Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer[1][2][3].
NQO1 substrate acts as an efficient NQO1 substrate and may be a new option for the treatment of NQO1-overexpresssing drug-resistant NSCLC[1].
Bis-PEG1-NHS ester is a nonclaevable 1-unit PEG linker for antibody-drug-conjugation (ADC).
Bendamustine hydrochloride is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.
A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines. Target: A-196 is a selective chemical probe for SUV420H1/H2. A-196 is the first potent and selective chemical probe for SUV420H1 and SUV420H2. The in vitro activity of A-196 includes inhibition of SUV420H1 with IC50 = 25 nM and SUV420H2 with IC50 = 144 nM for methylation of H4K20me and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cell assays, A-196 inhibits the di- and tri-methylation of H4K20me in multiple cell lines with IC50 < 1 μM. SUV420H1 and SUV420H2 are two highly homologous methyltransferases that di- and tri-methylate 'Lys-20' of histone H4.
RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC50 of 27.4 μM.
Merestinib dihydrochloride (LY2801653 dihydrochloride) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM.
SD-1008 is a potent JAK inhibitor. SD-1008 inhibits tyrosyl phosphorylation of STAT3, JAK2 and Src. SD-1008 also reduces STAT3-dependent luciferase activity. SD-1008 enhances apoptosis induced by Paclitaxel in ovarian cancer cells via directly blocking the JAK-STAT3 signaling pathway[1].
LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC50s of 32 and 27 nM for LDHA and LDHB, respectively.
N6-iso-Propyladenosine 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].
trans-Coniferyl aldehyde (compound 2) is a natural compound isolated from the buds of clove (Syzygium aromaticum).trans-Coniferyl aldehyde suppresses 63% of the UV mutable gene expression at 1.20 μM, and with an ID50 value of 0.76 μM,and has the antimutagenicactivities against furylfuramide, Trp-P-1, and activated Trp-P-1[1].
Flt-3 Inhibitor III is a potent and selective FLT3 kinase inhibitor with an 50 of 50 nM. Flt-3 Inhibitor III shows less active against other kinases. Flt-3 Inhibitor III has anticancer effects[1].
BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively[1]. Potential tools for the molecular imaging of activated MMPs with PET[2].
E3 ligase Ligand-Linker Conjugates 49 incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 49 can be used to design PROTAC degrader.
Otlertuzumab (TRU-016) is a humanized anti-CD37 monoclonal antibody that can be used for cancer research[1].
Notoginsenoside T5 is a dammarane 61 glycoside. Notoginsenoside T5 is isolated from the acidic deglycosylation of saponins from the roots of P. 62 notoginseng[1].
Epicornuin F is a prenylated flavonoid. Epicornuin F can be isolated from the leaves of Epimedium brevicornu. Epicornuin F has the cytotoxic activity against HepG2 cells with an IC50 value of 33.4 μM. Epicornuin F can be used for the research of cancer[1].
3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine (Compound 7) is an inhibitor of protein kinases, with IC50s of 0.092, 0.26, 0.77 μM for PKC-α, ROCK, ASK1. 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine shows potent cytotoxicity against PC-3 cancer cells with an IC50 value of 0.16 μM[1].
Mal-Phe-C4-VC-PAB-MMAE is made by MMAE conjugated to Mal-Phe-C4-VC-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.
JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. JNJ-67856633 in some cases lead to tumor stasis[1][2][3].
AU-16235 is an inactive epimer of AU-15330. AU-16235 has no effect on cancer cell survival and growth[1]
Androgen receptor degrader-1 (compound 18) is a potent androgen receptor degrader. Androgen receptor degrader-1 can be used in research of cancer[1].
Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent[1].
Custirsen is a highly specific antisense oligonucleotide that inhibits the production of clusterin , an antiapoptotic protein that is upregulated in response to chemotherapy and that confers treatment resistance.
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent Apoptosis. Bonannione A induces Autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity[1][2][3].
CDK9-IN-12 displays the optimal CDK9 inhibitory activity with an IC50 value of 5.41 nM.
Ald-Ph-amido-PEG3-C-COOH is a noncleavable linker used for the antibody-drug conjugate (ADC).
DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity[1].
TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth[1].
E3 ligase Ligand-Linker Conjugates 38 incorporates a cIAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 38 can be used to design PROTAC degrader[1].