c-Myc

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

NY2267 (Acetic acid, 2-[[6-[2-(cyclohexylamino)-1-[[(4-methoxyphenyl)methyl](2-pyridinylcarbonyl)amino]-2-oxoethyl]-2-naphthalenyl]oxy]-, 1,1-dimethylethyl ester) is a disruptor of Myc-Max interaction, with an IC50 of 36.5 μM.

EN4 (EN4 MYC inhibitor) MYC inhibitor is a covalent ligand that targets cysteine 171 (C171) of MYC. It is selective for c-MYC over N-MYC and L-MYC, and inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.

Trachelogenin ((-)-Trachelogenin), isolated from Combretum fruticosum, is an HCV entry inhibitor with anti-proliferative effects. Its mechanism is related to affecting the phosphorylation of key proteins such as β-Catenin, c-Myc and GSK3 in the β-Catenin signaling pathway. chemical and concentration-dependent. Trachelogenin has antiviral, anti-inflammatory and analgesic activities with IC50 of 0.325 and 0.259 μg mL in HCVcc and HCVpp models, respectively.

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

Lusianthridin is a natural product from Dendrobium venustum. Lusianthridin exhibits anti-migratory property at nontoxic concentrations. Lusianthridin enhances c-Myc degradation through the inhibition of Src-STAT3 signaling.

MYCMI-6 (NSC-354961) is a potent and selective inhibitor of endogenous MYC:MAX protein interactions,reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without severe side effects.

KJ Pyr 9 is an MYC inhibitor (Kd: 6.5 nM in vitro assay).

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.

APTO-253 (LOR-253) inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through the induction of the KLF4 tumor suppressor.

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.

IRES-C11 is a specific inhibitor of translation that targets the internal ribosome entry site (IRES) of the c-MYC gene. It functions by blocking the interaction between heterogeneous nuclear ribonucleoprotein A1, a trans-acting factor required for c-MYC IRES activity, and its corresponding IRES. Notably, IRES-C11 does not inhibit the IRES activity of BAG-1, XIAP, and p53.

CPI0610 (CPI-0610) is an effective, specific, and cell-active BET bromodomain inhibitor CPI-0610 inhibits BRD4-BD1 (IC50: nM).

10074-G5 is an inhibitor of c-Myc-Max dimerization.

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.

ML327 is a MYC blocker. ML327 can also de-repress E-cadherin transcription and reverse Epithelial-to-Mesenchymal Transition (EMT).

sAJM589 is a Myc inhibitor that dose-dependently disrupts Myc-Max heterodimers, thereby decreasing Myc protein levels. Myc is a multifunctional nuclear phosphoprotein that plays a key role in cell cycle progression, apoptosis, and cellular transformation. sAJM589 inhibits the cellular proliferation of a variety of Myc-dependent cancer cell lines and the adherent, non-dependent growth of Raji cells’ Growth.

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.

Mycro 3 is potent and selective for c-Myc in whole cell assays.

BTYNB (MDK6620) is an inhibitor of the oncofetal mRNA-binding protein IMP1 (IC50 = 5 μM for IMP1 binding to c-Myc mRNA). MDK6620 downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). It disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association

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.

CBP EP300-IN-2 is an inhibitor of CBP EP300 with IC50 values of 1.07 nM for CBP HTRF and 5.96 nM for Myc.

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.

SYHA1815, an orally active RET inhibitor (IC50=0.9 nmol L), demonstrates antitumor activity. It exhibits greater selectivity for RET over KDR (IC50=15.9 nmol L). SYHA1815 operates by downregulating c-Myc, arresting the G1 cell cycle, and inhibiting RET-driven cell proliferation.

CSI86 is a PROTAC degrader targeting MYC, exhibiting antiproliferative activity (IC50: 13-18 μM).

Moracin C and moracin D, new phytoalexins from diseased mulberry, are antifungal compounds. Moracin may be protective influence in tumor promotion, utilization of Moracin may open a new avenue in the treatment of tumerigenesis.

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].

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.

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.

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.

β-catenin-IN-8 (Compound 25) is an inhibitor of β-catenin. It effectively lowers the levels of both β-catenin and c-Myc proteins and suppresses Wnt target genes (Fgf20 and Sall4). Additionally, β-catenin-IN-8 exhibits anticancer activity against colorectal cancer and possesses metabolic stability.

Moracin treatment can inhibit the double 12-O-tetradecanoylphorbol 13-acetate (TPA) treatment-induced morphological changes reflecting inflammatory response, including leucocyte infiltration, hyperplasia and cell proliferation; moracin treatment furthermo

Aaptamine functions as a proteasome inhibitor, it activates p21 promoter in a p53-independent manner.

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

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.

Coronarin D shows promising antifungal activity against C. albicans in vitro, the minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) were 2 and 4 mg mL, respectively; it is active against tested Gram-positive bacteria, i

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

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.