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Art. -Nr.: HY-132223

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LH1306

LH1306 is a C2-symmetric inhibitor of PD-₁/PD-L₁ protein-protein interaction (PPI), with an IC₅₀ value of 25 nM. LH1306 can be used in anti-tumor research.

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CAS. Nr.: 2182653-84-3
Formel: C₃₈H₄₈N₆O₆
Molecular Weight:684.82

Speicherung:

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

Data Sheet (263 KB)

LH1306 Chemical Structure

CAS. Nr.: 2182653-84-3

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

LH1306 is a C2-symmetric inhibitor of PD-₁/PD-L₁ protein-protein interaction (PPI), with an IC₅₀ value of 25 nM. LH1306 can be used in anti-tumor research^[1].

IC₅₀ & Target

IC50: 25 nM (PD-₁/PD-L₁)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	GI₅₀	3.1 μM Compound: 2a	Cytotoxicity against CHOK1 cells stably expressing human PDL1 co-cultured with human Jurkat T cell expressing human PD1 assessed as growth inhibition measured after 24 hrs by XTT assay Cytotoxicity against CHOK1 cells stably expressing human PDL1 co-cultured with human Jurkat T cell expressing human PD1 assessed as growth inhibition measured after 24 hrs by XTT assay	[PMID: 31298541]
HEK293	IC₅₀	25 nM Compound: 2a	Inhibition of human Fc-tagged PD1 N-terminal domain (Leu25 to Gln167 residues) expressed in HEK293 cells/human His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction after 1 hr by APC-labeled anti-His antibody/Eu- Inhibition of human Fc-tagged PD1 N-terminal domain (Leu25 to Gln167 residues) expressed in HEK293 cells/human His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction after 1 hr by APC-labeled anti-His antibody/Eu-	[PMID: 31298541]
Jurkat	EC₅₀	334 nM Compound: 2a	Inhibition of PD1/PDL1 interaction in human Jurkat cells co-cultured with human U2OS cells expressing PDL1 assessed as reduction in SHP1 recruitment preincubated with U2OS cells for 60 mins followed by Jurkat cell addition and measured after 2 hrs by Path Inhibition of PD1/PDL1 interaction in human Jurkat cells co-cultured with human U2OS cells expressing PDL1 assessed as reduction in SHP1 recruitment preincubated with U2OS cells for 60 mins followed by Jurkat cell addition and measured after 2 hrs by Path	[PMID: 31298541]
Jurkat	EC₅₀	4214 nM Compound: 2a	Inhibition of human PD1 stably expressed in human Jurkat T cells co-expressing NFAT-induced luciferase/human PDL1 stably expressed in CHOK1 cells co-expressing aAPC protein-protein interaction assessed as increase in NFAT signaling measured after 6 hrs by Inhibition of human PD1 stably expressed in human Jurkat T cells co-expressing NFAT-induced luciferase/human PDL1 stably expressed in CHOK1 cells co-expressing aAPC protein-protein interaction assessed as increase in NFAT signaling measured after 6 hrs by	[PMID: 31298541]
Jurkat	GI₅₀	3.1 μM Compound: 2a	Cytotoxicity against human Jurkat T cell expressing human PD1 co-cultured with CHOK1 cells stably expressing human PDL1 assessed as growth inhibition measured after 24 hrs by XTT assay Cytotoxicity against human Jurkat T cell expressing human PD1 co-cultured with CHOK1 cells stably expressing human PDL1 assessed as growth inhibition measured after 24 hrs by XTT assay	[PMID: 31298541]

Chemical Information

CAS. Nr. 2182653-84-3
Molecular Weight 684.82
Formel C₃₈H₄₈N₆O₆
SMILES

CC(NCCNCC(C(OC)=N1)=CC=C1OCC2=CC=CC(C3=CC=CC(COC4=CC=C(C(OC)=N4)CNCCNC(C)=O)=C3C)=C2C)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (263 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Basu S, et al. Design, synthesis, evaluation, and structural studies of C 2-symmetric small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 protein–protein interaction[J]. Journal of Medicinal Chemistry, 2019, 62(15): 7250-7263. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Keywords

MOQ

Minimum order quantity

100 mg

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