2. Metabolic Enzyme/Protease Neuronal Signaling NF-κB Immunology/Inflammation Stem Cell/Wnt MAPK/ERK Pathway
  3. Glycosidase Amyloid-β NF-κB COX ERK NO Synthase Interleukin Related
  4. K284-6111

K284-6111 is a high-affinity and orally active CHI3L1 inhibitor, and inhibits CHI3L1 expression. K284-6111 inhibits ERK and NF-κB pathway. K284-6111 suppresses nuclear translocation of p50 and p65, and phosphorylation of IκB. K284-6111 improves memory dysfunction by alleviating amyloidogenesis and neuroinflammation, with the reduction of inflammatory proteins (eg: iNOS, COX-2, GFAP, and Iba-1). K284-6111 reduces atopic-like skin inflammation and inhibits LPS (HY-D1056) -induced liver injury. K284-6111 can be used for the study of Alzheimer's diseases and sepsis like hepatic injury.

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

K284-6111

K284-6111 Chemical Structure

CAS No. : 702668-62-0

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Based on 1 publication(s) in Google Scholar

K284-6111 Related Antibodies

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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COX COX-1 COX-2 COX-3

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ERK ERK1 ERK2 ERK5 ERK8

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nNOS iNOS eNOS

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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  • Purity & Documentation

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  • Customer Review

Description

K284-6111 is a high-affinity and orally active CHI3L1 inhibitor, and inhibits CHI3L1 expression. K284-6111 inhibits ERK and NF-κB pathway. K284-6111 suppresses nuclear translocation of p50 and p65, and phosphorylation of IκB. K284-6111 improves memory dysfunction by alleviating amyloidogenesis and neuroinflammation, with the reduction of inflammatory proteins (eg: iNOS, COX-2, GFAP, and Iba-1). K284-6111 reduces atopic-like skin inflammation and inhibits LPS (HY-D1056) -induced liver injury. K284-6111 can be used for the study of Alzheimer's diseases and sepsis like hepatic injury[1][2][3][4].

In Vitro

K284-6111 (0.5-2 μM, 24 h) decreases the NO concentration induced by Aβ or LPS (HY-D1056) in BV-2 cells and astrocytes[1][2].
K284-6111 (5 μM, 26 h) decreases the neuroinflammation in CHI3L1 overexpressing BV-2 cells[1].
K284-6111 (5 μM, 26 h) inhibits the expression of PTX3 in Aβ-induced BV-2 cells[1].
K284-6111 (0.5-2 μM, 6 h) prevents nuclear translocation of p50 and p65 in LPS-stimulated microglial BV-2 cells and astrocytes and TNF-α/IFN-γ-activated HaCaT cells[2][3].
K284-6111 (0.5-2 μM, 4 h) inhibits the level of CHI3L1, IL-1β, IL-4, IL-6, LTF and TSLP in HaCaT cells treated with TNF-α/IFN-γ combination[3].
K284-6111 (2 μM, 6 days) attenuates the inflammation in the atopic-like reconstructed human skin (RHS) model[3].
K284-6111 (0.5-22 μM, 1 h) reduces the expression of CHI3L1, CXCL3 and the release of cytokine in LPS-induced hepatic cells[4].
K284-6111 (2 μg/mL, 25 h) reduces IL-10 and IL-4 levels in both THLE-2 cells treated with human recombinant CXCL3 and LPS, and in CXCL3 knockdown THLE-2 cells treated with LPS[4].

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

K284-6111 Related Antibodies

Western Blot Analysis[1]

Cell Line: Aβ-induced BV2 cells and CHI3L1 overexpressing BV-2 cells
Concentration: 5 μM
Incubation Time: 26 h
Result: Reduced Aβ-induced expression of inflammatory proteins such as iNOS, COX-2, and IBA-1.

Real Time qPCR[1]

Cell Line: Aβ-induced BV2 cells and CHI3L1 overexpressing BV-2 cells
Concentration: 5 μM
Incubation Time: 26 h
Result: Reduced the mRNA expression level of pro-inflammatory cytokines such as Tnf, Il1b, Il6, and Cd86.

ELISA Assay[3]

Cell Line: HaCaT cells treated with TNF-α/IFN-γ combination
Concentration: 0.5, 1, 2 μM
Incubation Time: 4 h
Result: Decreased the level of CHI3L1, IL-1β, IL-4, IL-6 and TSLP.

Western Blot Analysis[3]

Cell Line: HaCaT cells treated with TNF-α/IFN-γ combination
Concentration: 0.5, 1, 2 μM
Incubation Time: 6 h
Result: Inhibited the nuclear translocation of p50 and p65 and p-IκBα.

Real Time qPCR[4]

Cell Line: LPS-induced hepatic cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 1 h
Result: Reduced the mRNA levels of M1 macrophage protein and cytokines (iNOS, CD86, TNF-α, and IL-6) and M2 macrophage cytokines (MRC1, Arg 1, IL-10, and IL-4).
In Vivo

K284-6111 (3 mg/kg, i.g., once daily, 4 weeks) alleviates memory impairment in Tg2576 AD mouse model[1].
K284-6111 (3 mg/kg, i.g., once daily, 4 weeks) prevents memory impairment in Aβ1-42-infused mice[2].
K284-6111 (1-2 mg/mL (10-20 μg/cm2), topical administration, 3 times a week, 4 weeks) inhibits Phthalic anhydride (HY-I0815)-induced atopic dermatitis[3].
K284-6111 (0.25-1 mg/kg, i.p., once every three days, 2 weeks) exhibits protective effects against LPS-induced liver injury[4].

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

Animal Model: Twelve-month-old Tg2576 mice[1]
Dosage: 3 mg/kg
Administration: i.g. once daily for 4 weeks
Result: Increased the mean time spent in the target quadrant.
Showed higher an average step-through latency.
Inhibited the accumulation of Aβ in Tg2576 mouse brain.
Reduced the number of iNOS and COX-2-reactive cells.
Decreased the expression of GFAP, IBA-1, iNOS, and COX-2.
Decreased the expression levels of the markers M1 microglia (Tnf, Il1b, Il6, and Cd86).
Did not affect M2 microglia markers such as Arg1, Mrc1, Tgfb, and Il10.
Reduced the levels of p-IκBα, p-ERK1/2, and p-JNK.
Reduced the levels of PTX3.
Animal Model: Aggregated Aβ1-42 (300 pmol) was unilaterally infused into the brains of 8- to 10-week-old male ICR mice over 14 days[2]
Dosage: 3 mg/kg
Administration: i.g. once daily for 4 weeks
Result: Showed a great reduction in escape latency on day 6.
Showed a shorter escape distance compared to Aβ1-42-infused mice.
Spent much more time in the quadrant zone.
Increased step-through latency.
Reduced the expression of CHI3L1, inflammatory proteins (iNOS and COX-2), and GFAP and Iba-1.
Decreased Aβ-induced mRNA levels of CHI3L1, TNF-α, IL-1β, and IL-6 in brain tissues.
Prevented amyloidogenesis and neuronal cell death in Aβ1-42-infused mice brain.
Decreased the expression of p50 p65 and p-IκBα.
Animal Model: C57BL/6J mice (8-week-old) applied with 5% Phthalic anhydride (PA) solution was spread on the back skin 3 times a week for 4 weeks[3]
Dosage: 1 mg/mL and 2 mg/mL (10 μg or 20 μg/cm2)
Administration: Topical administration 3 times a week for 4 weeks
Result: Reduced epidermal thickness.
Reduced the number of infiltrating mast cells in the skin.
Decreased the serum IgE concentration.
Reduced the lymph node weight.
Reduced the levels of CHI3L1, IL-1β, IL-4, IL-6 and TSLP.
Reduced the mRNA expression of AD-related genes such as TNF-α, IL-1β, IL-4, IL-5, IL-6, IL-13, IL-31, IL-33, and CCL17.
Inhibited the nuclear translocation of p50 and p65 in a dose-dependent manner.
Reduced LTF expression in PA-induced skin tissues.
Animal Model: C57BL/6J mice (8-week-old) were injected with LPS (i.p., 30 mg/kg)[4]
Dosage: 0.25, 0.5, 1 mg/kg
Administration: i.p. once every three days for 2 weeks
Result: Showed the induction of significant liver damage.
Reduced CHI3L1 expression and cytokine release (iNOS, COX-2) in LPS-induced liver injury.
Molecular Weight

535.70

Formula

C30H37N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(N=C(N1CCC3=CCCCC3)SC(CC)C(NC4=CC=C(CC)C=C4)=O)C=C(OC)C(OC)=C2
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 : 2 mg/mL (3.73 mM; ultrasonic and warming and heat to 60°C; 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 1.8667 mL 9.3336 mL 18.6672 mL
5 mM --- --- ---
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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  15% Cremophor EL    85% Saline

    Solubility: 1.67 mg/mL (3.12 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 99.94%

SDS (251 KB)

COA (248 KB) HNMR (271 KB) LCMS (97 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. 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 1.8667 mL 9.3336 mL 18.6672 mL 46.6679 mL
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K284-6111 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:

K284-6111702668-62-0GlycosidaseAmyloid-βNF-κBCOXERKNO SynthaseInterleukin Relatedβ-amyloid peptideAβAbetaNuclear factor-κBNuclear factor-kappaBCyclooxygenaseExtracellular signal regulated kinasesNitric oxide synthasesNOSILAlzheimer’s diseaseNeuroinflammationCHI3L1LactoferrinAtopic dermatitisInhibitorinhibitorinhibit

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