For the song, Tupac Shakur recruited the members of the former group Dramacydal whom he had worked with previously, and was eager to work with again. 'Hit 'Em Up' was written and recorded at Can-Am studios in late 1995. The song is widely regarded as among the greatest diss tracks ever recorded.

The controversy surrounding the song is due in part to Shakur's murder in a drive-by-shooting only three months after its release. Following its release, the East Coast rappers insulted in the song responded through tracks of their own. 'Hit 'Em Up' had a large role in exacerbating the East Coast–West Coast hip hop rivalry. The video, itself described as infamous, includes impersonations of Biggie, Puffy and M.A.F.I.A.

Reporter Chuck Philips, who interviewed Shakur at Can Am, described the song as 'a caustic anti–East Coast jihad in which the rapper threatens to eliminate Biggie, Puff, and a slew of Bad Boy artists and other New York acts.' The song was produced by long-time collaborator Johnny 'J'. A previous version of the song was recorded in October 1995. The song was recorded at Can Am Studios in 1996. (also referred to colloquially as Biggie Smalls). The song's lyrics contain vicious insults to several East Coast rappers, chiefly Shakur's former friend turned rival, the Notorious B.I.G. It is the B-side to the single ' How Do U Want It', released on June 4, 1996. ' Hit 'Em Up' is a diss track by hip hop artist 2Pac, featuring the Outlawz.

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