A peptide inhibitor of NTMT1
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DC432 (trifluoroacetate salt)

Item No. 36980

Technical Information
Formal Name
(S)-N-1,28-diamino-6S-carbamoyl-9S,12S,15S,18S,21S-pentakis(3-guanidinopropyl)-1-imino-8,11,14,17,20,23-hexaoxo-2,7,10,13,16,19,22-heptaazaoctacosan-24S-yl)-1-(2-(4-hydroxyphenyl)acetyl)pyrrolidine-2-carboxamide, trifluoroacetate salt
Molecular Formula
C55H100N28O10 • XCF3COOH
Formula Weight
Purity
≥98%
A solid
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 2 mg/mlPBS (pH 7.2): 2 mg/ml
SMILES
N=C(N)NCCC[C@@H](C(N)=O)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC([C@H](CCCCN)NC([C@H]1N(CCC1)C(CC2=CC=C(C=C2)O)=O)=O)=O)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C55H100N28O10.C2HF3O2/c56-22-2-1-10-34(82-49(93)40-17-9-29-83(40)41(85)30-31-18-20-32(84)21-19-31)44(88)78-36(13-5-25-72-52(62)63)46(90)80-38(15-7-27-74-54(66)67)48(92)81-39(16-8-28-75-55(68)69)47(91)79-37(14-6-26-73-53(64)65)45(89)77-35(12-4-24-71-51(60)61)43(87)76-33(42(57)86)11-3-23-70-50(58)59;3-2(4,5)1(6)7/h18-21,33-40,84H,1-17,22-30,56H2,(H2,57,86)(H,76,87)(H,77,89)(H,78,88)(H,79,91)(H,80,90)(H,81,92)(H,82,93)(H4,58,59,70)(H4,60,61,71)(H4,62,63,72)(H4,64,65,73)(H4,66,67,74)(H4,68,69,75);(H,6,7)/t33-,34-,35-,36-,37-,38-,39-,40-;/m0./s1
InChi Key
JZKDMDBVSPMBEJ-HVJIRRSLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    DC432 is a cell-permeable peptide inhibitor of N-terminal Xaa-Pro-Lys N-methyltransferase 1 (NTMT1; IC50 = 0.054 µM).1 It binds to NTMT1 and NTMT2 (Kds = 0.3 and 1 µM, respectively) and inhibits N-terminal dimethylation of regulator of chromosome condensation 1 (RCC1) by NTMT1 in a cell-free assay when used at concentrations of 10 and 50 µM. DC432 (100 µM) reduces trimethylation of the RCC1 SPKRIA motif in HCT116 cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mackie, B.D., Chen, D., Dong, G., et alSelective peptidomimetic inhibitors of NTMT1/2: Rational design, synthesis, characterization, and crystallographic studies. J. Med. Chem. 63(17), 9512-9522 (2020).