2. Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt JAK/STAT Signaling NF-κB
  3. Apoptosis Akt mTOR STAT NF-κB
  4. HBS-101

HBS-101 is a selectively, orally active, brain-penetrant, Midkine (MDK) inhibitor (KD = 38.4 nM). HBS-101 significantly reduces cell viability, clonogenic survival, and invasiveness and increases apoptosis. HBS-101 involves suppression of the Akt/mTOR, STAT3, and NF-κB pathways. HBS-101 can be used for the study of Triple-negative breast cancer (TNBC).

For research use only. We do not sell to patients.

HBS-101

HBS-101 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

HBS-101 Related Antibodies

Top Publications Citing Use of Products

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

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STAT3 STAT5 STAT6 STAT1

View All NF-κB Isoform Specific Products:

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HBS-101 is a selectively, orally active, brain-penetrant, Midkine (MDK) inhibitor (KD = 38.4 nM). HBS-101 significantly reduces cell viability, clonogenic survival, and invasiveness and increases apoptosis. HBS-101 involves suppression of the Akt/mTOR, STAT3, and NF-κB pathways. HBS-101 can be used for the study of Triple-negative breast cancer (TNBC)[1].

In Vitro

HBS-101 (0.1-10 μM, 5 days) significantly reduces cell viability of TNBC cell lines[1].
HBS-101 (0-5 μM) reduces the colony-forming ability of TNBC cells in a dose-dependent manner[1].
HBS-101 (20 μM, 24 h) induces apoptosis in TNBC cells, but not in normal mammary epithelial cells[1].
HBS-101 (20 μM, 20 h) significantly reduces the expression of MDK receptors, specifically Notch2, in HCC-70 cells; inhibits downstream signaling pathways, including mTOR, STAT3, and NF-κB; and increases cleaved caspase-3 levels[1].
HBS-101 (20 μM, 24 h) downregulates MDK target genes and significantly reduces STAT3 and NF-κB reporter activity in TNBC cells that stably express these reporters[1].

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

HBS-101 Related Antibodies

Cell Viability Assay[1]

Cell Line: SUM-159, BT-549, MDA-MB-468, MDA-MB-231, MDA-MB-231-BrM2-831, HCC-70, HCC-1937, HER2+ SKBR3, ER+ MCF7, MCF10A
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 5 days
Result: Significantly inhibited the viability of TNBC cell lines, with IC50 values ranging from 0.3 to 2.8 μmol/L.
Exhibited weaker inhibitory effects on HER2+ SKBR3, (IC50 ~ 16 μM) and ER+MCF7, (IC50 > 20 μM) breast cancer cell lines.
Showed no toxicity against normal breast epithelial MCF10A cells.

Western Blot Analysis[1]

Cell Line: HCC-70 cells
Concentration: 20 μM
Incubation Time: 20 h
Result: Reduced Notch2 receptor protein levels.
Inhibited the phosphorylation of mTOR, STAT3, and NF-κB, and increased the level of cleaved caspase-3, a marker of apoptosis.

RT-PCR[1]

Cell Line: MDA-MB-231 cells, BT-549 cells
Concentration: 20 μM
Incubation Time: 20 h
Result: Significantly reduced STAT3 and NF-κB reporter activity in TNBC cells that stably express these reporters.

Cell Invasion Assay[1]

Cell Line: MDA-MB-231 cells, BT-549 cells, MCF10A cells
Concentration: 20 μM
Incubation Time: 24 h
Result: Induced apoptosis in TNBC cells, but not in normal mammary epithelial cells.
Parmacokinetics
Species Dose Route Tmax Cmax AUCinf T1/2 CL/F
Rat 10 mg/kg i.p. 0.54 h 6271 ng/mL 5233 ng·h/mL 0.52 h 1971 mL/h/kg
In Vivo

HBS-101 (1 mg/kg (i.v.), 10 mg/kg (p.o.) has rapid in vivo disposition kinetics and extremely high oral bioavailability in rats[1].
HBS-101 (10 mg/kg, i.p.) can be rapidly absorbed and effectively penetrates the blood-brain barrier in mice[1].
HBS-101 (2-10 mg/kg, p.o., 5 days) doses up to 10 mg/kg (oral) for 5 consecutive days are safe and do not produce observable organ toxicity in mice[1].
HBS-101 (2 mg/kg, 5 mg/kg, p.o., 5 days) effectively inhibits the growth of TNBC orthotopic tumors with oral administration, and 5 mg/kg is determined to be the minimum effective dose in mice[1].
HBS-101 (5 mg/kg, p.o., 5 days a week) reduces the proliferative activity of tumors in MDA-MB-231 cells xenograft mice[1].
HBS-101 (10 mg/kg, i.p., 5 days a week) exhibits potent anti-tumor activity in a brain metastasis model in mice[1].

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

Animal Model: Rats[1].
Dosage: 1 mg/kg, 10 mg/kg
Administration: I.v., p.o.
Result: Had monoexponential disposition in vivo and had an estimated plasma half-life between 0.7 and 1.6 hours.
Had excellent oral bioavailability in rats.
Animal Model: Female C57BL/6 mice[1].
Dosage: 10 mg/kg
Administration: I.p., once
Result: Absorbed rapidly following i.p. administration, resembling an i.v. bolus drug administration.
Detected in the brain, with peak detectable levels reaching 1,654 ng/g 10 minutes after administration, suggesting that HBS-101 effectively crosses the blood-brain barrier.
Animal Model: Female C57BL/6 mice[1].
Dosage: 2 mg/kg, 5 mg/kg, 10 mg/kg
Administration: P.o., 5 days
Result: No abnormalities were detected during the gross pathological examination of the animals.
Animal Model: MDA-MB-231 cells (2 × 106) mixed with a 1:1 volume of Matrigel were injected into the mammary fat pad of the nude mice[1].
Dosage: 2 mg/kg, 5 mg/kg
Administration: P.o., 5 times a week
Result: Led to a significant dose-dependent reduction in tumor volume.
Not affected mouse body weight.
Significant decreased in Ki-67–positive cells.
Animal Model: Female SCID mice were used as recipients for 2 mm3 TNBC–PDX-96 tumor tissue implants to establish subcutaneous PDX tumor models[1].
Dosage: 5 mg/kg
Administration: P.o., 5 times a week
Result: Significantly inhibited PDX tumor growth, with tumor volume and weight significantly reduced. Significant decrease in Ki-67-positive cells.
Animal Model: 1.75 × 105 brain-metastatic MDA-MB-231-BrM2-831 cells were orthotopically injected into the right cerebral hemisphere of female NOD.CB17-Prkdcscid/NCrCrl mice[1].
Dosage: 10 mg/kg
Administration: I.p., 5 times a week
Result: Significantly reduced tumor progression and extended the survival of mice with orthotopic tumors.
Molecular Weight

346.41

Formula

C21H24F2O2
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](O)(C(F)(F)C#C)CC[C@@]1([H])[C@]3([H])CCC4=CC(CCC4=C3CC2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (288.68 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 2.8868 mL 14.4338 mL 28.8675 mL
5 mM 0.5774 mL 2.8868 mL 5.7735 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.8868 mL 14.4338 mL 28.8675 mL 72.1688 mL
5 mM 0.5774 mL 2.8868 mL 5.7735 mL 14.4338 mL
10 mM 0.2887 mL 1.4434 mL 2.8868 mL 7.2169 mL
15 mM 0.1925 mL 0.9623 mL 1.9245 mL 4.8113 mL
20 mM 0.1443 mL 0.7217 mL 1.4434 mL 3.6084 mL
25 mM 0.1155 mL 0.5774 mL 1.1547 mL 2.8868 mL
30 mM 0.0962 mL 0.4811 mL 0.9623 mL 2.4056 mL
40 mM 0.0722 mL 0.3608 mL 0.7217 mL 1.8042 mL
50 mM 0.0577 mL 0.2887 mL 0.5774 mL 1.4434 mL
60 mM 0.0481 mL 0.2406 mL 0.4811 mL 1.2028 mL
80 mM 0.0361 mL 0.1804 mL 0.3608 mL 0.9021 mL
100 mM 0.0289 mL 0.1443 mL 0.2887 mL 0.7217 mL
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HBS-101 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:

HBS-101HBS101HBS 101ApoptosisAktmTORSTATNF-κBPKBProtein kinase BMammalian target of RapamycinNuclear factor-κBNuclear factor-kappaBMidkineMDKTriple-Negative Breast CancerTNBCSTAT3Blood-Brain BarrierInhibitorinhibitorinhibit

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