CM-272 | G9a/DNMTs Inhibitor | AmBeed-信号通路专用抑制剂

CM-272 {[allProObj[0].p_purity_real_show]}

货号：A810645

CM-272是一种有效、选择性且可逆的双重小分子抑制剂，能够抑制 G9a 和 DNMTs 活性。

CM-272 化学结构
CAS号：1846570-31-7

CM-272 3D分子结构
CAS号：1846570-31-7

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组蛋白去乙酰化酶亚型比较

DNA甲基转移酶亚型比较

产品名称	HD1 ↓ ↑	HD2 ↓ ↑	HDAC ↓ ↑	HDAC1 ↓ ↑	HDAC10 ↓ ↑	HDAC11 ↓ ↑	HDAC2 ↓ ↑	HDAC3 ↓ ↑	HDAC4 ↓ ↑	HDAC5 ↓ ↑	HDAC6 ↓ ↑	HDAC7 ↓ ↑	HDAC8 ↓ ↑	HDAC9 ↓ ↑	其他靶点	纯度
Givinostat HCl monohydrate	++++ HD1-B, IC50: 7.5 nM HD1-A, IC50: 16 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM															96%
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													99%+
Scriptaid			✔													99%+
Valproic acid sodium			✔												Autophagy	97%
AR-42			+++ HDAC, IC50: 30 nM													99%+
Dacinostat			+++ HDAC, IC50: 32 nM													98+%
CUDC-101			++++ HDAC, IC50: 4.4 nM	++++ HDAC1, IC50: 4.5 nM	+++ HDAC10, IC50: 26.1 nM		+++ HDAC2, IC50: 12.6 nM	++++ HDAC3, IC50: 9.1 nM	+++ HDAC4, IC50: 13.2 nM	+++ HDAC5, IC50: 11.4 nM	++++ HDAC6, IC50: 5.1 nM	+ HDAC7, IC50: 373 nM	++ HDAC8, IC50: 79.8 nM	++ HDAC9, IC50: 67.2 nM	HER2,EGFR	99%+
M344			++ HDAC, IC50: 100 nM													99%+
Splitomicin			+ Sir2p, IC50: 60 μM													99%
Panobinostat			++++ HDAC (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												NF-κB,Nrf2	98%
Belinostat			+++ HDAC, IC50: 27 nM													98%
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								98%
Valproic acid				+ HDAC1, IC50: 0.4 mM												98%
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								99%+
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								98%
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					98+%
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									99%+
Parthenolide				✔											NF-κB,p53	97% HPLC
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								98%
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								98%
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					99%+
Fimepinostat				++++ HDAC1, IC50: 1.7 nM	++++ HDAC10, IC50: 2.8 nM	++++ HDAC11, IC50: 5.4 nM	++++ HDAC2, IC50: 5.0 nM	++++ HDAC3, IC50: 1.8 nM			+++ HDAC6, IC50: 27 nM					99%+
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								99%+
Santacruzamate A							++++ HDAC2, IC50: 119 pM									99%+
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								99%+
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						99%+
Tasquinimod									✔							99%+
CAY10603											++++ HDAC6, IC50: 2 pM					98%
Tubastatin A											+++ HDAC6, IC50: 15 nM					98%
Tubacin											++++ HDAC6, IC50: 4 nM					99%+
ACY-738											++++ HDAC6, IC50: 1.7 nM					99%+
Nexturastat A											++++ HDAC6, IC50: 5 nM					99%+
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			99%
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			98%
PCI-34051													+++ HDAC8, IC50: 10 nM			99%+
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			99%+
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			99%+
Abexinostat				++++ HDAC1, Ki: 7 nM	+++ HDAC10, IC50: 24 nM		+++ HDAC2, Ki: 19 nM	++++ HDAC3/SMRT, Ki: 8.2 nM			+++ HDAC6, Ki: 17 nM		+ HDAC8, IC50: 280 nM			98%+
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			99%+
HPOB				+ HDAC1, IC50: 2.9 μM	+ HDAC10, IC50: 3.0 μM		+ HDAC2, IC50: 4.4 μM	+ HDAC3, IC50: 1.7 μM			++ HDAC6, IC50: 56 nM		+ HDAC8, IC50: 2.8 μM			97%
Quisinostat 2HCl				++++ HDAC1, IC50: 0.11 nM	++++ HDAC10, IC50: 0.46 nM	++++ HDAC11, IC50: 0.37 nM	++++ HDAC2, IC50: 0.33 nM	++++ HDAC3, IC50: 4.86 nM	++++ HDAC4, IC50: 0.64 nM	++++ HDAC5, IC50: 3.69 nM			++++ HDAC8, IC50: 4.26 nM			97%
Domatinostat				+ HDAC1, IC50: 1.20 μM	+ HDAC10, IC50: 21 μM	+ HDAC11, IC50: 9.7 μM	+ HDAC2, IC50: 1.12 μM	+ HDAC3, IC50: 0.57 μM		+ HDAC5, IC50: 11.3 μM				+ HDAC9, IC50: 50 μM		99%+
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		99%+
Pracinostat				++ HDAC1, IC50: 49 nM	+++ HDAC10, IC50: 40 nM	++ HDAC11, IC50: 93 nM	++ HDAC2, IC50: 96 nM	+++ HDAC3, IC50: 43 nM	++ HDAC4, IC50: 56 nM	+++ HDAC5, IC50: 47 nM	+ HDAC6, IC50: 1.008 μM	++ HDAC7, IC50: 137 nM	++ HDAC8, IC50: 140 nM	++ HDAC9, IC50: 70 nM		99%+
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	DNA Methyltransferase ↓ ↑	纯度
6-Thioguanine	✔	98%
Zebularine	✔	98%
Procainamide HCl	✔	99%
5-Azacytidine	✔	95%
Decitabine	✔	99%
SGI-1027	++ DNMT3A, IC50: 7.5 μM DNMT1, IC50: 6 μM	99%+
RG108	+++ DNA methyltransferase, IC50: 115 nM	99%+
Guadecitabine sodium	✔	98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

CM-272 生物活性

描述

CM-272 is a potent, selective and reversible dual small molecule against G9a and DNMTs activity.

CM-272 细胞实验

Cell Line Healthy donor MSCs co-cultured with MM.1S cells Bone marrow-derived mesenchymal stromal cells (MSCs) Healthy fibroblasts (HDFa, HDFn) Liver cancer cell lines (HepG2, HepT1, Hep3B, HUH7) HB PDX cell lines (PDX214, PDX243, PDX282, PDX295, PDX303, PDX344, PDX364) OCI-Ly10 DLBCL cells CEMO-1 ALL cells MV4-11 AML cells OCI-AML-2 AML cells Lacun3 H23 A549 H358	Concentration	Treated Time	Description	References
Healthy donor MSCs co-cultured with MM.1S cells	50 nM	14 days	CM-272 partially reversed the effects of MM cells on MSC gene expression mediated by secretory mechanisms and restored osteogenic differentiation capacity.	Nat Commun. 2021 Jan 18;12(1):421.
Bone marrow-derived mesenchymal stromal cells (MSCs)	50 nM	7 days	CM-272 restored the expression of hypermethylated Homeobox genes in myeloma MSCs by inhibiting DNMT and G9a methyltransferase activity, promoting osteogenic differentiation.	Nat Commun. 2021 Jan 18;12(1):421.
Healthy fibroblasts (HDFa, HDFn)	5 nM to 100 µM	48 h	To evaluate the impact of CM-272 on the viability of healthy fibroblasts, results showed that CM-272 had minimal effects on healthy cells with IC50 values of 23 µM (HDFa) and 28 µM (HDFn).	Hepatol Commun. 2024 Jan 29;8(2):e0378.
Liver cancer cell lines (HepG2, HepT1, Hep3B, HUH7)	5 nM to 100 µM	48 h	To evaluate the impact of CM-272 on the viability of liver cancer cell lines, results showed that CM-272 significantly reduced cell viability with an IC50 of 6.4 µM.	Hepatol Commun. 2024 Jan 29;8(2):e0378.
HB PDX cell lines (PDX214, PDX243, PDX282, PDX295, PDX303, PDX344, PDX364)	5 nM to 100 µM	48 h	To evaluate the impact of CM-272 on the viability of HB PDX cell lines, results showed that CM-272 significantly reduced cell viability with an IC50 of 0.7 µM, while having minimal effects on healthy fibroblasts.	Hepatol Commun. 2024 Jan 29;8(2):e0378.
OCI-Ly10 DLBCL cells	125-1000 nM	48 h	inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death	Nat Commun. 2017 May 26;8:15424.
CEMO-1 ALL cells	455 nM	48 h	inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death	Nat Commun. 2017 May 26;8:15424.
MV4-11 AML cells	269 nM	48 h	inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death	Nat Commun. 2017 May 26;8:15424.
OCI-AML-2 AML cells	218 nM	48 h	inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death	Nat Commun. 2017 May 26;8:15424.
Lacun3	IC50 = 1.5 μM	48 h	To evaluate the effect of CM-272 on cell proliferation, results showed CM-272 reduced proliferation and induced cell death	Cell Death Dis. 2024 Nov 2;15(11):787.
H23	IC50 = 0.63 μM	48 h	To evaluate the effect of CM-272 on cell proliferation, results showed CM-272 reduced proliferation and induced cell death	Cell Death Dis. 2024 Nov 2;15(11):787.
A549	IC50 = 1.3 μM	48 h	To evaluate the effect of CM-272 on cell proliferation, results showed CM-272 reduced proliferation and induced cell death	Cell Death Dis. 2024 Nov 2;15(11):787.
H358	IC50 = 0.45 μM	48 h	To evaluate the effect of CM-272 on cell proliferation, results showed CM-272 reduced proliferation and induced cell death	Cell Death Dis. 2024 Nov 2;15(11):787.

Cell Line

Concentration

Treated Time

Description

References

Healthy donor MSCs co-cultured with MM.1S cells

50 nM

14 days

CM-272 partially reversed the effects of MM cells on MSC gene expression mediated by secretory mechanisms and restored osteogenic differentiation capacity.

Nat Commun. 2021 Jan 18;12(1):421.

Bone marrow-derived mesenchymal stromal cells (MSCs)

50 nM

7 days

CM-272 restored the expression of hypermethylated Homeobox genes in myeloma MSCs by inhibiting DNMT and G9a methyltransferase activity, promoting osteogenic differentiation.

Nat Commun. 2021 Jan 18;12(1):421.

Healthy fibroblasts (HDFa, HDFn)

5 nM to 100 µM

48 h

To evaluate the impact of CM-272 on the viability of healthy fibroblasts, results showed that CM-272 had minimal effects on healthy cells with IC50 values of 23 µM (HDFa) and 28 µM (HDFn).

Hepatol Commun. 2024 Jan 29;8(2):e0378.

Liver cancer cell lines (HepG2, HepT1, Hep3B, HUH7)

5 nM to 100 µM

48 h

To evaluate the impact of CM-272 on the viability of liver cancer cell lines, results showed that CM-272 significantly reduced cell viability with an IC50 of 6.4 µM.

Hepatol Commun. 2024 Jan 29;8(2):e0378.

HB PDX cell lines (PDX214, PDX243, PDX282, PDX295, PDX303, PDX344, PDX364)

5 nM to 100 µM

48 h

To evaluate the impact of CM-272 on the viability of HB PDX cell lines, results showed that CM-272 significantly reduced cell viability with an IC50 of 0.7 µM, while having minimal effects on healthy fibroblasts.

Hepatol Commun. 2024 Jan 29;8(2):e0378.

OCI-Ly10 DLBCL cells

125-1000 nM

48 h

inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death

Nat Commun. 2017 May 26;8:15424.

CEMO-1 ALL cells

455 nM

48 h

inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death

Nat Commun. 2017 May 26;8:15424.

MV4-11 AML cells

269 nM

48 h

inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death

Nat Commun. 2017 May 26;8:15424.

OCI-AML-2 AML cells

218 nM

48 h

inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death

Nat Commun. 2017 May 26;8:15424.

Lacun3

IC50 = 1.5 μM

48 h

To evaluate the effect of CM-272 on cell proliferation, results showed CM-272 reduced proliferation and induced cell death

Cell Death Dis. 2024 Nov 2;15(11):787.

H23

IC50 = 0.63 μM

48 h

To evaluate the effect of CM-272 on cell proliferation, results showed CM-272 reduced proliferation and induced cell death

Cell Death Dis. 2024 Nov 2;15(11):787.

A549

IC50 = 1.3 μM

48 h

To evaluate the effect of CM-272 on cell proliferation, results showed CM-272 reduced proliferation and induced cell death

Cell Death Dis. 2024 Nov 2;15(11):787.

H358

IC50 = 0.45 μM

48 h

To evaluate the effect of CM-272 on cell proliferation, results showed CM-272 reduced proliferation and induced cell death

Cell Death Dis. 2024 Nov 2;15(11):787.

CM-272 动物实验

Species NSG mice Nude mice (nude-Foxn1nu mice) BALB/cA Rag2−/−γc−/− mice Mice	Animal Model Myeloma model HB PDX model (HB-282) ALL, AML and DLBCL xenogeneic models A549 and Lacun3 subcutaneous xenograft models	Administration	Dosage	Frequency	Description	References
NSG mice	Myeloma model	Intraperitoneal injection	5 mg/kg	5 times/week for 4 weeks	CM-272 controlled tumor progression and prevented tumor-associated bone loss, demonstrating anti-myeloma activity and bone-anabolic effects in vivo.	Nat Commun. 2021 Jan 18;12(1):421.
Nude mice (nude-Foxn1nu mice)	HB PDX model (HB-282)	Intraperitoneal injection (i.p.)	5 mg/kg	5 days per week, until day 7	To evaluate the antitumor efficacy of CM-272 in vivo, results showed that CM-272 significantly inhibited tumor growth but caused severe side effects such as dramatic loss and tumor hemorrhage.	Hepatol Commun. 2024 Jan 29;8(2):e0378.
BALB/cA Rag2−/−γc−/− mice	ALL, AML and DLBCL xenogeneic models	Intravenous (i.v.)	2.5 mg/kg	Daily, for 4 weeks (ALL and AML) or 8 weeks (DLBCL)	Significantly prolongs survival of AML, ALL and DLBCL xenogeneic models	Nat Commun. 2017 May 26;8:15424.
Mice	A549 and Lacun3 subcutaneous xenograft models	Intraperitoneal injection	5 mg/kg	5 days a week for several weeks	To evaluate the effect of CM-272 on tumor volume, results showed CM-272 significantly reduced tumor volume	Cell Death Dis. 2024 Nov 2;15(11):787.

Species

NSG mice Nude mice (nude-Foxn1nu mice) BALB/cA Rag2−/−γc−/− mice Mice

Animal Model

Myeloma model HB PDX model (HB-282) ALL, AML and DLBCL xenogeneic models A549 and Lacun3 subcutaneous xenograft models

Administration

Dosage

Frequency

Description

References

NSG mice

Myeloma model

Intraperitoneal injection

5 mg/kg

5 times/week for 4 weeks

CM-272 controlled tumor progression and prevented tumor-associated bone loss, demonstrating anti-myeloma activity and bone-anabolic effects in vivo.

Nat Commun. 2021 Jan 18;12(1):421.

Nude mice (nude-Foxn1nu mice)

HB PDX model (HB-282)

Intraperitoneal injection (i.p.)

5 mg/kg

5 days per week, until day 7

To evaluate the antitumor efficacy of CM-272 in vivo, results showed that CM-272 significantly inhibited tumor growth but caused severe side effects such as dramatic loss and tumor hemorrhage.

Hepatol Commun. 2024 Jan 29;8(2):e0378.

BALB/cA Rag2−/−γc−/− mice

ALL, AML and DLBCL xenogeneic models

Intravenous (i.v.)

2.5 mg/kg

Daily, for 4 weeks (ALL and AML) or 8 weeks (DLBCL)

Significantly prolongs survival of AML, ALL and DLBCL xenogeneic models

Nat Commun. 2017 May 26;8:15424.

Mice

A549 and Lacun3 subcutaneous xenograft models

Intraperitoneal injection

5 mg/kg

5 days a week for several weeks

To evaluate the effect of CM-272 on tumor volume, results showed CM-272 significantly reduced tumor volume

Cell Death Dis. 2024 Nov 2;15(11):787.

CM-272 参考文献

CM-272 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.45mL

2.09mL

1.04mL

20.89mL

4.18mL

2.09mL

CM-272 技术信息

CAS号	1846570-31-7
分子式	C₂₈H₃₈N₄O₃
分子量	478.63
SMILES Code	CN1CCC(NC2=CC(C3=CC=C(C)O3)=NC4=CC(OCCCN5CCCC5)=C(OC)C=C24)CC1
MDL No.	MFCD31812316

别名
运输	蓝冰
InChI Key	RLQLKZTYUYIWDB-UHFFFAOYSA-N
Pubchem ID	118607432

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C

溶解方案

细胞实验：

DMSO: 120 mg/mL(250.72 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

CM-272 {[allProObj[0].p_purity_real_show]}

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CM-272 {[allProObj[0].p_purity_real_show]}

CM-272 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

CM-272 质控信息

CM-272 生物活性

CM-272 细胞实验

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CM-272 参考文献

CM-272 实验方案

CM-272 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

工作液计算器

细胞研究

临床研究

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