cmyc

MYCi975 (NUCC-0200975) is an orally active MYC inhibitor.

m-Se3 is a potent, selective inhibitor of c-MYC transcription with demonstrated capability to inhibit tumor growth and exhibit anti-cancer activity [1].

MDEG-541 is a potent MYC-MAX degrader that exhibits antiproliferative activity by downregulating the expression of GSPT1, MYC, GSPT2, and PLK1 proteins [1].

MYC-RIBOTAC, a ribonuclease-targeting chimera (RIBOTAC) specific to the MYC internal ribosome entry site (IRES), comprises an MYC mRNA-binding element tethered to a small molecule that recruits and activates RNase L1. This interaction promotes the degradation of MYC mRNA, subsequently reducing MYC protein levels and inducing apoptosis, thereby presenting potential applications in anticancer research [1].

Compound 67h, also known as c-Myc inhibitor 12, is a potent inhibitor of c-Myc, exhibiting a pEC50 value of 6.4 [1].

WBC100 (14-D-Valine-TPL) is a potent, selective, orally active c-Myc glue degrader targeting the ubiquitin E3 ligase CHIP-mediated 26S proteasome pathway, primarily used in research for c-Myc overexpressing tumors [1].

c-Myc inhibitor 11 (Compound 67e), a c-MYC inhibitor (p EC 50: 6.4), demonstrates high clearance, moderate volume of distribution, and a short half-life in rat pharmacokinetic assays, making it suitable for cancer research [1].

KSI-3716 is a c-Myc inhibitor used as a bladder chemotherapy agent. It blocks the formation of the c-MYC MAX complex with the target gene promoter and induces cell cycle arrest and apoptosis. It can be used for bladder cancer research.

NNK is a nicotinic nitrosylated derivative. It activates ERK1 2 and PKCα, and activates Bcl2 phosphorylation at Ser70, as well as c-Myc at Thr58 and Ser62.It can be used to construct mouse models of lung cancer, as well as to induce proliferation and survival of human lung cancer cells.

Cotylenin A is a phenanthraquinone compound that synergistically works with vitamin K2 to induce monocyte differentiation and growth arrest. It also inhibits c-Myc expression while inducing cyclin G2 expression in human leukemia HL-60 cells. Cotylenin A is applicable in acute myeloid leukemia research.

H122 is a TEADPROTAC degrader effective in degrading TEAD1 with a DC50 of 3 nM, and it shows strong affinity for TEAD2, TEAD3, and TEAD4 with Ki values of 2.0, 3.6, and 1.6 nM, respectively. H122 also downregulates Myc expression and inhibits the growth of MSTO-211H and NCI-H226 cells, with IC50 values of 21.3 nM and 0.6 nM, respectively, demonstrating antitumor activity in mouse models. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligaseCereblon)

Anticanceragent 263 (compound 7) is an effective anticancer agent. It binds with the G-quadruplex DNA (G4) sequence 22-mer Pu22 (a c-Myc DNA analog). As a structural modulator, Anticanceragent 263 significantly enhances the formation of protein α-helices and has the capacity to form a supramolecular network. Furthermore, Anticanceragent 263 exhibits no cytotoxicity.

γ-Sitosterol acts as an inhibitor of c-Myc. It suppresses the proliferation of cancer cells MCF-7 and A549, with IC50 values of 240.73 μg mL and 696.6 μg mL, respectively. γ-Sitosterol induces cell cycle arrest at the G2 M phase and triggers apoptosis (apoptosis). Additionally, it upregulates the expression of cyclin B E [cyclin B E].

BRD4 Inhibitor-40 (Compound 23) functions as an inhibitor of BRD, effectively targeting BRD4-BD1, BRD4-BD2, BRD2-BD1, and BRD2-BD2, with IC50 values of 16.1, 142.18, 29.35, and 302.35 nM, respectively. It modulates the expression of c-Myc and p21, induces cell cycle arrest in the G1 phase, and inhibits Pkd1-deficient (PN) renal cystic epithelial cells. Additionally, it prevents renal cyst formation in both Madin-Darby canine kidney and embryonic kidney cyst models, and demonstrates renal cyst inhibition activity in mouse models.

NSC308848 is an effective apoptosis (cell death) inducer that operates in a Myc-dependent manner. It acts by inhibiting Myc transactivation and disrupting the DNA binding activity of Myc family proteins.

XY221 (Compound 16o) selectively inhibits BRD4 BD2 with an IC50 of 5.8 nM. It demonstrates high selectivity for pan-BD2 and BRD4 BD2 domains, being 667 times more selective than for BRD4 BD1, and 9-32 times more selective than for BRD2 3 T BD2. XY221 can induce apoptosis in MV4-11 cells and exhibits anti-cancer activity.

PROTAC LZK-IN-1 (Compound 21A) is a PROTAC molecule that targets the degradation of LZK (leucine zipper kinase, encoded by MAP3K13). At a concentration of 10 μM, PROTAC LZK-IN-1 facilitates 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. This compound is applicable in anticancer research.

SYUIQ-5 is a ligand for G-quadruplex structures. It plays a role in stabilizing G-quadruplexes and inducing senescence. Additionally, SYUIQ-5 inhibits the activity of the c-myc gene promoter. By displacing TRF2 from telomeres, SYUIQ-5 induces telomeric damage, which triggers autophagy (autophagy) in cancer cells.

Nicotinamide N-oxide (Nicotinamide 1-oxide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.

10074-A4 is a c-Myc binding compound that associates with c-Myc[370–409] and acts as a ligand cloud around a protein cloud , exhibiting distinct characteristics compared to a non-binding ligand.

10058-F4 (c-Myc Inhibitor) is a cell-permeable thiazolidinone that specifically inhibits the c-Myc-Max interaction and prevents transactivation of c-Myc target gene expression; induces cell-cycle arrest and apoptosis.

MYCi361 (NUCC-0196361) is an inhibitor of MYC (binding to MYC with Kd of 3.2 μM).

C-MYC PEPTIDE EPITOPE TFA, the product of the c-myc proto-oncogene, is a helix-loop-helix leucine zipper phosphoprotein that regulates gene transcription in cell proliferation, cell differentiation and apoptosis. This peptide is a human c-myc epitope.

VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX. VPC-70063 exhibits Myc-Max transcriptional activity inhibition of 106% with an IC50 of 8.9 μM and Myc-Max UBE2C downstream pathway inhibition of 94%. VPC-70063 can be used for studies about anticancer.