MDM-2/p53 Inhibitor

MDM-2/p53 Inhibitors (100):

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-122670

VS-II-173	Inhibitor
VS-II-173 is a pan-Pim kinase inhibitor with IC₅₀ values of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPK_α1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC₅₀ > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations .

HY-162927

p53-MDM2-IN-6	Inhibitor
p53-MDM2-IN-6 (Compound 10a), a LSM-83177 hydrazone analog, is a potent p53-MDM2 inhibitor with an IC₅₀ value of 11.08 µg/mL. p53-MDM2-IN-6 arrests the cell cycle in the S phase and induces early and late Apoptosis with antiproliferative activity against HT29 cell lines with an IC₅₀ value of 10.44 µg/mL. p53-MDM2-IN-6 inhibits p53-MDM2 interaction with increment in p-53 level and decrease the expression of GST enzymes. p53-MDM2-IN-6 is promising for research of colorectal cancer.

HY-124070

ISA 27	Inhibitor
ISA 27 is a small-molecule MDM2-p53 protein-protein interaction inhibitor. ISA 27 inhibits MDM2-mediated p53 ubiquitination and degradation. ISA 27 is promising for research of p53-mutant solid tumors (e.g., thyroid, breast cancer).

HY-163661

p53-MDM2-IN-5	Inhibitor
p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity.

HY-16634

MI-888 TFA	Inhibitor
MI-888 (TFA) is an orally active MDM2-p53 interaction inhibitor with a K_i of 0.44 nM. MI-888 (TFA) can achieve rapid, complete, and sustained tumor regression in a xenograft mouse model of cancer.

HY-149988

UNP-6457	Inhibitor
UNP-6457 is a potent active MDM2-p53 interaction inhibitor with an IC₅₀ values of 8.9 nM.

HY-151171

MDM2/4-p53-IN-3	Inhibitor
MDM2/4-p53-IN-3 is a MDM2/4-p53 protein-protein interactions (PPIs) inhibitor (IC₅₀s: 18.5 nM for MDM2-p53, 14.8 nM for MDM4-p53). MDM2/4-p53-IN-3 can be used in the research of cancers, such as colon cancer.

HY-163275

MDM2-IN-24	Inhibitor
MDM2-IN-24 (compound A3f) exhibits MDM2-inhibiting and MDMX-activating properties in triple-negative breast cancer (TNBC) cells, with apoptotic and anti-proliferative activities.

HY-150620

BI-0282	Inhibitor
BI-0282 (Compound 1) is a potent MDM2-p53 interaction inhibitor.

HY-175538

USP10-IN-4	Inhibitor
USP10-IN-4 is a potent ubiquitin-specific protease 10 (USP10) inhibitor with an IC₅₀ of 10.87 μM and a K_d of 365 nM. USP10-IN-4 effectively inhibits USP10-mediated proteasomal degradation of downstream proteins YAP and p53, leading to the subsequent downregulation of CDK4 in the p53 signaling pathway. USP10-IN-4 promotes apoptosis in HCC cells and inhibits the onset and progression of liver cancer. USP10-IN-4 can used for the study of hepatocellular carcinoma (HCC).

HY-17493A

MI-773 TFA	Inhibitor	98.91%
MI-773 TFA is an orally active, selective MDM2-p53 interaction inhibitor with a K_i of 0.88 nM for MDM2. MI-773 TFA blocks the MDM2-TP53 interaction. MI-773 TFA potently activates p53. MI-773 TFA induces Apoptosis. MI-773 TFA causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 TFA exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma.

HY-12579

RO 2468	Inhibitor
RO 2468 is a potent, orally active and selective p53-MDM2 inhibitor. RO 2468 has anti-proliferative active. RO 2468 suppresses c growth in SJSA1 osteosarcoma models without obvious toxicity.

HY-175332

Apoptosis inducer 43	Inhibitor
Apoptosis inducer 43 is an apoptosis inducer. Apoptosis inducer 43 can induce apoptosis, SubG0-G1 cell cycle arrest, secondary necrosis, and upregulate caspase-3, p53, and Bax/Bcl-2 expression in HCT116 cells. Apoptosis inducer 43 can inhibit tumor growth in a solid Ehrlich carcinoma (SEC) mouse model. Apoptosis inducer 43 can be used to study cancers such as colon cancer, leukemia, and non-small cell lung cancer.

HY-168606A

p53-MDM2-IN-7 hydrochloride	Inhibitor
p53-MDM2-IN-7 (compound 6d) (hydrochloride) is a p53-MDM2 inhibitor. p53-MDM2-IN-7 has an IC₅₀ value of 8.13 μM against A549 cells. p53-MDM2-IN-7 can be used in anti-cancer research.

HY-145907

p53-HDM2-IN-1	Inhibitor
p53-HDM2-IN-1 is a potent inhibitor of p53-HDM2 protein-protein interaction, with an IC₅₀ of 0.103 μM. p53-HDM2-IN-1 can be used for the research of cancer.

HY-133760

MI-888	Inhibitor
MI-888 is an orally active MDM2 inhibitor with a K_i of 0.44 nM. MI-888 can inhibit the MDM2-p53 interaction. MI-888 has favorable pharmacokinetic properties and anti-tumor activity.

HY-170595

PROTAC LZK degrader 1	Inhibitor
PROTAC LZK degrader 1 (Compound 21A) is a PROTAC that targets the degradation of LZK (Leucine Zipper Kinase, encoded by MAP3K13). PROTAC LZK degrader 1 (10 μM) promotes the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. PROTAC LZK degrader 1 can be used in cancer research. PROTAC LZK degrader 1 consists of an E3 ligase ligand (blue part, HY-112078), a target protein ligand (red part, HY-170596), and a linker (black part, HY-W019543)[1].

HY-179378

XRF-1021	Inhibitor
XRF-1021 is an orally active HIPK2 inhibitor (IC₅₀ = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease.

HY-12430

SP-141 hydrochloride	Inhibitor
SP-141 (hydrochloride) is a specific inhibitor of MDM2. SP-141 (hydrochloride) promotes MDM2 auto-ubiquitination and degradation. SP-141 (hydrochloride) might be used for the research of pancreatic cancer and breast cancer cells.

HY-146806

YL93	Inhibitor
YL93 is a dual inhibitors of MDM2/4 with K_i values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. YL93 induces cell-cycle arrest and apoptosis. YL93 shows p53-dependent cell growth inhibition.

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