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KCC-07

  Cat. No.:  DC72487   Featured
Chemical Structure
315702-75-1
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More than 5000 active chemicals with high quality for research!
Field of application
KCC-07 is a potent, selective and brain-penetrant inhibitor of MBD2 (methyl-CpG-binding domain protein 2) with anticancer activity. It prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling.
Cas No.: 315702-75-1
Chemical Name: 3-{[4-(2-Pyridinyl)-1,3-thiazol-2-yl]amino}phenol
Synonyms: 3-{[4-(pyridin-2-yl)-1,3-thiazol-2-yl]amino}phenol;CBMicro_027305;Oprea1_718651;KCC 07;BDBM158506;NSC752630;US9034574, II;ST50028583;3-[[4-(2-Pyridinyl)-2-thiazolyl]amino]phenol;3-[(4-(2-pyridyl)-1,3-thiazol-2-yl)amino]phenol;3-{[4-(2-pyridinyl)-1,3-thiazol-2-yl]amino}phenol;3-(4-Pyridin-2-yl-thiazol-2-ylamino)-phenol;NS-04313;KCC-07
SMILES: S1C=C(C2C=CC=CN=2)N=C1NC1C=CC=C(C=1)O
Formula: C14H11N3Os
M.Wt: 269.321641206741
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: KCC-07 is a potent, selective and brain-penetrant inhibitor of MBD2 (methyl-CpG-binding domain protein 2) with anticancer activity. It prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling.
Target: MBD2 (methyl-CpG-binding domain protein 2)[1]
In Vivo: KCC-07 (100 mg/kg; intraperitoneal injection; 5 days/week; athymic nude mice) treatment inhibits tumor growth and significantly extends the survival of MB xenografts in vivo[1]. Animal Model: Outbred athymic nude mice (females; 8-10 weeks old) injected with MB cells[1] Dosage: 100 mg/kg Administration: Intraperitoneal injection; 5 days/week Result: Significantly extended the survival of MB xenografts in vivo.
In Vitro: KCC-07 (10 μM; 72 hours; MB cells) treatment clearly inhibited MB cell growth in vitro, consistent with induction of anti-proliferative BAI1/p53/p21 signaling[1]. KCC-07 (10 μM; 48 hours; MB cells) treatment largely abrogates MBD2 binding to the ADGRB1 promoter and restores BAI1 mRNA and protein expression in BAI1-silent MB cells[1]. Cell Viability Assay[1] Cell Line: Medulloblastomas (MB) cells Concentration: 10 μM Incubation Time: 72 hours Result: Clearly inhibited MB cell growth in vitro. Western Blot Analysis[1] Cell Line: Medulloblastomas (MB) cells Concentration: 10 μM Incubation Time: 48 hours Result: Largely abrogated MBD2 binding to the ADGRB1 promoter in BAI1-silent MB cells.
References: [1]. Dan Zhu, et al. BAI1 Suppresses Medulloblastoma Formation by Protecting p53 From Mdm2-Mediated Degradation. Cancer Cell. 2018 Jun 11;33(6):1004-1016.e5.
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