Search Result
Results for "
p53 Activator
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-148404
-
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MDM-2/p53
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Cancer
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p53 Activator 5 (compound 134A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 5 can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA. p53 Activator 5 shows anti-tumor activity . p53 Activator 5 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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-
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- HY-148402
-
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MDM-2/p53
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Cancer
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p53 Activator 3 (compound 87A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 3 can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA. p53 Activator 3 shows anti-tumor activity . p53 Activator 3 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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-
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- HY-148416
-
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MDM-2/p53
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Cancer
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p53 Activator 7 is a p53 mutation Y220C (MDM-2/p53) activator with an EC50 of 104 nM. p53 Activator 7 can bind to p53 mutant and restore its ability to bind DNA (WO2022213975A1; Example B-1) . p53 Activator 7 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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-
-
- HY-156919
-
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MDM-2/p53
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Cancer
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p53 Activator 8 (compound 5) is a p53 activator. p53 Activator 8 has potent anti-proliferative activity against MCF7 breast cancer cell lines with an IC 50 value of 0.5 μM .
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-
-
- HY-168636
-
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DNA Methyltransferase
MDM-2/p53
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Cancer
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p53 Activator 13 (compound 11) is a 6mA methyltransferase CamA inhibitor and a p53 activator. p53 Activator 13 intercalates into CamA-bound DNA via the minor groove, causing a conformational shift that moves the catalytic domain away from the DNA and elicits DNA damage response via p53 activation. p53 Activator 13 can be utilized in cancer research .
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- HY-158151
-
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MDM-2/p53
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Cancer
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p53 Activator 12 (compound 510B) is a potent p53 activator. p53 Activator 12 binds to mutant p53 and restores the ability of the p53 mutant to bind DNA .
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-
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- HY-160450
-
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MDM-2/p53
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Cancer
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p53 Activator 11 (compound A-1) is a potent p53 activator with an EC50 value of 0.478 µM for p53 (Y220C). p53 Activator 11 has the potential for the research of cancer .
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-
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- HY-160449
-
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MDM-2/p53
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Cancer
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p53 Activator 10 (Example C-2) is a compound that targets the y220c mutant of p53. p53 Activator 10 activation is involved in the downstream effects of tumor suppression .
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- HY-160448
-
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Others
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Cancer
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p53 Activator 9 (example D-4) is a p53 activator with EC50 of 1.699μM .
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-
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- HY-146095
-
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MDM-2/p53
DNA/RNA Synthesis
Apoptosis
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Cancer
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p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
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-
-
- HY-155974
-
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MDM-2/p53
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Cancer
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MeOIstPyrd is an anti-skin cancer agent. MeOIstPyrd inhibits cell proliferation, migration, and spheroid formation by activating the mitochondrial intrinsic apoptotic pathway. MeOIstPyrd induces DNA damage. MeOIstPyrd activates p53, and increases the half-life of p53 and stabilizes p53 by phosphorylating it at ser15. MeOIstPyrd binds to MDM2 in the p53 sub-pocket and blocks p53-MDM2 interaction .
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- HY-113843
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Others
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Cancer
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RETRA (hydrobromide) is a mutant p53-dependent activator of p73 that can inhibit cancer cells carrying mutant p53. RETRA (hydrobromide) increases the expression level of p73, induces transcriptional activation of several common to transcriptional targets p53 and p73, which leads to mutant p53- and p73-dependent inhibition of tumor growth, reduction of colony formation and induction of effector caspases .
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- HY-N12233
-
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Apoptosis
MDM-2/p53
Reactive Oxygen Species
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Cancer
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Condurango glycoside A is an activator of p53. Condurango glycoside A initiates ROS generation and up-regulates p53 expression. Condurango glycoside A induces apoptosis and pre-mature senescence associated with DNA damage in HeLa cells .
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- HY-151170
-
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MDM-2/p53
Apoptosis
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Cancer
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MDM2/4-p53-IN-2 (2q) is a potent dual MDM2/ MDM4 inhibitor and p53 activator with the IC50 values of 70.7 nM for MDM2- p53 and 81.4 nM for MDM4-p53 complexes. MDM2/4-p53-IN-2 regulates the cell cycle, induces cell apoptosis and has anticancer activity .
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- HY-108636
-
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MDM-2/p53
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Cancer
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RETRA is a mutant p53-dependent activator of p73 that suppresses mutant p53-bearing cancer cells. RETRA increases the expression level of p73, and a release of p73 from the blocking complex with mutant p53, which produces tumor-suppressor effects .
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- HY-107466
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MDM-2/p53
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Cancer
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WK298 is a potent inhibitor of the MDM2/MDMX-p53 interaction with good anti-tumor activity. WK298 can fully activate the p53 pathway by inhibiting the binding of MDM2 and MDMX to p53. The development of WK298 benefited from a deep understanding of the key elements of the p53-MDM2/MDMX interaction structure .
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- HY-19339
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-
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- HY-U00441
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DPBQ
1 Publications Verification
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MDM-2/p53
Apoptosis
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Cancer
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DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells .
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- HY-U00442
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CTX1
1 Publications Verification
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MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
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CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system .
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- HY-148408
-
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Sirtuin
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Cancer
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SIRT2-IN-11 (AEM1) is a selective SIRT2 inhibitor with an IC50 value of 18.5 μM. SIRT2-IN-11 p53-dependently induces apoptosis, activates expression of CDKN1A, PUMA and NOXA, and increases acetylation of p53. SIRT2-IN-11 can be used for the research of p53-related cancers .
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- HY-110088
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MDM-2/p53
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Cancer
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SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
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- HY-162247
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MDM-2/p53
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Cancer
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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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- HY-108638
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MDM-2/p53
Apoptosis
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Cancer
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NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and can be used for breast cancer research. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes .
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- HY-18329
-
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MDM-2/p53
STAT
Apoptosis
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Cancer
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TDP-665759 is an inhibitor for HDm2:p53 complex, and thus activates p53, inhibits STAT3 signaling pathway (EC50 of 5.90 μM) and the cell viability of p53 expressing A549R (IC50 of 7.02 μM). TDP-665759 induces apoptosis in HepG2. TDP-665759 exhibits antitumor efficacy in mouse models .
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- HY-19896
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COTI-2
2 Publications Verification
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MDM-2/p53
Apoptosis
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Cancer
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COTI-2, an anti-cancer agent with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation .
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- HY-162432
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MDM-2/p53
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Cancer
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MDM2-IN-27 targets MDM2 protein (Ki = 0.4 nM). MDM2-IN-27 activates the anti-tumor activity of p53 and induces apoptosis by blocking the negative regulation of p53 by MDM2 .
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- HY-110315
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Apoptosis
MDM-2/p53
Epigenetic Reader Domain
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Cardiovascular Disease
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Ischemin sodium is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin sodium salt inhibits p53-induced p21 activation with an IC50 value of 5 µM. Ischemin sodium salt also prevents apoptosis in ischemic cardiomyocytes. Ischemin sodium salt can be used in the study of cardiovascular diseases (such as myocardial ischemia) .
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- HY-120084
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Casein Kinase
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Cancer
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BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNA damage response (DDR) and p53, while stabilizing p53 antagonist MDM2.
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- HY-169240
-
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MDM-2/p53
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Cancer
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MX69-102 (compound MX69-102) is an MDM-2/p53 inhibitor, inducing MDM2 degradation, resulting in p53 activation and cancer cell apoptosis. MX69-102 shows effective inhibition on xenografted human MDM2-overexpressing ALL in SCID mice. .
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- HY-100354
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-
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- HY-115833
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Others
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Cancer
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Histamine H4 receptor antagonist-2 serves as a potent activator of p53, demonstrating significant antitumor efficacy.
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- HY-13423
-
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MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
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Cancer
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Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor .
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- HY-13811
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E1/E2/E3 Enzyme
Apoptosis
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Cancer
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NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity .
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- HY-125858
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MI-1061
1 Publications Verification
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
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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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- HY-169369
-
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XJZ-06-462
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MDM-2/p53
Autophagy
Apoptosis
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Cancer
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TRAP-1 (XJZ-06-462) is ap53 transcriptional activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. TRAP-1 rapidly upregulates p21 and other p53 target genes in pancreatic cell lines with p53Y220C. TRAP-1 inhibits cell proliferation, with IC50 values of 3.94 and 0.531 μM in BxPC-3 and A549 cells, respectively. TRAP-1 regulates autophagy in lung cancer cells and offers protective effects against oxidative stress and cell apoptosis .
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- HY-15869
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INZ
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Sirtuin
MDM-2/p53
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Cancer
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Inauhzin is a dual SirT1/IMPDH2 inhibitor, and acts as an activator p53, used in the research of cancer.
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- HY-125858A
-
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
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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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- HY-N4225
-
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Adrenergic Receptor
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Endocrinology
Cancer
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Aaptamine, a spongean alkaloid isolated from a sea sponge Aaptos aaptos, is a competitive antagonist of α-adrenoceptor and activates the p21 promoter in a p53-independent manner .
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- HY-P1562
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Bcl-2 Family
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Cancer
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PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
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- HY-118542
-
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MDM-2/p53
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Cancer
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Nutlin 1, an antagonist of MDM2, activates a major cellular function of the p53 pathway, with an IC50 value of 0.26 μM .
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-
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- HY-14714
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XI-006
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MDM-2/p53
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Cancer
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NSC-207895 (XI-006), a DNA damaging agent, is an anticancer agent and p53 activator .
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-
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- HY-P1562A
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Bcl-2 Family
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Cancer
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PUMA BH3 TFA is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM .
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- HY-122038
-
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MDM-2/p53
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Cancer
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NU-8165 is an inhibitor of the MDM2-p53 protein-protein interaction with anti-tumor activity. Optimization of NU-8165 was guided by MDM2 NMR titrations, which indicated key binding interaction regions. NU-8165 activated MDM2 and p21 transcription in cell-based assays and showed modest selectivity for wild-type p53 cell lines .
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- HY-19634
-
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Sirtuin
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Cancer
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YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells .
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-
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- HY-103640
-
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WR-1065 dihydrochloride
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MDM-2/p53
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Cancer
|
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Amifostine thiol (WR-1065) dihydrochloride can protect normal tissues from the toxic effects of certain cancer agents and activate p53 through a JNK-dependent signaling pathway.
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-
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- HY-W016181
-
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2-Phenylhydroquinone
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MDM-2/p53
ERK
p38 MAPK
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Inflammation/Immunology
|
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Phenylhydroquinone (PHQ) is an orally active thymic atrophy inducer which can up-regulate apoptosis through activation of p53. PHQ can be used for research of thymic atrophy .
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-
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- HY-13735B
-
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Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrate
|
Parasite
Apoptosis
Autophagy
Mitophagy
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Infection
Cancer
|
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Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis .
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- HY-163083
-
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MDM-2/p53
Apoptosis
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Cancer
|
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JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC50 values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis .
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-
- HY-N7526
-
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DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone
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Apoptosis
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Neurological Disease
Cancer
|
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Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects .
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- HY-18935A
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Curaxin-137 hydrochloride; CBL-C137 hydrochloride
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MDM-2/p53
NF-κB
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Cancer
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CBL0137 hydrochloride is an inhibitor of the histone chaperone, FACT. CBL0137 hydrochloride can also activate p53 and inhibits NF-κB with EC50s of 0.37 and 0.47 µM, respectively.
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- HY-16271
-
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4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride
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MDM-2/p53
Apoptosis
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Cancer
|
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Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells .
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- HY-13735A
-
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Mepacrine dihydrochloride; SN-390 dihydrochloride
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Parasite
Apoptosis
Autophagy
Mitophagy
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Infection
Cancer
|
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Quinacrine (Mepacrine) dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis .
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- HY-13735E
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Mepacrine methanesulfonate; SN-390 methanesulfonate
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Parasite
Apoptosis
Autophagy
Mitophagy
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Infection
Cancer
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Quinacrine (Mepacrine) methanesulfonate is a potent, orally active antimalarial agent with antitumor effects in vitro and in vivo. Quinacrine dihydrochloride inhibits NF-κB and activates p53 signaling, inducing apoptosis in tumor cells .
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- HY-130437
-
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MDM-2/p53
TGF-β Receptor
Caspase
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Infection
Metabolic Disease
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p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].
non-alcoholic fatty liver disease .
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- HY-125858B
-
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Drug-Linker Conjugates for ADC
MDM-2/p53
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Others
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(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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- HY-16271S
-
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Isotope-Labeled Compounds
MDM-2/p53
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Cancer
|
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Kevetrin (hydrochloride)- 13C2, 15N3 is the 13C-labeled and 15N-labeled Kevetrin (hydrochloride). Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
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- HY-108433
-
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Carnitine palmitoyltransferase 2
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Apoptosis
MDM-2/p53
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Metabolic Disease
Cancer
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CPT2 (Carnitine palmitoyltransferase 2), an enzyme that participates in fatty acid oxidation, also is a colorectal cancer (CRC) prognostic biomarker. CPT2 overexpression can activate p-p53 to increase p53 expression, thereby inhibiting tumor proliferation and promoting apoptosis. CPT2 deficiency results in the most common inherited disorder of long-chain fatty acid oxidation affecting skeletal muscle. Downregulation of CPT2 is also highly correlated with the progression of various cancers and has potential for cancer research .
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- HY-N2693
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-
- HY-18330
-
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MDM-2/p53
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Cancer
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MI 63 is an activator for p53, by targeting the MDM2 (Ki is 3 nM). MI 63 inhibits the proliferation of embryonic and alveolar rhabdomyosarcoma (ERMS and ARMS) cells (IC50 is 0.58 μM in RH36 cells), and induces apoptosis in ERMS and ARMS .
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- HY-137864
-
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WR-1065
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MDM-2/p53
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Cancer
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Amifostine thiol (WR-1065) is an active metabolite of the cytoprotector Amifostine (HY-B0639). Amifostine thiol is a cytoprotective agent with radioprotective abilities. Amifostine thiol activates p53 through a JNK-dependent signaling pathway .
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- HY-118375
-
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ISC-4
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Apoptosis
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Cancer
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Phenylbutyl isoselenocyanate (ISC-4) is a selective apoptosis inducer that increases reactive oxygen species levels to inhibit androgen receptor (AR) and activate p53 pathway. Phenylbutyl isoselenocyanate induces apoptosis in LNCaP prostate cancer cells and has anti-prostate cancer properties.
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- HY-N2602
-
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MDM-2/p53
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Cancer
|
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Sanggenol L induces caspase-dependent and caspase-independent apoptosis in melanoma skin cancer cells . Sanggenol L induces of apoptosis via suppression of PI3K/Akt/mTOR signaling and cell cycle arrest via activation of p53 in p
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- HY-103640R
-
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MDM-2/p53
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Cancer
|
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Amifostine thiol (dihydrochloride) (Standard) is the analytical standard of Amifostine thiol (dihydrochloride). This product is intended for research and analytical applications. Amifostine thiol (WR-1065) dihydrochloride can protect normal tissues from the toxic effects of certain cancer agents and activate p53 through a JNK-dependent signaling pathway.
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- HY-124739
-
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Deubiquitinase
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Cancer
|
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HBX 28258 is a selective USP7 inhibitor, with an IC50 of 22.6 μM. HBX 28258 can covalently binds to Cys223 located in the catalytic core of USP7, inhibits its deubiquitinating activity, promotes MDM2 protein degradation, and activates p53 .
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- HY-13735AR
-
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Parasite
Apoptosis
Autophagy
Mitophagy
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Infection
Cancer
|
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Quinacrine (dihydrochloride) (Standard) is the analytical standard of Quinacrine (dihydrochloride). This product is intended for research and analytical applications. Quinacrine (Mepacrine) dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis .
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-
- HY-147783
-
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MDM-2/p53
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Cancer
|
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Anticancer agent 68 is (Compound 12) is an anti-cancer agent. Anticancer agent 68 arrests the cells at the G2/M phase and induces programmed cell death. Anticancer agent 68 induces upregulation of tumor suppression via activation of p53 & PTEN .
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- HY-15186
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Ipatasertib
Maximum Cited Publications
39 Publications Verification
GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
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Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-15186C
-
|
GDC-0068 tosylate; RG7440 tosylate
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-131031
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity .
|
-
- HY-W011434
-
|
TGIC
|
MDM-2/p53
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via?p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research .
|
-
- HY-136479
-
|
|
Sirtuin
|
Cancer
|
|
F0911-7667 is a SIRT1 activator that induces autophagic cell death in U87MG and T98G cells by activating the AMPK-mTOR-ULK complex. CWR tripeptide was also identified as a SIRT1 activator that reduced p53 acetylation in IMR32 neuroblastoma cells and protected cells from cell death induced by Aβ fragments .
|
-
- HY-139149
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC50 value of 0.35 μΜ. NiCur, which blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins .
|
-
- HY-155532
-
|
|
Apoptosis
|
Cancer
|
|
10m/ZS44 is a blood-brain barrier-permeable Glioblastoma (GBM) inhibitor. 10m/ZS44 significantly inhibits GBM tumor growth in a mouse xenograft model. 10m/ZS44 also activates the SIRT1/p53-mediated apoptosis pathway, thereby inhibiting the proliferation of U251 cells .
|
-
- HY-158210
-
|
|
Wnt
β-catenin
MDM-2/p53
|
Cancer
|
|
Wnt/β-catenin-IN-3 (compound 17) is a Wnt/β-catenin inhibitor with low micromolarGI50s against various cancer cells. Wnt/β-catenin-IN-3triggers G2/M cell cycle arrest though activation of p53-p21 pathway as well as intrinsic and extrinsic apoptotic death of colon cancer cells .
|
-
- HY-N0636
-
|
|
Apoptosis
|
Cancer
|
|
Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
|
-
- HY-18935
-
|
Curaxin 137; CBL-C137
|
Histone Acetyltransferase
MDM-2/p53
NF-κB
|
Cancer
|
|
CBL0137, a curaxin compound, is a histone chaperone facilitates chromatin transcription (FACT) inhibitor. CBL0137 downregulates NF-?B and activates p53. CBL0137 restores both histone H3 acetylation and trimethylation. CBL0137 is an anticancer agent. CBL0137 induces cancer cell apoptosis .
|
-
- HY-143412
-
|
|
HDAC
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo .
|
-
- HY-17548
-
|
|
Caspase
Apoptosis
|
Cancer
|
|
VMY-1-103 is an inhibitor for cyclin/Cdk complex, that arrests the cell cycle at G1 phase. VMY-1-103 reduces mitochondrial membrane potential, induces p53 phosphorylation and and PARP cleavage, activates caspase-3, and thus induces apoptosis in prostate cancer cell LNCaP .
|
-
- HY-100035
-
|
|
ROCK
ERK
CDK
Apoptosis
|
Cancer
|
|
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity .
|
-
- HY-114372
-
|
|
Lipoxygenase
Caspase
Apoptosis
|
Cancer
|
|
Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity . Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation .
|
-
- HY-134823
-
|
|
MDM-2/p53
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
|
MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects .
|
-
- HY-156135
-
|
|
RET
|
Others
|
|
NSC194598 is a p53 DNA-binding inhibitor with IC50 value of 180 nM and 2-40 μM for in vitro and in vivo, respectively. NSC194598 interferes with transcriptional activation of mutated RET gene in human medullary thyroid carcinoma TT cells. NSC194598 can be used for acute toxicity to normal tissues by radiation and chemotherapy research .
|
-
- HY-117857
-
-
- HY-143411
-
|
|
HDAC
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts .
|
-
- HY-Y0148
-
|
NSC 15139; 10-HDAA
|
Parasite
Autophagy
NF-κB
Interleukin Related
NO Synthase
MDM-2/p53
TNF Receptor
RANKL/RANK
Caspase
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid derived from 10-hydroxy-trans-2-decenoic acid, which can be isolated from royal jelly. 10-Hydroxydecanoic acid exhibits various biological activities, including anti-inflammatory, insecticidal, anti-malarial, and anti-Leishmania properties, as well as enhancing antigen-specific immune responses. The anti-inflammatory effects of 10-Hydroxydecanoic acid are primarily mediated by inhibiting the activation of NF-κB and the translation of interferon regulatory factor 1 (IRF-1), which reduces the production of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, 10-Hydroxydecanoic acid alleviates neuroinflammatory responses through the p53-autophagy pathway and the p53-NLRP3 pathway. Finally, 10-Hydroxydecanoic acid enhances antigen-specific immune responses by promoting the effective uptake of antigens by microfold cells .
|
-
- HY-N6771
-
|
|
Calcium Channel
5-HT Receptor
MDM-2/p53
Apoptosis
RSV
|
Infection
|
|
Cyclopiazonic acid is an endoplasmic reticulum calcium ATPase (ECAs) inhibitor and human respiratory syncytial virus (RSV) inhibitor (EC50 value of 4.13 μ M), which can reduce the antagonistic effect of 5-HT receptors in rat thoracic aorta, induce p53 dependent cell apoptosis and reproductive toxicity in mouse testes, and inhibit the biological activation of aflatoxin B [1][4][5].
|
-
- HY-146516
-
|
|
MDM-2/p53
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer .
|
-
- HY-N0636R
-
|
|
Apoptosis
|
Cancer
|
|
Eriocitrin (Standard) is the analytical standard of Eriocitrin. This product is intended for research and analytical applications. Eriocitrin is a flavonoid isolated from lemons that is a powerful antioxidant. Eriocitrin inhibits the proliferation of liver cancer cells by arresting the cell cycle in the S phase by upregulating p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating intrinsic signaling pathways involving mitochondria .
|
-
- HY-W011434R
-
|
|
MDM-2/p53
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Triglycidyl isocyanurate (Standard) is the analytical standard of Triglycidyl isocyanurate. This product is intended for research and analytical applications. Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via?p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research .
|
-
- HY-15510
-
|
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
|
Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH) .
|
-
- HY-15510B
-
|
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
|
Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH) .
|
-
- HY-107426
-
|
Muconomycin A
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53 .
|
-
- HY-125010
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Dicycloplatin is a DNA damage inducer. Dicycloplatin induces DNA damage by activating biphosphorylated checkpoint kinase 2 (CHK2), breast cancer 1 (BRCA1) and triphosphorylated p53. Dicycloplatin can induce cell cycle arrest, inhibit proliferation and lead to apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. Dicycloplatin can be used in cancer researchr .
|
-
- HY-B0294
-
|
|
Parasite
Microtubule/Tubulin
STAT
MDM-2/p53
Apoptosis
Autophagy
|
Infection
Cancer
|
|
Flubendazole is an anthelmintic drug based on altering microtubule structure, inhibition of tubulin polymerization and disruption of microtubule function. Flubendazole induces apoptosis in human colorectal cancer (CRC) by blocking the STAT3 signaling axis and activation of autophagy. Flubendazole induces P53 expression and reduced Cyclin B1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites .
|
-
- HY-13721
-
|
Idronoxil; Dehydroequol; Haginin E
|
Caspase
Apoptosis
Topoisomerase
|
Cancer
|
|
Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner .
|
-
- HY-123929
-
|
|
MDM-2/p53
Wnt
IKK
Apoptosis
Caspase
|
Cancer
|
|
PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model .
|
-
- HY-118912
-
|
|
Orphan Receptor
Others
|
Inflammation/Immunology
Cancer
|
|
BMH-9 (Compound Z54) is a modulator for nuclear receptor subfamily 2, group F, member 6 (NR2F6) (also known as nuclear orphan receptor Ear2) . BMH-9 is an activator for p53 signaling pathway through interaction with DNA. BMH-9 inhibits proliferation of human cancer cells, exhibits antitumor efficacy in NOD-SCID mouse models .
|
-
- HY-B0413
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
Cancer
|
|
Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-100671
-
|
|
Histone Acetyltransferase
STAT
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an?IC50?of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment .
|
-
- HY-10412
-
|
KT7515
|
JNK
Mixed Lineage Kinase
MDM-2/p53
|
Neurological Disease
|
|
CEP-1347 is an inhibitor of the JNK/SAPK pathway with neuroprotective effects. CEP-1347 blocks JNK1 activation induced by members of the mixed lineage kinase (MLK) family (MLK3, MLK2, MLK1, dual leucine zipper kinase, and leucine zipper kinase). As an inhibitor of MDM4, CEP-1347 can more effectively inhibit the growth of glioma cells expressing wild-type p53 .
|
-
- HY-B0294R
-
|
|
Parasite
Microtubule/Tubulin
STAT
MDM-2/p53
Apoptosis
Autophagy
|
Infection
Cancer
|
|
Flubendazole (Standard) is the analytical standard of Flubendazole. This product is intended for research and analytical applications. Flubendazole is an anthelmintic drug based on altering microtubule structure, inhibition of tubulin polymerization and disruption of microtubule function. Flubendazole induces apoptosis in human colorectal cancer (CRC) by blocking the STAT3 signaling axis and activation of autophagy. Flubendazole induces P53 expression and reduced Cyclin B1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites .
|
-
- HY-169002
-
|
|
Phosphatase
|
Cancer
|
|
PP5-IN-2 is an orally active and selective protein phosphatase 5 (PP5) inhibitor with an IC50 value of 0.9 μM. PP5-IN-2 activates p53 and downregulates cyclin D1 and MGMT, which shows potency in cell cycle arrest and reverses Temozolomide (TMZ) (HY-17364) resistance in the U87 MG cell line. PP5-IN-2 effectively inhibits tumor growth in the xenograft mouse model .
|
-
- HY-162886
-
|
|
JNK
Reactive Oxygen Species
|
Cancer
|
|
BSO-07 is a ROS/JNK activator with significant anticancer effects, having an IC50 value of 24.81 μM against human breast cancer (BC) cells. BSO-07 induces apoptosis (Apoptosis) and paraptosis by activating JNK and increasing ROS levels, including enhancing the expression of apoptosis-associated proteins such as PARP, Bax, phosphorylated p53, ATF4, and CHOP, while decreasing the levels of anti-apoptotic proteins like Bcl-2, Bcl-xL, and Survivin. BSO-07 holds promise for research in the field of breast cancer .
|
-
- HY-B0413R
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
|
|
Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-122815
-
|
Fusicoccin A
|
Apoptosis
|
Cancer
|
|
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity .
|
-
- HY-127057
-
|
|
Androgen Receptor
CDK
MDM-2/p53
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
|
Lambertianic acid is a bioactive diterpene with anti-allergic, antibacterial and anticancer activities. Lambertianic acid decreases androgen receptor protein levels, cellular and secretory levels of prostate-specific antigen. Lambertianic acid also suppresses cell proliferation by inducing G1 arrest, downregulating CDK4/6 and cyclin D1, activating p53, p21 and p27. Lambertianic acid induces Apoptosis and the expression of related proteins, including cleaved caspase-3/9, c-PARP and BAX, and inhibited BCl-2. Lambertianic acid is promising for research of prostate cancer .
|
-
- HY-161874
-
|
|
Apoptosis
MDM-2/p53
Bcl-2 Family
Caspase
PARP
Autophagy
|
Cancer
|
|
RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrial membrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity .
|
-
- HY-130326
-
|
Ru(η6-p-cymene)Cl2(pta)
|
Apoptosis
Caspase
|
Cardiovascular Disease
Cancer
|
|
RAPTA-C (Ru(η6-p-cymene)Cl2(pta)) acts as an anti-cancer and anti-angiogenic agent. RAPTA-C exhibits anti-metastatic, anti-angiogenic, and anti-tumoral activities through protein and histone-deoxyribonucleic acid alterations. RAPTA-C exhibits cell growth inhibition by triggering G(2)/M phase arrest in cancer cells. RAPTA-C also enhances the levels of p53 and triggers the mitochondrial Apoptotic pathway, resulting in cytochrome C release and caspase-9 activation. RAPTA-C reduces the growth of tumors with the inhibition of angiogenesis in a ovarian carcinoma model .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1562
-
|
|
Bcl-2 Family
|
Cancer
|
|
PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
|
-
- HY-P1562A
-
|
|
Bcl-2 Family
|
Cancer
|
|
PUMA BH3 TFA is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N12233
-
-
-
- HY-100354
-
-
-
- HY-N7526
-
-
-
- HY-N2602
-
-
-
- HY-N0636
-
-
-
- HY-Y0148
-
|
NSC 15139; 10-HDAA
|
Structural Classification
Animals
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Inflammation/Immunology
Disease Research Fields
|
Parasite
Autophagy
NF-κB
Interleukin Related
NO Synthase
MDM-2/p53
TNF Receptor
RANKL/RANK
Caspase
|
|
10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid derived from 10-hydroxy-trans-2-decenoic acid, which can be isolated from royal jelly. 10-Hydroxydecanoic acid exhibits various biological activities, including anti-inflammatory, insecticidal, anti-malarial, and anti-Leishmania properties, as well as enhancing antigen-specific immune responses. The anti-inflammatory effects of 10-Hydroxydecanoic acid are primarily mediated by inhibiting the activation of NF-κB and the translation of interferon regulatory factor 1 (IRF-1), which reduces the production of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, 10-Hydroxydecanoic acid alleviates neuroinflammatory responses through the p53-autophagy pathway and the p53-NLRP3 pathway. Finally, 10-Hydroxydecanoic acid enhances antigen-specific immune responses by promoting the effective uptake of antigens by microfold cells .
|
-
-
- HY-N6771
-
-
-
- HY-N4225
-
-
-
- HY-N2693
-
-
-
- HY-N0636R
-
-
-
- HY-122815
-
-
-
- HY-127057
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-16271S
-
|
|
|
Kevetrin (hydrochloride)- 13C2, 15N3 is the 13C-labeled and 15N-labeled Kevetrin (hydrochloride). Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
|
-
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