A dynein 1 and dynein 2 inhibitor
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Dynapyrazole-A

Item No. 45370

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[1-(4-chlorophenyl)cyclopropyl]-4,5-dihydro-7-iodo-5-oxo-pyrazolo[1,5-a]quinazoline-3-carbonitrile
CAS Number
2226517-75-3
Molecular Formula
C20H12ClIN4O
Formula Weight
486.7
Purity
≥95%
Formulation (Request formulation change)
A solid
SMILES
N#CC(C(C1(CC1)C2=CC=C(C=C2)Cl)=NN3C4=CC=C(C=C45)I)=C3NC5=O
InChi Code
InChI=1S/C20H12ClIN4O/c21-12-3-1-11(2-4-12)20(7-8-20)17-15(10-23)18-24-19(27)14-9-13(22)5-6-16(14)26(18)25-17/h1-6,9H,7-8H2,(H,24,27)
InChi Key
VABPBCMFKJDOHP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $75

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    10 mg

    $143

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    25 mg

    $300

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    50 mg

    $525

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    Product Description

    Dynapyrazole-A is an inhibitor of the motor proteins dynein 1 and dynein 2.1 It inhibits the microtubule-stimulated ATPase activity of dynein but not its basal microtubule-independent activity. Dynapyrazole-A inhibits dynein 1- and dynein 2-mediated microtubule gliding in a cell-free assay (IC50s = 2.3 and 2.6 µM, respectively). It also inhibits hedgehog pathway stimulation induced by SAG (Item No. 11914) in a reporter assay using NIH3T3 cells (IC50 = 1.9 µM). Dynapyrazole-A (10 µM) reversibly reduces the speed of intraflagellar retrograde and, to a lesser extent, anterograde transport in mouse inner medullary collecting duct (mIMCD-3) cells. It also reduces lysosomal transport in catecholamine A-differentiated (CAD) cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Steinman, J.B., Santarossa, C.C., Miller, R.M., et al. Chemical structure-guided design of dynapyrazoles, cell-permeable dynein inhibitors with a unique mode of action. Elife 6, e25174 (2017).