Cat. No.: HY-148510

HKB99

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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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Pureté: 99.65%
CAS No.: 2414908-90-8
Formule: C₂₃H₁₈N₂O₆S
Masse moléculaire:450.46

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

HKB99 Chemical Structure

CAS No.: 2414908-90-8

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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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.

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.

Chemical Information

CAS No. 2414908-90-8
Appearance Solid
Masse moléculaire 450.46
Formule C₂₃H₁₈N₂O₆S
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2200 mL

11.0998 mL

22.1995 mL

5 mM

0.4440 mL

2.2200 mL

4.4399 mL

10 mM

0.2220 mL

1.1100 mL

2.2200 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Liang Q, et al. HKB99, an allosteric inhibitor of phosphoglycerate mutase 1, suppresses invasive pseudopodia formation and upregulates plasminogen activator inhibitor-2 in erlotinib-resistant non-small cell lung cancer cells. Acta Pharmacol Sin. 2021 Jan;42(1):115-119. [Content Brief]

[2]. Huang K, et al. A Novel Allosteric Inhibitor of Phosphoglycerate Mutase 1 Suppresses Growth and Metastasis of Non-Small-Cell Lung Cancer. Cell Metab. 2019 Dec 3;30(6):1107-1119.e8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Phosphatase Inhibitor Library

Anti-Cancer Metabolism Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform ERK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

HKB99 Related Classifications

HY-148510 Related Classifications