1. Immunology/Inflammation
  2. MyD88
  3. MyD88-IN-1

MyD88-IN-1 (Compound c17) is an orally active MyD88 inhibitor. MyD88-IN-1 inhibits the interaction of TLR4 and MyD88 and suppressed the NF-κB pathway. MyD88-IN-1 can be used in research of cancer and inflammatory.

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MyD88-IN-1

MyD88-IN-1 Chemische Struktur

CAS. Nr. : 2911609-80-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 5 publication(s) in Google Scholar

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Beschreibung

MyD88-IN-1 (Compound c17) is an orally active MyD88 inhibitor. MyD88-IN-1 inhibits the interaction of TLR4 and MyD88 and suppressed the NF-κB pathway. MyD88-IN-1 can be used in research of cancer and inflammatory[1].

Cellular Effect
Cell Line Type Value Description References
J774.A1 IC50
2.17 3
Compound: c17
Anti-inflammatory activity in mouse J774.A1 cells assessed as inhibition of LPS-induced IL-6 production pre-stimulated with LPS for 24 hrs followed by compound addition and measured after 0.5 hrs by ELISA analysis
Anti-inflammatory activity in mouse J774.A1 cells assessed as inhibition of LPS-induced IL-6 production pre-stimulated with LPS for 24 hrs followed by compound addition and measured after 0.5 hrs by ELISA analysis
[PMID: 37130331]
J774.A1 IC50
2.17 3
Compound: c17
Anti-inflammatory activity in mouse J774.A1 cells assessed as inhibition of LPS-induced IL-6 production pre-stimulated with LPS for 24 hrs followed by compound addition and measured after 0.5 hrs by ELISA analysis
Anti-inflammatory activity in mouse J774.A1 cells assessed as inhibition of LPS-induced IL-6 production pre-stimulated with LPS for 24 hrs followed by compound addition and measured after 0.5 hrs by ELISA analysis
[PMID: 37130331]
J774.A1 IC50
8.17 3
Compound: c17
Anti-inflammatory activity in mouse J774.A1 cells assessed as inhibition of LPS-induced TNF-alpha production pre-stimulated with LPS for 24 hrs followed by compound addition and measured after 0.5 hrs by ELISA analysis
Anti-inflammatory activity in mouse J774.A1 cells assessed as inhibition of LPS-induced TNF-alpha production pre-stimulated with LPS for 24 hrs followed by compound addition and measured after 0.5 hrs by ELISA analysis
[PMID: 37130331]
J774.A1 IC50
8.17 3
Compound: c17
Anti-inflammatory activity in mouse J774.A1 cells assessed as inhibition of LPS-induced TNF-alpha production pre-stimulated with LPS for 24 hrs followed by compound addition and measured after 0.5 hrs by ELISA analysis
Anti-inflammatory activity in mouse J774.A1 cells assessed as inhibition of LPS-induced TNF-alpha production pre-stimulated with LPS for 24 hrs followed by compound addition and measured after 0.5 hrs by ELISA analysis
[PMID: 37130331]
In Vitro

MyD88-IN-1 (10 μM, 24 h) exhibits significant anti-inflammatory effects in LPS (HY-D1056)-induced J774A.1 macrophages[1].
MyD88-IN-1 (40 or 80 μM, 2 h) restores IκB-α expression and inhibits p65 phosphorylation and nuclear translocation, indicating that it exerts anti-inflammatory effects by suppressing the NF-κB signaling pathway[1].
MyD88-IN-1 (40 or 80 μM, 2 h) exerts its anti-inflammatory activity in J774A.1 macrophages by inhibiting TLR4-MyD88 interaction[1].

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

Western Blot Analysis[1]

Cell Line: J774A.1 macrophages (mouse-derived)
Concentration: 40 μM, 80 μM
Incubation Time: 2 h
Result: Restored IκB-α expression, inhibited p65 phosphorylation and nuclear translocation.
In Vivo

MyD88-IN-1 (20 mg/kg, p.o., single dose) exhibits significant anti-inflammatory effects and alleviates lung tissue injury in the LPS (HY-D1056)-induced ALI mouse model[1].

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

Animal Model: LPS (HY-D1056)-induced acute lung injury (ALI) in C57BL/6L mice[1]
Dosage: 20 mg/kg
Administration: Oral gavage (p.o.), single dose, Administered 30 minutes before LPS induction
Result: Significantly reduced TNF-α and IL-6 levels in BALF and serum;
Decreased wet/dry lung ratio and total protein concentration;
Alleviated lung tissue histopathological changes.
Molekulargewicht

528.54

Formel

C23H24N6O7S

CAS. Nr.
Appearance

Solid

Color

Yellow to orange

SMILES

O=[N+](C1=CC=CC(CN2CCN(CC2)C3=CC=C(S(=O)(NC4=CN=C(C=C4)OC)=O)C=C3[N+]([O-])=O)=C1)[O-]

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 100 mg/mL (189.20 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 1.8920 mL 9.4600 mL 18.9200 mL
5 mM 0.3784 mL 1.8920 mL 3.7840 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.

  • Molaritätsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation

Purity: 99.95%

Verweise

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 1.8920 mL 9.4600 mL 18.9200 mL 47.3001 mL
5 mM 0.3784 mL 1.8920 mL 3.7840 mL 9.4600 mL
10 mM 0.1892 mL 0.9460 mL 1.8920 mL 4.7300 mL
15 mM 0.1261 mL 0.6307 mL 1.2613 mL 3.1533 mL
20 mM 0.0946 mL 0.4730 mL 0.9460 mL 2.3650 mL
25 mM 0.0757 mL 0.3784 mL 0.7568 mL 1.8920 mL
30 mM 0.0631 mL 0.3153 mL 0.6307 mL 1.5767 mL
40 mM 0.0473 mL 0.2365 mL 0.4730 mL 1.1825 mL
50 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9460 mL
60 mM 0.0315 mL 0.1577 mL 0.3153 mL 0.7883 mL
80 mM 0.0237 mL 0.1183 mL 0.2365 mL 0.5913 mL
100 mM 0.0189 mL 0.0946 mL 0.1892 mL 0.4730 mL
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  • 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.

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Produktname:
MyD88-IN-1
Art. -Nr.:
HY-149992
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