CD147 degrader 1 is a PROTAC targets CD147 with an DC50 value of 6.72 µM. CD147 degrader 1 inhibits cell proliferation, migration and invasion. CD147 degrader 1 decreases the expression of CD147, MMP9, and p-STAT3 protein. CD147 degrader 1 shows anti-cancer acyivity[1].
Y-29794 (Compound 2) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a Ki of 0.95 nM. Y-29794 can be used for studying neurodegenerative diseases and cancer[1].
Icrucumab (Anti-VEGFR1/FLT1 Reference Antibody; IMC-18F1) is a humanized Anti-VEGFR-1 IgG1 monoclonal antibody. Icrucumab has the potential for the research of advanced solid tumors[1].
ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC50 of 2.8 μM.
PQR620 is a novel potent and selective brain penetrant inhibitor of mTORC1/2.
GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC50 of 7 nM.
M5N36 is a potent and selective Cdc25C inhibitor with IC50 values of 0.15, 0.19, 0.06 µM for Cdc25A, Cdc25B, Cdc25C, respectively. M5N36 shows anti-proliferative activity and increases the expression of p-CDK1 and p-CDK2[1].
Lipoic acid ((R)-(+)-α-Lipoic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. (R)-(+)-α-Lipoic acid is more effective than racemic Lipoic acid.
LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines[1][2].
Tidutamab (XmAb-18087) is a humanized and affinity-optimized bispecific antibody (bsAb) targeting SSTR2 binding domain and T-cell binding domain (CD3). Tidutamab possesses a full Fc domain to maintain long serum half-life.Tidutamab eliminates SSTR+ tumor cells by stimulating redirected T cellmediated cytotoxicity (RTcC)[1].
AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.
Nezutatug is an anti-HER3 antibody, and used for cancer research[1].
Apaziquone (EO-9), an analog of Mitomycin C, is a prodrug that is activated to DNA damaging species by oxidoreductases (particularly NQO1). Apaziquone has the ability to kill aerobic and/or hypoxic cancer cells. Apaziquone, a bioreductive alkylating agent, inhibits cell proliferation and induces apoptosis in oral squamous cell carcinoma (OSCC) cells. Apaziquone significantly reduces oral tumor xenograft volume in immunocompromised NOD/SCID/Crl mice[1][2].
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3’-dC(Bz)-2’-phosphor amidite 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].
(S)-Trichostatin A ((S)-TSA) 是一种 HDAC6 选择性抑制剂，对斑马鱼 HDAC6 和人 HDAC6 的 IC50 值分别为 9.88 nM和 11.1 nM。(S)-Trichostatin A 弱抑制其他人 HDAC。
Vantictumab (OMP-18R5) is a fully human IgG2 monoclonal antibody. Vantictumab inhibits Wnt pathway signaling by binding to FZD1/2/5/7/8 receptors. Vantictumab is being studied against cancers such as metastatic HER2-negative breast cancer and metastatic pancreatic adenocarcinoma[1][2].
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein)[1].
ATR-IN-24 (Compound 1) is a ATR inhibitor. ATR-IN-24 has anticancer activity[1].
BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.IC50 value:Target: ERα inhibitorBHPI is effective because it elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis. BHPI distorts a newly described action of estrogen-ERα: mild and transient UPR activation. In contrast, BHPI elicits massive and sustained UPR activation, converting the UPR from protective to toxic. In ERα(+) cancer cells, BHPI rapidly hyperactivates plasma membrane PLCγ, generating inositol 1,4,5-triphosphate (IP3), which opens EnR IP3R calcium channels, rapidly depleting EnR Ca(2+) stores.
Anticancer agent 119 (compound 15) is an N-acylated ciprofloxacin derivative, which has certain antibacterial activity and induces ROS production to promote cancer cell apoptosis[1].
FQI1 is a Late SV40 Factor (LSF) inhibitor. FQI1 inhibits cell proliferation, with IC50s of 3, 0.79, 6.3 μM for NIH/3T3, HeLa, A549 cells. FQI1 can be used for cancer research[1].
Podocarpusflavone A is a DNA topoisomerase I inhibitor, have moderated anti-proliferative activity induce cell apoptosis in MCF-7, is developing anti-tumor drugstarget: DNA topoisomerase IIn vitro: podocarpusflavone-A show significant inhibitions against DLD, KB, MCF-7, HEp-2 tumor cell lines (ED50 4.56-16.24 μg/mL) and induce cell apoptosis in MCF-7 via mainly sub-G1/S phase arrest. PF (40 ug/mL, 24 hr) significantly induced about 10 folds of cell deaths and growth arrest in S-phase than the control group.
B-Raf IN 2 is a potent and selective BRAF inhibitor extracted from patent WO2021116055A1, compound Ia. B-Raf IN 2 can be used for the research of cancer[1].
3’-Azido-N6-benzoyl-3’-deoxyadenosine 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].
LSD1-IN-7 Methylbenzenesulfonate is an orally bioavailable inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity extracted from patent WO2017079670A1, compound 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile[1].
EN523 is a OTUB1 recruiter. EN523 targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1[1].
M-110 is a novel and highly selective inhibitor of PIM kinases; inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 uM, with no activity on normal human peripheral blood mononuclear cells up to 40 uM.IC50 value:Target: Pim inhibitorin vitro: Treatment of DU-145 cells with M-110 or with a structurally unrelated PIM inhibitor, SGI-1776, significantly reduces pSTAT3Tyr705 expression without affecting the expression of STAT3. Furthermore, treatment of DU-145 cells with M-110 attenuates the interleukin-6–induced increase in pSTAT3Tyr705 [1]. M-110 treatment of APC-mutant DLD-1 cells, preferentially attenuated constitutive TOPFLASH activity as compared with FOPFLASH, and had no effect on the CMV-β-galactosidase control reporter. In SW480 cells, M-110 also decreased the levels of free cytoplasmic β-catenin as determined by E-cadherin pull down assays. M-110 also blocked Wnt signaling when other destruction complex components were disrupted, including abrogation of AXIN1/2 expression using siRNAs or inhibition of GSK3β activity using LiCl or I3M [2].
Inezetamab is a bispecific anti-CD40 and anti-MSLN IgG1 monoclonal antibody[1].
Imvotamab (IGM-2323) is a CD20xCD3 bispecific IGM antibody with dual action mechanism. Imvotamab is used to induce physiological T cell activation to prevent over-stimulation and subsequent down-regulation of immune function. Imvotamab is currently being developed for the treatment of B-cell malignant tumors, multiple myeloma (MM) and non-Hodgkin's lymphoma (NHL)[1][2][3][4].