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RMC-6236 is an orally effective and novel triple complex RAS (ON) MULTI inhibitor, which is a potent non covalent inhibitor of multiple RAS variants in GTP binding state. RMC-6236 has anti-tumor activity and can be used in research related to RAS driven tumors. With rich experience in compound synthesis, we can provide fast customized synthesis services for this product according to your research needs.

Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and anticancer activities, blocking tumor growth driven by receptor tyrosine kinases and inhibiting Sox4 translation, inducing apoptosis.

DT-061, an orally bioavailable protein phosphatase 2A (PP2A) activator, may be used in the therapy of KRAS-mutant and MYC-driven tumorigenesis.

Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.

RTC-5 (TRC-382) is a phenothiazine compound that has been specifically enhanced for its potent anti-cancer properties. It exhibits considerable effectiveness against an EGFR-driven cancer xenograft model. The mechanism behind its efficacy can be attributed to the simultaneous inhibition of PI3K-AKT and RAS-ERK signaling pathways.

SKLB 1028 (Ruserontinib) is a new type of oral multikinase inhibitor of EGFR, FLT3, and Abl. SKLB 1028 shows excellent activity in FLT3-driven AML models and considerable potency in CML models containing Abl mutants.

COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is used to prevent colorectal cancer. COX-2-IN-6 can be used to prevent colorectal cancer.

XMU-MP-2 is a potent and selective protease inhibitor with anticancer activity that inhibits the growth of oncogenic BRK-driven tumors in a mouse xenograft model.

(Rac)-SHIN2, a serine hydroxymethyltransferase (SHMT) inhibitor, enhances NOTCH1-driven in vivo survival of primary T-ALL in mice and is useful for studying T-cell acute lymphoblastic leukemia (T-ALL).

MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level. MSU-42011 has demonstrated antitumor activity in a [kras]-driven mouse model of lung cancer and is effective for the treatment of preclinical [kras]-driven lung cancer with immunomodulatory activity.

AP-1 NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation (IC50 = 1 μM), without blocking basal transcription driven by the β-actin promoter. It has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells [1].

S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in basal and microtubule-stimulated states (IC50s = 1,000 and 140 nM, respectively). It is selective for Eg5 over nine other human kinesins in an enzyme-coupled assay. It reversibly inhibits Eg5-driven microtubule sliding velocity with an IC50 value of 500 nM using X. laevis recombinant Eg5. It induces cell cycle arrest in HeLa cells (IC50 = 700 nM), reversibly halting the cell cycle in the mitotic phase by inhibiting the separation of duplicated chromosomes and preventing bipolar spindle formation. S-trityl-L-Cysteine inhibits the growth of cancer cells in vitro when tested against the National Cancer Institute (NCI) 60 human cancer cell line panel (average GI50 = 1.3 μM) and in mouse xenograft models.

Histidine (abbreviated as His or H) is an alpha-amino acid. The L-isomer is one of the 22 proteinogenic amino acids, i.e., the building blocks of proteins. It is classified as a charged, polar because of the hydrophilic nature of the imidazole side chain.

Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) (CAPE) inhibits the activation of nuclear transcription factor NF-kappa B and may suppress p70S6K and Akt-driven signaling pathways, with antineoplastic, cytoprotective and immunomodulating activities. CAPE is the phenethyl alcohol ester of caffeic acid and a bioactive component of honeybee hive propolis. In addition, CAPE inhibits PDGF-induced proliferation of vascular smooth muscle cells through the activation of p38 mitogen-activated protein kinase (MAPK) and hypoxia-inducible factor (HIF)-1alpha and subsequent induction of heme oxygenase-1 (HO-1).

(-)-(S)-Equol (4',7-Dihydroxyisoflavan) is an orally bioavailable, non-steroidal estrogen naturally produced by the metabolism of the isoflavonoid daidzein by human intestinal microflora, with potential chemoprotective and estrogen receptor (ER) modulating activities. S-equol preferentially binds to and activates the beta isoform of ER in certain target tissues, while having an antagonistic effect in other tissues. This modulates the expression of ER-responsive genes in a tissue-specific manner. This agent may increase bone mineral density, affect vasomotor symptoms, and may decrease the proliferation rate of susceptible cancer cells. In addition, this agent interferes with the activity of enzymes involved in steroid biosynthesis. S-equol inhibits dihydrotestosterone (DHT) production and may inhibit the proliferation of androgen-driven prostate cancer. S-equol is the biologically active enantiomer while R-equol is essentially inactive and has a weak affinity for alpha-ER.

CX5461 is an rRNA synthesis inhibitor with oral activity that inhibits Pol I-driven rRNA transcription. CX5461 activates the DNA damage response and has antitumor activity in tumors such as ovarian cancer.

NVP-QAV-680 is a potent and selective antagonist of CRTh2 receptor. NVP-QAV-680 has nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro.

Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa.

A-9758 is a RORγ ligand and selective RORγt inverse agonist (IC50: 5 nM) that effectively suppresses IL-17A release, Th17 differentiation, and Th17 effector function, significantly attenuating IL-23 driven psoriasiform dermatitis.

CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor with an IC50 of 0.89 μM and suppresses EGFR (pY1068) and AKT phosphorylation induced by EGF.

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.

RORγt Inverse agonist 6 is an agonist of RORγt inverse. RORγt Inverse agonist 6 can be used in research on Th17-driven autoimmune diseases.

T025 is a pan CLK inhibitor with Kds of 4.8, 0.096, 6.5, 0.61, and 0.074 nM for CLK1-4, respectively. T025 displays anti-proliferative activities with IC50s of 30-300 nM in hematological and solid cancer cell lines. T025 can be used in studies about MYC-driven diseases.

T6167923 is a potent, selective inhibitor of MyD88-dependent signaling pathways. It achieves this by directly binding to the Toll IL1 receptor (TIR) domain of MyD88, preventing MyD88 homodimer formation. Subsequently, T6167923 impedes NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity and boasts improved anti-inflammatory effects, with IC50s values of 2.7 μM for IFN-γ, 2.9 μM for IL-1β, and 2.66 μM each for IL-6 and TNF-α, demonstrating its efficacy across multiple inflammatory mediators [1].