OK2

• CAT Number: I040976
• Molecular Formula: C42H62N14O9
• Molecular Weight: 907.03
• Purity: ≥95%
• Synonyms: 2-[3-[(3S,6S,9S,12S,15S,18S,21S)-9-(4-aminobutyl)-12,15-bis[(1R)-1-hydroxyethyl]-6-(1H-imidazol-5-ylmethyl)-18-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazabicyclo[19.3.0]tetracosan-3-yl]propyl]guanidine
• InChI: InChI=1S/C42H62N14O9/c1-22(57)33-39(63)50-28(11-5-6-14-43)35(59)52-31(18-25-20-46-21-49-25)36(60)51-29(12-7-15-47-42(44)45)41(65)56-16-8-13-32(56)38(62)53-30(37(61)54-34(23(2)58)40(64)55-33)17-24-19-48-27-10-4-3-9-26(24)27/h3-4,9-10,19-23,28-34,48,57-58H,5-8,11-18,43H2,1-2H3,(H,46,49)(H,50,63)(H,51,60)(H,52,59)(H,53,62)(H,54,61)(H,55,64)(H4,44,45,47)/t22-,23-,28+,29+,30+,31+,32+,33+,34+/m1/s1
• InChIKey: DNITVPPEDHWZSB-MLYITYKWSA-N
• SMILES: CC(C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)N1)CC3=CNC4=CC=CC=C43)CCCN=C(N)N)CC5=CN=CN5)CCCCN)C(C)O)O

OK2, a specific inhibitor of the CCN2/EGFR interaction, efficiently blocks CCN2/EGFR interaction through binding to the CT domain of CCN2. OK2 can be used for kidney fibrosis and chronic kidney disease research[1].
OK2 (0-100 μM; 24 hours) inhibits EGFR activation, STAT3 phosphorylation, and ECM protein synthesis in HK-2 cells[1].
OK2 (50 μg/kg, i.p., for 14 days) blocks CCN2-induced EGFR/STAT3 activation and impede kidney fibrosis in the unilateral ureteric obstruction (UUO) mice model[1].
OK2 (1 mg/kg, s.c.) shows a T1/2 of 0.9 h and Cmax of 1057.8 ng/mL in male Sprague Dawley rats[1].
Pharmacokinetic parameters for OK2 in male Sprague Dawley rats [1]

Route
Dose (mg/kg)
Cmax (ng/mL)
Tmax (h)
T1/2 (h)
AUC0-t (h•ng/mL)

s.c.
1
1057.8
1.0
0.9
3032.0

Reference

[1]. Dong J, et.al. Discovery and Design of Novel Cyclic Peptides as Specific Inhibitors Targeting CCN2 and Disrupting CCN2/EGFR Interaction for Kidney Fibrosis Treatment. J Med Chem. 2023 Jun 22;66(12):8251-8266.
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