MM-102 (HMTase Inhibitor IX)

카탈로그 번호S7265 배치:S726501

인쇄

기술 자료

화학식

C35H49F2N7O4
분자량 669.8 CAS 번호 1417329-24-8
용해도 (25°C)* 시험관 내(In vitro) DMSO 100 mg/mL (149.29 mM)
Ethanol 100 mg/mL (149.29 mM)
Water 50 mg/mL (74.64 mM)
생체 내(In Vivo) (개별적으로 순서대로 용매를 제품에 첨가하십시오.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Selleck 연구소에서 검증했습니다. 이 제형에 대한 조정이 필요한 경우 맞춤형 테스트를 위해 당사 영업팀에 문의하십시오.

 5.000mg/ml (7.46mM)
5% DMSO 95% Corn oil

Selleck 연구소에서 검증했습니다. 이 제형에 대한 조정이 필요한 경우 맞춤형 테스트를 위해 당사 영업팀에 문의하십시오.

 0.830mg/ml (1.24mM)
* <1 mg/ml은 약간 용해되거나 불용해됨을 의미합니다.
* Selleck은 모든 화합물의 용해도를 자체적으로 테스트하며, 실제 용해도는 게시된 값과 약간 다를 수 있습니다. 이는 정상적인 현상이며, 약간의 배치 간 변동으로 인해 발생합니다.
* 실온 배송 (안정성 테스트 결과 이 제품은 냉각 조치 없이 배송될 수 있음을 보여줍니다.)

원액 준비

생물학적 활성

설명 MM-102 (HMTase Inhibitor IX) is a high-affinity peptidomimetic inhibitor of the WDR5/MLL1 protein-protein interaction, which bind to WDR5 with Ki < 1 nM and IC50 =2.4nM.This product may precipitate when dissolved in saline solution or PBS solution. It is recommended to prepare the stock solution in DMSO solution.
표적
WDR5
(Cell-free assay)
2.4 nM
시험관 내(In vitro) MM-102, as a MLL1 mimetic, shows high binding affinities to WDR5 with IC50 of 2.9 nM and Ki of < 1 nM. In the MLL1-AF9 transduced murine cells, this compound specifically reduces expression of two critical MLL1 target genes (HoxA9 and Meis-1), which are required for MLL1 mediated leukemogenesis. In addition, it effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins.

프로토콜 (참조)

키나아제 분석:

[1]
  • In Vitro Histone Methyltransferase (HMT) Assay

    The HMT assay is performed in 50 mM HEPES pH 7.8, 100 mM NaCl, 1.0 mM EDTA, and 5% glycerol at 22 °C. Each reaction contains 1.5 μCi of the co-factor, 3H-S-adenosylmethionine. H3 10-residue peptide is used as the substrate at 50 μM. This compound is added at concentrations ranging from 0.125 to 128 μM and incubated with the pre-assembled WDR5/RbBP5/ASH2L complex at a final concentration of 0.5 μM for each protein for 2–5 min. Reactions are initiated by addition of the MLL1 protein at a final concentration of 0.5 μM and allowed to proceed for 30 min before preparing scintillation counting. To count samples, reactions are spotted on separate squares of P81 filter paper and precipitated by submerging in freshly prepared 50 mM sodium bicarbonate buffer with pH 9.0. After washing and drying, samples are vortexed in Ultima Gold scintillation fluid and counted. As a negative control, assays are performed using 0.5 μM MLL1/WDR5/RbBP5/ASH2L complex assembled with the non-interacting mutant, WDR5D107A.
세포 분석:

[1]
  • 세포주

    MV4;11, KOPN8, and K562 cells

  • 농도

    ~100 μM

  • 배양 시간

    7 days

  • 방법

    MV4;11, KOPN8, and K562 cells are cultured in RPMI 1640 medium (ATCC) supplemented with 10% fetal bovine serum and 100 U/L penicillin-streptomycin and incubated at 37 °C under 5% CO2. Cells are seeded into 12-well plates for suspension at a density of 5 × 105 per well (1 mL) and treated with either vehicle control (DMSO, 0.2%) or MM-102 for 7 days. The medium is changed every 2 days, and this compound is resupplied. The CellTiter-Glo Luminescent Cell Viability Assay kit is used following the manufacturer’s instruction. First, 100 μL of the assay reagent is added into each well, and the content is mixed for 2 min on an orbital shaker to induce cell lysis. After 10 min incubation at room temperature, the luminescence is read on a microplate reader.

참조

  • https://pubmed.ncbi.nlm.nih.gov/23210835/

고객 제품 검증

Immunofluorescence staining of H3K4me2/3 (red) in the IVF, SCNT and MM-102-NT embryos. The nuclei (blue) were stained with DAPI. The merged images of H3K4me2/3 and DNA were purple. Scale bars: 50 μm.

데이터 출처 [ , , Cell Physiol Biochem, 2018, 45(4):1529-1540 ]

(D) ChIP-qPCR analysis of the H3K4me3 levels in hESCs synchronized in mitosis with or without MLL1/2 inhibitors. DMSO, cells treated with DMSO only; Noc, cells blocked in mitosis with nocodazole; Noc + MLL Inh, cells blocked in mitosis with nocodazole in the presence of Mi-2 and MM-102 (20 μM each). Values for percent input are normalized to the IgG control (n = 2). One-way analysis of variance followed by Tukey−2; ****, P < 10−5; ns, not significant. (E) Reverse transcription-qPCR analysis of RNA expression levels for bivalent genes after induction of differentiation in unsynchronized H9 ES cells pretreated with MLL inhibitors. Differentiation was induced using E6 medium containing 1 μM RA per 24 h. DMSO, cells pretreated with DMSO only; MLL Inh, cells pretreated with Mi-2 and MM-102 (20 μM each) for 24 h. Unpaired parametric t test with Welch's corrections was performed. Two-tailed P values were calculated. *, P < 10−2; **, P < 10−3; ***, P < 10−4; ns, not significant. Log2 RNA levels were normalized against HPRT1 RNA levels and expressed as fold change between undifferentiated and differentiated cells.'/>

데이터 출처 [ , , Mol Cell Biol, 2015, 36(4):615-27 ]

(d-e) The viability of cells treated with cisplatin and MM-102 for 24h in concentrations as indicated was determined CCK-8 assay.

데이터 출처 [ , , Int J Biol Sci, 2018, 14(9):1122-1132 ]

NHMCs were incubated 24 h in 5.6 (white bars) or 25 mM glucose (black bars) in the presence or absence of TSA (200 nM) or MM-102 (50 μM) as indicated. mRNA was extracted from the cells after incubation and SPP1 expression was quantified by qPCR and normalized to housekeeping genes HPRT and PPIb expression. The values represent the mean ± SEM of five to eleven independent experiments. *p < 0.05, ***p < 0.001 vs. 5.6 mM glucose without inhibitors; yp < 0.05 vs. 25 mM glucose without inhibitors.

데이터 출처 [ , , Biochem Biophys Res Commun, 2016, 469(1):108-13 ]

Selleck's MM-102 (HMTase Inhibitor IX) 인용됨 34 출판물

Coordinated action of multiple active histone modifications shapes the zygotic genome activation in teleost embryos [ Nat Commun, 2025, 16(1):5222] PubMed: 40523893
The long non-coding RNA RSDR protects against acute kidney injury in mice by interacting with hnRNPK to regulate DHODH-mediated ferroptosis [ Nat Commun, 2025, 16(1):7483] PubMed: 40796740
Targeting pancreatic cancer glutamine dependency confers vulnerability to GPX4-dependent ferroptosis [ Cell Rep Med, 2025, 6(2):101928] PubMed: 39879992
Histone methyltransferase KMT2A promotes pulmonary fibrogenesis via targeting pro-fibrotic factor PU.1 in fibroblasts [ Clin Transl Med, 2025, 15(2):e70217] PubMed: 39888275
MLL1 downregulation drives hair cell ferroptosis via mitochondrial and endoplasmic reticulum stress mechanisms through PERK-eIF2α-Atf4-Chop and PI3K/Akt-Lrp1 signaling pathway [ Chin Med J (Engl), 2025, 10.1097/CM9.0000000000003633] PubMed: 40640087
Targeting MLL1/WDR5-Mediated Epigenetic Regulation Mitigates Peritoneal Fibrosis by Reducing p16INK4a [ FASEB J, 2025, 39(8):e70543] PubMed: 40232893
Fibroblast-specific PRMT5 deficiency suppresses cardiac fibrosis and left ventricular dysfunction in male mice [ Nat Commun, 2024, 15(1):2472] PubMed: 38503742
Arachidonic acid released by PIK3CA mutant tumor cells triggers malignant transformation of colonic epithelium by inducing chromatin remodeling [ Cell Rep Med, 2024, S2666-3791(24)00179-4] PubMed: 38614093
MBD2 regulates the progression and chemoresistance of cholangiocarcinoma through interaction with WDR5 [ J Exp Clin Cancer Res, 2024, 43(1):272] PubMed: 39350229
Bcl-xL is translocated to the nucleus via CtBP2 to epigenetically promote metastasis [ Cancer Letters, 2024, 217240]

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