2. Metabolic Enzyme/Protease Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway Immunology/Inflammation NF-κB
  3. Phosphatase Apoptosis Akt ERK Reactive Oxygen Species (ROS)
  4. HKB99

HKB99 是磷酸甘油酸突变酶 1 的变构抑制剂 (PGAM1)。HKB99 诱导细胞凋亡 (apoptosis)。HKB99 抑制细胞侵袭性伪足的形成并抑制迁移。HKB99 增加氧化应激，激活 JNK/c-Jun，抑制 AKT 和 ERK。HKB99 可用于非小细胞肺癌 (NSCLC) 的研究。

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HKB99

HKB99 Chemical Structure

CAS No. : 2414908-90-8

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1 mg ￥2163
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5 mg ￥4760
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HKB99 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 induces apoptosis. HKB99 inhibits the formation of invasive pseudopodia and inhibits migration. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC)[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 EC50
5.62 μM
Compound: 5; HKB99
Antitumor activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antitumor activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36215859]
HCC827 EC50
1.02 μM
Compound: 5; HKB99
Antitumor activity against erlotinib-resistant human HCC827 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antitumor activity against erlotinib-resistant human HCC827 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36215859]
HCC827 EC50
1.705 μM
Compound: 5; HKB99
Antitumor activity against human HCC827 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
Antitumor activity against human HCC827 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
[PMID: 36215859]
体外研究
(In Vitro)

HKB99 (1-5 μM，6 小时) 可抑制侵袭性伪足形成，并上调 Erlotinib (HY-50896) 耐药的非小细胞肺癌细胞 (NSCLC) 中的 PAI-2[1]。
HKB99 (72 小时) 以浓度依赖性方式显著抑制 NSCLC 细胞 (PC9、HCC827、H1975 和 A549) 的增殖，IC50 值分别为 0.79、1.22、1.34、5.62 μM[2]。
HKB99 (1-5 μM，6 小时) 可抑制 NSCLC 细胞 PGAM1 和 ACTA2 的相互作用，破坏细胞迁移[2]。
HKB99 (1-5 μM，6-48 小时) 通过激活 JNK/cJun 信号通路诱导 NSCLC 细胞中 ROS 依赖性细胞凋亡，(0.1-10 μM，72 小时) 且在获得性 Erlotinib (HY-50896) 耐药的 HCC827ER 细胞中诱导的细胞凋亡高于其亲本 HCC827 细胞[1][2]。

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

HKB99 相关抗体:

Cell Viability Assay[1]

Cell Line: HCC827 and HCC827ER cells
Concentration: 0.1-10 μM
Incubation Time: 72 h
Result: Preferentially suppresses cellular proliferation in acquired Erlotinib (HY-50896)-resistant HCC827ER cells, and it has higher potency (IC50 value of 1.020 μM) and efficacy than is achieved in the parental HCC827 cells (IC50 value of 1.705 μM).

Cell Migration Assay [2]

Cell Line: PC9, HCC827, HCC827ER9 cells
Concentration: 0.2, 0.4, 5 μM
Incubation Time: 3, 20 h
Result: Quickly disrupted the invadopodia-like structures at 0.4 μM in HCC827ER9 cells.
The level of F-actin was significantly decreased at 5 μM in HCC827ER9 cells.
Completely ablated cell migration of PC9 and HCC827 cells in 20 h.

Apoptosis Analysis[2]

Cell Line: PC9, 16HBE, HCC827
Concentration: 0.5, 1, 5 μM
Incubation Time: 24 h
Result: Caused remarkable apoptosis with fraction from 5% to 28% in PC9.
No apoptosis was stimulated under the same condition in 16HBE cells.
Consistently induced apoptosis in HCC827 cells

Western Blot Analysis[1]

Cell Line: HCC827 and HCC827ER cells
Concentration: 1, 5 μM (HCC827), 1.25, 2.5μM (HCC827ER)
Incubation Time: 6 h
Result: Notably increased the level of PAI-2 at a low concentration of 1.25 μM in HCC827ER.
Increased the level of PAI-2 at 5 μM in HCC827.

Western Blot Analysis[2]

Cell Line: HCC827 and HCC827ER cells
Concentration: 5 μM (HCC827), 1, 5μM (HCC827ER)
Incubation Time: 6 h
Result: Inhibited the interaction of PGAM1 with ACTA2, while no difference was observed in the total amount of ACTA2
体内研究
(In Vivo)

HKB99 (35-100 mg/kg；腹腔注射；每日一次或每 3 天一次) 显著抑制肿瘤生长，并增强 Erlotinib 在小鼠异种移植瘤中的杀瘤作用。HKB99 可抑制静脉注射非小细胞肺癌细胞后的肿瘤转移[2]。

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

Animal Model: Female BALB/c nu/nu mice (4 weeks) (NSCLC cells were injected subcutaneously on two sites per mouse) or (HCC827-Luc and HCC827ER9-Luc cells about 5 x 106 were injected through the tail vein injection)[2]
Dosage: 35, 100 mg/kg
Administration: Intraperitoneal injection (i.p.); daily or once every 3 days
Result: Attenuated tumor growth of PC9 xenografts in a murine subcutaneous model.
The T/C ratio was 32.97%, while tumors in combination with Erlotinib were almost completely abrogated (T/C ratio of 9.46%) in PC9 xenografts.
Induced much tumor necrosis in the PC9 xenografts.
Tumor weight was relevantly regressed in PC9 xenografts.
Combination with Erlotinib caused complete ablation of the tumors in HCC827 xenografts.
Significantly inhibited the HCC827ER9 xenografts’ growth with a T/C ratio of 34.76%.
Ablated the massive colonization and metastasis foci of HCC827-Luc and HCC827ER9-Luc, while the control group showed areas of high fluorescence, representing tumor foci, mainly in the lungs and abdominal organs.
The average bioluminescence intensity did not increase.
No death or weight loss over 10% was documented, indicating no subacute toxicity.
分子量

450.46

Formula

C23H18N2O6S
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 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 : 125 mg/mL (277.49 mM; 超声助溶; 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 2.2200 mL 11.0998 mL 22.1995 mL
5 mM 0.4440 mL 2.2200 mL 4.4399 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

HKB99 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 2.2200 mL 11.0998 mL 22.1995 mL 55.4988 mL
5 mM 0.4440 mL 2.2200 mL 4.4399 mL 11.0998 mL
10 mM 0.2220 mL 1.1100 mL 2.2200 mL 5.5499 mL
15 mM 0.1480 mL 0.7400 mL 1.4800 mL 3.6999 mL
20 mM 0.1110 mL 0.5550 mL 1.1100 mL 2.7749 mL
25 mM 0.0888 mL 0.4440 mL 0.8880 mL 2.2200 mL
30 mM 0.0740 mL 0.3700 mL 0.7400 mL 1.8500 mL
40 mM 0.0555 mL 0.2775 mL 0.5550 mL 1.3875 mL
50 mM 0.0444 mL 0.2220 mL 0.4440 mL 1.1100 mL
60 mM 0.0370 mL 0.1850 mL 0.3700 mL 0.9250 mL
80 mM 0.0277 mL 0.1387 mL 0.2775 mL 0.6937 mL
100 mM 0.0222 mL 0.1110 mL 0.2220 mL 0.5550 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:

HKB992414908-90-8HKB 99HKB-99PhosphataseApoptosisAktERKReactive Oxygen Species (ROS)PKBProtein kinase BExtracellular signal regulated kinasesallosteric inhibitorNSCLCAKToxidative stressinvasive pseudopodiaInhibitorinhibitorinhibit

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