MDM-2/p53 Activator

TRAP-1 (XJZ-06-462) is a transcriptional activator of p53 (TRAP) with JQ-1 carboxylic acid (HY-78695) as its target protein ligand. TRAP-1 forms a ternary complex with p53^Y220C and BRD4, potently activates p53 transcription, and inhibits the growth and proliferation of tumor cells. TRAP-1 upregulates p21 and other p53 target genes in pancreatic cell lines carrying p53^Y220C, and induces cellular senescence and apoptosis. TRAP-1 can be used in cancer research involving p53^Y220C-carrying tumors.

Glycocholic acid (Standard) is the analytical standard of Glycocholic acid (HY-N1423). This product is intended for research and analytical applications. Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways.

GN25 is a specific p53-Snail binding inhibitor with antitumor effects.

Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product that can be obtained from the natural active molecule Dragon's blood. Dracorhodin perchlorate inhibits PI3K/Akt and NF-κB activation, upregulates p53 expression, activates caspase, produces ROS, and promotes Apoptosis. Dracorhodin perchlorate regulates the TLR4. Dracorhodin perchlorate promotes wound healing, improves diabetes. Dracorhodin perchlorate has anti-tumor activity against prostate cancer, breast cancer, cervical cancer and other cancers.

Briciclib (ON 014185) is a eukaryotic translation initiation factor 4E (eIF4E) inhibitor. Briciclib exhibits broad-spectrum anti-cancer activity, including in mantle cell leukemia, breast cancer, gastric cancer, and esophageal cancer cells. Briciclib reduces the expression of cyclin D1 and c-Myc, and enhances the expression of P53 and Cleaved Caspase 3 pro-apoptotic proteins. Briciclib can be used for the study of hematological system tumors and solid tumors.

Dibenzo (a,i) pyrene is a polycyclic aromatic hydrocarbon and also a carcinogenic ligand of the TCDD (Ah) receptor. Dibenzo (a,i) pyrene binds to the TCDD (Ah) receptor in rat liver. Dibenzo (a,i) pyrene induces DNA adduct formation and upregulates the protein levels of p53 and p21^WAF1 in diploid lung fibroblasts. Dibenzo (a,i) pyrene alters the cell cycle distribution of diploid lung fibroblasts, increasing the proportion of cells in the S phase, decreasing the proportions of cells in the G0/G1 and G2/M phases, and causing S phase delay/arrest. Dibenzo (a,i) pyrene is applicable for cancer research.

Lenalidomide (Standard) (CC-5013 (Standard)) is the analytical standard of Lenalidomide (HY-A0003). This product is intended for research and analytical applications. Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8⁺ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.

Notoginsenoside R2 (20(S)-Notoginsenoside R2; Ginsenoside Ng-R2) is an orally active notoginsenoside. Notoginsenoside R2 activates P90RSK and Nrf2 via the MEK1/2-ERK1/2 pathway to inhibit 6-OHDA-induced apoptotic damage in nerve cells. Notoginsenoside R2 upregulates SOX8/β-catenin by reducing miR-27a, thereby suppressing Aβ_25-35-induced neuronal apoptosis and inflammatory responses. Notoginsenoside R2 alleviates lipid accumulation and mitochondrial dysfunction in diabetic nephropathy by inhibiting c-Src. Notoginsenoside R2 alleviates hepatic fibrosis by inducing hepatic stellate cell senescence and inhibiting the inflammatory microenvironment via JAK/STAT3 suppression. Notoginsenoside R2 can be used in research related to Parkinson's disease, Alzheimer's disease, diabetic nephropathy and hepatic fibrosis.

Dammarenediol II is a ginsenoside precursor. Dammarenediol II reduces the activity of O-GlcNAc transferase (OGT) and downregulates the global O-GlcNAcylation level. Dammarenediol II inhibits the phosphorylation of Akt, mTOR and GSK3β. Dammarenediol II inhibits human carboxylesterase activity, VEGF-induced ROS production, stress fiber formation and vascular endothelial cadherin disruption. Dammarenediol II promotes cell apoptosis (apoptosis), increases the levels of cleaved PARP1 and p53, and inhibits retinal microvascular leakage. Dammarenediol II can be used in studies related to liver cancer and diabetic retinopathy.

Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases γH2AX and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice.

Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat formic induces apoptosis and has anti-tumour effects.

Lumisterol (9β,10α-Ergosterol) is a photoproduct of 7-dehydrocholesterol, present in the skin, and acts as an orally active VDR non-genomic modulator and ROR inverse agonist. Lumisterol binds to the SARS-CoV-2 Mpro substrate-binding pocket and the RdRP active site, inhibiting enzyme activity. Lumisterol induces NRF2-regulated antioxidant responses, p53 phosphorylation and nuclear translocation, and intracellular free radical scavenging. Lumisterol inhibits the proliferation of epidermal keratinocytes and melanoma cells, modulates cell cycle progression, and suppresses basal and TNFα-induced NFκB transcriptional activity. Lumisterol inhibits RORγ transcriptional activity and IL-17 production. Lumisterol is used in research on UVB-induced skin damage, melanoma, psoriasis, vitamin D deficiency, and COVID-19.

SLMP53-2 is a mutant p53 reactivator. SLMP53-2 restores wild-type-like conformation and DNA-binding ability of mutp53-Y220C by enhancing its interaction with the Hsp70, leading to the reestablishment of p53 transcriptional activity. SLMP53-2 can induce cell cycle arrest, apoptosis and endoplasmic reticulum (ER) stress. SLMP53-2 exhibits antitumor activity.

Sodium glycocholate hydrate, 98% is a bile acid derivative. Sodium glycocholate hydrate, 98% downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Sodium glycocholate hydrate, 98% inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Sodium glycocholate hydrate, 98% modulates related bile acid receptor signaling. Sodium glycocholate hydrate, 98% suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Sodium glycocholate hydrate, 98% can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

Polyporenic acid C is a lanostane-type triterpenoid. Polyporenic acid C can be isolated from Poria cocos. Polyporenic acid C causes the cleavage of caspase-8 and caspase-3, as well as the cleavage of PARP. Polyporenic acid C reduces the phosphorylation level of Akt (Ser473), increases the phosphorylation of PTEN and p53 (Ser15), and activates JNK. Polyporenic acid C induces Apoptosis. Polyporenic acid C shows anticancer activity against non-small cell lung cancer.

PSF-IN-2 (Compound (C)-30) is a PSF inhibitor with an IC₅₀ value of 0.005 pM. PSF-IN-2 exhibits anti-cancer activity, and its IC₅₀ value for inhibiting the proliferation of 22Rv1 cells is 0.5 μM. PSF-IN-2 activates the p53 signaling pathway by inhibiting the binding of PSF to RNA, inducing the expression of related genes, promoting apoptosis, and inhibiting the cell cycle. PSF-IN-2 can be used in cancer research.

Antineoplaston A10 is an antineoplaston that inhibits the growth of human hepatoma cells by inducing apoptosis. Antineoplaston A10 can be used in the study of liver cancer and breast cancer.

PROTAC DAPK1 Degrader-1 is a death-associated protein kinase 1 (DAPK1) degrader with a DC₅₀ of 119.6 nM. PROTAC DAPK1 Degrader-1 significantly increases MDM2 protein levels and inhibits neuronal apoptosis in ceramide-induced cells. PROTAC DAPK1 Degrader-1 can be used to study neurological disorders such as cerebral ischemia and traumatic brain injury.

Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.