The present invention, among other things, provides compounds and compositions thereof for use in the modulation of Hsp70. In some embodiments, the present invention provides a method for inhibiting Hsp70 activity. In some embodiments, the present invention provides a method of treating a subject suffering from or susceptible to a disease, disorder, or condition responsive to Hsp70 inhibition comprising administering to the subject a therapeutically effective amount of a provided compound. In some embodiments, the present invention provides a method for treating or preventing cancer in a subject suffering therefrom, comprising administering to a patient in need thereof a therapeutically effective amount of a provided compound.本發明尤其提供用於調節Hsp70之化合物及其組合物。在一些實施例中,本發明提供一種抑制Hsp70活性之方法。在一些實施例中,本發明提供一種治療患有或易患對Hsp70抑制起反應之疾病、病症或病狀之個體的方法,其包含投與該個體治療有效量之所提供化合物。在一些實施例中,本發明提供一種治療或預防罹患癌症之個體的癌症的方法,其包含投與有需要之患者治療有效量之所提供化合物。