2202678-04-2
Chemical Structure
HH2853
- CAS No.: 2202678-04-2
- Formula:C31H36F3N7O3
- Molecular Weight:611.66
IUPAC Name: (5S,6R,7R,9R)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9-tetrahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacene-14,16(15H)-dione
InChIKey: BIABSPVTTUDBEO-UHFFFAOYSA-N
SMILES: O=C(C1=CC2=C(C3=NN=C(C)C=C3)C=CN2C(C(C)N4CCN(CC(F)(F)F)CC4)=C1C)NCC5=C(OC)C=C(C)NC5=O
Biological Activity: HH2853 is an orally active EZH1/EZH2 inhibitor, with an IC50 of 9.26 nM for EZH1 and IC50 values ranging from 2.21 to 3.75 nM for both wild-type and mutant EZH2. HH2853 simultaneously inhibits the methyltransferase activities of EZH1 and EZH2, blocks the compensatory pathway that arises following EZH2 inhibition, and reduces H3K27me3 levels. HH2853 upregulates the expression of c-Myc and TfR-1 to induce intracellular iron accumulation, and stabilizes GPX4 via HSPA5 to suppress ferroptosis. HH2853 combined with Erastin (HY-15763) synergistically inhibits EZH2 wild-type DLBCL cell proliferation. HH2853 alone shows weak activity against EZH2 wild-type DLBCL and is well tolerated. HH2853 is applicable for research related to diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, epithelioid sarcoma, and follicular lymphoma[1][2].
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HH2853 | HH2853 is an orally active EZH1/EZH2 inhibitor, with an IC50 of 9.26 nM for EZH1 and IC50 values ranging from 2.21 to 3.75 nM for both wild-type and mutant EZH2. HH2853 simultaneously inhibits the methyltransferase activities of EZH1 and EZH2, blocks the compensatory pathway that arises following EZH2 inhibition, and reduces H3K27me3 levels. HH2853 upregulates the expression of c-Myc and TfR-1 to induce intracellular iron accumulation, and stabilizes GPX4 via HSPA5 to suppress ferroptosis. HH2853 combined with Erastin (HY-15763) synergistically inhibits EZH2 wild-type DLBCL cell proliferation. HH2853 alone shows weak activity against EZH2 wild-type DLBCL and is well tolerated. HH2853 is applicable for research related to diffuse large B-cell lymphoma, non-Hodgkin's lymphoma, epithelioid sarcoma, and follicular lymphoma. | |||||||||||||||||||||
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References
- [1]. Yu L, et al. Dysregulation of iron homeostasis by TfR-1 renders EZH2 wild type diffuse large B-cell lymphoma resistance to EZH2 inhibition. Acta pharmacologica Sinica. 2023 Oct;44(10):2113-2124.
- [2]. Chen X, et al. Pyrido five-element aromatic ring compound, preparation method therefor and use thereof: U.S. Patent 10,968,215[P]. 2021-4-6.
