3031522-14-9
Chemical Structure
HB-230
- CAS No.: 3031522-14-9
- Formula:C66H86N10O14S2
- Molecular Weight:1307.58
InChIKey: ILCHGSXJNAIGGG-AFAVFPMXSA-N
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
Biological Activity: 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)[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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HB-230 | 91.2% | 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). | ||||||||||||||||||||
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References
- [1]. Loppinet E, et al. LRP-1 links post-translational modifications to efficient presentation of celiac disease-specific T cell antigens. Cell chemical biology. 2023 Jan 19;30(1):55-68.e10.
- [2]. Chaitan K, et al. COMPOSITIONS AND METHODS FOR TRANSGLUTAMINASE-MEDIATED ENDOCYTOSIS. WO/2024/049543. WIPO. 07.03.2024