Boditrectinib is a potent tyrosine kinase inhibitor. Boditrectinib serves as an antineoplastic agent. Boditrectinib is useful in the research of cancer, inflammation, neurodegenerative diseases and certain infectious diseases[1][2].
MYCi361 (NUCC-0196361) is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 (NUCC-0196361) suppresses tumor growth and enhances anti-PD1 immunotherapy[1].
HA15 is a molecule that targets specifically BiP/GRP78/HSPA5target: BiP, GRP78, HSPA5 [1]In vitro: HA15 induces ER stress leading to cancer cell death. kills cancer cells by targeting BiP to increase ER stress, leading to melanoma cell death by concomitant induction of autophagic and apoptotic mechanisms. HA15 exhibits strong efficacy in melanoma cells. The 50% inhibitory concentration (IC50) in A375 cells was between 1 and 2.5 mM HA15. [1]In vivo: HA15 induces ER stress leading to cancer cell death. HA15 also exhibited strong efficacy in xenograft mouse models with melanoma cellseither sensitive or resistant to BRAF inhibitors. [1]
(S)-CCG-1423 is an inhibitor of Rho signaling that blocks the nuclear import of MRTF-A. (S)-CCG-1423 reduces the nuclear accumulation of MRTF-A and improves glucose uptake and tolerance in insulin-resistance mice in vivo. (S)-CCG-1423 exhibits higher inhibition activity than the SR- and the R-isomers of CCG-1423 (HY-13991). (S)-CCG-1423 can be used for the research of cancer and diabetes[1].
3β-[N-(N′,N′-Dimethylaminoethyl)carbamoyl]cholesterol, a cationic liposome reagent, has been investigated in cancer gene therapy and vaccine delivery system[1].
Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker Azido-PEG4-Val-Cit-PAB-OH[1].
Amino-PEG2-NH-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Guajadial, a caryophyllene-based meroterpenoid, has anti-estrogenic and anticancer effect. Guajadial reverses multidrug resistance in cancer. Guajadial can be isolated from Psidium guajava leaves[1][2].
KTX-612 is an orally active IRAK4 degrader with a DC50 value of 7 nM. KTX-612 can be used for the research of oncology[1].
GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
Mal-PEG4-PFP ester is a nonclaevable ADC linker containing a Maleimide group, 4-unit PEG and a PFP ester.
2’-O-Phthalimidopropyl cytidine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Etoposide is a chemotherapy medication used for the treatments of a number of types of cancer. Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA.
GSTO-IN-2 is a glutathione S-transferase inhibitor with IC50s of 3.6, 16.3, and 1.4 μM for GSTA2, GSTM1, and GSTP1-1.
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
ICMT-IN-22 (compound 62) is an inhibitor of ICMT (IC50=0.63 μM)[1].
Aspirin (Acetylsalicylic Acid) lithium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin lithium induces apoptosis. Aspirin lithium inhibits the activation of NF-κB. Aspirin lithium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis[1][2][3][4][5][6].
Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering drug; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity.
Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells[1].
Malotilate is a liver protein metabolism improved compound, which selectively inhibit the 5-lipoxygenase. IC50 Value:Target: 5-lipoxygenasein vitro: In an in vitro invasion assay using rat lung endothelial (RLE) cells, invasion of tumor cells which had been treated with MT (10 ng/ml, 24 h) was not affected; however, when RLE cells had been treated with MT, invasion was significantly inhibited in three cell lines (SAS, Ca9-22 and HSC-4) and a tendency to inhibition was also observed in other cell lines [1].in vivo: The improvement rates for choline esterase activity were significantly greater in the malotilate group than in the control group. Serum albumin levels significantly increased in the malotilate group but not in the control group [2]. In the rats treated with MT for 19 days after i.v. inoculation of c-SST-2 cells, lung metastasis was also significantly suppressed [3]. Malotilate prevented increases in serum markers of type III and IV collagen synthesis as well as accumulation of the collagens, laminin and fibronectin in the liver [4].Toxicity: Malotilate cytotoxicity to PBMCs, assessed by trypan blue dye exclusion and lactate dehydrogenase (LDH) release into the culture media, was found to be markedly increased by the addition of the NADPH generating system, indicating that metabolites play a significant role in toxicity [5].
CFI-402257 is a highly selective and orally bioavailable TTK and Mps1 inhibitor with Kis of 0.1 and 0.09 nM, respectively.
Saracatinib (AZD0530) difumarate is a potent Src inhibitor with IC50 values of 2.7-11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr and Blk, and is selective for other tyrosine kinases. [1].
ARRY-520 R enantiomer is the R-enantiomer of ARRY-520. ARRY-520 is a synthetic kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.
Tuvonralimab (PSB-205; QL1706) is a dual immune checkpoint blockade containing a mixture of anti-PD-1 IgG4 and anti-CTLA-4 IgG1 antibodies, Iparomlimab and Tuvonralimab[1].
8-Azidoadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
MC-1-F2 is a FOXC2 inhibitor that reduces epithelial-mesenchymal transition (EMT) markers in breast cancer cells, suppresses cancer stem cell (CSC) properties and reduces invasiveness in castration-resistant prostate cancer (CRPC) cells. There is a synergistic effect between MC-1-F2 and Docetaxel, which has the potential to be used in combination to study CRPC[1].
D-NMAPPD ((1R,2R)-B13) is an acid ceramidase inhibitor. D-NMAPPD regulates NMDA receptor properties by enhancing endogenous production of ceramides. D-NMAPPD has anticancer effecs[1][2].