MDM-2/p53 p53 Activator

BW-AQ-113 is an Anthraquinone (HY-N0354) derivative. BW-AQ-113 can specifically degrade MDM2 and activate the p53 pathway. BW-AQ-113 can induce apoptosis by downregulating anti-apoptotic gene Bcl-2 and regulating pro-apoptotic gene Bax and CASP3. BW-AQ-113 can be used for research of p53 wild-type hematological malignancies.

Bcl-2-IN-7 (compound 6) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC₅₀ values of 20.17, 22.64, 45.57, and 51.50 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively.

Dimethyl bisphenolate (Compound DMB) is a natural neolignan derivative with orally active anti-tumor activity. Dimethyl bisphenolate can inhibit cancer cells proliferation, invasion and migration. Dimethyl bisphenolate can activate the p53 signaling pathway, upregulate the expression of p21 protein, inhibit the activity of the CDK1-cyclin B1 complex, and cause cells to stall at the G2/M phase. Dimethyl bisphenolate can induce ROS production, upregulate pro-apoptotic proteins Noxa and Bim, downregulate anti-apoptotic protein Bcl-2, activate caspase-9 and caspase-3, and ultimately induce cell apoptosis. Dimethyl bisphenolate can be used for research of glioblastoma.

CK1α-IN-1 (Compound 7a) is a selective CK1α inhibitor with an IC₅₀ of 10.96 nM. CK1α-IN-1 dose-dependently stabilizes p53 protein. CK1α-IN-1 has anticancer activity against acute monocytic leukemia.

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.

Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.

Bcl-2-IN-26 is an inhibitor targeting β-tubulin and BCL-2. Bcl-2-IN-26 disrupts the intracellular microtubule network and interferes with cell mitosis, inducing G2/M phase cell cycle arrest. Bcl-2-IN-26 suppresses antiapoptotic BCL-2 function via p53 upregulation, thereby triggering mitochondrial dysfunction, elevated ROS production and robust tumor cell apoptosis. Bcl-2-IN-26 can be used in lung cancer research.

PinA1 is a selective Molecular glue degrader of CK1α with an EC₅₀ of 2.09 µM. PinA1 induces the formation of a stable CRBN-PinA1-CK1α ternary complex to promote the polyubiquitination and subsequent proteasomal degradation of CK1α. PinA1 activates the p53 signaling pathway. PinA1 induces G1 cell cycle arrest. PinA1 induces p53-dependent Apoptosis. PinA1 can be used in studies related to acute myeloid leukemia.

NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC₅₀ values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer.

Amifostine sodium (WR2721 sodium) is a phosphorus sulfate with radioprotective activity. Amifostine sodium can cause splenic vasodilation and may block autonomic ganglia. Amifostine sodium is clinically used to prevent cisplatin-induced ototoxicity.

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.

p38α inhibitor 6 (compound 19) is a p38α inhibitor with the IC₅₀ of 0.68 μM. p38α inhibitor 6 induces cell apoptosis and arrests cell cycle at G0 and G2/M phase. p38α inhibitor 6 decreases the TNF-α concentration as well as increased the expression of tumor suppressor gene p53, Bax/BCL-2 ratio and caspase 3/7.

p53 Activator 9 (example D-4) is a p53 activator with EC₅₀ of 1.699μM.

CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC₅₀ of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer.

Nrf-2/HMOX-1-IN-1 is a Nrf-2 and HMOX-1 inhibitor, as well as a Ferroptosis inducer. Nrf-2/HMOX-1-IN-1 inhibits GPX activity and upregulates p53 gene expression. Nrf-2/HMOX-1-IN-1 increases intracellular ROS and MDA levels, reduces GSH content, and elevates intracellular iron levels simultaneously. Nrf-2/HMOX-1-IN-1 exerts selective anticancer effects against breast cancer. Nrf-2/HMOX-1-IN-1 can be used in breast cancer-related research.

HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC₅₀ values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC₅₀ of 1.41 μM.

P53 mutant stabilizer-1 (compound 274) is a covalent mutant p53 stabilizer. P53 mutant stabilizer-1 can be used for the study of wild-type function of p53 mutants, such as cancers associated with p53 mutation.

Anticancer agent 65 (compound 4c) shows excellent activity in cancer cell lines, especially A549 cells, with an IC₅₀ of 1.07 μM. Anticancer agent 65 induces S-phase arrest in A549 cells and increases the expression level of p53 and p21. Anticancer agent 65 causes apoptosis, ROS generation and collapse of MMP in A549 cells.

Minocycline-d₆ is deuterium labeled Minocycline (HY-17412A). Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.

Tebufenozide-d₉ is the deuterium labeled Tebufenozide (HY-B2054). Tebufenozide is a nonsteroidal ecdysone agonist used to control pest. Tebufenozide has cytotoxic and induces apoptosis in HeLa and insect Tn5B1-4 cells.