CMP-5

COA

级别和纯度:

≥95%

CAS编号: 880813-42-3
分子式: C₂₁H₂₁N₃
分子量: 315.41
PubChem编号: 4722595

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货号 (SKU)	包装规格	是否现货
C647447-5mg	5mg	期货
C647447-10mg	10mg	期货
C647447-50mg	50mg	期货

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Histone Modification (3105) 组蛋白甲基转移酶 (190) 表观遗传学 (1497)

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基本描述

规格或纯度	≥95%
英文名称	CMP-5
生化机理	CMP-5 是一种强效、特异性和选择性 PRMT5 抑制剂，对 PRMT1、PRMT4 和 PRMT7 没有活性。CMP-5 通过抑制组蛋白制备物上 PRMT5 甲基转移酶的活性，选择性地阻止 S2Me-H4R3。CMP-5 可阻止 Eps
储存温度	-20°C储存
运输条件	超低温冰袋运输
作用类型	抑制剂
产品介绍	CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1 , PRMT4 , and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected In Vitro CMP-5 (0-100 μM; 24-72 hours) is selectively toxic to lymphoma cells, but shows a limited toxicity to normal resting B lymphocytes even after prolonged incubation. CMP-5 (40 μM; 24 hours) decreases p-BTK and pY(416)SRC expression in 60A cells when it compares to the DMSO-treated group. CMP-5 (0-40 μM; 24 hours) preferentially suppresses the proliferation of human Th1 cells over Th2 cells (43 versus 9% inhibition, respectively). The sensitivity of Th1 cells over Th2 cells to PRMT5 inhibition is different, the IC 50 values are 26.9 μM and 31.6 μM in human Th1 cells and Th2 cells, respectively. CMP-5 (25 μM; 24 hours) alone inhibits mouse Th1 cell proliferation by 91%, when added different doses IL-2, IL-2 enhances proliferation and reaches a peak at 5 ng/ml. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: 60A cells Concentration: 40 μM Incubation Time: 24 hours Result: Inhibited p-BTK and pY(416)SRC protein level. Cell Viability AssayCell Line: Human Th1 cells and Th2 cells Concentration: 25 μM Incubation Time: 24 hours Result: Inhibited mouse Th1 cell proliferation, but addition of IL-2 dose-dependently increased cell proliferation. Form:Oil IC50& Target:IC50: 3.7 μM (mTh1 cells), 9.2 μM (mTh2 cells) IC50: 26.9 μM (hTh1 cells), 31.6 μM (hTh2 cells)
纯度	≥95%

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	小分子
IIUPAC Name	1-(9-ethylcarbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
INCHI	1S/C21H21N3/c1-2-24-20-9-4-3-8-18(20)19-13-16(10-11-21(19)24)14-22-15-17-7-5-6-12-23-17/h3-13,22H,2,14-15H2,1H3
InChi Key	YPJMOVVQKBFRNH-UHFFFAOYSA-N
Smiles	CCN1C2=C(C=C(C=C2)CNCC3=CC=CC=N3)C4=CC=CC=C41
Isomeric SMILES	CCN1C2=C(C=C(C=C2)CNCC3=CC=CC=N3)C4=CC=CC=C41
PubChem CID	4722595
分子量	315.41

化学和物理性质

溶解性	DMSO : 125 mg/mL (396.31 mM; Need ultrasonic)
分子量	315.400 g/mol
XLogP3	3.500
氢键供体数Hydrogen Bond Donor Count	1
氢键受体数Hydrogen Bond Acceptor Count	2
可旋转键计数Rotatable Bond Count	5
精确质量Exact Mass	315.174 Da
单同位素质量Monoisotopic Mass	315.174 Da
拓扑极表面积Topological Polar Surface Area	29.900 Å²
重原子数Heavy Atom Count	24
形式电荷Formal Charge	0
复杂度Complexity	399.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	0
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

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