PROTAC ABL binding moiety 4, the Dasatinib (ABL inhibitor) moiety, binds to IAP ligand via a linker to form SNIPER [1].
6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin[1][2].
FAP-2286, a fibroblast activation protein (FAP)-binding peptidic macrocycle coupled to the radionuclide chelator DOTA. FAP-2286 has potent affinity to human FAP protein with a Kd of 1.1 nM. FAP-2286, a tumor imaging agent, is a useful tool for the research of positron emission tomography (PET). FAP-2286 has antitumor activity[1][2].
IDO-IN-9 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50s of 0.011 μM (Kinase) and 0.0018 μM (Hela Cell), extracted from patent WO 2016041489 A1, compound 6.
ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities[1].
CB2R/FAAH modulator-2 (compound 26) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-2 are 10.8 and 152.9 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 6.2 μM. CB2R/FAAH modulator-2 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection[1].
Ponatinib D8 (AP24534 D8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
SR31527 is a novel allosteric Kinesin-like protein KIFC1 inhibitor that inhibits microtubule-stimulated KIFC1 ATPase activity with IC50 of 6.6 uM, binds directly to KIFC1 with Kd of 25.4 nM; prevents bipolar clustering of extra centrosomes in TNBC cells and significantly reducesTNBC cell colony formation and viability (MDA-MB-231, BT549 and MDA-MB-435s cells IC50=20-30 uM), with less toxicity to normal fibroblasts.
AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0).IC50 value: pIC50 = 8.0 (pIC50, for P2X3)Target: P2X3/P2X2/3 receptorin vitro: AF-353 is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1]in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced.[2]
Taccalonolide E is a microtubule stabilizer and induces cancer cell apoptosis.
LY3143921 (LY-3143921) is an orally available, potent, selective inhibitor of Cdc7 kinase inhibitor, inhibits CDC7/DBF4 I and pMCM2 (S53) with IC50 values of 3.3 nM and 290 nM, respectively. Solid Tumors Phase 1 Clinical
2-Aminomethyl adenosine 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].
5-Bromoindole is a chemical intermediate that can be used for the synthesis of GSK-3 inhibitors and anti-cancer agents[1][2].
CFI-402257 hydrochloride is a highly selective and orally bioavailable TTK/Mps1 inhibitor with an IC50s of 1.7 nM for TTK in vitro. CFI-402257 hydrochloride has anti-cancer activity[1].
Epitulipinolide diepoxide (compound 9) is a natural compound isolated from the herbs of Liriodendron chinense (Hemsl.) Sarg. Epitulipinolide diepoxide displays cytoxicity in A375 cells, with the IC50 of 52.03 μM[1].
5α-Pregnane-3β,6α-diol-20-one is a mitogenic metabolite of progesterone, and it can be produced in starved androgen-responsive prostate cancer cells.
Cyclooctyne-O-PFP ester is a used as an ADC cytotoxin, which connects antibody and linker[1].
Paltimatrectinib (compound I-147) is a potent tyrosine kinase inhibitor with an IC50 of <10 nM for tropomyosin kinases A (TrkA). Paltimatrectinib has the potential for cancer and inflammatory diseases[1].
MAC glucuronide linker-2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Nesiritide is an agonist of natriuretic peptide receptors (NPRs), with Kd values of 7.3 and 13 pM for NPR-A and NPR-C, respectively. Sequence: Ser-Pro-Lys-Met-Val-Gln-Gly-Ser-Gly-Cys-Phe-Gly-Arg-Lys-Met-Asp-Arg-Ile-Ser-Ser-Ser-Ser-Gly-Leu-Gly-Cys-Lys-Val-Leu-Arg-Arg-His.
Deoxythymidine-5'-triphosphate-13C10,15N2 (dTTP-13C10,15N2) dilithium is 13C and 15N-labeled Deoxythymidine-5'-triphosphate (HY-138615). Deoxythymidine-5'-triphosphate (dTTP) is one of the four nucleoside triphosphates. Deoxythymidine-5'-triphosphate (dTTP) is used in the synthesis of DNA.
Benz-AP is a potent photosensitizer. Benz-AP produces singlet oxygen, with a negative correlation with hCES2 (Human carboxylesterase 2) activity. Benz-AP displays a higher photocytotoxicity potency in cancer cells under low hCES2 environments. Upon TPE (Two-photon excitation), Benz-AP produces ROS and kills cancer cells and tumor spheroids[1].
ABP 215 (Bevacizumab-awwb), a Bevacizumab (Bevacizumab (HY-P9906)) biosimilar, is a humanized IgG1 monoclonal antibody targeting VEGFA (VEGFR). ABP 215 has anticancer effects, and can be used metastatic colorectal cancer (mCRC) research[1][2].
DC4, a ADC cytotoxin, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4 can be used for the targeted treatment of cancer[1].
Porfiromycin is a bioreductive alkylating agent that preferentially kill hypoxic tumor cells relative to other aerobic counterparts.
PF-543 is a novel cell-permeant inhibitor of SPHK1 with a Ki of 4.3 nM and more than 100-fold selectivity for SPHK1 over SPHK2.
ER degrader 1 is a potent degrader of estrogen receptor (ER). The estrogen signaling system plays an important role in regulating cell growth, differentiation and apoptosis. ER degrader 1 has the potential for the research of cancer diseases (extracted from patent WO2021139756A1, compound 11)[1].
Elsilimomab (B-E8) is a IgG1 monoclonal antibody against interleukin-6 (IL-6), with a KD of 22 pM and an IC50 of 1.4 nM. Elsilimomab can be used for the research of multiple myeloma, renal cell carcinoma, and rheumatoid arthritis (RA)[1][2][3].
SI-113(SI113;SI 113) is a potent, specific inhibitor of the SGK1 kinase activity, induces autophagy, apoptosis and ER stress in cancer cells; blocks insulin-dependent phosphorylation of the Sgk1 substrate Mdm2, and induces necrosis and apoptosis in RKO cells; potentiates the effects of paclitaxel on cell viability; active in vivo.
MNK inhibitor 9 is a potent, selective MAPK-interacting kinase (MNK1 and MNK2) inhibitor with IC50 of 3 nM for both, with no activity aginst CDK1/2 (IC50>25 uM); displays excellent selectivity against a 53 kinase panel, with 4 kinases with IC50 <1 uM; inhibits eIF4E phosphorylation in KMS11-luc myeloma with IC50 of 0.6 nM, exhibits inhibition of cell proliferation in human multiple myeloma tumor cell line with EC50 of 1.7 uM; has good solubility and permeability, and is a suitable in vivo tool compound.