DC Chemicals Limited
China
Product Name: MI 2 (Menin-MLL Inhibitor)
Price: $450.0/100mg $800.0/250mg $1500.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 4-(4-(5,5-DIMETHYL-4,5-DIHYDROTHIAZOL-2-YL)PIPERAZIN-1-YL)-6-PROPYLTHIENO[2,3-D]PYRIMIDINE
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

1271738-62-5

1271738-62-5 structure

1271738-62-5 structure

Name: MI-2
Chemical Name: 4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine
CAS Number: 1271738-62-5
Molecular Formula: C₁₈H₂₅N₅S₂
Molecular Weight: 375.555
Catalog: Biochemical Inhibitor Epigenetics Histone Methyltransferase inhibitor
Create Date: 2018-06-22 09:20:47
Modify Date: 2024-01-07 18:48:05
MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM.

Name	4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine
Synonyms	4-[4-(5,5-dimethyl-4H-1,3-thiazol-2-yl)piperazin-1-yl]-6-propylthieno[2,3-d]pyrimidine Thieno[2,3-d]pyrimidine, 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-propyl- 4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-propylthieno[2,3-d]pyrimidine 4-[4-(5,5-Dimethyl-4,5-dihydro-1,3-thiazol-2-yl)-1-piperazinyl]-6-propylthieno[2,3-d]pyrimidine MI-2 Menin-MLL Inhibitor

Description	MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM.
Related Catalog	Signaling Pathways >> Epigenetics >> Histone Methyltransferase Research Areas >> Cancer
Target	IC50: 446±28 nM (Menin-MLL)[1]
In Vitro	The menin-MLL inhibitor MI-2 very effectively blocks proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 values of about 5 μM. Assessment of diverse hydrophobic groups at R1 led to the development of several compounds with IC50 values in the nanomolar range, including MI-2 (IC50= 446±28 nM) and MI-3 (IC50=648±25 nM).The dissociation constants measured for the menin-MLL inhibitors are at the nanomolar level, Kd=158 nM for MI-2. MI-2 can access the protein target and very effectively inhibit the menin-MLL-AF9 interaction in human cells. Furthermore, MI-2 shows only a small effect on the cell growth of E2A-HLF transduced BMC (GI50>50 μM), which may be due to inhibition of the menin interaction with wild-type MLL. Treatment with MI-2 results in GI50 values below 10 μM in MV4;11 (harboring MLL-AF4; GI50=9.5 μM), KOPN-8 (MLL-ENL; GI50=7.2 μM) and ML-2 (MLL-AF6; GI50=8.7 μM), and in MonoMac6 (MLL-AF9; GI50=18 μM)[1].
Cell Assay	5×105 HEK 293 cells/mL are plated in 12-well plates (1 mL/well) and treated with compounds (e.g., MI-2) (0.25% final concentration of DMSO for each condition) or 0.25% DMSO control and incubated for 48h at 37°C in a 5% CO2 incubator. After incubation, 1.5×105 cells are harvested and resuspended in 100 μL 1× Annexin V binding buffer from the Annexin V-FITC Apoptosis kit, incubated with 4 μL of AnnexinV-FITC and 6 μL of Propidium iodide at room temperature in the dark for 10 minutes and analyzed by flow cytometry on a LSR II instrument. Data analysis is performed using WinList software. The experiments are performed three times in triplicates with calculation of mean and standard deviation for each condition[1].
References	[1]. Grembecka J, et al. Menin-MLL inhibitors reverse oncogenic activity of MLL fusion proteins in leukemia. Nature Chemical Biology (2012), 8(3), 277-284.

Density	1.4±0.1 g/cm3
Boiling Point	538.0±60.0 °C at 760 mmHg
Molecular Formula	C₁₈H₂₅N₅S₂
Molecular Weight	375.555
Flash Point	279.2±32.9 °C
Exact Mass	375.155121
PSA	98.16000
LogP	3.59
Vapour Pressure	0.0±1.4 mmHg at 25°C
Index of Refraction	1.712
Storage condition	-20°C

HS Code	2934999090

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%