DHTP is a kinesin-13 family of microtubule depolymerases selective allosteric inhibitor that inhibits kinesin-13 ATPase activity and microtubule depolymerization activity. DHTP inhibits Kif2a and MCAK with IC50 values of 1.2 μM and 4.6 μM, respectively, and does not inhibit other kinesin families. DHTP modulates microtubule dynamics in cells, leading to less dynamic microtubules. DHTP links kinesin-13 overexpression to cancer and Paclitaxel resistance. DHTP can be used for the research of cancer [1].
In Vitro, DHTP (0.01-100 μM) inhibits kinesin-13 ATPase activity selectively (IC50 MCAK=4.6 μM, Kif2a=1.2 μM)[1]. DHTP (5 μM, 10 μM, 20 μM) selectively reduces MCAK-induced microtubule depolymerization rate (74% at 5 μM, 89% at 10 μM) without affecting Eg5-driven gliding[1]. DHTP (10 μM; 15-20 minutes post-treatment) modulates microtubule dynamics in Drosophila S2 cells, increasing pause time and persistent growth while reducing catastrophe frequency[1].
References:
[1]. Talje L, et al. DHTP is an allosteric inhibitor of the kinesin-13 family of microtubule depolymerases. FEBS Lett. 2014;588(14):2315-2320.
In Vitro, DHTP (0.01-100 μM) inhibits kinesin-13 ATPase activity selectively (IC50 MCAK=4.6 μM, Kif2a=1.2 μM)[1]. DHTP (5 μM, 10 μM, 20 μM) selectively reduces MCAK-induced microtubule depolymerization rate (74% at 5 μM, 89% at 10 μM) without affecting Eg5-driven gliding[1]. DHTP (10 μM; 15-20 minutes post-treatment) modulates microtubule dynamics in Drosophila S2 cells, increasing pause time and persistent growth while reducing catastrophe frequency[1].
References:
[1]. Talje L, et al. DHTP is an allosteric inhibitor of the kinesin-13 family of microtubule depolymerases. FEBS Lett. 2014;588(14):2315-2320.