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

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).

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HKB99 Chemical Structure

HKB99 Chemical Structure

CAS No. : 2414908-90-8

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HKB99 Related Antibodies

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Description

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].

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]
In Vitro

HKB99 (1-5 μM, 6 h) suppresses invasive pseudopodia formation and up-regulates PAI-2 in Erlotinib (HY-50896)-resistant NSCLC cells[1].
HKB99 (72 h) significantly inhibits the proliferation of NSCLC cells (PC9, HCC827, H1975, and A549) in a concentration-dependent manner with the IC50 values of 0.79, 1.22, 1.34, 5.62 μM, respectively[2].
HKB99 (1-5 μM, 6 h) inhibits the interaction of PGAM1 and ACTA2, disrupts cellular migration in NSCLC cells[2].
HKB99 (1-5 μM, 6-48 h) induces ROS-dependent cell apoptosis via activation of JNK/cJun signaling pathway in NSCLC cells, HKB99 (0.1-10 μM, 72 h) induces more apoptosis in acquired Erlotinib (HY-50896)-resistant HCC827ER cells compared with its parental HCC827 cells[1][2].

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

HKB99 Related Antibodies

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
In Vivo

HKB99 (35-100 mg/kg; i.p.; daily or once every 3 days) significantly suppresses tumor growth and augments the tumoricidal effect of Erlotinib in mouse xenografts. HKB99 restrains the tumor metastasis after intravenous NSCLC cell injection[2].

MedChemExpress (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.
Molecular Weight

450.46

Formula

C23H18N2O6S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(C=C(NS(C3=CC=C(N4CCC4)C=C3)(=O)=O)C(O)=C2O)C(C5=CC=CC=C51)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (277.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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HKB99 Related Classifications

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 SpeciesPKBProtein kinase BExtracellular signal regulated kinasesallosteric inhibitorNSCLCAKToxidative stressinvasive pseudopodiaInhibitorinhibitorinhibit

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