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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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
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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