HB-230
Based on 1 Customer Validation
HB-230 is a Transglutaminase-2 (TG2) (human IC50 = 4.9 μM) inhibitor and a selective fluorescent imaging probe for active TG2 localization. HB-230 modifies TG2 Cys277 to sustain the enzyme open conformation. HB-230 forms a ternary complex with TG2 and α2-macroglobulin, undergoes receptor-mediated endocytosis, and trafficks directly to lysosomes without early/late endosome fusion. HB-230 exhibits TG2 activity-dependent and α2-macroglobulin-dependent uptake. HB-230 can be used for the research of celiac disease, (Ex/Em = 649/665 nm).
For research use only. We do not sell to patients.
- Purity : 91.2%
- CAS No.: 3031522-14-9
- Formula: C66H86N10O14S2
- Molecular Weight:1307.58
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
HB-230 potently inhibits purified human TG2 with an IC50 of 4.9 μM[1].
HB-230 (1 μM; 3 h) labels active TG2 in wild-type MEFs with a punctate intracellular pattern near the nucleus, while showing no specific labeling in TG2-knockout MEFs[1].
HB-230 uptake in MEFs is dependent on LRP1, as uptake is robust in wild-type MEFs and severely reduced in LRP1-knockout MEFs[2].
HB-230 is metabolized by chymotrypsin and carboxypeptidase, undergoing sequential cleavage to form a C-terminal carboxylic acid metabolite and a truncated tetrapeptide[2].
HB-230 (1 μM; 90 min) undergoes α2M-dependent uptake into NRK cells via receptor-mediated endocytosis, and the resulting HB-230/TG2/α2M ternary complex is trafficked directly to lysosomes[1].
HB-230 undergoes α2M-dependent endocytosis by NRK cells and localizes to lysosomes, not early endosomes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 3031522-14-9
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Appearance Solid
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Molecular Weight 1307.58
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Formula C66H86N10O14S2
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Color Blue to dark blue
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SMILES
O=C(N1[C@@H](CCC1)C(N[C@H](C(N)=O)CC2=CC=CC=C2)=O)[C@@H](NC([C@H](CC/C=C/C(N(C)C)=O)NC([C@H]3N(CCC3)C(C)=O)=O)=O)CCNC(CCCCC[N+]4=C(/C=C/C=C/C=C5C(C)(C6=CC(S(=O)(O)=O)=CC=C6N\5C)C)C(C)(C)C7=CC(S(=O)([O-])=O)=CC=C47)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HB-230 Related Classifications
HY-165426 Related Classifications
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