rex1. Induces a 15-fold increase in Oct3/4 expression in human primary fibroblasts.

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LSD1 inhibitor
5714 | S 2101

IC50 = 990 nM; Ki = 610 nM. Exhibits selectivity for LSD1 over MAO-B and MAO-A (Ki values are 17 and 110 μM, respectively).

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Potent and selective PI 3-kinase β inhibitor
5832 | TGX 221

IC50 values are 0.007, 0.1, 3.5 and 5 μM for β, δ, γ and α isoforms, respectively. Shows >1,000-fold selectively for PI 3-kinase β over a range of other kinases. Inhibits thrombus formation in animal models.

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May 2016

Potent TBK1 inhibitor
5067 | MRT 68601

IC50 = 6 nM. Inhibits the formation of autophagosomes in lung cancer cells.

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Potent and selective SMYD2 inhibitor
5365 | LLY 507

IC50 = 15 nM. Exhibits >100-fold selectivity for SMYD2 over 25 other methyltransferases including SMYD3, SUV420H1 and SUV420H2. Also exhibits selectivity over a panel of GPCRs, nuclear receptors and cytochrome P450 enzymes. Inhibits SMYD2-mediated p53 methylation in vitro. Also inhibits proliferation of a range of esophageal, liver and breast cancer cell lines.

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Potent Nurr1 activator
5699 | IP7e

EC50 = 3.9 nM. Delays onset and reduces severity of symptoms in mice with experimental autoimmune encephalomyelitis (EAE). Also suppresses NF-κB signaling. Brain penetrant and orally bioavailable.

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High affinity and selective presynaptic CHT inhibitor
5725 | ML 352

Ki = 92 nM. Exhibits selectivity for CHT over dopamine, serotonin and noradrenaline transporters; acetylcholinesterase and cholineacetyltransferase; and a panel of 65 other GPCRs, ion channels and transporters.

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CXCR4 allosteric agonist
5795 | ATI 2341

EC50 = 194 nM. Induces chemotaxis in CXCR4-expressing cells in vitro. Mobilizes polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) from bone marrow niche in vivo. Exhibits biased signaling towards Gi proteins over G13 and β-arrestin.

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April 2016

Potent Chk2 inhibitor
4968 | CCT 241533

IC50 = 3 nM. Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes.

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High affinity and selective CB2 inverse agonist
5039 | SR 144528

Ki = 0.6 nM. Exhibits >700-fold selectivity for CB2 over CB1 receptors. Blocks the effects of CP 55,940 (Cat. No. 0949) on forskolin-sensitive adenylyl cyclase activity and MAPK in CHO cells expressing CB2 receptors. Also blocks CP 55,940-induced B-cell activation. Orally bioavailable.

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Potent and selective CXCR2 antagonist
5660 | NVP CXCR2 20

IC50 = 40 nM. Exhibits selectivity for CXCR2 over a panel of 49 other GPCRs. Orally bioavailable.

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Potent and selective GPR139 agonist
5666 | JNJ 63533054

EC50 = 16 nM. Selective for GPR139 over a panel of GPCRs, ion channels and transporters, including GPR142. Brain and cell penetrant. Orally bioavailable.

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Selective CBP/p300 bromodomain inhibitor
5801 | PF CBP1

IC50 values are 125 and 363 nM for CBP and p300, respectively. Exhibits >100-fold selectivity for CBP over BRD4. Also exhibits selectivity over a panel of other bromodomains. Reduces LPS-induced IL-1β, IL-6 and IFN-β expression in macrophages in vitro. Also downregulates RGS4 expression in primary cortical neurons in vitro.

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March 2016

Potent and selective breast tumor kinase (Brk) inhibitor
5579 | Tilfrinib

IC50 = 3.15 nM. Exhibits >1000-fold selectivity for Brk over a panel of other kinases. Inhibits proliferation of breast cancer cells in vitro.

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Potent and selective dual mTORC1 and 2 inhibitor
5615 | AZD 3147

IC50 = 1.5 nM. Exhibits >300-fold selectivity for mTOR over PI 3-kinase isoforms. Orally bioavailable.

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Potent LXR antagonist
5694 | GSK 2033

pIC50 = 7.5. Enhances T-cell proliferation and blocks T 0901317-antiproliferative activity on T-cells. Cell permeable.

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Potent γ-secretase inhibitor
5751 | PF 3084014

IC50 values are 1.2 and 6.2 nM in whole cell and cell-free assays, respectively. Reduces Aβ in brain, CSF and plasma in mice and guinea pigs.

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High affinity 15-PGDH inhibitor
5759 | SW 033291

Ki = 0.1 nM. Increases PGE2 levels in A549 cells in vitro, as well as in bone marrow, colon, lung and liver in mice. Promotes hematopoiesis, recovery from DSS-induced colitis, and hepatocyte proliferation after partial hepatectomy in mice.

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February 2016

Potent and selective GRK2/3 inhibitor
5642 | CMPD101

Potent and selective GRK2/3 inhibitor (IC50 values are 32 and 54 nM for GRK3 and GRK2, respectively). Exhibits selectivity for GRK2/3 over GRK1/5. Reduces DAMGO-induced desensitization and internalization of μ-opioid receptors.

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OX2 receptor antagonist; orally bioavailable
5645 | IPSU

OX2 receptor antagonist. Exhibits approximately six-fold selectivity for OX2 versus OX1 receptors. Decreases activity and increases sleep time in mice during the active phase, without affecting REM/NREM balance. Orally bioavailable. Brain penetrant.

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Potent and selective HDAC2/3 inhibitor
5647 | MI 192

Potent and selective HDAC2/3 inhibitor (IC50 values are 16 and 30 nM, respectively). Exhibits >250-fold selectivity for HDAC2/3 over other HDAC isoforms. Promotes apoptosis of leukemia cell lines in vitro. Also attenuates IL-6 production in rheumatoid arthritis PBMCs in vitro.

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Potent FXR antagonist
5656 | DY 268

Potent FXR antagonist (IC50 = 7.5 nM). Exhibits no detectable cytotoxicity in cell-based assays.

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MAP4K4 (HGK) inhibitor
5752 | PF 06260933

MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active.

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January 2016

Potent stearoyl-CoA desaturase 1 inhibitor
4845 | A 939572

IC50 = 0.4 nM. Selective for SCD1 over a range of kinases and hERG channels. Inhibits proliferation of squamous cell carcinoma FaDu cells in vitro. Also induces cell death of undifferentiated human embryonic stem cells (ESCs). Orally bioavailable.

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Potent and selective NHE1 inhibitor
5512 | BIX NHE1 inhibitor

IC50 = 31 nM. Selective for NHE1 over NHE2 and NHE3. Prevents ischemic damage in an ischemia reperfusion injury isolated rat heart model ex vivo. Prevents phenylephrine-induced cardiomyocyte hypertrophy in vitro, and attenuates cardiac hypertrophy and left ventricular dysfunction postinfarction in rats. Orally bioavailable.

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Potent and selective PERK inhibitor
5517 | AMG PERK 44

IC50 = 6 nM. Exhibits >160-fold selectivity for PERK over B-Raf and GCN2, as well as a panel of 387 other kinases. Orally bioavailable.

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Selective BAZ2A and BAZ2B inhibitor
5635 | GSK 2801

IC50 values are 0.40 and 0.43 μM, respectively. Selective for BAZ2A/B over TAF1L and BRD9. Cell permeable and orally available.

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Potent LRRK2 inhibitor; neuroprotective
5716 | PF 06447475

IC50 = 3 nM. Attenuates α-synuclein-induced dopaminergic neurodegeneration and neuroinflammation in G2019S-LRRK2 expressing rats. Also neuroprotective in wild type rats. Brain penetrant.

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