标签归档：bomedemstat

Bomedemstat(Synonyms: IMG-7289)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Bomedemstat (Synonyms: IMG-7289)

Bomedemstat (IMG-7289) 是一种有效的，具有口服活性的，不可逆的赖氨酸特异性脱甲基酶 1 (LSD1) 抑制剂，具有表观遗传活性。Bomedemstat 可用于急性髓性白血病 (AML) 和骨髓纤维化 (MF) 的研究。具有抗肿瘤活性。

Bomedemstat(Synonyms: IMG-7289)

Bomedemstat Chemical Structure

CAS No. : 1990504-34-1

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

Bomedemstat (IMG-7289) is an orally active and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity[1].

体外研究
(In Vitro)

Bomedemstat (IMG-7289) selectively inhibits proliferation and induces apoptosis of JAK2V617F cells by concomitantly increasing expression and methylation of p53, and, independently, the pro-apoptotic factor PUMA and by decreasing the levels of its antiapoptotic antagonist BCL-XL[1]. 
Bomedemstat (25  nM, 50  nM) and Ruxolitinib (175  nM) synergize in inhibiting JAK2V617F-driven proliferation[1].
Bomedemstat (50 and 100 nM) exerts a pro-apoptotic effect on 3 key regulators of programmed cell death, TP53, BCL-XL, and PUMA[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: The human cell lines SET-2 (ATCC 608) and HEK293
Concentration: 25  nM, 50 nM
Incubation Time: 96 hours
Result: 25 nM alone significantly reduced colony formation.

Western Blot Analysis[1]

Cell Line: SET-2 cells
Concentration: 50 and 100 nM
Incubation Time:
Result: Decreased levels of the antiapoptotic protein BCL-XL and increased levels of the pro-apoptotic protein PUMA.

体内研究
(In Vivo)

Once-daily treatment with Bomedemstat (IMG-7289; 45  mg/kg) normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mx1cre-Jak2V617F mice[1]
Dosage: 45  mg/kg
Administration: Administered daily by oral gavage for either 14, 42, or 56 consecutive days
Result: In this Mx-Jak2V617F model of myeloproliferative neoplasm (MPN), mice developed severe splenomegaly (up to 10-fold increase in spleen weight). Splenic architecture was completely destroyed, eliminating demarcation of the white and red pulp. Treatment significantly reduced splenomegaly with a few treated mice normalizing their spleen weight. Remarkably, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.

分子量

519.61

Formula

C28H34FN7O2
CAS 号

1990504-34-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Jonas S Jutzi,et al. LSD1 Inhibition Prolongs Survival in Mouse Models of MPN by Selectively Targeting the Disease Clone. Hemasphere.2018 Jun 8;2(3):e54.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Bomedemstat ditosylate(Synonyms: IMG-7289 ditosylate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Bomedemstat ditosylate (Synonyms: IMG-7289 ditosylate)

Bomedemstat (IMG-7289) ditosylate 是一种有效的，具有口服活性的，不可逆的赖氨酸特异性脱甲基酶 1 (LSD1) 抑制剂，具有表观遗传活性。Bomedemstat ditosylate 可用于急性髓性白血病 (AML) 和骨髓纤维化 (MF) 的研究。具有抗肿瘤活性。

Bomedemstat ditosylate(Synonyms: IMG-7289 ditosylate)

Bomedemstat ditosylate Chemical Structure

CAS No. : 1990504-72-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity[1].

体外研究
(In Vitro)

Bomedemstat (IMG-7289) ditosylate selectively inhibits proliferation and induced apoptosis of JAK2V617F cells by concomitantly increasing expression and methylation of p53, and, independently, the pro-apoptotic factor PUMA and by decreasing the levels of its antiapoptotic antagonist BCL-XL[1]. 
Bomedemstat (25  nM, 50 nM) ditosylate and Ruxolitinib (175 nM) synergize in inhibiting JAK2V617F-driven proliferation[1].
Bomedemstat (50 and 100 nM) ditosylate exerts a pro-apoptotic effect on 3 key regulators of programmed cell death, TP53, BCL-XL, and PUMA[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: The human cell lines SET-2 (ATCC 608) and HEK293
Concentration: 25  nM, 50 nM
Incubation Time: 96 hours
Result: 25 nM alone significantly reduced colony formation.

Western Blot Analysis[1]

Cell Line: SET-2 cells
Concentration: 50 and 100 nM
Incubation Time:
Result: Decreased levels of the antiapoptotic protein BCL-XL and increased levels of the pro-apoptotic protein PUMA.

体内研究
(In Vivo)

Once-daily treatment with Bomedemstat (IMG-7289; 45 mg/kg) ditosylate normalizes or improves blood cell counts, reduces spleen volumes, restores normal splenic architecture, and reduces bone marrow fibrosis[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mx1cre-Jak2V617F mice[1]
Dosage: 45  mg/kg
Administration: Administered daily by oral gavage for either 14, 42, or 56 consecutive days
Result: In this Mx-Jak2V617F model of myeloproliferative neoplasm (MPN), mice developed severe splenomegaly (up to 10-fold increase in spleen weight). Splenic architecture was completely destroyed, eliminating demarcation of the white and red pulp. Treatment significantly reduced splenomegaly with a few treated mice normalizing their spleen weight. Remarkably, the 56-day course led to partial restoration of lymph follicles and spleen architecture by histological examination.

分子量

864.02

Formula

C42H50FN7O8S2
CAS 号

1990504-72-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Jonas S Jutzi,et al. LSD1 Inhibition Prolongs Survival in Mouse Models of MPN by Selectively Targeting the Disease Clone. Hemasphere.2018 Jun 8;2(3):e54.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务