A spastin inhibitor
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Spastazoline

Item No. 43034

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[5-(1,1-dimethylethyl)-1H-pyrazol-3-yl]-2-[(3R)-3-(1-methylethyl)-1-piperazinyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
CAS Number
2351882-11-4
Molecular Formula
C20H30N8
Formula Weight
382.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥ 10 mg/mlEthanol: Soluble: ≥ 10 mg/ml
SMILES
CC(C)[C@@H](NCC1)CN1C2=NC(NC3=NNC(C(C)(C)C)=C3)=C4C(NC=C4)=N2
InChi Code
InChI=1S/C20H30N8/c1-12(2)14-11-28(9-8-21-14)19-24-17-13(6-7-22-17)18(25-19)23-16-10-15(26-27-16)20(3,4)5/h6-7,10,12,14,21H,8-9,11H2,1-5H3,(H3,22,23,24,25,26,27)/t14-/m0/s1
InChi Key
HNOLTAKAPDKZRY-AWEZNQCLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    5 mg

    $152

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    10 mg

    $273

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    50 mg

    $835

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    100 mg

    $1,367

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    Product Description

    Spastazoline is an inhibitor of spastin (IC50 = 99 nM for the human enzyme).1 It is selective for spastin over a panel of 64 kinases but does inhibit tropomyosin-related kinase A (TrkA) by 65% at 2 µM. Spastazoline (10 µM) increases the number of cells with intracellular bridges during cell division, indicating microtubule stabilization, in HeLa cells expressing the recombinant human M87 isoform of spastin that contains the alternatively spliced exon 4 (M87e4). It inhibits neurite outgrowth in primary mouse hippocampal neurons when used at concentrations of 1 and 5 µM. Spastazoline (20 mg/kg, i.p.) increases spinal cord injury-induced motor impairments in mice, but it does not affect motor function in sham mice.2 It also delays spinal cord inflammation resolution in the same mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cupido, T., Pisa, R., Kelley, M.E., et al. Designing a chemical inhibitor for the AAA protein spastin using active site mutations. Nat. Chem. Biol. 15(5), 444-452 (2019).

    2. Yang, J., Zhang, Y., Cai, Z., et al. Inhibition of spastin impairs motor function recovery after spinal cord injury. Brain Res. Bull. 205, 110806 (2023).