125313-92-0

125313-92-0 structure

Name: MKC-1
Chemical Name: 3-(1-methylindol-3-yl)-4-(1-methyl-6-nitroindol-3-yl)pyrrole-2,5-dione
CAS Number: 125313-92-0
Molecular Formula: C₂₂H₁₆N₄O₄
Molecular Weight: 400.38700
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2017-12-29 08:39:05
Modify Date: 2025-08-25 19:25:57
MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family[1][2][3].

Name	3-(1-methylindol-3-yl)-4-(1-methyl-6-nitroindol-3-yl)pyrrole-2,5-dione
Synonyms	MKC-1 UNII-DNZ11VPY7Q Bisindolylmaleimide deriv. 44 3-(1-methyl-3-indolyl)-4-(1-methyl-6-nitro-3-indolyl)-1H-pyrrole-2,5-dione Ro-31-7453

Description	MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family[1][2][3].
Related Catalog	Signaling Pathways >> PI3K/Akt/mTOR >> mTOR Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin Signaling Pathways >> PI3K/Akt/mTOR >> Akt Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin
In Vivo	MKC-1 (200 mg/kg, orally, daily) significantly increased the median survival time (MST) of mice bearing Caki-1 renal cell xenograft tumors[3].
References	[1]. Wang M, et al. The first design and synthesis of [11C]MKC-1 ([11C]Ro 31-7453), a new potential PET cancer imaging agent. Nucl Med Biol. 2010 Oct;37(7):763-75. [2]. Faris JE, et al. A phase 2 study of oral MKC-1, an inhibitor of importin-β, tubulin, and the mTOR pathway in patients with unresectable or metastatic pancreatic cancer. Invest New Drugs. 2012 Aug;30(4):1614-20. [3]. Burke P, et al. MKC-1 significantly increases survival of mice bearing renal cell carcinoma Caki-1 xenograft tumors through inhibition of the Akt/mTOR pathway[J]. Molecular Cancer Therapeutics, 2007(12):3524S-3525S.