Cat. No.: HY-148013

K284-6111

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

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.

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Pureté: 99.94%
CAS No.: 702668-62-0
Formule: C₃₀H₃₇N₃O₄S
Masse moléculaire:535.70

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

K284-6111 Chemical Structure

CAS No.: 702668-62-0

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform NF-κB :

Voir tous les produits spécifiques à Isoform COX :

Voir tous les produits spécifiques à Isoform ERK :

Voir tous les produits spécifiques à Isoform NO Synthase :

Voir tous les produits spécifiques à Isoform Interleukin Related :

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.

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 Aβ_1-42-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 Aβ_1-42 (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 Aβ_1-42-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 Aβ_1-42-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.

Chemical Information

CAS No. 702668-62-0
Appearance Solid
Masse moléculaire 535.70
Formule C₃₀H₃₇N₃O₄S
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Life Sci

CHI3L1 promotes macrophage pyroptosis in ulcerative colitis via the BCAT1/NF-κB axis. [Abstract]

2026 Jan 1:384:124108. PMID: 41314595
Mol Cell Biochem

CHI3L1: a novel regulator of vascular remodeling in pulmonary arterial hypertension. [Abstract]

2026 May;481(5):2063-2081. PMID: 41910909

Solvant et solubilité

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)

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10 mg

Concentration

Solvent

Mass

1 mM

1.8667 mL

9.3336 mL

18.6672 mL

5 mM

---

10 mM

---

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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Pureté et documentation

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Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
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Références

[1]. Ham HJ, et al. K284-6111 alleviates memory impairment and neuroinflammation in Tg2576 mice by inhibition of Chitinase-3-like 1 regulating ERK-dependent PTX3 pathway. J Neuroinflammation. 2020 Nov 22;17(1):350. [Content Brief]

[2]. Choi JY, et al. K284-6111 prevents the amyloid beta-induced neuroinflammation and impairment of recognition memory through inhibition of NF-κB-mediated CHI3L1 expression. J Neuroinflammation. 2018 Aug 11;15(1):224. [Content Brief]

[3]. Jeon SH, et al. Inhibition of Chitinase-3-like-1 by K284-6111 Reduces Atopic Skin Inflammation via Repressing Lactoferrin. Immune Netw. 2021 Jun 29;21(3):e22. [Content Brief]

[4]. Inhibition of Chitinase-3-like-1 expression by K284 ameliorates lipopolysaccharide-induced acute liver injury through down regulation of CXCL3.

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	1.8667 mL	9.3336 mL	18.6672 mL	46.6679 mL

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K284-6111

2 Cited Publications

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K284-6111

Immunology/Inflammation Compound Library

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Publications Citing Use of MedChemExpress (MCE) K284-6111

Voir tous les produits spécifiques à Isoform NF-κB

Voir tous les produits spécifiques à Isoform COX

Voir tous les produits spécifiques à Isoform ERK

Voir tous les produits spécifiques à Isoform NO Synthase

Voir tous les produits spécifiques à Isoform Interleukin Related

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

K284-6111 Related Classifications

HY-148013 Related Classifications