2. Apoptosis
  3. Bcl-2 Family Apoptosis
  4. Mcl-1 inhibitor 6

Mcl-1 inhibitor 6 

目录号: HY-132307 纯度: 98.40%
COA 产品使用指南

摩尔计算器

Mcl-1 inhibitor 6 是一种口服有效的，选择性的骨髓细胞白血病 1 (Mcl-1) 蛋白抑制剂，Kd 值为 0.23 nM，Ki 值为 0.02 μM。Mcl-1 inhibitor 6 对 Mcl-1 的选择性高于其他 Bcl-2 家族成员 (Bcl-2、Bcl2A1、Bcl-xL 和 Bcl-w，Kd>10 μM)。Mcl-1 inhibitor 6 是一种有效的抗肿瘤剂。

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Mcl-1 inhibitor 6 Chemical Structure

Mcl-1 inhibitor 6 Chemical Structure

CAS No. : 2598978-56-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1990
In-stock
5 mg ￥1750
In-stock
10 mg ￥2800
In-stock
25 mg ￥5900
In-stock
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Customer Review

Mcl-1 inhibitor 6 相关抗体

Top Publications Citing Use of Products

查看 Bcl-2 Family 亚型特异性产品:

查看所有亚型
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent[1].

IC50 & Target[1]

Mcl-1

0.23 nM (Kd)

Mcl-1

0.02 μM (Ki)

Bcl-2

>10 μM (Kd)

Bcl2A1

>10 μM (Kd)

Bcl-xL

>10 μM (Kd)

Bcl-W

>10 μM (Kd)

Bcl-2

10 μM (Ki)

Bfl-1

1.57 μM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
K562 IC50
> 30 μM
Compound: 40
Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
MV4-11 IC50
0.7 μM
Compound: 40
Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
NCI-H23 IC50
3.02 μM
Compound: 40
Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H23 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
NCI-H929 IC50
0.36 μM
Compound: 40
Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H929 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
SK-BR-3 IC50
2.84 μM
Compound: 40
Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human SK-BR-3 cells assessed as decrease in cell viability measured after 72 hrs by MTT assay
[PMID: 34342996]
体外研究
(In Vitro)

Mcl-1 inhibitor 6 has Kis of 10 μM and 1.57μM for Bcl-2 and Bfl-1, respectively[1].
Mcl-1 inhibitor 6 (1, 5 μM; for 48 h) significantly induces apoptosis in a concentration-dependent manner[1].
Mcl-1 inhibitor 6 (0.1, 5 μM; for 4 h) remarkably upregulates PARP cleavage in H929 cells in a concentration-dependent manner[1].
Mcl-1 inhibitor 6 (for 72 h) shows antiproliferative activities against the tumor cell lines (H929, MV4-11, SK-BR-3, NCI-H23; IC50=0.36-3.02 μM). Mcl-1 inhibitor 6 shows ideal selectivity against CML cell line K562 (IC50>30 μM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Mcl-1 inhibitor 6 相关抗体:

Apoptosis Analysis[1]

Cell Line: H929 cells
Concentration: 1, 5 μM
Incubation Time: For 48 hours
Result: Significantly induced apoptosis in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: H929 cells
Concentration: 0.1, 0.5, 1, 5 μM
Incubation Time: For 4 hours
Result: Remarkably upregulated PARP cleavage in H929 cells in a concentration-dependent manner.
体内研究
(In Vivo)

Mcl-1 inhibitor 6 (compound 40; 60 mg/kg with PO or 20 mg/kg with IP; every two days for 14 days) shows desired in vivo tumor growth inhibition activity[1].
Mcl-1 inhibitor 6 (3 mg/kg with IV or 10 mg/kg with PO) has a T1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c nude female mice (7 weeks) loaded with MV4-11 xenografts[1]
Dosage: 60 mg/kg (PO) or 20 mg/kg (IP)
Administration: IP or PO; every two days for 14 days
Result: Showed desired in vivo tumor growth inhibition activity (T/C = 37.30% and 5.52% by po and ip administration, respectively).
Animal Model: SD rats (200-250 g)[1]
Dosage: 3 mg/kg (IV) or 10 mg/kg (PO) (Pharmacokinetic Analysis)
Administration: IV or PO
Result: Had a T1/2 of 2.3 hours, a CL of 15.18 mL/min•kg by IV.
Had a T1/2 of 2.1 hours, a CL of 36.8 mL/min•kg and a Cmax of 2012.95 ng/mL.
分子量

518.02

Formula

C26H28ClNO6S
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (193.04 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9304 mL 9.6521 mL 19.3043 mL
5 mM 0.3861 mL 1.9304 mL 3.8609 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Mcl-1 inhibitor 6 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9304 mL 9.6521 mL 19.3043 mL 48.2607 mL
5 mM 0.3861 mL 1.9304 mL 3.8609 mL 9.6521 mL
10 mM 0.1930 mL 0.9652 mL 1.9304 mL 4.8261 mL
15 mM 0.1287 mL 0.6435 mL 1.2870 mL 3.2174 mL
20 mM 0.0965 mL 0.4826 mL 0.9652 mL 2.4130 mL
25 mM 0.0772 mL 0.3861 mL 0.7722 mL 1.9304 mL
30 mM 0.0643 mL 0.3217 mL 0.6435 mL 1.6087 mL
40 mM 0.0483 mL 0.2413 mL 0.4826 mL 1.2065 mL
50 mM 0.0386 mL 0.1930 mL 0.3861 mL 0.9652 mL
60 mM 0.0322 mL 0.1609 mL 0.3217 mL 0.8043 mL
80 mM 0.0241 mL 0.1207 mL 0.2413 mL 0.6033 mL
100 mM 0.0193 mL 0.0965 mL 0.1930 mL 0.4826 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mcl-1 inhibitor 62598978-56-2Bcl-2 FamilyApoptosisorallyPARPH929MV4-11SK-BR-3NCI-H23Inhibitorinhibitorinhibit

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