MDM-2/p53 p53 Activator

PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC₅₀ values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces Apoptosis in cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML).

Rezatapopt (Standard) is the analytical standard of Rezatapopt (HY-156633). This product is intended for research and analytical applications. Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation.

Pancracine is an alkaloid. Pancracine upregulates p27, phosphorylated p38 MAPK and phosphorylated p53, while downregulating phosphorylated Akt and phosphorylated Rb. Pancracine induces G₁ cell cycle arrest and Apoptosis in cells. Pancracine inhibits the replication of pseudotyped HIV-1 and Dengue virus. Pancracine can be used in research related to lung adenocarcinoma, acute lymphoblastic leukemia, cutaneous epidermoid carcinoma, human immunodeficiency virus infection and dengue virus infection.

Decarbamoylmitomycin C, an analog of Mitomycin C (MC), is an DNA-alkylating agent. Decarbamoylmitomycin C (DMC) activates p53-independent ataxia telangiectasia and rad3 related protein (ATR) chromatin eviction.

NSC 146109 hydrochloride (Standard) is the analytical standard of NSC 146109 (hydrochloride) (HY-108638). This product is intended for research and analytical applications. 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.

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.

Benfluron hydrochloride is an Apoptosis inducer and inhibitor of the HIV-1 Rev-RRE complex, with an IC₅₀ of 5.0 μM against the HIV-1 Rev-RRE complex. Benfluron hydrochloride induces p53 activation, and triggers phosphorylation of Chk1 at serine 345, Chk2 at threonine 68, as well as ERK1/2 at threonine 202 and tyrosine 204. Benfluron hydrochloride activates Caspase 8, Caspase 9 and Caspase 3/7, inhibits HIV-1 viral transcription, and acts as a substrate for 11β-HSD 1 and cytosolic carbonyl reductase. Benfluron hydrochloride can be used in research related to leukemia and HIV-1 infection.

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.

MIRA-1 (Standard) is the analytical standard of MIRA-1 (HY-108639). This product is intended for research and analytical applications. MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutant p53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 has anticancer activity.

GO-Y078 is a curcumin (HY-N0005) analog. GO-Y078 activates p38/JNK1/2. GO-Y078 activates the MAPK pathway, Caspase 3/8/9, PARP, AP-1, DR5, and TP53, while inhibiting cIAP-1, XIAP, and NF-κB. GO-Y078 induces sub-G₁/G₂/M phase arrest and Apoptosis. GO-Y078 impairs angiogenesis. GO-Y078 can be used in research related to osteosarcoma, cervical cancer, oral squamous cell carcinoma, and peritoneal metastasis of gastric cancer.

SCH529074 (Standard) is the analytical standard of SCH529074 (HY-110088). This product is intended for research and analytical applications. SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a K_i 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).

PhiKan 083 (Standard) is the analytical standard of PhiKan 083 (HY-108637). This product is intended for research and analytical applications. PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a K_d of 167 μM. PhiKan 083 can be used for cancer research.

Versicolorin A is a biosynthetic precursor of Aflatoxin B1 (HY-N6615). Versicolorin A induces phosphorylation of p53. Versicolorin A activates the aryl hydrocarbon receptor AhR and significantly induces the expression of CYP1A1. Versicolorin A exerts genotoxic and cytotoxic effects. Versicolorin A enhances the genotoxicity of aflatoxin B1 in cells by promoting CYP450-mediated bioactivation of aflatoxin B1. Versicolorin A can be used in research related to colorectal cancer and hepatocellular carcinoma.

COTI-2 hydrochloride is an orally active thiosemicarbazone anticancer agent and p53 mutant activator. COTI-2 hydrochloride induces Apoptosis. COTI-2 hydrochloride triggers the activation of AMPK and the inhibition of the mTOR pathway. COTI-2 hydrochloride induces DNA damage and replication stress responses. COTI-2 hydrochloride binds to misfolded mutant p53 proteins, thereby inducing conformational changes that restore p53 to its normal state and reactivate its function. COTI-2 hydrochloride acts on a variety of cancer cell lines and xenografts. COTI-2 hydrochloride can be used in research related to colorectal cancer, small cell lung cancer, glioblastoma, breast cancer, and ovarian cancer.

KYP-2047 (Standard) is the analytical standard of KYP-2047 (HY-100475). This product is intended for research and analytical applications. KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation.