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Chemical Structure| 1417329-24-8 Chemical Structure| 1417329-24-8

Structure of MM-102
CAS No.: 1417329-24-8

Chemical Structure| 1417329-24-8

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MM-102 is a high-affinity peptidomimetic MLL1 inhibitor with IC50 of 0.4 μM in a cell-free assay.

Synonyms: HMTase Inhibitor IX

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Product Details of MM-102

CAS No. :1417329-24-8
Formula : C35H49F2N7O4
M.W : 669.80
SMILES Code : O=C(C1(NC([C@@H](NC(C(NC(C(C)C)=O)(CC)CC)=O)CCCNC(N)=N)=O)CCCC1)NC(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3
Synonyms :
HMTase Inhibitor IX
MDL No. :MFCD28015099

Safety of MM-102

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of MM-102

epigenetics

Isoform Comparison

Biological Activity

Target
  • Histone Methyltransferase

    MLL1, IC50:0.4 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Recombinant H3 protein 1.6 µM 2 hours To study the inhibitory effect of MM-102 on MLL1 methyltransferase activity. Results showed that MM-102 efficiently inhibited the activity of wild-type MLL1, but had no inhibitory effect on the R3864C and R3841W mutants. Mol Oncol. 2017 Apr;11(4):373-387.
Primary chondrocytes 20 µM 24 hours MM-102 pretreatment effectively rescued the negative impact of FSS on chondrocytes, which may lay a foundation of epigenetic-based therapy on OA. J Inflamm Res. 2021 Nov 19;14:6067-6083.
HEK293 cells 0.8 µM 3 hours To study the interaction of MLL1 with the WRA complex and its methyltransferase activity. Results showed that MLL1 activity was significantly enhanced in the presence of the WRA complex. Mol Oncol. 2017 Apr;11(4):373-387.
MV4;11 cells 25 µM, 50 µM 7 days MM-102 dose-dependently inhibits cell growth in the MV4;11 and KOPN8 leukemia cell lines, completely inhibiting cell growth at 75 μM. J Am Chem Soc. 2013 Jan 16;135(2):669-82.
K562 cells 50 µM, 75 µM 7 days In the K562 leukemia cell line, MM-102 has no significant effect at 50 μM and only minimal effect at 75 μM. J Am Chem Soc. 2013 Jan 16;135(2):669-82.
RA synovial fibroblasts 300 pM 72 hours To investigate the effect of MM-102 on H3K4me3 and mRNA levels in RA synovial fibroblasts, the results showed that MM-102 significantly reduced H3K4me3 and mRNA levels of CCL5, CXCL9, CXCL10, and CXCL11 genes. Sci Rep. 2024 May 9;14(1):10610.
Bovine embryonic stem cells (bESCs) 50 µM MLL1 inhibition improved the pluripotency and differentiation potential of bESCs via the up-regulation of stem cell signaling pathways such as PI3K-Akt and WNT. Int J Mol Sci. 2023 Jul 25;24(15):11901.
TFK1 cells 50 µM MM-102 inhibited the expression of ABCB1 in CCA cells and decreased the chemoresistance of CCA to cisplatin. J Exp Clin Cancer Res. 2024 Sep 30;43(1):272.
RBE cells 50 µM MM-102 inhibited the expression of ABCB1 in CCA cells and decreased the chemoresistance of CCA to cisplatin. J Exp Clin Cancer Res. 2024 Sep 30;43(1):272.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Primary CCA mouse model Intraperitoneal injection 15 mg/kg Once daily for 7 days MM-102 significantly suppressed the proliferation, migration and chemoresistance of CCA cells, increasing the sensitivity of CCA to cisplatin. J Exp Clin Cancer Res. 2024 Sep 30;43(1):272.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.49mL

0.30mL

0.15mL

7.46mL

1.49mL

0.75mL

14.93mL

2.99mL

1.49mL

References

 

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