2. Apoptosis
  3. Apoptosis
  4. HG106

HG106 is an effective SLC7A11 inhibitor. HG106 mediates apoptosis by increasing oxidative stress and endoplasmic reticulum stress, and it has antitumor activity.

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HG106 Chemical Structure

HG106 Chemical Structure

CAS No. : 928712-10-1

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Based on 1 publication(s) in Google Scholar

HG106 Related Antibodies

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Description

HG106 is an effective SLC7A11 inhibitor. HG106 mediates apoptosis by increasing oxidative stress and endoplasmic reticulum stress, and it has antitumor activity[1].

IC50 & Target

SLC7A11
In Vitro

HG106 (1.25-10 μM, 3 min) shows a concentration-dependent inhibition of [14C] cystine consumption and glutathione production[1].
HG106 (0.1-100 μM, 72 h) has a stronger cytotoxic effect on KRAS mutant cell lines[1].
HG106 (0-10 μM, 6 h) dose-dependently increases the total ROS levels in A549 cells[1].
HG106 (0-5 μM, 24 h) causes mitochondrial dysfunction and endoplasmic reticulum stress in A549 cells[1].
HG106 (0-10 μM, 72 h) significantly induces apoptosis in KRAS mutant LUAD cells and inhibits colony formation[1].

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

HG106 Related Antibodies

Cell Viability Assay[1]

Cell Line: H441 KRAS(G12V), HPNE, HPNE/KRAS
Concentration: 0.1, 1, 10, 100 μM
Incubation Time: 72 h
Result: Inhibited cell proliferation, with greater effects on KRAS mutant cell lines.

Western Blot Analysis[1]

Cell Line: A549
Concentration: 0, 1.25, 2.5, 5 μM
Incubation Time: 24 h
Result: Increased activation of ER stress-related markers IRE1α, PERK and GRP78.

Apoptosis Analysis[1]

Cell Line: KRAS mutant LUAD
Concentration: 0, 1.25, 2.5, 5, 10; 0, 0.5, 1, 2 μM
Incubation Time: 72 h
Result: Did not cause cell autophagy, induced cell apoptosis, and inhibited colony formation.
In Vivo

HG106 (0-4 mg/kg, once a day, intraperitoneal injection, 26 days) inhibits tumor growth in A549 mouse transplant model[1].
HG106 (0-4 mg/kg, once a day, intraperitoneal injection, 20 days) inhibits tumor growth in mice in a xenograft model and induces apoptosis by triggering endoplasmic membrane stress[1].

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

Animal Model: A549 mouse transplant model[1]
Dosage: 0, 1, 2, 4 mg/kg; daily; 26 days
Administration: Intraperitoneal injection (i.p.)
Result: Inhibited tumor growth and prolonged the inhibition time of tumor growth.
Animal Model: LUAD patient-derived xenograft (PDX) models harboring the G12V mutation in KRAS[1]
Dosage: 0, 1, 2, 4 mg/kg; daily; 20 days
Administration: Intraperitoneal injection (i.p.)
Result: Inhibited tumor growth, increased ROS generation and TUNEL signal in patient-derived xenografts validated that HG106 triggered endoplasmic membrane stress-induced apoptosis in vivo.
Molecular Weight

316.74

Formula

C15H13ClN4O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(NC1=CC2=NN(C3=CC=C(OC)C=C3)N=C2C=C1)CCl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (394.65 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 3.1572 mL 15.7858 mL 31.5716 mL
5 mM 0.6314 mL 3.1572 mL 6.3143 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 (sealed storage, away from moisture and light). 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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This equation is commonly abbreviated as: C1V1 = C2V2

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

Purity: 99.95%

COA (244 KB) HNMR (139 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture and light). 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 3.1572 mL 15.7858 mL 31.5716 mL 78.9291 mL
5 mM 0.6314 mL 3.1572 mL 6.3143 mL 15.7858 mL
10 mM 0.3157 mL 1.5786 mL 3.1572 mL 7.8929 mL
15 mM 0.2105 mL 1.0524 mL 2.1048 mL 5.2619 mL
20 mM 0.1579 mL 0.7893 mL 1.5786 mL 3.9465 mL
25 mM 0.1263 mL 0.6314 mL 1.2629 mL 3.1572 mL
30 mM 0.1052 mL 0.5262 mL 1.0524 mL 2.6310 mL
40 mM 0.0789 mL 0.3946 mL 0.7893 mL 1.9732 mL
50 mM 0.0631 mL 0.3157 mL 0.6314 mL 1.5786 mL
60 mM 0.0526 mL 0.2631 mL 0.5262 mL 1.3155 mL
80 mM 0.0395 mL 0.1973 mL 0.3946 mL 0.9866 mL
100 mM 0.0316 mL 0.1579 mL 0.3157 mL 0.7893 mL
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HG106 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:

HG106928712-10-1HG 106HG-106ApoptosisSLC7A11cysteineglutathione biosynthesisA549KARSInhibitorinhibitorinhibit

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