A MLK inhibitor
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URMC-099

Item No. 19147

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(1H-indol-5-yl)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridine
CAS Number
1229582-33-5
Molecular Formula
C27H27N5
Formula Weight
421.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 1 mg/ml
λmax
211, 244, 267 nm
SMILES
CN1CCN(CC2=CC=C(C3=CC(C(C4=CC=C(NC=C5)C5=C4)=CN6)=C6N=C3)C=C2)CC1
InChi Code
InChI=1S/C27H27N5/c1-31-10-12-32(13-11-31)18-19-2-4-20(5-3-19)23-15-24-25(17-30-27(24)29-16-23)21-6-7-26-22(14-21)8-9-28-26/h2-9,14-17,28H,10-13,18H2,1H3,(H,29,30)
InChi Key
QKKIWEILHCXECO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $66

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    10 mg

    $109

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    25 mg

    $179

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    Product Description

    URMC-099 is an orally bioavailable, brain-penetrant inhibitor of mixed-lineage kinases (MLKs) with IC50 values of 19, 42, 14, and 150 nM for MLK1, MLK2, MLK3, and the related MLK family member DLK, respectively.1 It also inhibits LRRK2 activity with an IC50 value of 11 nM.1 In vitro, URMC-099 has been shown to reduce inflammatory cytokine production by HIV-1 Tat-exposed microglia and to prevent destruction and phagocytosis of cultured neuronal axons by these cells.2 In rodent models of HIV-associated neurocognitive disorders, URMC-099 demonstrates anti-inflammatory and neuroprotective effects.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Quadro, L., Blaner, W.S., Salchow, D.J., et al. Impaired retinal function and vitamin A availability in mice lacking retinol-binding protein. EMBO J. 18(17), 4633-4644 (1999).

    2. Marker, D.F., Tremblay, M.É., Puccini, J.M., et al. The new small-molecule mixed-lineage kinase 3 inhibitor URMC-099 is neuroprotective and anti-inflammatory in models of human immunodeficiency virus-associated neurocognitive disorders. J. Neurosci. 33(24), 9998-10010 (2013).