4′,5′-Didehydro-5′-deoxy-5-methyluridine 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].
6-Methyl-9-(β-D-xylofuranosyl)purine 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].
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML)[1][2].
HPK1-IN-9 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-9 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 112) [1].
Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation[1][2][3].
ZD-4190 is a potent, orally available inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for the treatment of cancer.
4'-Demethylpodophyllotoxin is an aryltetralin lignin contained in the root of Podophyllum hexandrum and P. peltatum. 4'-Demethylpodophyllotoxin exhibits cytotoxic potential in diverse cancer cell lines[1][2].
CypK (N-Cyclopropene-L-Lysine), a cyclopropene derivative of lysine, is efficiently incorporated into antibodies through genetic-code expansion. CypK is a minimal bioorthogonal handle for the creation of stable therapeutic protein conjugates[1][2].
QD394 is a reactive oxygen species (ROS) inducer that can induce lipid peroxidation, increase intracellular ROS accumulation, inhibit STAT3 phosphorylation, and induce ferroptosis[1].
Silvestrol aglycone, a aglycone of potential anticancer rocaglate derivative from Aglaia foveolata, induces apoptosis in LNCaP cells through the mitochondrial/apoptosome pathway without activation of executioner caspase-3 or -7; 5'myc-UTR-LUC inhibtior (IC50= 0.8 nM).IC50 value:Target: Apoptosis inducerin vitro: Silvestrol induced an apoptotic response, disrupted the mitochondrial trans-membrane potential and caused cytochrome c release into the cytoplasm. Immunoblot analysis indicated that, at the protein level, silvestrol produced an increase of Bcl-xl phosphorylation with a concomitant increase of bak. Furthermore, caspase-2, -9 and -10 appeared to be involved in silvestrol-mediated apoptosis. In contrast, the involvement of caspase-3 and -7 was not detected, either by immunoblot or caspase-3/-7-like activity analysis, indicating that these pathways do not play a crucial role in silvestrol-induced apoptosis [1]. The ability of silvestrol and analogues to selectively inhibit the translation of proteins with high requirement on the translation-initiation machinery (i.e., complex 5'-untranslated region UTR) relative to simple 5'UTR was determined by a cellular reporter assay. Simplified analogues of silvestrol such as compounds 74 and 76 were shown to have similar cytotoxic potency and better ADME characteristics relative to those of silvestrol [2].in vivo:
BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM[1].
AKT-IN-9 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1)[1].
Cys-C-cGMP is a autophagy tag for AUTACs. Cys-C-cGMP can increase the K63-linked ubiquitination of mitochondria in HeLa cells[1].
Morusignin L is an active compound that shows anti-osteoporosis activities[1][2].
A novel potent LIMK inhibitor with IC50 of 0.3 nM and 1 nM for LIMK1 and LIMK2, respectively; inhibits cofilin phosphorylation and increase αTubulin acetylation in cells; shows significant sensitivity against 656 cancer cell lines, and rhabdomyosarcoma, neuroblastoma and kidney cancer cells (mean EC50=19.2 uM).
Blu667 is a highly potent and selective RET inhibitor with an IC50 of 0.4 nM for wild type RET kinase.
CSV0C018875 is a quinoline-based EHMT2/G9a inhibitor. CSV0C018875 exhibits lesser cytotoxicity than BIX-01294[1].
Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.
EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.target: HIF1αIC 50：20-40 nM.[1]in vitro : EL102 is a cytotoxic agent and also displays cytostatic properties, through flow cytometric analysis of PI-stained cells cultured for 24, 48 and 72?h, following treatment. EL102 induces apoptosis and causes G2/M arrest, preventing the cell from entering into mitosis.In vivo: CWR22 tumours were taken from an in vivo passage, cut into small fragments and transplanted subcutaneously (s.c.) into the flank of 48 nude mice. At day 13, when the tumours were palpable, mice were randomised into 10 groups with 8 mice each and treatment initiated. EL102 12?mg?kg?1 via p.o. (0700 hours and 1700 hours daily).[1]
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively.
DGKα-IN-7 is a DGKα inhibitor with the IC50 of 6.225 nM, extracted from patent WO2022271684 (compound 100). DGKα-IN-7 has the potential for cancer study.
Bifikafusp alfa (L19-IL2) is an immunotherapy fusion protein consisting of human L19 antibodies fused to the human cytokine interleukin 2 (IL2).Bifikafusp alfa is specific to the EDB domain of fibronectin. Bifikafusp alfa has anticancer activity[1].
4′,5′-Didehydro-5′-deoxy-2′-O-methyluridine 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].
NSC 48160 inhibits the growth of the pancreatic cancer cells with IC50s of 84.3 μM for CPFAC-1 and 94.5 μM for BxPC-3. NSC 48160 also induces pancreatic cancer cell apoptosis. NSC 48160 can improve metabolic syndromes, such as NASH, obesity and lipid metabolism disorders[1][2].
BGB-8035 is an orally active, highly selective bruton's tyrosine kinase (BTK) inhibitor with IC50s of 1.1 nM, 99 nM, 621 nM for BTK, TEC, EGFR, respectively. BGB-8035 has antitumor and anti-arthritis activity. BGB-8035 has the potential for B-cell malignancies and autoimmune diseases research[1].
Guadecitabine (SGI-110) is a DNA methyltransferases (DNMT) inhibitor.
Val-Ala-PAB-MMAE is a Drug-Linker Conjugate for ADC, consisting of ADC linker (Val-Ala-PAB) and MMAE. MMAE is an effective inhibitor of tubulin.
20-Deoxocarnosol (compound 7) is a potent anti-cancer agent that can be found in the roots of Salvia deserta. 20-Deoxocarnosol shows cytotoxicity in cancer cells[1].
YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC50 value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC50 value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer[1].
5-N-Boc-aminomethyluridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].