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Cat. No.: HY-189658

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SMU-H1

SMU-H1 is a TLR2 agonist with a K_D of 12.1 nM for mouse TLR2 and an EC₅₀ of 5.14 nM in HEK-Blue hTLR2 cells. SMU-H1 binds TLR2 and activates MyD88-dependent signaling. SMU-H1 activates the NF-κB and MAPK signaling pathways. SMU-H1 induces proinflammatory cytokine production. SMU-H1 promotes M1 macrophage polarization and dendritic cell activation. SMU-H1 can be used for research on Lewis lung cancer.

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CAS No.: 2410782-67-9
화학식: C₁₈H₁₆F₃N₃O₃S
분자량:411.40

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

SMU-H1 Chemical Structure

CAS No.: 2410782-67-9

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

TLR2

12.1 nM (Kd)

TLR2

5.14 nM (EC₅₀)

NF-κB

MyD88

p38 MAPK

IKKα

IKKβ

p65

p38

JNK1

JNK2

ERK1

ERK2

IL-6

IL-1β

All Toll-like Receptor (TLR) Isoforms :

All NF-κB Isoforms :

All p38 MAPK Isoforms :

All IKK Isoforms :

All ERK Isoforms :

All JNK Isoforms :

All Interleukin Related Isoforms :

In Vitro

SMU-H1 (6.25-100 μM) directly binds recombinant mouse TLR2 with a K_D of 12.1 nM in SPR^[1].
SMU-H1 (0.001-10 μM; 24 h) is a specific TLR2 agonist with an EC₅₀ of 5.14 nM in HEK-Blue hTLR2 cells^[1].
SMU-H1 (0.02-100 μM; 24-72 h) shows detectable cytotoxicity against HEK-Blue hTLR2 and RAW 264.7 cells only at 100 μM, while exhibiting no obvious cytotoxicity against LLC cells^[1].
SMU-H1 (5-10 μM; 15-30 min) activates NF-κB and MAPK signaling in wild-type peritoneal macrophages in a TLR2-dependent manner^[1].
SMU-H1 (24 h) promotes M1-like macrophage polarization and dendritic cell activation through the TLR2 signaling pathway^[1].
SMU-H1 (0.01-10 μM; 24 h) induces TNF-α, IL-6, and IL-1β production in RAW 264.7, THP-1, and mouse peritoneal macrophages in a dose-dependent and TLR2-dependent manner^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

HEK-Blue hTLR2 cells, RAW 264.7 cells, and LLC cells
Concentration:

0.02 μM; 0.05 μM; 0.14 μM; 0.41 μM; 1.23 μM; 3.70 μM; 11.11 μM; 33.33 μM; 100 μM
Incubation Time:

24, 48, 72 h
Result:

Exerted detectable cytotoxic effects on HEK-Blue hTLR2 cells and RAW 264.7 cells only at a high concentration of 100 μM, and no obvious cytotoxic effect was observed in LLC cells.

Western Blot Analysis^[1]

Cell Line:

Wild-type peritoneal macrophages
Concentration:

5 μM; 10 μM
Incubation Time:

15 min; 30 min
Result:

Significantly induced the phosphorylation of IKKα/β, p65, p38, JNK1/2 and ERK1/2. Reduced the expression of phosphorylated IκBα.

Parmacokinetics

Species	Dose	Route	T_max	T_1/2	C_max	AUC_0-t	AUC_0-∞	F
Rat^[1]	2 mg/kg	i.v.	0.2 h	7.40 h	482.38 μg/L	2442.14 μg/L·h	2460.04 μg/L·h	/
Rat^[1]	20 mg/kg	p.o.	9 h	6.64 h	149.26 μg/L	2260.59 μg/L·h	2294.92 μg/L·h	9.26 %

In Vivo

SMU-H1 (10 mg/kg; intraperitoneal injection; once every 2 days; days 14-26) combined with 5-FU (5-Fluorouracil) (HY-90006) (5 mg/kg; intraperitoneal injection; once every 2 days; days 14-26) produces stronger antitumor effects than either single agent in the LLC mouse model, including reducing excised tumor weight^[1].
SMU-H1 (10 mg/kg; intraperitoneal injection; once every 2 days; days 14-26) inhibits LLC tumor growth in C57BL/6 mice, reduces excised tumor weight, and promotes intratumoral immune cell infiltration^[1].

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

Animal Model:

C57BL/6 (male, 6-8 weeks)^[1]
Dosage:

SMU-H1 10 mg/kg
Administration:

i.p.; every 2 days; days 14-26
Result:

The vehicle group showed accelerated tumor growth, resulting in markedly larger tumor volume and heavier tumor weight than the SMU-H1- and 5-FU-treated groups.
The vehicle group exhibited heavier tumor weight than the SMU-H1-treated group.
Frequencies of total lymphocytes, NK cells, DCs, and M1-like macrophages within tumor tissue were significantly increased by SMU-H1.
Compared with the vehicle group, the SMU-H1 group had markedly higher proportions of CD4⁺ T cells and CD8⁺ T cells within tumor-infiltrating lymphocytes.
The numbers of NK cells, DCs, and M1-like macrophages in tumors were also proportionally elevated.
No significant differences in body weight were observed between the vehicle group and SMU-H1- and 5-FU-treated groups.

Animal Model:

C57BL/6 (male, 6−8 weeks)^[1]
Dosage:

SMU-H1 10 mg/kg combined with 5-FU 5 mg/kg
Administration:

i.p.; every 2 days; days 14-26
Result:

Combined administration of 5-FU and SMU-H1 exerted stronger antitumor efficacy than either alone, leading to further reduction in tumor volume.
In the same LLC efficacy study, excised tumors were dissected and weighed on day 27, and the vehicle group exhibited markedly heavier tumor weight than the combination-treated group.

Related Protocols :

Chemical Information

CAS No. 2410782-67-9
분자량 411.40
화학식 C₁₈H₁₆F₃N₃O₃S
SMILES

O=S(C1=CC=C(NC)C(N2C=C(C3=CC=C(C(F)(F)F)C=C3O)N=C2)=C1)(C)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Pan Y, et al. Design and Synthesis of Novel TLR2 Agonists for Regulating Tumor Microenvironment in Immunotherapy of Lung Cancer. J Med Chem. 2026;69:21483–21504.

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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SMU-H1

All Toll-like Receptor (TLR) Isoforms

All NF-κB Isoforms

All p38 MAPK Isoforms

All IKK Isoforms

All ERK Isoforms

All JNK Isoforms

All Interleukin Related Isoforms