HW02, a pyruvate dehydrogenase inhibitor, is a newly developed herbicide for broadleaf weed control in wheat, maize and turf in China. Greenhouse and field experiments were conducted to evaluate its efficacy against weeds and safety to winter wheat. In the greenhouse experiment, this herbicide had higher activities than 2,4-D against Descurainia sophia (L.) Schur., Amaranthus retroflexus L., Capsella bursa-pastoris (L.) Medic., and Malachium aquaticum (L.) Fries.. When it was applied at late tillering stage of winter wheat in spring, the herbicide provided weed biomass reduction of 98%–100% at the rates 225–525 g a.i. ha−1 and was safe to the crop at the rate of up to 900 g a.i. ha−1. These results showed HW02 could be an alternative herbicide for resistant weed management because its mode of action is different from herbicides presently used.