PERK Inhibitor

RMC-8839 is an orally active selective RAS (ON) G13C inhibitor with a K_i value of 28.3 nM. RMC-8839 disrupts the interaction between KRAS^G13C and RAF1 (RBD). RMC-8839 inhibits RAS-MAPK pathway signaling by reducing DUSP6 mRNA levels and pERK levels. RMC-8839 induces cytotoxicity, apoptosis (apoptosis) and antiproliferative effects in KRAS^G13C-mutated cells. RMC-8839 induces tumor stasis or regression in mice. RMC-8839 can be used in research related to non-small cell lung cancer.

Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) is an anti-mouse E-Cadherin/CD324 IgG1 monoclonal antibody. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can downregulate the HER signaling axis and PI3K/Akt/mTOR signaling pathway. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can inhibit the proliferation of tumor cells and induce their apoptosis. Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) can be used for researches on cancer and inflammation conditions such as breast cancer, chronic compression injury (CCI) and asthma.

eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a K_D of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice.

EGFR-IN-154 (compound 4c) is an EGFR inhibitor with EC₅₀ values of 0.16 μM, 21.73 μM and 41.56 μM against EGFR Del19, EGFR WT and EGFR L858R, respectively. EGFR-IN-154 shows anticancer activity on various cance cell lines. EGFR-IN-154 induces mitochondrial apoptosis, and decreases pERK1/2 and pAkt levels, but increases pJNK and pp38 levels.

PERK-IN-4-d₃ is the d₃-labeled PERK-IN-4 (HY-137813). PERK-IN-4 is a PERK inhibitor with a human IC₅₀ of 0.3 nM and selectivity relative to other kinases. PERK-IN-4 displays moderate rat blood clearance and pharmacokinetic properties.

(S)-PERK-IN-5 is the S-enantiomer of PERK-IN-5. (S)-PERK-IN-5 (example 39) is a PERK inhibitor, with an IC₅₀ of 0.101-0.250 μM.

(S)-N-trans-feruloyloctopamine is an isomer of N-trans-feruloyloctopamine (HY-N2232). N-trans-feruloyloctopamine is a natural hydroxycinnamic acid amide compound derived from garlic husk, possessing tyrosinase inhibitory, FGF2 inhibitory, anti-melanogenic, and anti-tumor activities, and is used in research related to hepatocellular carcinoma, pigmentation disorders, and UVB-induced skin damage.

AM-8719 is an orally active, blood-brain barrier-penetrant KRAS^G12C inhibitor. AM-8719 binds covalently to KRAS^G12C, inhibits SOS1-catalyzed GDP/GTP exchange, and suppresses downstream ERK phosphorylation. AM-8719 exhibits antiproliferative activity against KRAS^G12C tumor cells. AM-8719 can be used for the research of KRAS^G12C-positive cancers.

Dehydrodiisoeugenol-d₄ is the deuterium labeled Dehydrodiisoeugenol (HY-N0589). Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.

YF135 is a KRAS^G12C PROTAC degrader that mediates proteasomal degradation of KRAS^G12C in a reversible manner. In KRAS^G12C-mutant H358 and H23 lung cancer cells, the DC₅₀ values of YF135 for KRAS degradation are 3.61 μM and 4.53 μM, respectively. YF135 attenuates the pERK signaling pathway in cancer cells. YF135 is applicable for lung cancer-related research.

FGFR-IN-27 is an orally active, broad-spectrum FGFR inhibitor, with an IC₅₀ of 0.24 nM against human FGFR1, 0.71 nM against FGFR2, 0.87 nM against FGFR3, and 6.50 nM against FGFR4. FGFR-IN-27 inhibits cancer cell proliferation and blocks tumor growth. FGFR-IN-27 reduces the phosphorylation levels of AKT and ERK, induces apoptosis and ferroptosis, increases ROS levels, and decreases GSH levels. FGFR-IN-27 can be used in the research of hepatocellular carcinoma.

(S)-IP-DK143 is a polymeric micellar formulation. (S)-IP-DK143 inhibits the proliferation of cervical cancer cells, induces ROS-mediated apoptosis, and triggers mitochondrial dysfunction. (S)-IP-DK143 activates the p38 MAPK signaling pathway, increases the phosphorylation level of p38. (S)-IP-DK143 can be used for the research of cervical cancer.

KD36 is a selective KRAS-G12C inhibitor with an IC₅₀ value of 0.92 μM. KD36 can inhibit the phosphorylation of ERK and AKT, induce the accumulation of reactive oxygen species (ROS), reduce mitochondrial membrane potential, thereby leading to apoptosis of KRAS-G12C mutant cells. KD36 can be used in the research of non-small cell lung cancer (NSCLC).

Anticancer agent 319 is an anticancer agent. Anticancer agent 319 inhibits the proliferation of liver cancer cells. Anticancer agent 319 inhibits AKT phosphorylation and blocks the PI3K/AKT signaling axis; meanwhile, it inhibits ERK1/2 phosphorylation and blocks the MAPK/ERK signaling axis. Anticancer agent 319 induces G2/M phase cell cycle arrest, triggers apoptosis, and reduces mitochondrial membrane potential in liver cancer cells. Anticancer agent 319 can be used for the research of hepatocellular carcinoma.

Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC₅₀ values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis.

CK37 is a competitive choline kinase-α inhibitor. CK37 inhibits purified recombinant human choline kinase-α activity. CK37 suppresses MAPK and PI3K/AKT signaling, disrupts actin cytoskeletal organization. CK37 diminishs activating phosphorylations of ERK. CK37 exhibits anticancer activity against cervical cancer, melanoma, Lewis lung carcinoma, lung adenocarcinoma, breast cancer, and leukemia.

Ibt-DOX is a BTK inhibitor with an IC₅₀ of 2.89 nM. Ibt-DOX is also a targeted covalent activated chemotherapeutic agent composed of the targeting ligand Ibrutinib (HY-10997), Doxorubicin (DOX) (HY-15142A), α-MAA (HY-W017180), and a linker (HY-Y0892). Ibt-DOX specifically binds to BTK and releases DOX, synergistically achieving BTK inhibition and chemotherapeutic killing, significantly enhancing toxicity against B-cell lymphoma cells and greatly reducing the toxic side effects of DOX on BTK-negative cells. Ibt-DOX can be used in lymphoma-related research.

LWY713 is a FLT3 PROTAC degrader with a DC₅₀ of 0.64 nM. LWY713 selectively induces FLT3 degradation in a cereblon- and proteasome-dependent manner. LWY713 induces G0/G1 cell cycle arrest and triggers apoptosis. LWY713 upregulates PARP and cleaved caspase 3, and inhibits the phosphorylation of FLT3, STAT5, AKT and Erk. LWY713 exhibits antitumor activity in xenograft mouse models. LWY713 can be used for the research of acute myeloid leukemia.

KRAS-IN-56 (Compound 18) is a KRAS inhibitor with an EC₅₀ of 33 μM. KRAS-IN-56 inhibits the interaction between GTP-KRAS and SOS1. KRAS-IN-56 induces a decrease in p-ERK levels. KRAS-IN-56 can be used in research related to lung cancer.

MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC₅₀ values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines.