Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis[1][2].
Tesetaxel is a orally active, semisynthetic microtubule inhibitor of the taxane class for the treatment of cancer, including colorectal and gastric cancer.
N6-(4-Methoxybenzyl)adenosine 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].
I-138 is an orally active compound structurally related to ML323 (HY-17543). I-138 and ML-323 are potent reversible inhibitors of USP1-UAF1. I-138 displays synergistic binding with ubiquitin and mutual exclusive binding with ML323. I-138 induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells, increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells. I-138 ablates USP1 autocleavage in cells[1].
Ald-Ph-amido-PEG2-C2-Pfp ester is a nonclaevable 2-unit PEG linker for antibody-drug-conjugation (ADC).
Ganoderic acid D, a highly oxygenated tetracyclic triterpenoid, is the major active component of Ganoderma lucidum. Ganoderic acid D upregulates the protein expression of SIRT3 and induces the deacetylated cyclophilin D (CypD) by SIRT3. Ganoderic acid D inhibits the energy reprogramming of colon cancer cells including glucose uptake, lactate production, pyruvate and acetyl-coenzyme production in colon cancer cells[1]. Ganoderic acid D can inhibit the growth of numerous cancer cell lines and it inhibits HeLa human cervical carcinoma cells with an IC50 of 17.3 mM[2].
Cdc25A (80-93) (human) is a polypeptide that controls the cell proliferation and tumorigenesis by a change in expression of proteins involved in cyclin D1 regulation and G1/S transition. Cdc25A (80-93) (human) can be used in cancer research[1].
PROTAC IRAK4 degrader-7 (Compound I-417) is an orally active PROTAC IRAK4 degrader with antitumor activities[1].
SAR125844 is a potent, highly selective, reversible and ATP-competitive MET receptor tyrosine kinase (RTK) inhibitor for intravenous administration, with an IC50 of 4.2 nM. Shows inhibition of MET autophosphorylation in cell-based assays[1].
Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research[1][2].
Varlilumab (CDX-1127) is a first-in-class human IgG1 anti-CD27 monoclonal antibody. Varlilumab has an anti-tumor activity[1].
Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
9-Dehydroxyeurotinone is an anthraquinone derivative that can be found in Eurotium rubrum. 9-Dehydroxyeurotinone shows cytotoxicity with an IC50 value of 25 µg/mL for SW1990 cells[1].
Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC)[1].
p-Coumaric acid-d6 is the deuterium labeled p-Coumaric acid (HY-N0351). p-Coumaric acid is the abundant isomer of cinnamic acid which has antitumor and anti-mutagenic activities[1][2].
Taxuspine B is a natural product, that can be isolated from Japanese yew Taxus. Taxuspine B exhibits appreciable taxol-like activity to reduce CaCl2-induced depolymerixation of microtubules among the taxoids[1].
O6-Methyldeoxy guanosine; DNA adduct 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].
Rezatapopt is an antineoplastic agent, used to inhibit solid tumor with p53 mutation[1].
SHP2-IN-20 (compound 193) is a SHP2 inhibitor with an IC50 value of 3 nM. SHP2-IN-20 can be used for glioblastoma research[1].
Antitumor agent-65 (Compound 5) is an analogue/derivative of (-)-cleistenolide. Antitumor agent-65 has the potential for the research of cancer diseases[1].
Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species[1][2].
OSS_128167 is a selective SIRT6 inhibitor with IC50s of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.
Falnidamol (BIBX 1382) is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).
Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
Folinic acid is an adjuvant used in cancer chemotherapy involving the drug methotrexate.Target: AntifolateFolinic acid is a 5-formyl derivative of tetrahydrofolic acid. It is readily converted to other reduced folic acid derivatives (e.g., tetrahydrofolate), and, thus, has vitamin activity that is equivalent to that of folic acid. Since it does not require the action of dihydrofolate reductase for its conversion, its function as a vitamin is unaffected by inhibition of this enzyme by drugs such as methotrexate. In 1980s, however, folinic acid was found to reactivate the dihydrofolate reductase itself even when methotrexate exists. Although the mechanism is not very clear, the polyglutamylation of methotrexate and dihydrofolate in malignant cells is considered to play an important role in the selective reactivation of dihydrofolate reductase by folinic acid in normal cells [1]. Folinic acid is generally administered along with MTX as a rescue agent to decrease MTX-induced toxicity. However, information regarding the inhibitory effect of folinic acid against cytogenetic damage caused by MTX is limited. This study was conducted to assess the cytogenetic effect of MTX and its inhibition by folinic acid (FA) using the micronucleus and chromosomal aberration assays concurrently [2].
KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
TAS0612 is an orally novel inhibitor of RSK、AKT and S6K. TAS0612 has broad-spectrum activity against tumor models via inhibiting cell growth[1].
Pomalidomide-C11-NH2 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-C11-NH2 can be connected to the ligand for protein by a linker to form PROTAC[1].
Bizine, a Phenelzine analogue, is a potent and selective LSD1 inhibitor, with a b>Ki of 59 nM. Bizine can modulate bulk histone methylation in cancer cells. Bizine shows neuroprotective effects[1].