(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells[1].
7ACC1(DEAC; Coumarin D 1421; D 1421) selectively interfere with lactate fluxes in the lactate-rich tumor microenvironment; inhibits lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters.IC50 value: 0.86 uM(Lactate uptake inhibition) [1]Target: MCT inhibitor; lactate transport inhibitorContrary to the reference MCT1 inhibitor AR-C155858, 7ACC unexpectedly inhibited lactate influx but not efflux in tumor cells expressing MCT1 and MCT4 transporters. 7ACC delayed the growth of cervix SiHa tumors, colorectal HCT116 tumors, and orthoptopic MCF-7 breast tumors. MCT target engagement was confirmed by the lack of activity of 7ACC on bladder UM-UC-3 carcinoma that does not express functional MCT. 7ACC also inhibited SiHa tumor relapse after treatment with cisplatin. Finally, we found that contrary to AR-C155858, 7ACC did not prevent the cell entry of the substrate-mimetic drug 3-bromopyruvate (3BP) through MCT1, and contributed to the inhibition of tumor relapse after 3BP treatment.
Iristectorin A, a natural product from Iris tectorum, has anti-cancer activities in breast cancer[1].
Agathisflavone is a flavonoid with antioxidant, anti-inflammatory, antiviral, antiparasitic, cytotoxic, neuroprotective, and hepatoprotective activities. Agathisflavone can improve tissue repair in a spinal cord injury model in rats[1][2][3].
RAD51-IN-17 is a quinazolinone derivative that inhibts homologous recombinase RAD51, effectively inhibits both RAD51 foci formation in response to DNA damage, and proliferation of TNBC cell lines; also sensitizes aggressive metastatic TNBC to DNA damage induced by irradiation; a valuable research tool for developing combination therapies to overcome RAD51 driven resistance and relapse in a variety of cancers.
Anticancer agent 170 (compound 3a) is a ketone derivative, and shows potency anti-cancer activity against A549, with the IC50 of 6.62 μM[1].
Uracil-d2-1 is the deuterium labeled Uracil[1]. Uracil is a common and naturally occurring pyrimidine derivative and one of the four nucleobases in the nucleic acid of RNA[2].
ART558 is a nanomolar potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer[1].
CDK7-IN-17 is a potent inhibitor of CDK7. CDK7-IN-17 is a pyrimidinyl derivative compound. CDK7-IN-17 has the potential for the research of various cancers, especially the cancer with transcriptional dysregulation (extracted from patent CN114249712A, compound 1)[1].
ARS-2102 is a potent covalent KRAS G12C inhibitor for use in cancer research[1].
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Benzothiazole-d4 is a deuterium labeled Benzothiazole (HY-W012634). Benzothiazole is a natural occurring heterocyclic nuclei. Benzothiazole nucleus possesses a number of biological activities such as anticancer, antimicrobial, antidiabetic, anti-inflammatory, antileishmanial, and antiviral[1][2].
Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis[1].
MCL-1/BCL-2-IN-2 (Compound 6) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor[1].
Shatavarin IV is a steroidal saponin, that can be isolated from the roots of Asparagus racemosus (Liliaceae). Shatavarin IV shows anticancer activity. Shatavarin IV elicits lifespan extension and alleviates Parkinsonism in Caenorhabditis elegans[1].
GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research[1][2].
MS-444 inhibits the activity of purified smooth muscle myosin light chain kinase (MLCK) with an IC50 value of 10 μM.
PK095 is a p53 mutant stabilizer. PK095 can be used for research of cancer[1].
Salicin is a natural COX inhibitor.
(rel)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (rel)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC)[1].
Rosamultic acid is an A-ring contracted triterpene, that can be isolated from the roots of Rosa rnultiflora. Rosamultic acid inhibits gastric cancer cells proliferation by inducing Apoptosis mediated through cell cycle arrest, downregulation of cell cycle related protein expressions, inhibition of cell migration, DNA damage, and activation of caspases[1][2].
(1S,2S)-ML-SI3 is the trans-isomer of ML-SI3, a TRPML inhibitor. The (-)-isomer is a potent inhibitor of TRPML1 and TRPML2 (IC50=1.6 μM/2.3 μM) and a weak inhibitor of TRPML3 (IC50=12.5 μM), whereas the (+)-enantiomer is an inhibitor on TRPML1 (IC50=5.9 μM), but an activator on TRPML 2 and 3[1].
RMC-6291 is an orally active and covalent inhibitor of KRASG12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRASG12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRASG12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 elicits deep and durable suppression on RAS pathway activity in KRASG12C tumor models[1].
TTP 22 is a potent CK2 inhibitor, with an IC50 of 100 nM and a Ki of 40 nM.
c-Met-IN-15 (compound S3) is a c-Met kinase inhibitor. c-Met-IN-15 inhibits c-Met kinase activity of 21.1% at the concentration of 10 μM[1].
Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
2-Methylthioadenosine 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].
Z-IETD-pNA (Z-Ile-Glu-Thr-Asp-pNA) is a colorimetric caspase-8 and granzyme B substrate. Z-IETD-pNA is hydrlyzed by caspase 8 to generate pNA[1].
IACS-15414 is a potent and orally bioavailable SHP2 inhibitor with an IC50 value of 122 nM.
Thapsigargin is an inhibitor of microsomal Ca2+-ATPase.