2136246-72-3
2136246-72-3
Chemical Structure
MD-222
- CAS No.: 2136246-72-3
- Formula:C48H47Cl2FN6O6
- Molecular Weight:893.83
IUPAC Name: (3'R,4'S,5'R)-6''-chloro-4'-(3-chloro-2-fluorophenyl)-N-(4-((5-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)pentyl)carbamoyl)phenyl)-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-indoline]-5'-carboxamide
InChIKey: RRSNDVCODIMOFX-MPKOGUQCSA-N
SMILES: O=C1[C@]2(C3=CC=C(Cl)C=C3N1)C4(CCCCC4)N[C@H]([C@]2([H])C5=C(C(Cl)=CC=C5)F)C(NC6=CC=C(C=C6)C(NCCCCCC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8)=O)=CC=C7)=O)=O
Biological Activity: MD-222 is a potent MDM2 PROTAC degrader. MD-222 recruits the CRBN E3 ubiquitin ligase to target and degrade MDM2, and activates the wild-type p53 pathway in cells. MD-222 is used in relevant research on leukemia and breast cancer[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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MD-222 | 98.03% | MD-222 is a potent MDM2 PROTAC degrader. MD-222 recruits the CRBN E3 ubiquitin ligase to target and degrade MDM2, and activates the wild-type p53 pathway in cells. MD-222 is used in relevant research on leukemia and breast cancer. | ||||||||||||||||||||
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MD-224 | 99.60% | MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent. MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | ||||||||||||||||||||
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MI-1061 | 99.08% | MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity. | ||||||||||||||||||||
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MI-1061 TFA | 97.47% | MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity. | ||||||||||||||||||||
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(S,R,S)-MI-1061 | (S,R,S)-MI-1061 is the isomer of MI-1061(HY-125858). (S,R,S)-MI-1061 can used to synthesize Antibody-Drug Conjugates (ADCs). MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity. | |||||||||||||||||||||
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MG-277 | 98.68% | MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity. | ||||||||||||||||||||
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MI-2103 | MI-2103 is a MDM2 inhibitor with an IC50 of 48.1 nM. MI-2103 inhibits the growth of leukemia and breast cancer cells; it exerts no growth-inhibitory effect on cancer cells with p53 mutation or deletion. MI-2103 serves as a target protein ligand for the synthesis of MG-277 (HY-130122). MI-2103 is applicable to the research of leukemia and breast cancer. | |||||||||||||||||||||
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MI-1063 | MI-1063 is an inhibitor for MDM-2, that blocks the MDM2-p53 interaction, and activates the tumor suppressor function of p53. MI-1063 inhibits the growth of cancer cell RS4-11 and MV4-11 with IC50 of 179 nM and 93 nM. MI-1063 can be used as target protein ligand in synthesis of PROTAC degrader MD-265 (HY-169327). | |||||||||||||||||||||
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MDM2-IN-26 | MDM2-IN-26 (compound A3) is an MDM2 inhibitor that can activate the tumor suppressor function of p53 by blocking the interaction between MDM2 and p53 (MDM2 is the main negative regulator of p53). MDM2-IN-26 can be used for cancer research. | |||||||||||||||||||||
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MD-265 | 99.31% | MD-265 is a PROTAC degrader targeting MDM2, which activates p53 in cancer cells carrying wild-type p53. MD-265 induces MDM2 degradation by recruiting the CRL4-CRBN ligase complex via the ubiquitination and proteasomal degradation pathway. MD-265 upregulates p53 target genes, induces apoptosis, reduces Mcl-1 levels, increases caspase-3 cleavage, and inhibits colony formation of wild-type p53 leukemia stem cells. MD-265 can be used in research related to leukemia and acute myeloid leukemia. | ||||||||||||||||||||
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Seldegamadlin | 98.53% | Seldegamadlin (KT-253) is a cereblon-recruiting PROTAC degrader of MDM2, with a DC50 of 0.4 nM. Seldegamadlin catalyzes the ubiquitination and proteasomal degradation of MDM2, disrupts the MDM2/p53 autoregulatory feedback loop, induces apoptosis, caspase activation and p53 target gene expression, and inhibits the growth of wild-type p53 hematologic tumor cells and solid tumor cells. Seldegamadlin is applicable for the research of acute myeloid leukemia, acute lymphoblastic leukemia, diffuse large B-cell lymphoma and wild-type p53 solid tumors. | ||||||||||||||||||||
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References
- [1]. Yang J, et al. Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders. Journal of medicinal chemistry. 2019 Nov 14;62(21):9471-9487. [Content Brief]
- [2]. Anifowose A, et al. Anticancer strategies by upregulating p53 through inhibition of its ubiquitination by MDM2. Medicinal Chemistry Research 29.7 (2020): 1105-1121.
- [3]. Li Y, et al. Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression. Journal of medicinal chemistry. 2019 Jan 24;62(2):448-466. [Content Brief]
