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CC-3060 is a Cereblon modulator that promotes ZBTB16 degradation. CC-3060 degrades ZBTB16 with a DC50 of 0.47 nM in HT-1080 cells. CC-3060 targets ZBTB16 for degradation by primarily engaging distinct structural degrons on different zinc finger domains .
Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells .
3-Methylcarbazole is an carbazole alkaloid compound with anticancer effects. 3-Methylcarbazole shows growth inhibitory activity (IC50 of 25 μg/mL) on human fibrosarcoma HT-1080 cells .
UAMC-4821 is an inhibitor for ferroptosis with an IC50 of 5.2 nM. UAMC-4821 scavenges free radicals, blocks the lipid peroxidation, inhibits ML162 (HY-100002)-induced ferroptosis, and exhibits protective effect in HT-1080 cell. UAMC-4821 exhibits good pharmacokinetics characteristics in mouse with an oral bioavailability of 63%. UAMC-4821 can cross blood-brain barrier .
Ferroptosis-IN-11 (compound 43) is a ferroptosis inhibitor. Ferroptosis-IN-11 can inhibit Erastin (HY-15763) induced ferroptosis in HT-1080 human fibroblasts (EC50=36 nM). Ferroptosis-IN-11 can be used in the study of cardiovascular disease and neurodegeneration .
Paclitaxel octadecanedioate (compound PTX-FA18) is comprised of Paclitaxel (HY-B0015) conjugated to 1,18-octadecanedioic acid (HY-W005178). Paclitaxel octadecanedioate mixed with human serum albumin (HAS) is cytotoxic to HT-1080, PANC-1, HT-29 and Hela cells (IC50s = 12, 2.48, 8.62, and 64.42 nM, respectively) .
GDCNF-11 is a HIM-PROTAC GPX4 degrader based on the chaperone protein HSP90. GDCNF-11 promotes the ubiquitination and degradation of GPX4 through the HSP 90 chaperone complex, reduces endogenous GPX4 expression to induce ferroptosis in HT-1080 cells, and the DC50 value is 0.08 μM (Pink: Target protein ligand (HY-153748); Blue: HSP90 ligand (HY-10212); Black: Linker (HY-W169526)) .
CID-663143 targets microtubule-associated proteins, not tubulin itself, to inhibit the polymerization process within cells. CID-663143 inhibits cancer cell growth (IC50: <100 nM for HT-1080, BJeLR, MCF10A cells) .
1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one (compound 6) shows antiproliferative activity with ED50s of 57.7, 78.8 μM for 26-L5 and HT-1080 cells, respectively. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one inhibits melanogenesis in B16 melanoma 4A5 cells. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one has the potential for the research of skin disorders .
1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one (compound 39), a diarylheptanoid, exhibits antiproliferative activity towards human HT-1080 fibrosarcoma and murine colon 26-L5 carcinoma cells .
Ferrostatin-1 (Fer-1), a potent and selective ferroptosis inhibitor, suppresses Erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM). Ferrostatin-1, a synthetic antioxidant, acts via a reductive mechanism to prevent damage to membrane lipids and thereby inhibits cell death. Ferrostatin-1 exhibits antifungal activity .
Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent .
Ferroptosis inducer-4 (Compound 5) is a ferroptosis (Ferroptosis) inducer with a structure featuring terminal double bonds introduced at the sn-2 position of phospholipids. Ferroptosis inducer-4 exhibits significant cytotoxicity towards HT-1080 cells, with an IC50 of 18 μM. This cytotoxic mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane triggered by the terminal double bonds. Ferroptosis inducer-4 can be used for research on ferroptosis regulation .
OncoACP3 (Compound s43) is a high affinity radioligand for prostatic acid phosphatase (ACP3). OncoACP3, radiolabelled with lutetium-177, selectively accumulates in enzyme-expressing tumors and shows a potent anti-tumor activity with excellent tumor-selective payload deposition in HT1080.hACP3 and PC3.hACP3 tumor-bearing mice model. OncoACP3 can be used for prostate cancer research .
Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells .
Stigmasta-4,22-dien-3-one is an antitubercular agent. Stigmasta-4,22-dien-3-one shows cytotoxicity against human HT1080 tumoral cell line with an IC50 of 0.3 mM .
Cetzole (Compound 1) is a ferroptosis inducer that induces cell death through ROS accumulation. The CC50 values of Cetzole for NCI-H522, NCI-H522 GFP-SCL7A11 #8, NCI-H522 RV-GFP, HT-1080, NARF2, and MDA-MB-231 are 2.56, 10.31, 2.71, 3.07, 14.9, and 6.28 μM, respectively. Cetzole holds potential for research in the field of cancer .
NYY-6a is a Ferroptosis inhibitor. NYY-6a shows significant inhibitory activity against RSL3-induced ferroptosis across 786-O and HT-1080 cells with EC50s of 52 and 50 nM, respectively. NYY-6a functions as a radical trapping antioxidant (RTA) with efficacy of diminishing lipid peroxidation comparable to ferrostatin-1 and liproxtatin-1. NYY-6a is potential for ferroptosis related pathologies reasearch .
Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin (HY-B0075) and Tamoxifen (HY-13757A), which is a potent antagonist of ERα (IC50=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (Ki=3.1 nM) and promotes β-arrestin (EC50=914 nM) and ERK activation (EC50=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC50s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively.
Stigmasta-4,22-dien-3-one-d5 is the deuterium labeled Stigmasta-4,22-dien-3-one (HY-N9596). Stigmasta-4,22-dien-3-one is an antitubercular agent. Stigmasta-4,22-dien-3-one shows cytotoxicity against human HT1080 tumoral cell line with an IC50 of 0.3 mM .
DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in cells. DIF-3 induces reactive oxygen species (ROS) and autophagy. DIF suppresses the growth of Trypanosoma. cruzi in HT1080 cells. DIF-3 exerts antitumor effects both in vitro and in vivo .
mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research .
PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)) .
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
ZX782 is a Hty-type PROTAC targeting GPX4 and a ferroptosis inducer, which induces GPX4 degradation and significantly increases lipid ROS accumulation in HT1080 cells. ZX782 can be used to treat AD by reducing the size and/or number of brain amyloid plaques and by inhibiting the spread of IL-1beta-positive microglial-like cells around amyloid plaques. ZX782 is labeled with hydrophobic benzyl alcohol (HBA) and appears bright blue under acidic conditions, which can be used for quantitative determination . ZX782 is composed of target protein ligand (red part) ML-210 (HY-100003), PROTAC linker (black part) Bromo-PEG2-CH2-Boc (HY-141371) and Hty molecule (blue part) Adamantan-1-ylmethanamine (HY-W037848). The conjugate consisting of Hyt and linker parts is Adamantan-C-amide-PEG2-C-Br (HY-161974), and the activity control of the target protein ligand is Hydroxyl-ML-210 (HY-161973).
BAY-593 (hydrochloride) is an orally active GGTase-I inhibitor. BAY-593 (hydrochloride) can block YAP1/TAZ signaling in animals and has antitumor activity .
FINO2 is a potent ferroptosis inducer. FINO2 inhibits GPX4 activity. FINO2 is a stable oxidant that oxidizes ferrous iron and stable at varying pH levels. FINO2 causes widespread lipid peroxidation .
IDH1 Inhibitor 9 (compound 11S) is a potent IDH1 inhibitor with IC50 values of 124.4, 95.7 nM for IDH1 R132H, IDH1 R132C, respectively. IDH1 Inhibitor 9 induces apoptosis and cell cycle arrest at the S phase. IDH1 Inhibitor 9 shows anti-tumor activity .
Piperazine erastin is an analog of erastin which induces an iron-dependent form of non-apoptotic cell death, termed ferroptosis. Piperazine erastin can be used in cancer research .
GSK3178022 is a human IgG1 monoclonal antibody (mAb) targeting LRP6. GSK3178022 inhibits the expression of WNT target genes SP5 and AXIN2. GSK3178022 has antitumor activity in the RSPO fusion model of colorectal cancer. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
Antitumor agent-88 exhibits potent antimitotic activity and arrests cell in the G2/M phase. Antitumor agent-88 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells. Antitumor agent-88 is also a competitive inhibitor of CYP1A1 (Ki: 1.4 μM) .
GPX4 activator 1 (Compound A9) is a allosteric activator of GPX4 (Kd = 5.86 μM, EC50 = 19.19 μM). GPX4 activator 1 can selectively act on ferroptosis and prevent the accumulation of intracellular lipid peroxides caused by ferroptosis inducers .
Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively . Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection [2].
Fentomycin is a bifunctional Lipolysis-Targeting Chimera (LIPTAC). Fentomycin can target plasma membrane phospholipids, activate lysosomal iron upon endocytosis, and promote oxidative degradation of phospholipids and ferroptosis. Fentomycin can effectively kill primary sarcoma and pancreatic ductal adenocarcinoma cells, especially targeting CD44 high-expression metastatic and drug-resistant cell subpopulations. Fentomycin has anti-tumor activity .
DDO-6691 is a heat shock protein 90 (HSP90) inhibitor. DDO-6691 has antiproliferative effects on a variety of tumor cells, with HCT-116 colon cancer cells being the most sensitive (IC50: 1.08 μM). DDO-6691 exhibits potent tumor growth inhibition in the HCT-116 xenograft mouse model .
Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 .
Geiparvarin is an anticancer agent and an inhibitor of MAO-B (pIC50 = 6.84 μM). Geiparvarin exerts anti-tumor effects by downregulating COX2 expression and inhibiting angiogenesis. Geiparvarin blocks the cell cycle at the G1 phase and induces apoptosis of cancer cells. Geiparvarin has anti-microtubule activity and destroys the cytoskeleton to exert anti-proliferative effects. Geiparvarin has research significance for lung cancer, leukemia, and breast cancer .
GSK3178022 is a human IgG1 monoclonal antibody (mAb) targeting LRP6. GSK3178022 inhibits the expression of WNT target genes SP5 and AXIN2. GSK3178022 has antitumor activity in the RSPO fusion model of colorectal cancer. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
3-Methylcarbazole is an carbazole alkaloid compound with anticancer effects. 3-Methylcarbazole shows growth inhibitory activity (IC50 of 25 μg/mL) on human fibrosarcoma HT-1080 cells .
Stigmasta-4,22-dien-3-one is an antitubercular agent. Stigmasta-4,22-dien-3-one shows cytotoxicity against human HT1080 tumoral cell line with an IC50 of 0.3 mM .
Geiparvarin is an anticancer agent and an inhibitor of MAO-B (pIC50 = 6.84 μM). Geiparvarin exerts anti-tumor effects by downregulating COX2 expression and inhibiting angiogenesis. Geiparvarin blocks the cell cycle at the G1 phase and induces apoptosis of cancer cells. Geiparvarin has anti-microtubule activity and destroys the cytoskeleton to exert anti-proliferative effects. Geiparvarin has research significance for lung cancer, leukemia, and breast cancer .
Stigmasta-4,22-dien-3-one-d5 is the deuterium labeled Stigmasta-4,22-dien-3-one (HY-N9596). Stigmasta-4,22-dien-3-one is an antitubercular agent. Stigmasta-4,22-dien-3-one shows cytotoxicity against human HT1080 tumoral cell line with an IC50 of 0.3 mM .
CDC123 Antibody (YA2773) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2773), targeting CDC123, with a predicted molecular weight of 39 kDa (observed band size: 39 kDa). CDC123 Antibody (YA2773) can be used for WB, IP, FC experiment in human, mouse, rat background.
Cetzole (Compound 1) is a ferroptosis inducer that induces cell death through ROS accumulation. The CC50 values of Cetzole for NCI-H522, NCI-H522 GFP-SCL7A11 #8, NCI-H522 RV-GFP, HT-1080, NARF2, and MDA-MB-231 are 2.56, 10.31, 2.71, 3.07, 14.9, and 6.28 μM, respectively. Cetzole holds potential for research in the field of cancer .
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