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Butyrolactone 3 (MB-3) is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM). Butyrolactone 3 can be used in studies of cancer, metabolic, autoimmune and neurological diseases .
MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344, a liver-targeted thyroid hormone receptor-β agonist . MB-07811 has cholesterol and triglycerides lowering activity .
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects .
Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70 .
MB05032 is a special and efficacious gluconeogenesis inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM.
Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT2C receptor with an EC50 of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB) .
Tetrabutylammonium hydrosulfate is a quaternary ammonium salt that is commonly used as a phase transfer catalyst, acid catalyst and reagent in various chemical reactions, especially in organic synthesis. Tetrabutylammonium hydrosulfate has unique chemical properties that allow it to facilitate the transfer of ions or molecules from one phase to another, making it an important ingredient in a variety of industrial processes.
Narmafotinib (AMP-945) is an orally active inhibitor of the enzyme focal adhesion kinase (FAK, KD=0.21 nM). Narmafotinib inhibits autophosphorylation of 397Y-FAK in MDA-MB-231 cells with an IC50=7 nM and exhibits low general cellular toxicity (IC50=2.7 μM, MDA-MB-231 cells). Narmafotinib can be used for anti-cancer study .
3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division .
Anti-Mouse CD20 Antibody (MB20-11) is a kind of mouse IgG2c antibody inhibitor, targeting to CD20. Anti-Mouse CD20 Antibody (MB20-11) can deplete mature B cells in lymphoid tissues. Anti-Mouse CD20 Antibody (MB20-11) can be used for the researches of cancer, immunology and metabolic Disease, such as lymphoma and diabetes .
C188 (CPD188) is a STAT3 inhibitor with anticancer effects. C188 inhibits STAT3 SH2/pY-peptide binding (IC50 of 20 µM against pY-peptide binding) and IL-6-mediated STAT3 phosphorylation. C188 is selective for STAT3 over STAT1. C188 inhibits nuclear-to-cytoplasmic translocation of Stat3. C188 shows highly active induces apoptosis in breast cancer cell lines with constitutive Stat3 activation (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively) .
Notoginsenoside Fe (Notoginseng triterpenes; Ginsenoside Mb) is a saponin with anti-obesity and anti-neuroblastoma activities. Notoginsenoside Fe can be isolated from leaves of Panax notoginseng. Notoginsenoside Fe specifically activates paraventricular nucleus neurons in the hypothalamus, effectively reducing body weight, improving fasting blood glucose and protecting liver function by decreasing food intake, increasing resting metabolic rate and enhancing energy expenditure. Notoginsenoside Fe also inhibits the c-Src signaling pathway, blocks the proliferation and viability of human neuroblastoma cells, while improving mitochondrial dysfunction and alleviating apoptosis. Notoginsenoside Fe can be used in studies related to diet-induced obesity and neuroblastoma .
VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth .
MB710, an aminobenzothiazole derivative, is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds tightly to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1 μM. MB710 shows anticancer activity in p53-Y220C cell lines .
LC-MB12 is an orally activePROTAC compound targets FGFR2 degradation with a DC50 of 11.8 nM. LC-MB12 contains BGJ398 (a FGFR2 inhibitor), PROTAC linker and CRBN.LC-MB12 inhibits FGFR2 signaling in gastric cancer cells and has anti-tumor activity .
Clorgyline (M&B 9302) is an orally active, blood-brain barrier permeable and selective monoamine oxidase A (MAO-A) inhibitor. Clorgyline's selective inhibition of MAO-A leads to reduced metabolism of neurotransmitters such as serotonin (5-hydroxytryptamine), which accumulates in the brain. Clorgyline can be used in the study of depression and neurodegenerative diseases .
MB-07344 is a potent thyroid hormone receptor (TR)-β agonist with a Ki of 2.17 nM. MB-07344 has additive cholesterol lowering activity in combination with Atorvastatin (HY-B0589) in rabbits, dogs and monkeys .
UR-MB108 is a selective ABCG2 inhibitor with an IC50 value of 79 nM. UR-MB108 acts as a potent inhibitor of ABCG2 transport and ATPase activity. UR-MB108 can be used in cancer-related research .
Ninerafaxstat trihydrochloride (IMB-1018972 trihydrochloride) is the trihydrochloride salt form of Ninerafaxstat (HY-139577). Ninerafaxstat trihydrochloride is a novel orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat trihydrochloride competitively inhibits 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation, and shifts cardiac energy metabolism from free fatty acid oxidation to glucose oxidation, regulating myocardial substrate utilization and thereby improving cardiac efficiency. Ninerafaxstat trihydrochloride can be used for research on cardiovascular diseases .
MB-07729 is a potent fructose 1,6-bisphosphatase (FBPase) noncompetitive inhibitor with IC50 values of 31, 121, and 189 nM for human, monkey, and rat, respectively.
Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
MB07803 is an orally available prodrug of a potent, noncompetitive inhibitor (MB07729) of fructose 1,6-bisphosphatase (FBPase), with EC50 of 140 nM and t1/2 of 7.6±2.9 h.
MB-VC-MGBA is a agent-linker conjugate for ADC with potent antitumor activity by using MGBA (minor-groove-binding DNA-alkylating agent), linked via the ADC linker MB-VC .
MB-07344 sodium is a potent thyroid hormone receptor (TR)-β agonist with a Ki of 2.17 nM. MB-07344 sodium has additive cholesterol lowering activity in combination with Atorvastatin (HY-B0589) in rabbits, dogs and monkeys .
MB-66 (MAPP-66) is a fully human IgG1 antibody that targets HSV and HIV. MB-66 is a monoclonal antibody film for vaginal application. The isotype control for MB-66 can refer to Human IgG1 kappa, Isotype Control (HY-P99001) .
Duocarmycin MB is an antibody agent conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MB can be used against multi-agent resistant cell lines.
hMAO-B/MB-COMT-IN-1 is a dual MAO-B/MB-COMT inhibitor (IC50s: 2.5 μΜ for hMAO-B, 3.84 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-1 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-1 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD) .
CFM-5 inhibits CARP-1/CCAR1-APC-2 interaction with an IC50 value of 0.75 μM. CFM-5 inhibits medulloblastoma (MB) cell proliferation and induces apoptosis .
MitoBloCK-1 (MB-1) is an inhibitor that blocks the import of substrates that use the TIM22 import pathway. MitoBloCK-1 inhibits import by preventing binding of substrate to tim9/10 complex to the substrate, thus the substrate failed to be reach the TIM22 translocon. MitoBloCK-1 inhibits protein import of TIM22 substrates into mitochondria. MitoBloCK-1 attenuates the import of the carrier proteins including the ADP/ATP and phosphate carriers. MitoBloCK-1 also inhibits the import of an additional carrier protein, PiC, and the outer membrane protein Tom40 .
JNN-5 is a potent and selective JAK2 inhibitor with an IC50 of 0.41 nM. JNN-5 shows strong antiproliferative activities in the TNBC cell lines (MDA-MB-468, MDA-MB-213, HCC70, MDA-MB-157) .
Mordant Blue 13 is a synthetic dye used in the textile industry. It belongs to a class of metal complex dyes that are able to form strong bonds with fabrics and other materials. Mordant Blue 13 is commonly used for dyeing cotton, wool and silk fibres, it produces a fast blue color. It can be applied to textiles by a variety of methods including impregnation, padding and printing.
GPX4-IN-15 (Compound C1) is an inhibitor for GPX4, that inhibits 19.8% GPX4 at 1 μM. GPX4-IN-15 inhibits the proliferation of cancer cell MDA-MB-468, BT-549 and MDA-MB-231 with IC50 of 0.86, 0.96 and 0.48 μM .
Mps1-IN-10 (Compound 9) is an inhibitor for Mps1 with an IC50 of 6.4 nM. Mps1-IN-10 inhibits the proliferation of cancer cell MDA-MB-231 with a GI50 of 11 nM. Mps1-IN-10 exhibits anti-tumor efficacy in mice MDA-MB-231 xenograft models .
MB-Buf is a conjugation of methylene blue (HY-14536) and bufalin (HY-N0877) . MB-Buf can targeting degrade GPX4 upon light activation. MB-Buf can induce cell apoptosis, ferroptosis, and ROS production. MB-Buf can be used for the research of cancer, such as breast cancer .
MB-11362 is an orally active, selective HCV NS5B polymerase inhibitor and 4′-azidouridine triphosphate prodrug. MB-11362 can be converted to 4′-azidouridine triphosphate after oral administration. MB-11362 can be used in the research of HCV infection .
MB076 is a novel heterocyclic triazole with improved plasma stability. MB076 inhibits seven different Class C Acinetobacter-derived cephalosporinases (ADCs) β-lactamase variants with Ki values <1 μM. MB076 acts synergistically in combination with multiple cephalosporins to restore pBCSK(-) susceptibility .
MB-0223 is a potent and selective dynamin-related GTPase Drp1 partial inhibitor (IC50=1.3 μM) over other dynamin family members, Opa 1 and dynamin-1 (IC50>100 μM) .
(Rac)-Managlinat dialanetil ((Rac)-MB06322) is a compound for the inhibition of type 2 diabetes that is in Phase II clinical trials and works by inhibiting gluconeogenesis.
Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol (compound 45) is a camptothecin compound that can inhibit cell proliferation, with an IC50 of 2.92 ng/mL for MDA‑MB‑468 cells. Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol can be used for the research of cancer .
AZD3409 is a prenyl inhibitor that exhibits inhibitory activity against both farnesyl transferase and geranylgeranyl transferase I. AZD3409 inhibits the growth of breast cancer cells, with IC50s of 220 nM (MDA-MB-468), 180 nM (MDA-MB-361), and 290 nM (SK-Br-3). AZD3409 significantly reduces the activation level of AKT in breast cancer cell lines. AZD3409 induces G0/G1 phase arrest in MDA-MB-468 cells, causes G2/M phase arrest in MDA-MB-361 cells. AZD3409 can be used for the study of breast cancer .
TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer .
PhAc-ALGP-Dox, a peptide-drug conjugate, is a novel anticancer prodrug, with IC50 values ranged from 311 nM to 34.25 μM for TNBC (E0771), normal murine epithelium (HC-11), human TNBC (MDA-MB-231 and MDA-MB-468), human CrC (LS 174T), normal human epithelium (HME-1) cells .
KT53 is a highly active, selective, and cell penetrable GSTO1 inhibitor. KT53 can effectively inhibit GSTO1 activity in MDA-MB-435 (IC50 = 35 nM) cells. KT53 significantly enhances the killing effect of cisplatin (HY-17394) on MDA-MB-435 cancer cells. KT53 can be used for cancer research .
ROR1-IN-4 is a selective ROR1 inhibitor with a Kd of 52 nM. ROR1-IN-4 shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 75 nM). ROR1-IN-4 reduces colony formation, induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. ROR1-IN-4 demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts. ROR1-IN-4 can be used for the study of triple-negative breast cancer (TNBC) .
PROTAC PARP1 degrader-2 (Compound 72) is a PROTAC degrader for PARP with a DC50<10 nM in MDA-MB-231 cell. PROTAC PARP1 degrader-2 inhibits the cell viability of MDA-MB-436 with an IC50 <100 nM. (Blue: ligand for target protein (HY-160937); Pink: ligand for E3 ligase (HY-W998262))
SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg) .
Thailanstatin A cyclohexane diamine formic is an analog of Spliceostatin (HY-16466). Thailanstatin A cyclohexane diamine formic inhibits proliferations of cells N87 (IC50 is 0.33 μM), BT474 (IC50 is 0.34 μM), MDA-MB-361-DYT2 (IC50 is 0.88 μM) and MDA-MB-468 (IC50 is 0.27 μM). Thailanstatin A cyclohexane diamine formic is used as a drug-linker conjugate for ADC molecule .
MB-314 is a human IgG1 monoclonal antibody (mAb) targeting Lewis Y. MB-314 induces enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. MB-314 increases the release of IFN-γ, TNF-α, MCP-1, and IL-6. MB-314 can be used in cancer research .
MB-311 is a humanized antibody expressed in CHO cells, targeting Lewis Y. MB-311 has a huIgG1 heavy chain and a huλ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for MB-311 can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
POP-3MB (compound 1b) is an ICMT inhibitor (IC50: 2.5 μM). POP-3MB changes the subcellular localization of K-Ras and inhibits Ras activation. POP-3MB also inhibits Erk phosphorylation .
MB327 is a bipyridine nonoxime compound that restores neuromuscular function. MB327 restores the activity of nicotinamide acetylcholine receptors (nAChRs) for carbachol desensitization in a typical type II PAM manner. MB327 can neutralize nerve agent poisoning .
MB 488 NHS ester is a fluroescent agent with a terminal NHS ester group. MB 488 NHS ester is a green fluorescent, very hydrophilic dye molecule that has a maximal absorption of 501 nm and emission at 524 nm. The NHS ester can be applied to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.
HDAC-MB a probe that is activated by HDAC6 and can detect and eliminate glioma cells through activation by HDAC6. HDAC-MB reveals antimetastatic and antiproliferative properties, inhibits glioma invasion and induces cellular apoptosis .
hMAO-B/MB-COMT-IN-2 is a dual MAO-B/MB-COMT inhibitor (IC50s: 4.27 μΜ for hMAO-B, 2.69 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-2 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-2 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD) .
MB 660R DBCO is a bright and photostable far-red dye that emits fluorescence at about 685 nm in the borderline spectral region between far-red and near-IR. Although the absorption maximum is at around 665 nm, this dye can be sufficiently excited by the 633 or 635 nm laser. MB 660R DBCO is water soluble and pH-insensitive from pH 4 to pH 10. MB 660R DBCO is a rhodamine-based dye, and like rhodamine dyes in general, it is very bright and exceptionally photostable.
MB 660R NHS Ester is a fluroescent agent with a terminal NHS ester group.MB 660R NHS Ester is a far-red fluorescent dye that has a maximal absorption of 665 nm and emission at 690 nm. The NHS ester can be applied to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.
MB Human Pre-designed siRNA Set A contains three designed siRNAs for MB gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Mb Mouse Pre-designed siRNA Set A contains three designed siRNAs for Mb gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
MB21D2 Human Pre-designed siRNA Set A contains three designed siRNAs for MB21D2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
2'-O-MB-cGMP (2′-O-Monobutyryl-cGMP) sodium is a cyclic GMP-specific phosphodiesterase inhibitor with an I50 value of 35 µM. 2'-O-MB-cGMP (2′-O-Monobutyryl-cGMP) sodium inhibits Ca 2+ dependent phosphodiesterase hydrolysis using cAMP or cGMP as substrate .
Anti-Mouse CD45RB Antibody (MB23G2) is a rat-derived IgG2a κ type antibody inhibitor, targeting to mouse CD45RB. Anti-Mouse CD45RB Antibody (MB23G2) blocks CD45RB and induces transplantation tolerance. Anti-Mouse CD45RB Antibody (MB23G2) can be used for the researches of infection, immunology and metabolic disease, such as diabetes and Mem71 (H3N1) virus-infection .
MC3629 is an inhibitor of histone methyltransferase (EZH2) with anti-tumor activity. MC3629 inhibits SHH MB cancer cell proliferation and self-renewal and induces apoptosis. MC3629 can be used to study drug resistance in tumor aggressiveness .
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
DLC-50 is a dual inhibitor for PARP-1 and HDAC-1 with IC50 of 1.2 nM and 31 nM. DLC-50 inhibits the proliferation of cancer cells MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 of 0.3, 2.7 and 2.41 μM. DLC-50 induces apoptosis in MDA-MB-231, arrests the cell cycle at G2 phase .
Anticancer agent 249 (Compound 89) is an inhibitor for Hsp90β with IC50 of 16.5 μM in PC3MM2 cell. Anticancer agent 249 inhibits proliferation of cancer cells MCF-7, T47D, MDA-MB-231, MDA-MB-468 and SKBr3 with IC50 of 1.8-5.3 μM. Anticancer agent 249 induces apoptosis in MDA-MB-231. Anticancer agent 249 exhibits antitumor efficacy in mice .
Anticancer agent 267 (Compound 5q) is the activator for RIPK3 and MLKL. Anticancer agent 267 inhibits the proliferation in a variety of cancer cell lines (IC50 for MDA-MB-231, MDA-MB-486 and MCF-7 is 9.79, 10.77 and 5.94 μM, respectively), arrests cell cycle at subG1 phase, and induces necroptosis in cell MDA-MB-231. Anticancer agent 267 exhibits antitumor activity in mouse xenograft models .
Danazol standard inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
Anticancer agent 231 (Compound P5) is a tyrosine protein kinase inhibitor with a IC50 value of 3.95 μM. Anticancer agent 231 inhibits the cell viability, cell proliferation, cell migration and cancer dryness of triple negative breast cancer (TNBC) cells by targeting EGFR-ERK 1/2 signaling pathway, and is expected to play an important role in the field of TNBC disease therapy .
WZ-2-033 is a potent STAT3 inhibitor. WZ-2-033 inhibits MDA-MB-231, HCC70, and MDA-MB231-4175 cells proliferation, colony survival, migration, and invasion with IC50s of 0.7, 1.3, and 1.3 μM, respectively .
Antiproliferative agent-22 (compound 2) is an anticancer agent. Antiproliferative agent-22 shoes anti-proliferative activities against MCF-7, MDA-MB-231 and MDA-MB-468 cells with IC50 values of 6.2 μM, 3.3 μM and 3.3 μM, respectively .
JMX0293 is an O-alkylamino-tethered salicylamide derivative compound. JMX0293 maintains good potency against MDA-MB-231 cell line (IC50 = 3.38 μM) while exhibiting very low toxicity against human non-tumorigenic breast epithelial cell line MCF-10A (IC50> 60 μM). JMX0293 inhibits STAT3 phosphorylation and contribute to apoptosis in TNBC MDA-MB-231 cells. JMX0293 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo without significant toxicity .
Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
N-[4-(2,4-Dimethylphenyl)-2-thiazolyl]-4-pyridinecarboxamide is a derivative of INH1 with anticancer activity. It is cytotoxic to MDA-MB-231, MDA-MB-488, HeLa, and K562 cells (IC50s=1.1, 3.4, 1.6, and 1.2 μM, respectively).
FAK-IN-11 (Compound 4l) is a FAK inhibitor. FAK-IN-11 binds to the ATP binding pocket of FAK, and inhibits phosphorylation of FAK protein. FAK-IN-11 shows cytotoxic activity against the MDA-MB-231 cells with an IC50 of 13.73? μM. FAK-IN-11 induces non-apoptotic cell death in MDA-MB-231 cells .
RIDR-PI-103 is a reactive oxygen species (ROS)-induced agent release proagent with a self-cyclizing moiety linked to a pan-PI3K inhibitor (PI-103). Doxorubicin and RIDR-PI-103 shows a synergistic effect in MDA-MB-361 and MDA-MB-231 cells to inhibit cancer cell proliferation .
Apoptosis inducer 32 (Compound 7g) is an apoptosis inducer with a KD of 42 μM, showing anti-tumor activity. Apoptosis inducer 32 caused significant cellular morphological changes in MDA-MB-231 cells, including membrane bubbling, nuclear fragmentation, and apoptotic body formation. The IC50 of Apoptosis inducer 32 in MCF-7, MDA-MB-231, and HEK cells is 4.77, 6.56 and 337.8 μM respectively .
MB4253 is an orally active aliphatic amide and schistosomicidal agent. MB4253 acts against Schistosoma mansoni. MB4253 can be used for the research of schistosomiasis .
MB725 is an ethylamide analogue of MB710 (HY-120373). MB725 increases mRNA levels of a range of p53 target genes, notably PUMA, p21, MDM2, NOXA and BAX. MB725 shows selective anticancer activity against p53-Y220C cancer .
MB-m-borate is a double-locked near-infrared fluorescence-activated probe (Ex/Em ≈ 647 nm/684 nm). MB-m-borate undergoes cascade activation by hydrogen peroxide and tyrosinase to release the fluorophore methylene blue, thereby generating a fluorescence activation response. MB-m-borate enables precise detection of melanoma in melanoma cells and mouse models. MB-m-borate can be used for melanoma research .
MB 543 DBCO is a fluroescent agent with a terminal DBCO group. The DBCO group is commonly used for copper-free Click Chemistry reactions due to its strain promoted high energy. MB 543 Alkyne is a very hydrophilic, water-soluble, orange fluorescent dye that has a maximal absorption of 543 nm and emission at 566 nm. The compound is also pH insensitive from pH 3 to pH 10.
3MB-PP1 (Standard) is the analytical standard of 3MB-PP1 (HY-102069). This product is intended for research and analytical applications. 3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division .
Mb Rat Pre-designed siRNA Set A contains three designed siRNAs for Mb gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
2'-O-MB-cAMP (sodium) (Standard) is the analytical standard of 2'-O-MB-cAMP (sodium). This product is intended for research and analytical applications.
DN1679 is a potent, selective and orally active CRBN-dependent CDK12/13 PROTAC dual degrader. DN1679 shows DC50 of 8.8/9.8 nM (MDA-MB-231), 5.1/6.4 nM (MDA-MB-157) and 17.2/15.8 nM (MDA-MB-468) for CDK12/13. DN1679 can downregulate DNA damage response gene mRNA levels, such as ATM, ATR, BRCA1 and RAD51. DN1679 demonstrates a potent synergistic anti-tumor effect companied with Olaparib (HY-10162). DN1679 can be used for research of triple-negative breast cance .
Pz 285 is an anti-cancer agent. Pz 285 shows significant inhibitory effect on the viability of MDA-MB-231 breast cancer cells, with an IC50 of 15.0 μM. Pz 285 exhibits remarkable antitumor effects in the mouse tumor xenograft model constructed with highly lung-metastatic MDA-MB-231 LM24 Her2+ breast cancer cells. Pz 285 can be used for the study of breast cancer, especially metastatic breast cancer .
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) .
Apoptosis inducer 44 is an apoptosis inducer. Apoptosis inducer 44 triggers apoptosis in MDA-MB-231 cells by increasing the levels of Bax and Cyt C, reducing Bcl-2, and initiating caspase-3 cleavage. Apoptosis inducer 44 suppresses the invasion and migration of MDA-MB-231 cells by down-regulating MMP-2 and MMP-9 expression and up-regulating E-cadherin protein levels. Apoptosis inducer 44 can be used for the study of breast cancer .
PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTACHsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively .
EGFR-IN-137 (Compound 4c) is an inhibitor for aromatase and EGFR with IC50s of 1.67 μg/mL and 0.08 μg/mL. EGFR-IN-137 inhibits the proliferation of cancer cell MCF-7 and MDA-MB-231 with IC50s of 1.62 µM and 4.14 µM. EGFR-IN-137 arrests the cell cycle at G0/G1 phase in MDA-MB-231, and induces apoptosis through caspase-dependent pathway .
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .
PMMB-187 is a selective STAT3 inhibitor with an IC50 value of 1.81 μM for MDA-MB-231 cells. PMMB-187 induces apoptosis (Apoptosis) in MDA-MB-231 cells by inhibiting STAT3 transcriptional activity, nuclear translocation, and downstream target gene expression, while also reducing mitochondrial membrane potential, generating reactive oxygen species (ROS), and upregulating the expression levels of apoptosis-related proteins. PMMB-187 has potential applications in cancer research .
CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
PROTAC FAK degrader 2 (Compound F2) is a PROTAC degrader for focal adhesion kinase (FAK), with DC50 of 27.72 and 60.1 nM, for total FAK and phosphorylated p-FAK. PROTAC FAK degrader 2 inhibits cell viability of cancer cells 4T1, MDA-MB-231, MDA-MB-468 and MDA-MB-435, with IC50s of 0.73-5.84 μM. PROTAC FAK degrader 2 reverses the multidrug resistance (MDR) through inhibition of AKT and ERK signaling pathway. PROTAC FAK degrader 2 exhibits antitumor efficacy in HCT/8 xenograft mouse model. (Pink: ligand for target protein Ifebemtinib (HY-122844); Black: linker (HY-Y0681); Blue: ligand for E3 ligase Thalidomide (HY-14658))
ZD-4190 hydrochloride is a potent VEGFR inhibitor with anti-tumor activity. ZD-4190 hydrochloride can delay the growth of MDA-MB-435 tumors by inhibiting tumor cell proliferation and angiogenesis .
Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells .
Anhydrosecoisolariciresinol is from the flower of Wedelia biflora, has anti-tumor activities .
Anhydrosecoisolariciresinol decreases the growth of human breast cancer MCF-7 and MDA-MB-231 cell lines .
BG11 induces the accumulation of Fe 2+ and intracellular lipid peroxides, induces ferroptosis. BG11 regulates the expression of Bax and Bcl-2 proteins, and induces apoptosis in MDA-MB-231 cell. BG11 arrests the cell cycle at G0/G1 and S phase, inhibits the proliferation of TNBC cancer cell (IC50 for MDA-MB-231 and BT549 is 0.49 μM and 0.52 μM), and inhibits the cell migration and invasion. BG11 exhibits antitumor efficacy in mouse models .
Anticancer agent 280 (Compound 65) is an anti-cancer agent targeting triple-negative breast cancer (TNBC). Anticancer agent 280 exhibits IC50 values of Anticancer agent 280 for MDA-MB-231, MDA-MB-231/LM2-4, Jurkat, and MCF-7 of 7.1, 11.65, 6.99, and 21.51 μM respectively. Anticancer agent 280 can cause significant arrest of cells in the S phase and induce cell apoptosis. Anticancer agent 280 can be used for the study of TNBC .
ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
DS-1-38 is an EYA1 antagonist that blocks Sonic Hedgehog (SHH) signaling. EYA1 is a haloacid dehalogenase phosphatase and transcription factor that regulates tumorigenesis and proliferation in SHH medulloblastoma (SHH-MB) .
ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
Antitumor agent-93 (compound 7D) is an anticancer agent that can effectively inhibit the growth of several tumor cell lines, such as MDA-MB-231 and HCT-116 cell lines .
FAK-IN-17 is a focal adhesion kinase (FAK) inhibitor. FAK-IN-17 possesses anticancer activity against A549 and MDA-MB-231 cell lines with IC50 values of 130 nM and 94 nM .
ZINC194100678 is a potent PAK1 inhibitor with an IC50 value of 8.37 μM. ZINC194100678 can inhibit MDA-MB-231 cell proliferation. ZINC194100678 can be used for researching anticancer .
anti-TNBC agent-10 is an anti-TNBC agent. anti-TNBC agent-10 shows potent anti-TNBC activity against BT549 cells (IC50 = 0.018 μM) and maintains activity against MDA-MB-231 cells (IC50 = 4.16 μM). anti-TNBC agent-10 9 demonstrates significant anti-tumor efficacy in mice bearing subcutaneous MDA-MB-231 TNBC xenografts. anti-TNBC agent-10 can be used for the study of triple-negative breast cancer (TNBC) .
Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM .
SR 13915 is a structural analog of EGCG (HY-13653), a green tea polyphenol, and exhibits an IC50 greater than 100 μM against both MCF‑7 and MDA‑MB‑231 cell lines .
Sinopodophylline B (compound 2) is a flavonoid glycoside compound that is cytotoxic to breast cancer cells. For example, the IC50 of Sinopodophylline B is 1.5 μM (T47D) and 44.2 μM (MDA-MB-231), respectively .
ST6GAL1-IN-1 is an orally active selective ST6GAL1 inhibitor (IC50 = 20 μM). ST6GAL1-IN-1 exhibits high antimetastatic potential, effectively inhibiting the migration of MDA-MB-231 cells at noncytotoxic concentrations. ST6GAL1-IN-1 can disrupt integrin sialylation in MDA-MB-231 cells. ST6GAL1-IN-1 inhibits tumor angiogenesis and cancer metastasis via the Integrin/VEGFR2-mediated signaling pathway. ST6GAL1-IN-1 effectively suppresses both tumor growth and cancer metastasis on the MDA-MB-231 xenograft model. ST6GAL1-IN-1 can be used for the study of Triple-negative breast cancer (TNBC) .
Anticancer agent 280 TFA (Compound 65) is an anti-cancer agent targeting triple-negative breast cancer (TNBC). Anticancer agent 280 TFA exhibits IC50 values of Anticancer agent 280 TFA for MDA-MB-231, MDA-MB-231/LM2-4, Jurkat, and MCF-7 of 7.1, 11.65, 6.99, and 21.51 μM respectively. Anticancer agent 280 TFA can cause significant arrest of cells in the S phase and induce cell apoptosis. Anticancer agent 280 TFA can be used for the study of TNBC .
iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM) .
FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer .
Pinostrobin chalcone is found to be potent natural cytotoxic compounds against MDA-MB-231 and HT-29 colon cancer cell lines(IC50 = 20.42±2.23 and 22.51±0.42 μg/mL) .
MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
Bacilotetrin C analogue is cytotoxic to triple-negative breast cancer cell line MDA-MB-231 with an IC50 of 0.48 μM. Bacilotetrin C analogue can induce tumor cell autophagy and has anti-tumor activity .
Carlina oxide is an AChE inhibitor and antioxidant that kills Culex pipiens larvae (LC50=1.39 μg/mL). Carlina oxide is cytotoxic to vertebrate cells, human dermis, HCT116 and MDA-MB231 cell lines .
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
LM-41 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2. LM-41 inhibits migration of human MDA-MB-231 breast cancer cells .
SG3683 is a DNA-targeted cytotoxic agent belonging to pyrrolobenzodiazepine (PBD) dimers. SG3683 exerts antitumor activity with an IC50 value of 0.74 nM in MDA-MB-436 cells. SG3683 is promising for research of cancers, such as breast cancer .
Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity .
HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
HC-258 (compound 26) binds with the cysteine in TEAD’s PA pocket. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells .
EGFR-IN-153 (Compound 5l) is an EGFR inhibitor. EGFR-IN-153 can inhibit the proliferation (IC50: 0.73 μM) and induce apoptosis of MDA-MB-231 cell. EGFR-IN-153 can be used for the research of breast cancer .
COMT-IN-2 (compund 9) is the potent COMT inhibitor, showing selective inhibition of brain (IC50=24 nM) and liver (IC50=81 nM) MB-COMT compared to the liver S-COMT (IC50=620 nM) isoform .
USP1-IN-7 (Compound 3) is an inhibitor for ubiquitin specific peptidase 1 (USP1) and its cofactor UAF1, with IC50 ≤50 nM. USP1-IN-7 inhibits proliferation of MDA-MB-436 with IC50 ≤50 nM .
Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively .
PHGDH-IN-2 is a potent and NAD + competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells .
USP1-IN-8 (Compound 16) is an inhibitor for ubiquitin specific peptidase 1 (USP1) and its cofactor UAF1, with IC50 ≤50 nM. USP1-IN-8 inhibits proliferation of MDA-MB-436 with IC50 ≤50 nM .
Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
PARP1-IN-20 (compound 19A10) is a potent inhibitor of PARP1, with the IC50 of 4.62 nM and has similar low PARP-Trapping effect compared with Veliparib (HY-10129), IC50 (MDA-MB-436) >100 μM .
BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively .
Breast cancer targeting peptide 18–4 is a KRT1 receptor-targeting peptide, with a Kd of 0.98 μM. The amino acid sequence of Breast cancer targeting peptide 18–4 is WxEAAYQrFL, and it is an analogue of P160 peptide (HY-P10789). When covalently conjugated with the anticancer peptide MccJ25, Breast cancer targeting peptide 18–4 significantly increases the cellular uptake of MccJ25 in breast cancer cells and enhances its anticancer activity. The covalent conjugate exhibits IC50 values of 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR cells, respectively .
MARY1 is a selective 5-HT2BR antagonist with an IC50 of 380 nM and a Ki of 764 nM (human
5-HT2BR). MARY1 induces renal mitochondrial biogenesis (MB) and enhances renal mitochondrial function by increasing mitochondrial respiratory capacity, mitochondrial protein levels, and mitochondrial number in renal proximal tubular cells (RPTCs). MARY1 induces MB through 5-HT2BR and dual PI3K/AKT and RAS/MEK/ERK cell signaling pathways in RPTCs. MARY1 can be used to study renal diseases associated with metabolic and mitochondrial dysfunction .
TTK-IN-5 is an orally active covalent threonine tyrosine kinase (TTK) inhibitor with selectivity (IC50 = 8.918 nM). TTK-IN-5 exhibits anti-proliferative potencies against MDA-MB-231, A2780, HCT116, HCC1569 and MKN1 cell lines (IC50 values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively). TTK-IN-5 potently suppresses tumor growth without notable toxicity in A2780 and MDA-MB-231 xenograft mouse models. TTK-IN-5 can be used for the research of cancer such as breast cancer and ovarian cancer .
SYL3C aptamer sodium is a DNA aptamer that targets epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets a variety of human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd values of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III are 38 nM and 67 nM, respectively. SYL3C aptamer sodium possesses stability, high binding affinity and selectivity, and can be used for targeted cancer cell imaging and circulating tumor cell detection .
Bt354 is an orally active STAT3 inhibitor with IC50 values of 4.6 μM (DU145), 6.5 μM (MDA-MB-435) and 7.2 μM (MDA-MB-231), respectively. Bt354 induces cell cycle arrest and apoptosis, and downregulates epithelial-mesenchymal transition-related genes. Bt354 exhibits anti-angiogenic and anti-inflammatory activities, attenuates the polarization of M1 microglia and A1 astrocytes, suppresses inflammasome-related signaling pathways, and alleviates mechanical hyperalgesia and thermal hyperalgesia. Bt354 can be used in research related to glioblastoma multiforme, triple-negative breast cancer, prostate cancer and neuropathic pain .
Anticancer agent 230 (example 65) is a caseinolytic protease P (ClpP) activator with anticancer activity. Anticancer agent 230 is able to induce the degradation of mitochondrial proteins in SUM159 and MDA-MB-231 triple-negative breast cancer cells in a time-dependent manner .
KIF18A-IN-11 (Compound 13) is a potent KIF18A inhibitor, with IC50 values of less than 100 nM in OVCAR3 and MDA-MB-157 cells. KIF18A-IN-11 can be used for the research of cancer .
Anticancer agent 180 (compound 4) is a secondary metabolite present in fungal strains and extracted through physical interaction with Streptomyces sp. Anticancer agent 180 has potential anti-tumor activity and can inhibit the migration of MDA-MB-231 breast cancer cells .
2-Epitripdiolide is a diterpenoid compound derived from Tripterygium hypoglaucum with significant antitumor activity. Its IC50 values against A549, KB, KBvin, and MDA-MB-231 cells are 1.34, 0.4, 4.4, and 1.2 nM, respectively .
HJC0152 (free base) is an orally active and potent inhibitor of STAT3. HJC0152 (free base) inhibits cell cycle progression and induces apoptosis. HJC0152 (free base) significantly suppresses MDA-MB-231 xenograft tumor growth in mice .
AuM1Phe, an N-Heterocyclic carbene (NHC) metal complexe, blocks the human topoisomerase I activity and actin polymerization reaction. AuM1Phe affects the growth of MDA-MB-231 breast cancer cells, with an IC50 value of 1.2 μM .
Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties.? Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways .
Sempervirine is an indole alkaloid isolated from Gelsemium sempervirens with anti-tumor activities. Sempervirine is against sempervirine-sensitive tumor cells with EC50 values of 2.7 μM, 1.77 μM, and 1.96 μM for Raji, MDA-MB-231 and HeLa cells, respectively .
Anticancer agent 178 (compound C2) is a potent anticancer agent. Anticancer agent 178 inhibits MDA-MB 231 cells proliferation and metabolic activity with IC50s of 1.1 and 4.2 μM. Anticancer agent 178 induces ferroptosis and necroptosis in cells .
iPRMT1 is a potent and selective PRMT1 inhibitor for breast cancer research. iPRMT1 inhibits breast cancer cell growth in vitro and in vivo with EC50 values of 90, 70, and 9 nM in MCF7, T47D, and MDA-MB-231 cells, respectively .
EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .
R1-11 is an indole ICMT inhibitor with an IC50 of 0.6 μM and has anticancer activity. R1-11 inhibits MDA-MB231 and PC3 cells with IC50s of 2.2 μM and 2.0 μM, respectively .
PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model .
Aurora A inhibitor 3 (Compound 5h) inhibits Aurora-A kinase with an IC50 value of 0.78 μM. Aurora A inhibitor 3 is cytotoxic, with GI50 values of 0.12 μM and 0.63 μM for MCF-7 and MDA-MB-231 cells, respectively .
HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769) .
CDK7-IN-28 (CDK7-1276) is a potent CDK7 inhibitor(IC50＜5 nM). CDK7-IN-28 can inhibit proliferation of MDA-MB-468 cell line by blocking cell cycle and inhibiting DNA replication .
SDU-071 is a potent and orally active inhibitor of BRD4-p53 inhibitor. SDU-071 inhibits MDA-MB-231 cells proliferation with an IC50 of 10.5 μM. SDU-071 induces cell cycle arrest and apoptosis .
Tubulin polymerization-IN-55 is a potent inhibitor of Tubulin Polymerization. Tubulin polymerization-IN-55 has antiproliferative activity against A549, K562, HepG2, MDA-MB-231 and HFL-1 with IC50 s of 8, 3, 9, 24 and 62 nM, respectively .
Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes .
BGC4 is a biphenyl-based gold(III) complex. BGC4 inhibits human recombinant thioredoxin reductase (TrxR) with an IC50 of 10.7 μM, exhibits cytotoxicity (IC50 for MDA-MB-231 is 5.4 μM), and induces apoptosis. BGC4 exhibits antitumor efficacy in mouse models .
HDAC6-IN-35 (compound C4 (ZINC000077541942)) is a potent and BBB-penetrated HDAC6 inhibitor with the IC50 of 4.7 μM. HDAC6-IN-35 shows cell toxicity against MDA-MB-231 with EC50 of 40.6 μM .
KIF18A-IN-10 (Compound 24) is a potent KIF18A inhibitor, with an IC50 value of 23.8 nM. KIF18A-IN-10 has anticancer activity, with IC50 values of less than 100 nM in OVCAR3 and MDA-MB-157 cells .
PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells. PROTAC eEF2K degrader-1 mediates eEF2K degradation .
KIF18A-IN-9 (Compound 1) is a potent KIF18A inhibitor, with an IC50 value of 3.8 nM. KIF18A-IN-9 has anticancer activity, with IC50 values of less than 100 nM in OVCAR3 and MDA-MB-157 cells .
ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells .
Crispene E is a STAT3 inhibitor with an IC50 of 10.27 μM against STAT3 dimerization. Crispene E exerts specific cytotoxicity against STAT3-dependent MDA-MB-231 breast cancer cells. Crispene E is applicable to research related to breast cancer .
Hck-IN-2 (Compound 8e) is an HCK inhibitor. Hck-IN-2 is cytotoxic to tumor cells, with IC50 values of 19.58 μM and 1.42 μM against MDA-MB231 and MCF-7, respectively. Hck-IN-2 has anti-tumor activity .
PAD-IN-4 is a potent PAD inhibitor (PAD 1/4, IC50 = 0.273/0.24 μM). PAD-IN-4 shows no significant cytotoxicity against A549 or MDA-MB-231 cells. PAD-IN-4 can be used for the study of cancer and autoimmune diseases .
ICMT-IN-53 (compound 12) is an ICMT inhibitor (IC50=0.96 μM) with PAMPA permeability and antiproliferative activity. ICMT-IN-53 inhibits the proliferation of MDA-MB-231 and PC3 with IC50s of 5.14 μM and 5.88 μM, respectively .
Anthragallol 1,2-dimethyl ether (compound 11) can be isolated from O. umbellata. Anthragallol 1,2-dimethyl ether has cytotoxicity, with IC50 values of 5.9 and 8.8 μg/ml against A549 cells and MDA-MB-231 cells, respectively .
AGPS-IN-1 (Compound 2i) is an effective AGPS binder. AGPS-IN-1 reduces ether lipids levels and cell migration rate. AGPS-IN-1 inhibits epithelial-mesenchymal transition (EMT) in prostate PC-3 and breast MDA-MB-231 cancer cells .
VEGFR-IN-3 (compound 3f) is a VEGFR inhibitor. VEGFR-IN-3 inhibits OVCAR-4 and MDA-MB-468 cancer cells growth with IC50s of 0.29 and 0.35 μM, respectively. VEGFR-IN-3 can be used for the research of cancer .
Anticancer agent 158 (compound 7c) is a potent anticancer agent. The IC50s for inhibiting HepG-2, MDA-MB-231, and HCT-116 cell lines are 7.93 μM, 9.28 μM, 13.28 μM, and 181.89 μM, respectively .
Anticancer agent 245 (Compound 115) inhibits proliferation of cancer cell SKOV3, MDA-MB-231 and HCT-116 with IC50 of 0.021, 0.056 and 0.11 μM, respectively. Anticancer agent 245 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
Hit 14 is an inhibitor for C-X-C chemokine receptor type 4 (CXCR4) with IC50 of 254 nM. Hit 14 inhibits the migration and invasion of cell MDA-MB-231. Hit 14 inhibits the Akt phosphorylation, exhibits anti-inflammatory activity, and ameliorateds the ear swelling and damage in mouse models .
(−)-Voacangarine is an indole alkaloid, which exhibits cytotoxic effects against cancer cells HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 of 5~20 mg/mL. (−)-Voacangarine inhibits the cultivation of Saccharomyces cerevisiae wildtype and repair-deficient mutants .
(Rac)-IBR120 is the racemate of IBR120 (HY-176549A). IBR120 is a RAD51 inhibitor that has significant growth inhibition activity against MDA-MB-468 cells. (Rac)-IBR120 can be used for the research of difficult-to-treat cancers like triple negative breast cancer .
SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM) .
USP1-IN-10 (compound 2) is a potent tricyclic USP1 inhibitor with an IC50 of 7.6 nM. USP1-IN-10 inhibits MDA-MB-436 viability (IC50=21.58 nM). USP1-IN-10 has the potential for cancers research .
EGFR-IN-83 (Compound 9) is an EGFR inhibitor (IC50: 2.53 nM). EGFR-IN-83 has antiproliferative activity against MCF-7 and MDA-MB-231 cells, with IC50 of 2.50 μM and 1.96 μM. EGFR-IN-83 can induce cell apoptosis .
CTX-0294885 hydrochloride is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 hydrochloride is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo .
Apoptosis inducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer (IC50: 12.8 μM) and can induce early apoptosis in breast cancer cells. Apoptosis inducer 27 can bind to DNA molecules, Bax and Bcl-2 proteins, and induce DNA damage .
UNC 0631 (Standard) is the analytical standard of UNC 0631. This product is intended for research and analytical applications. UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM .
YX862 is a selective HDAC8 PROTAC degrader and induces the degradation of HDAC8 with maximum degradation ＞ 95% at 250 nM in MDA-MB-231 cells(Sturcture Note:(Blue: VHL E3 ligand (HY-112078), Black: linker；Pink: HDAC8 inhibitor (HY-163846)) .
CTX-0294885 is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
N-Deacetylthiocolchicine is a tubulin inhibitor with an IC50 value of 2.2 nM in MDR-negative MDA-MB 231 breast cancer cells. N-Deacetylthiocolchicine exerts antiproliferative activity by binding to tubulin to interfere with microtubule assembly, arresting cells in mitosis during the cell cycle. N-Deacetylthiocolchicine is promising for research of malignancies such as breast cancer .
LASSBio-2389 is a selective ROCK2 inhibitor with an IC50 of 0.051 μM and an IC50 of 1.143 μM against ROCK1. LASSBio-2389 reduces the viability of MDA-MB-231 cells and inhibits cell migration. LASSBio-2389 is applicable to the research of triple-negative breast cancer .
Pyoluteorin is an antibiotic that inhibits Oomycete fungi, including the plant pathogen Pythium ultimum, and suppresses plant diseases caused by this fungus . Pyoluteorin induces human triple-negative breast cancer MDA-MB-231 cells apoptosis in vitro. Pyoluteorin can be used for the research of human triple-negative breast cancer .
MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM .
WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3 Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis .
ZM-32 is an inhibitor for human antigen R (HuR), that downregulates the expression of VEGF-A and MMP9, and thus inhibits breast cancer tumor angiogenesis. ZM-32 exhibits broad-spectrum anti-proliferative effects in a variety of cancer cell lines, and exhibits antitumor efficacy against MDA-MB-231 in mouse models .
PS21M is a negative control of CPS-021 (HY-174247). PS21M cannot effectively degrade PAK4 in MDA-MB-231 cells. (Pink: Target Protein Ligand (HY-174822); Black: Linker; Blue: E3 Ligase Ligand (HY-W586822)) .
Pinostrobin chalcone (Standard) is the analytical standard of Pinostrobin chalcone. This product is intended for research and analytical applications. Pinostrobin chalcone is found to be potent natural cytotoxic compounds against MDA-MB-231 and HT-29 colon cancer cell lines(IC50 = 20.42±2.23 and 22.51±0.42 μg/mL) .
KGP591 is a tubulin polymerization inhibitor (IC50 0.57 µM). KGP591 induces significant G2/M stagnation, inhibits cell migration, disrupts microtubule structure and cell morphology in MDA-MB-231 cells. KGP591 shows antitumor activity in orthotopic model of kidney cancer (RENCA) .
Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
FAK-IN-29 is a selective FAK inhibitor with an IC50 of 0.5 nM. FAK-IN-29 can inhibit the proliferation and colony formation of MDA-MB-231 cells, and induce cell cycle arrest and apoptosis. FAK-IN-29 exhibits antitumor activity and can be used for the research of tumors such as triple-negative breast cancer .
Anticancer agent 232 (compound 12f) is a glycohybrid designed using 1-azidoglycosides derived from d-glucose, d-galactose, and d-mannose. The IC50 values of anticancer agent 232 against MCF-7 and MDA-MB231 cells are 1.05 μM and 18.03 μM, respectively .
CDC20-IN-1 (Compound E1) is a specific inhibitor of CDC20 and can be used in triple-negative breast cancer research. CDC20-IN-1 can induce autophagy in cancer cells and inhibit MDA-MB-231 cell proliferation, with an IC50 value of 1.43 μM .
PHGDH-IN-5 (Compound B12) is a covalen inhibitor of PHGDH with an IC50 value of 0.29 μM. PHGDH-IN-5 can inhibit cell proliferation in cancer cell lines overexpressing PHGDH. PHGDH-IN-5 can reduce the production of serine derived from glucose in MDA-MB-468 cells .
SN-38-CM2 is a split esterase, and shows >95% conversion to SN-38 within 5 min in vitro. SN-38-CM2 induces protein-protein interactions (PPI)-dependent esterase to mediate cell death in MDA-MB-231 cells .
Astragaloside IV (Standard) is the analytical standard of Astragaloside IV. This product is intended for research and analytical applications. Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis .
AR ligand 40 (compound 19c) is an Adenosine A1 Receptor ligand with antagonist activity. AR ligand 40 exhibits antiproliferative effect on SW480, SW48, HCT116, K562, MDA-MB-231, and A549 cells with EC50s of 7, 10, 12, 13, 15 and 39 μM .
Camsirubicin (GPX-150) is a non-cardiotoxic Doxorubicin (HY-15142) analog that selectively targets topoisomerase IIβ. Camsirubicin reduces cell viability and clone formation of MDA-MB-468 breast cancer cells. Camsirubicin increases the exposure of CALR and HSP90 on the cell surface. Camsirubicin can be used for the study of breast cancer .
O-Me Eribulin is a derivative of Eribulin and is an ADC cytotoxin that can be used for ADC synthesis. O-Me Eribulin can inhibit the cell viability of SKBR3, MDA-MB-468, and A549 cells, with IC50 values of 0.2052, 0.1827, and 0.5151 nM, respectively. O-Me Eribulin can be used for tumor research .
ML179 (SR-1309) is a inverse LRH1/NR5A2 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer .
PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1 −/−) and Capan-1 (BRCA2 −/−) cells with IC50 values below 0.3 nM .
KUNB106 is a selective Hsp90β inhibitor with KDs of 91 nM and 38 μM against Hsp90β and Hsp90α. KUNB106 exhibits antiproliferative activity against MDA-MB-231 cells, A549 and SKOV-3 cells. KUNB106 can be used for the study of triple negative breast cancer .
CNBCA is a potent, selective, competitive SHP2 enzyme inhibitor, with the IC50 of 0.87 μM. CNBCA binds to full-length SHP2 and inhibits enzyme activity. CNBCA inhibits pAkt and pERK1/2, and the cell growth of BT474 and MDA-MB468 cells. CNBCA can be used for breast cancer study .
Asperphenamate (Standard) is the analytical standard of Asperphenamate. This product is intended for research and analytical applications. Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively[1][2].
Antiproliferative agent-33 (Compound 2g) is an anti-proliferative, antifungal, and antibacterial agent. Antiproliferative agent-33 inhibits MDA-MB-231 cell proliferation (IC50: 16.38 μM). Antiproliferative agent-33 inhibits gram-negative bacteria growth, and inhibits S. faecalis with an MIC value of 8 μg/mL .
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
NMac1 is an orally active Nm23/NDPK activator. NMac1 directly binds to Nm23-H1 and activates the NDPK activity of recombinant Nm23-H1 with an EC50 of 10.7 uM. NMac1 induces AMPK activation and inhibits mTOR and ERK, leading to mitochondrial OXPHOS dysregulation and suppressing mitochondrial ROS production, which in turn induces mitochondrial dysfunction in MDA-MB-231 cells. NMac1 inhibits Complex I activity and suppresses changes in morphology and actin cytoskeleton organization following Rac1 activation in MDA-MB-231 cells. NMac1 inhibits tumor invasion, migration and metastasis. NMac1 is useful for studying metastatic tumors, such as breast cancer. NMac1 can be isolated from the ginger cassumunar Roxb .
Vitexin B-1 is an inhibitor of Bcl-2 and the agonist of Caspase. Vitexin B-1 has cytotoxic effect and induces apoptosis in MCF-7, ZR-75-1, MDA-MB-231, and COC1 cells with IC50s of 3.2, 2.1, 1.8 and 0.39 μM, respectively .
EHop-016 is a potent and selective Rac GTPase Rac1 and Rac3 inhibitor. EHop-016 inhibits Rac1 activity with an IC50 of 1.1 μM in MDA-MB-435 cells. EHop-016 inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration .
Frangulin B (Compd 11g), a potent anticancer agent, is a potential pan RecQ helicase inhibitor . Frangulin B (Compd 11g) induces apoptosis in both HCT-116 and MDA-MB-231 cell lines, but also causes an G2/M phase cell cycle arrest in HCT-116 cells .
Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models) .
JNK-IN-23 (Compound K12) is an inhibitor of JNK. JNK-IN-23 inhibits the proliferation of MDA-MB-231 (GIC50: 30 nM). JNK-IN-23 blocks TNBC metastatic growth in vivo. JNK-IN-23 inhibits the growth of lung metastases by dual targeting of glutaminase-1 (GLS) and pyruvate dehydrogenase complex (PDHC) .
N,O-Diacetyltyramine is a compound with antibacterial activity and cytotoxicity that can be isolated from the actinomycete Pseudonocardia endophytica VUK-10. N,O-Diacetyltyramine has antibacterial activity against Gram-positive and Gram-negative bacteria and fungi. N,O-Diacetyltyramine is cytotoxic to MDA-MB-231, HeLa, MCF-7 and OAW-42 cells .
eIF4E-IN-2 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e) with an IC50 of 13 nM. eIF4E-IN-2 inhibits MDA-MB-361 cells proliferation. eIF4E-IN-2 can be used for the study of breast cancer .
Tubulin polymerization-IN-53 (compound 4b) is an inhibitor of β-tubulin polymerization. Tubulin polymerization-IN-53 can arrest the cell cycle at the G2/M stage. Tubulin polymerization-IN-53 has antiproliferative efficacy against the MDA-MB-231 cell line with an IC50 value of 3.24 μM .
JY-21 is a BRD4PROTAC degrader with a DC50 of 3.797 μM. JY-21 has a potent anticancer activity against MDA-MB-231 cells . Pink: BRD4 ligand (HY-78695); Blue: E3 ligase ligand (HY-174994); Black: linker (HY-151862)
Sophoraflavanone G (Standard) is the analytical standard of Sophoraflavanone G. This product is intended for research and analytical applications. Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties. Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways .
CDK7-IN-26 (compound 36) is an orally active CDK7 inhibitor (IC50: 7.4 nM). CDK7-IN-26 potently inhibits the growth of triple-negative breast cancer (TNBC) cell line-derived xenograft (CDX) tumors in vivo and inhibits MDA-MB-453 cells in vitro with an IC50 of 0.15 μM .
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .
CN009543V is an epidermal growth factor receptor (EGFR) agonist. CN009543V enhances tyrosine phosphorylation of EGFR at Tyr1068 and Tyr1173, thereby activating the MAPK/ERK cascade. CN009543V inhibits the activity of PTP-1B in MDA MB468 cells. CN009543V can be used in cancer research .
Nampt-IN-10 (Compound 4) is an efficient inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). Nampt-IN-10 exhibits nanomolar-level inhibitory activity against cell lines such as MDA-MB453, NCI-N87, and NCI-H526. Nampt-IN-10 can be used as an ADC payload, and the ADC constructed with it as the core demonstrates significant anti-tumor activity .
HIF-1α-IN-2 hydrochloride is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 hydrochloride suppresses HIF-1α expression by blocking transcription and protein translation .
Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer .
Ilexsaponin A (Standard) is the analytical standard of Ilexsaponin A. This product is intended for research and analytical applications. Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes .
Pantinin-3 is an antimicrobial peptide with antitumor activity found in the venom of the emperor scorpion (Pandinus imperator). Pantinin-3 shows selective toxicity against breast cancer cells (MDA-MB-231) and prostate cancer cells (DU-145). Pantinin-3 can induce apoptosis in tumor cells. Pantinin-3 can be used in cancer research .
Catechol O-methyltransferase, porcine liver (COMT), the magnesium-dependent transfer of methyl groups from S-adenosyl methionine to a hydroxyl group on dopamine, converting it to 3-methoxytyramine. Catechol O-methyltransferase has two forms in tissues, a soluble form (S-COMT) and a membrane-bound form (MB-COMT). Catechol O-methyltransferase is to regulate epinephrine, norepinephrine, and dopamine levels in the brain .
MGB1Y is a noncovalent DNA minor groove binder (MGB). MGB1Y potently inhibits cancer cells proliferation and topoisomerase I activity. MGB1Y downregulates their breast cancer-related genes in MCF7 and MDA-MB-231 cells. MGB1Y has a broad-spectrum anticancer activity, such as breast cancer, colon cancer, and leukemia .
PROTAC DYRK2 degrader 1 is a DYRK2PROTAC degrader with DC50 values of 1.607 μM (MDA-MB-231 cells) and 3.265 μM (HeLa cells), respectively. PROTAC DYRK2 degrader 1 induces DYRK2 degradation via the ubiquitin-proteasome system. It is applicable to the research of triple-negative breast cancer and cervical cancer .
SK3 Channel-IN-1 (compound 7a) is a potent and specific SK3 channel modulator. SK3 Channel-IN-1 has efficient effect on breast cancer MDA-MB-435 cell migration while exhibiting low cytotoxicity in other cell lines. SK3 Channel-IN-1 can modulate ion channels’activity in cancer .
ZYJ-25e is a potent histone deacetylase inhibitor (HDACi) with IC50s of 0.047 μM and 0.139 μM for HDAC6 and HDAC8, respectively. ZYJ-25e is a tetrahydroisoquinoline-bearing hydroxamic acid analogue. ZYJ-25e shows marked antitumor potency in the MDA-MB231 xenograft model .
C12-Ceramide (N-Lauroyl-D-erythro-sphingosine), a naturally occurring ceramide, is formed by hydrolysis of C12 sphingomyelin. C12-Ceramide can enhance the Doxorubicin toxicity in MDA-MB-231 cells. C12-Ceramide also can be used to diagnose types A and B Niemann-Pick disease .
FD2056 is a potent and orally active PI3K inhibitor. FD2056 inhibits PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ with IC50s of 0.30, 0.80, 1.10, 0.42 nM. FD2056 also inhibits CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 of 115.95 and 2782.15 nM. FD2056 inhibits breast cancer cell proliferation with IC50s of 1.06, 0.04, 1.40 μM for MDA-MB-231, MDA-MB-468, MCF-7 cells. FD2056 also induces cancer apoptosis and inhibits tumor growth .
PI3K-IN-58 (Compound 17f) is a PI3Kα inhibitor (IC50: 0.039 μM). PI3K-IN-58 exhibits significant antiproliferative effects on PC-3, 22RV1, MDA-MB-231 and MDA-MB-453 cell lines with IC50s of 3.48 μM, 1.06 μM, 2.21 μM and 0.93 μM, respectively. PI3K-IN-58 induces apoptosis by downregulating the expression levels of anti-apoptotic proteins Bcl-XL and Bcl-2 and upregulating the expression of anti-apoptosis protein BAX. PI3K-IN-58 can be used in PI3K-targeted cancer research .
Polθ-IN-9 is an orally active Polθ polymerase inhibitor (IC50 = 9.6 nM, Kd = 47.5 nM). Polθ-IN-9 shows remarkable selectivity with no inhibitory activity against other human DNA polymerases, including Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. Polθ-IN-9 exhibits strong antiproliferative activity in DLD1 BRCA2 KO cells (IC50 = 2.9 μM), and high sensitivity to MDA-MB-436 cells (IC50 = 4.9 μM). Polθ-IN-9 increases DNA damage accumulation, induces γH2AX levels, and inhibits tumor growth in combination with Olaparib (HY-10162), in the MDA-MB-436 xenograft model. Polθ-IN-9 can be used for the research of homologous recombination (HR)-deficient cancers such as breast cancer .
VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism .
SBT-100 (His Tag) is a human monoclonal antibody (mAb) targeting STAT3. SBT-100 (His Tag) inhibits IL-6-mediated P-STAT3 nuclear translocation in HEp-2 and PANC-1 cells. SBT-100 (His Tag) has tumor growth inhibitory effects on MDA-MB-231 .
BMS-986158 (Standard) is the analytical standard of BMS-986158 (HY-101567). This product is intended for research and analytical applications. BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively .
ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC50 value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .
hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC50 of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC50 of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .
HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research .
LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively .
HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation .
LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively .
FB49 is a highly selective inhibitor of Bcl-2-associated athanogene 3 (BAG3), with the Ki of 45 μM. FB49 inhibits the cell growth in human tumoral cells, but has no toxicity in human peripheral mononuclear cells. FB49 block cell cycle in G1 phase and to induce apoptosis as well as autophagy in medulloblastoma HD-MB03 treated cells .
1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone is a xanthone that can be isolated from Garcinia xanthochymus. 1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone shows moderate cytotoxicities against MDA-MB-435S and A549 cell lines with IC50s of 1.3 and 3.86 μg/ml, respectively .
EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC50 values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC50 of 1.69 µM .
VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability .
CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis .
Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
EGFR-IN-166 (Compound 2) is a EGFR inhibitor. EGFR-IN-166 has potent anticancer activity against breast cancer cells with IC50s of 69.63 and 22.84 μM for MCF-7 and MDA-MB-231 cells, respectively. EGFR-IN-166 significantly inhibits cell migration and EGFR expression. EGFR-IN-166 can be used for breast cancer research .
GSPT1 degrader-11 is a CRBN-dependent G1 to S phase transition 1 (GSPT1) molecular glue degrader (DC50 = 67.7 nM, Dmax = 97%). GSPT1 degrader-11 can inhibit MDA-MB-231 CRBN-WT cells proliferation (IC50 = 2.07 μM). GSPT1 degrader-11 can be used for the research of cancer .
PBE-AMF is a prodrug that activates H2O2 with anticancer activity. PBE-AMF impedes tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing apoptosis, and arresting the cell cycle. PBE-AMF potently and selectively inhibits the proliferation of MDA-MB-231 cells (IC50=6.4 μM) while sparing non-cancerous MCF-10A cells .
Hyp-dBET1 is a PROTAC degrader targeting BRD4. Hyp-dBET1 has an IC50 value of 3.4 μM in MDA-MB-231 cells. Hyp-dBET1 can be activated by hypoxia and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study .
EGFR-IN-183 (Compound 5q) is an EGFR inhibitor. EGFR-IN-183 strongly binds to EGFR (T790M/L858R) mutants. EGFR-IN-183 exhibits anti-proliferative activity against MDA-MB-231, with an IC50 value of 16.4 μM. EGFR-IN-183 can be used for research on triple-negative breast cancer .
VEGFR-2-IN-78 (Compound 6b) is a potent VEGFR-2 inhibitor with an IC50 of 0.21 μM. VEGFR-2-IN-78 exhibits selective cytotoxicity against A-498 and MDA-MB-231 cells. VEGFR-2-IN-78 has antioxidant activity. VEGFR-2-IN-78 can be used in anti-angiogenesis research .
anti-TNBC agent-7 (Compound 13c) possesses anticancer activity, serving as a molecular probe to recognize and regulate the signal transduction of the USP21/JAK2/STAT3 axis, exhibiting nanomolar-level cytotoxicity against MDA-MB-231 and HCC-1806 cancer cells, effectively combating triple-negative breast cancer (TNBC) .
10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC50 value of 10.47 μM against DPPH radical, an IC50 value of 1.68 μM against superoxide radical and an IC50 value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol can be used in research on various common cancers such as ovarian cancer and colon cancer, as well as colitis and neurodegenerative diseases .
Apoptosis inducer 46 is an apoptosis inducer. Apoptosis inducer 46 exhibits potent and selective growth inhibitory effects on metastatic triple-negative breast cancer (TNBC) cells. Apoptosis inducer 46 induces G2/M phase cell cycle arrest and apoptotic cell death in MDA-MB-231 cells, and blocks NF-κB nuclear translocation. Apoptosis inducer 46 can be used for the study of TNBC .
Cath-L-dBET1 is a PROTAC degrader targeting BRD4. Cath-L-dBET1 has an IC50 value of 2.8 μM in MDA-MB-231 cells. Cath-L-dBET1 can be activated by cathepsin L (Cath-L) and recruit the E3 ubiquitin ligase and degrade BRD4 through ubiquitin-proteasome system. Hyp-dBET1 can be used for anti-tumor study .
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
c-Met/HDAC-IN-4 is a dual inhibitor of c-Met/HDAC. The IC50 value of c-Met/HDAC-IN-4 for c-Met is 28.92 nM. c-Met/HDAC-IN-4 can induce G0/G1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines .
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .
MDI-117740 is a dual LIMK1/2 inhibitor. MDI-117740 shows effective cellular target engagement with LIMK1 (pIC50 = 6.73) and LIMK2 (pIC50 = 7.18) in HEK293 cells. MDI-117740 exerts significant anti-migratory activity in MDA-MB-231 cells. MDI-117740 can be used for the study of cancers and neurodegenerative disorders .
Erufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC50: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia .
Hsp90β-IN-2 (Compound 16B) is a selective Hsp90β inhibitor with KDs of 225 nM and 73.32 μM against Hsp90β and Hsp90α. KUNB106 exhibits antiproliferative activity against MDA-MB-231 cells, A549 and SKOV-3 cells. KUNB106 can be used for the study of triple negative breast cancer .
MerTK-IN-2 (compound 15f) is an orally active MerTK inhibitor with an IC50 of 37.5 nM. MerTK-IN-2 can induce apoptosis. MerTK-IN-2 has antitumor activity with IC50 values of 1.79, 18.32, and 2.18 μM for human ovarian cancer cells A2780, breast cancer cells MDA-MB-231, and colon cancer cells HCT116, respectively .
HIF-1α-IN-6 (compound 3s) is a HIF-1α inhibitor with IC50 values of 0.6 and 53.3 nM observed in MiaPaCa-2 and MDA-MB-231 cells. HIF-1α-IN-6 can inhibit HIF-1α expression by decreasing the level of HIF-1α mRNA .
IBI-397 is a human monoclonal antibody (mAb) targeting SIRPα/CD172a . IBI-397 promotes human monocyte-derived dendritic cell-mediated T cell proliferation and increases the expression of CD86 and HLA-DR. IBI-397 has antitumor activity in the mouse MDA-MB-231 tumor model. IBI-397 can be used in Myeloma research .
LDR102 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. LDR102 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. LDR102 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM .
Aurora kinase-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora kinase-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora kinase-IN-4 can be used for research of triple negative breast cancer (TNBC) .
eIF4A3-IN-15 (compound 52) is a Silvestrol (HY-13251) analogue. eIF4A3-IN-15 interferes the assembling of eIF4F translation complex with EC50s of 11, 700 and 120 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-15 can be used for the research of human cancer pathogenesis .
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer .
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
MAGL-IN-222 (Compound ZQ-7) is a covalent inhibitor targeting monoacylglycerol lipase (MAGL) with an IC50 of 42.31 μM. MAGL-IN-222 can reduce the breakdown of 2-arachidonoylglycerol (2-AG) and increase the intracellular 2-AG level, thereby inhibiting the proliferation and migration of MDA-MB-231 breast cancer cells. MAGL-IN-222 can be used in the research of breast cancer and other related diseases .
BMS-871 is an orally active pan-Notch inhibitor with IC50 values of 4/1/4/3 nM for Notch1/2/3/4, respectively. BMS-871 significantly inhibited the proliferation of TALL-1 and MDA-MB-157 cells and demonstrated significant antitumor activity in T-acute lymphoblastic leukemia and triple-negative breast cancer xenograft models. BMS-871 can be used to study leukemia and breast cancer .
eIF4A3-IN-10 (compound 58) is a Silvestrol (HY-13251) analogue. eIF4A3-IN-10 interferes the assembling of eIF4F translation complex with EC50s of 35 and 100 nM for myc-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-10 can be used for the research of human cancer pathogenesis .
Coccinine ((-)-Coccinine) is a weak inhibitor of SERT (IC50: 196.3 μM; Ki: 106.8 μM) and P-gp (IC50: 0.96 mM). Coccinine exhibits significant anti-tumor activity against various cancer cell lines, such as breast cancer (MCF7, Hs578T, MDA-MB-231), colon cancer (HCT-15), and lung cancer (A549). Coccinine can be used in the research of tumors and neurological diseases .
Anticancer agent 253 (Compound 26) has anti-cancer activity against breast cancer cells, with IC50s of 6 μM (MCF-7), 10 μM (MDA-MB-231) and 6.4 μM (4T1 cells). Anticancer agent 253 arrests cell cycle and induces mitochondria-mediated apoptosis in cancer cells. Anticancer agent 253 inhibits Akt phosphorylation in human breast and prostate cancer .
Apoptosis inducer 39 is an apoptosis inducer with IC50s of 4.53 and 15.42 μM against MDA-MB-231 and A549 cells. Apoptosis inducer 39 exerts in vitro anti-tumor activity by decreasing the expression of the anti-apoptotic protein Bcl-2 while increasing the expression of the pro-apoptotic protein Bax. Apoptosis inducer 39 can be used for the study of breast cancer and non-small lung cancer .
Anticancer agent 260 (Compound 3g/4d) is an orally active anticancer agent, that inhibits the proliferation of cancer cell HCT-116, MIA-PaCa2 and MDA-MB231 with IC50s of 98.7, 81.0, and 77.2 µg/mL, respectively. Anticancer agent 260 exhibits promotes ulcer formation and lipid peroxidation, anti-inflammatory and analgesic efficacy .
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively .
hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research .
TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity .
KWZY-11 (Compound 11) is a potent PARP/CDK6 dual inhibitor with IC50 values of 156.8, 197.3, and 13.3 nM for PARP1, PARP2, and CDK6, respectively. KWZY-11 inhibits tumor cell proliferation by regulating the Wnt/β-catenin signaling pathway. KWZY-11 induces excessive DNA damage and apoptosis in MDA-MB-231 breast cancer cells .
VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer, with an IC50 value of 0.33 μM. VEGFR-2-IN-50 (Compound 10f) has growth inhibitory activity on MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, which is expected to be used in the study of breast cancer diseases .
STAT3-IN-33 (compound 7f) is a potent STAT3 inhibitor with anti-cancer activity. STAT3-IN-33 exhibits antiproliferative activity in HCT116, MCF-7, and MDA-MB-231 cells, with IC50s of 6.44, 3.29, and 4.86 μM, respectively. STAT3-IN-33 can be used for breast and colon cancer research .
IITZ-02 is a lysosomotropic Autophagy inhibitor. IITZ-02 enhances autophagosome accumulation but inhibits autophagosomal degradation by impairing lysosomal function, finally inducing the inhibition of autophagy. IITZ-02 abolishes mitochondrial membrane potential and induces apoptosis through the mitochondria-mediated pathway. IITZ-02 has a potent antitumor activity in MDA-MB-231 xenograft mouse models. IITZ-02 can be used for cancers research .
eIF4A3-IN-12 (compound 62) is a Silvestrol (HY-13251) analogue. eIF4A3-IN-12 interferes the assembling of eIF4F translation complex with EC50s of 4, 70 and 5 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-12 can be used for the research of human cancer pathogenesis .
ZMF-10 is a highly potent PAK1 inhibitor, with IC50s of 174 nM, 1.038 μM and 1.372 μM for PAK1, PAK2 and PAK3, respectively. ZMF-10 can inhibit PAK1 activity to affect PAK1-regulated apoptosis, ER-Stress and migration in MDA-MB-231 cells. ZMF-10 can be used for researching anticancer .
SW116 free base is a selective fluorescent ligand for sigma-2 receptor with a Ki of 14 nM. SW116 free base exhibits in methanol a maximal excitation wavelength of 333 nM, and a maximal emission wavelength of 506 nM. SW116 free base can be internalized into MDA-MB-435 cells, and reach 50% maximum fluorescent intensity in 24 minutes. SW116 free base can be as a fluorescent probe used in cancer research .
PBD dimer-4 (Compound 7) is a C1-subsitituted PBD dimer. PBD dimer-4 has high DNA-binding affinity, DNA cross-linking ability and potent cytotoxicity against MDA-MB-231 cells (IC50: 236 nM). PBD dimer-4 can be used as a payload of ADC Loncastuximab tesirine (HY-P99349) to treat several different cancer types .
10-Gingerol (Standard) is the analytical standard of 10-Gingerol (HY-N0448). This product is intended for research and analytical applications. 10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC50 value of 10.47 μM against DPPH radical, an IC50 value of 1.68 μM against superoxide radical and an IC50 value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol is promising for research of ulcerative colitis .
AQ-13 (Compound 7) is a Chloroquine (HY-17589A) analogue with anti-breast cancer property. AQ-13 shows antiproliferative activities against MDA-MB231 and MCF7 with GI50 of 27.81 and 17.85 μM. AQ-13 shows low cytotoxicity against non-cancerous breast epithelial cells MCF10A (GI50 = 65.26 μM). AQ-13 can be used for the research of breast cancer .
ETM-305 is a degradation product of the anticancer agent ET-743 (HY-50936). ET-743 (Ecteinascidin 743; Trabectedin) is a tetrahydroisoquinoline alkaloid that binds to the minor groove of DNA, blocks the transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cell apoptosis, and increases ROS production in MCF-7 and MDA-MB-453 cells. Trabectedin is used in the research of soft tissue sarcoma and ovarian cancer .
Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively .
ST09 is an efficient and low toxicity Curcumin (HY-N0005) derivative. ST09 significantly inhibits cell migration and downregulates the expression of MMP1, MMP2, and Vimentin. ST09 has strong cytotoxicity to breast cancer cells, such as MDA-MB-231, MCF7 and T47D cells. ST09 induces cell apoptosis by upregulating Bax and cleaved caspase-3/9. ST09 can be used in the research of cancer such as breast cancer .
BRITE-338733 is an inhibitor of E. coliRecA ATPase activity (IC50: 4.7 μM). BRITE-338733 also inhibits the ATP hydrolysis activity of RSC chromatin remodeling enzyme by binding to its ATP-binding pocket and DNA (IC50: 0.316 μM). BRITE-338733 exhibits cytotoxicity against MCF-7 and MDA-MB-231 breast cancer cells. BRITE-338733 can be used in studies on antibacterial adjuvants and anticancer research .
(S)-PI3K-IN-2, an enantiomer of PI3K-IN-2 (HY-101517), is a ΡΙ3Κβ/δ inhibitor, with IC50s of 0.198 and 0.282 μΜ, respectively. (S)-PI3K-IN-2 can inhibit phospho AKT (ser473) in MDA-MB-468 cells (IC50=27 nM) .
AKCI is a type of AURKC-IκBα interaction inhibitor, with an IC50 value of 24.9 μM. In MDA-MB-231 cells, AKCI can induce G2/M cell cycle arrest by regulating the p53/p21/CDC2/cyclin B1 pathway, inhibit cell migration and invasion, and reduce colony formation and tumor growth. AKCI can be used for research on breast cancer .
eIF4A3-IN-17 (compound 61) is a Silvestrol (HY-13251) analogue. eIF4A3-IN-17 interferes the assembling of eIF4F translation complex with EC50s of 0.9, 15 and 1.8 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-17 can be used for the research of human cancer pathogenesis .
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) .
BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells .
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice .
SK-575-NEG (compound 28), a methylation counterpart of SK-575, is synthesized by methylation of the amino group of piperidine-2,6-dione in SK-575 as an control compound. SK-575-NEG is strongly bound to PARP1, with an IC50 of 2.64 nM. SK-575-NEG was completely ineffective in inducing PARP1 degradation in MDA-MB-436 and Capan-1 cells at concentrations up to 1 μM .
Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis .
SHP1 activator 1 (Compound 3n) is an activator for src homology-2 domain-containing protein tyrosine phosphatase 1(SHP1) with an EC50 of 17.66 μM. SHP1 activator 1 inhibits the proliferation of ABC-DLBCL cells, induces apoptosis by inhibiting STAT3 signaling pathway. SHP1 activator 1 emitts blue and green fluorescence signalis in MDA-MB-231 cell, and can be used as a cell imaging agent .
Apoptosis inducer 51 (Compound 5d) is an apoptosis inducer. Apoptosis inducer 51 exhibits strong inhibitory activity against MDA-MB-231 cells. Apoptosis inducer 51 inhibits cell invasion and migration, induces G2/M phase cell cycle arrest and cell apoptosis. Apoptosis inducer 51 causes DNA damage, ROS burst and mitochondrial membrane potential (MMP) collapse. Apoptosis inducer 51 can be used for the study of triple-negative breast cancer.
eIF4A3-IN-11 (compound 56) is a Silvestrol (HY-13251) analogue. eIF4A3-IN-11 interferes the assembling of eIF4F translation complex with EC50s of 0.2, 4 and 0.3 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-11 can be used for the research of human cancer pathogenesis .
MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .
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 .
Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .
C12-Ceramide (Standard) is the analytical standard of C12-Ceramide. This product is intended for research and analytical applications. C12-Ceramide (N-Lauroyl-D-erythro-sphingosine), a naturally occurring ceramide, is formed by hydrolysis of C12 sphingomyelin. C12-Ceramide can enhance the Doxorubicin toxicity in MDA-MB-231 cells. C12-Ceramide also can be used to diagnose types A and B Niemann-Pick disease .
IS20 is a Prokineticin receptor 1 (PKR1) agonist. IS20 diminishes Doxorubicin (HY-15142A) mediated apoptosis and ROS production by activating Akt or MAPK pathways. IS20 protects the heart against Doxorubicin-induced cardiovascular toxicity and improves the survival rate and cardiac function in mouse models. IS20 does not alter the cytotoxicity and antitumor activity of acute DOX treatment in breast cancer cells and MDA-MB-231 xenograft mouse models. IS20 can be used for cancers research .
HA-CD44 interaction inhibitor 3 (compound 5d) is a Hyaluronic acid (HY-B0633A) (HA)-CD44 interaction inhibitor with antiproliferative activities. HA-CD44 interaction inhibitor 3 inhibits MDA-MB-231 (CD44++) cells and MCF-7 cells (CD44--) with EC50s of 4.24 μM and 14.74 μM, respectively. HA-CD44 interaction inhibitor 3 shows the potential for cancer research .
STAT3-IN-1 (Standard) is the analytical standard of STAT3-IN-1 (HY-100753). This product is intended for research and analytical applications. STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis .
EG31 is an EGFR inhibitor. EG31 effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells (GI50 values of MDA-MB-231 and Hs578T cells are 498.90 nM and 740.73 nM, respectively) and induces apoptosis by inhibiting the EGFR signaling pathway. EG31 still maintains antiproliferative activity against 5-fluorouracil (5-FU)-resistant TNBC cells (GI50: 519.5 nM). EG31 can be used to study TNBC resistance .
anti-TNBC agent-2 (3j) an anti-Triple negative breast cancer (TNBC) purine derivative. anti-TNBC agent-2 induces MDA-MB-231 cells apoptosis, and inhibits its migration and angiogenesis. anti-TNBC agent-2 inhibits tumor growth and metastasis and reduces the expression of Ki67 and CD31 protein in TNBC xenograft models. anti-TNBC agent-2 can be used for Triple negative breast cancer (TNBC) research .
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PARP1-IN-40 is a highly selectively and orally active PARP1 inhibitor (IC50: 0.19 nM for PARP1, 26 nM for PARP2). PARP1-IN-40 kills tumor cells by inhibiting PARP1, leading to accumulation of DNA damage. PARP1-IN-40 has high antitumor activity against BRCA mutant MDA-MB-436 cells. PARP1-IN-40 can be used in combination with chemotherapy for cancer-related research .
Anticancer agent 239 (Compound 5) is a ligand of hTERT promoter G-quadruplex DNA structures (hTERT G4) (Kd = 1.1 μM), and downregulates hTERT expression. Anticancer agent 239 decreases telomerase activity, shortens telomere length, and induces DNA damage, acute cellular senescence, and apoptosis. Anticancer agent 239 causes mitochondrial dysfunction, disrupts iron metabolism and activates ferroptosis in cancer cells. Anticancer agent 239 inhibits tumor growth in MDA-MB-231 xenograft mouse model .
XH-30 is a potent, selective, and orally active PKMYT1 inhibitor, with an IC50 of 4.1 nM. XH-30 suppresses the proliferation of P53-mutated triple-negative breast cancer (TNBC) cells by inducing G2/M phase release, DNA damage, and apoptosis. XH-30 demonstrates antitumor effects in an MDA-MB-231 mouse model. XH-30 can be used for P53-mutated TNBC research .
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
STAT3-IN-49 (compound B16) is a potent and selective STAT3 inhibitor. STAT3-IN-49 binds to the SH2 domain of STAT3, thereby suppressing its phosphorylation and nuclear translocation. STAT3-IN-49 inhibits triple-negative breast cancer (TNBC) cell migration, invasion, and colony formation. STAT3-IN-49 inhibits tumor growth in an MDA-MB-231 xenograft mouse model. STAT3-IN-49 can be used for TNBC research .
SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50 = 3.59 μM). SPP-037 inhibits integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 inhibits cancer cell proliferation, migration and exhibits antiangiogenic activity. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used for the research of triple-negative breast cancer .
Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells .
PROTAC FAK degrader 4 (Compound 9C) is an efficient and selective FAK PROTAC degrader. PROTAC FAK degrader 4 has a DC50 of 3.6 nM in MDA-MB-231 cells. PROTAC FAK degrader 4 significantly inhibits tumor cell proliferation, migration, and invasion, and enhances chemotherapy sensitivity to cisplatin (HY-17394). PROTAC FAK degrader 4 can be used for research on cancer. (Pink: FAK Ligand (HY-43760); Blue: VHL Ligand (HY-125845); Black: Linker (HY-W208616))
HL389-NHC2-PEG3-C2NH inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389-NHC2-PEG3-C2NH can be utilized as a conjugate of an E3 ligase ligand and a linker, for the synthesis of PROTAC degrader HL435 (HY-161769) .
Antiproliferative agent-64 (Compound 76) is an inhibitor for eukaryotic translation initiation factor 4E (eIF4E), that block the secondary structure of mRNA, thereby inhibiting protein translation. Antiproliferative agent-64 inhibits the 5' untranslated region (5'UTR) of c-Myc (c-myc 5'UTR) with an EC50 of 1.2 nM, inhibits 5'UTR encoding tubulin (tub 5'UTR) with an EC50 of 40 nM. Antiproliferative agent-64 inhibits the proliferation of MDA-MB-231 with an EC50 of 7 nM .
PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis .
TfR-1-IN-1 (compound C4) is an inhibitor of transferrin receptor 1 (TfR-1) with anticancer activity. TfR-1-IN-1 strongly increases intracellular iron (II) levels as a driving force for the induction of ferroptosis. TfR-1-IN-1 significantly reduces the metabolic activity of ovarian cancer (A2780cis), breast cancer (MDA-MB 231), and leukemia (HL-60) cell lines with IC50 values of 0.51, 0.46, and 0.48 μM, respectively .
ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (HDAC) (IC50=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization .
BTR2004 is a selective BET family (BRD2/3/4) protein PROTAC degrader. BTR2004 forms a ternary complex with BRD proteins and KLHL20, inducing ubiquitination and proteasomal degradation through the UPS pathway. BTR2004 is promising for research of PC3 prostate cancer and MDA-MB-231 breast cancer cell lines. Pink: (+)-JQ1-OH (HY-161125); Blue: BTR2000 (HY-172563); Black: Linker (HY-W015236) .
ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC50s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model .
CDK9/EZH2-IN-1 (Compound D16) is a CDK9/EZH2 dual-target inhibitor (IC50: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC50 values are 136.3, 171.3 and 315.7 nM, respectively) .
TQFL13 is derivative of Thymoquinone (TQ) (HY-D0803) with potent anti-breast cancer activity. TQFL13 exhibits higher cytotoxicity against breast cancer cells (BT549, MDA-MB-231, 4T1). TQFL13 increases apoptosis and blocks the cell cycle at S and G2/G1 phases in breast cancer cells. TQFL13 shows dose-dependent anti-tumor efficacy in mouse breast cancer allograft model. TQFL13 can be used for the study of breast cancer .
ATR/PARP1-IN-1 is a potent ATR and PARP1 dual inhibitor with IC50s of 17.3 nM and 0.38 nM, respectively. ATR/PARP1-IN-1 effectively reduces cell viability, induces apoptosis and DNA damage. ATR/PARP1-IN-1 significantly impairs triple-negative breast cancer (TNBC) colony formation, migration, and invasion. ATR/PARP1-IN-1 suppresses tumor growth effectively in MDA-MB-468 xenografted mice, with no significant body weight change .
PROTAC OSBP Degrader-1 (Compound 5) is a Oxysterol-binding protein (OSBP)PROTAC degrader with a DC50 of 322 nM (24 h). PROTAC OSBP Degrader-1 can rapidly penetrate into cells and induce massive recruitment of OSBP at the Trans-Golgi network. PROTAC OSBP Degrader-1 has potent anticancer activity with potent cytotoxicity against U-87 MG, A549, MCF7, HeLa and MDA-MB-231 cells . Pink: OSBP ligand (HY-178035); Blue: CRBN ligase ligand (HY-10984); Black: linker
Grp94-IN-3 (Compound 47) is a selective ATP competitive inhibitor of Grp94, with a Kd value of 76 nM. Grp94-IN-3 has a much lower affinity for Hsp90α, with a Kd value of 9.17 μM. Grp94-IN-3 induces the degradation of integrin α2 (Integrin α2) in MDA-MB-231 cells and reduces the intracellular accumulation of mutant cardiac proteins in human trabecular meshwork cells. Grp94-IN-3 can be used for the study of metastatic cancer and open-angle glaucoma .
BRK/PTK6-IN-1 (Compound 51) is a highly efficient and selective BRK inhibitor (IC50 = 3.37 nM, Kd = 44 nM). BRK/PTK6-IN-1 can reduce MMP-9 protein expression and inhibit IGF-1 induced AKT phosphorylation in MDA-MB-231 cells. BRK/PTK6-IN-1 significantly inhibits migration, invasion, and colony formation but does not affect cell proliferation. BRK/PTK6-IN-1 is often used in the research of breast cancer and other cancers .
Saikosaponin B1 (Standard) is the analytical standard of Saikosaponin B1. This product is intended for research and analytical applications. Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT2C receptor with an EC50 of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB) .
STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC) .
Copper(II) diethyldithiocarbamate (Diethyldithiocarbamic acid copper salt) is a Copper(II) and diethyldithiocarbamate coordination polymer. Copper(II) diethyldithiocarbamate binds tightly to NPL4 and induces its aggregation, disrupting the p97-NPL4-UFD1 pathway. Copper(II) diethyldithiocarbamate causes ubiquitinated proteins accumulation and impairs waste proteins degradation, thus resulting in cell apoptosis. Copper(II) diethyldithiocarbamate inhibits tumor growth in MDA-MB-231 xenograft mice models. Copper(II) diethyldithiocarbamate can be used for the research of cancer, such as breast cancer .
eIF4A3-IN-16 (compound 60) is a Silvestrol (HY-13251) analogue. eIF4A3-IN-16 inhibits MBA-MB-231cell growth with an EC50 value of 1 nM. eIF4A3-IN-16 interferes the assembling of eIF4F translation complex with a myc-LUC EC50 value of 1 nM and a tub-LUC EC50 value of 30 nM. eIF4A3-IN-16 can be used for triple negative breast cancer (TNBC) research .
4-oxo Docosahexaenoic acid (4-oxo DHA) is a putative metabolite of Docosahexaenoic acid (HY-B2167) with antiproliferative and PPARγ agonist activity. It inhibits the growth of several triple negative breast cancer cell lines (MCF-10F, trMCF, bsMCF, MDA-MB-231, and BT549) at 50-100 μM, however it increased proliferation of MCF-7 cells. 4-oxo DHA binds covalently to PPARγ and activates gene transcription in luciferase reporter assays and in dendritic cells with EC50 values of approximately 8-16 μM.
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer .
Copper ionophore I is an efficient copper ion carrier. Copper ionophore I can regulate various intracellular copper levels to induce cuproptosis, such as 4T1 (IC50 = 0.45 μM) and MDA-MB-231(IC50 = 1.21 μM) cells. Copper ionophore I can induce an increase in ROS and cause mitochondrial dysfunction. Copper ionophore I can reduce the expression of FDX1, DLAT, and LIAS proteins. Copper ionophore I can activate immune related pathways and promote T cell infiltration. Copper ionophore I can be used for cancer research .
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells .
eIF4A3-IN-18 (compound 74) is a Silvestrol (HY-13251) analogue. eIF4A3-IN-18 interferes the assembling of eIF4F translation complex with EC50 values of 0.8, 35 and 2 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-18 also has cytotoxicity to RMPI-8226 cells with an LC50 of 0.06 nM. eIF4A3-IN-18 can be used for the research of human cancer pathogenesis .
Antitumor agent-169 (Compound B3) is a dual inhibitor PD-1/PD-L1 interaction and PARP7, with IC50s of 0.426 μM and 2.50 nM. Antitumor agent-169 exhibits an affinity to human PD-L1, with Ki of 20.2 nM. Antitumor agent-169 restores the T cell function, increases IFN-γ secretion. Antitumor agent-169 inhibits cell viability of MDA-MB-231 and Jurkat T, exhibits antitumor efficacy against melanoma in mouse model and good pharmacokinetic characteristics .
N1-Phenylsuberamide is an organic amide compound, and its structure can be regarded as a simplified analogue of Vorinostat (HY-10221). N1-Phenylsuberamide exhibits moderate anti-proliferative activity against MDA-MB-231 and MCF-7 cells. N1-Phenylsuberamide does not show significant HDAC inhibitory activity and can only weakly induce the expression of the p21 gene. N1-Phenylsuberamide has extremely low relative binding affinity of estrogen receptor. N1-Phenylsuberamide can be used as a control compound .
CHNQD-01281, a derivative of Brefeldin A (HY-16592), is a EGFR modulator. CHNQD-01281 has strong antiproliferative activities against cancer cells (IC50: 0.079 and 0.081 μM for T24 and J82 cells, respectively). CHNQD-01281 regulates both EGFR/PI3K/AKT and EGFR/ERK pathways and mediates the chemotactic effect of chemokines on immune effector cells. CHNQD-01281 remarkably inhibits tumor growth in T24 xenograft mice model and prolongs the survival time in MB49 allogeneic mice model via inducing infiltration of cytotoxic T cells .
PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. PFKFB4-IN-1 exhibits >12-fold selectivity over PFKFB1/4 and PFKFB3/4. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and inhibits cell migration. PFKFB4-IN-1 inhibits tumor growth in the MDA-MB-231 xenograft mouse model. PFKFB4-IN-1 can be used for breast, lung and liver cancer research .
ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.) .
Patrinoside aglucone (Compound 8) is an iridoid glucoside that can be isolated from the Valeriana tuberosa. Patrinoside aglucone has potent anticancer activity with G2/M phase tumor cell cycle arrest and apoptosis induction. Patrinoside aglucone also significantly inhibits the proliferation of cancer stem cells (such as MDA-MB-231 and U-251MG cells). Patrinoside aglucone has great anti-inflammatory activity by inhibiting NO release (IC50: 43.44 μM) and significantly reduces the level of TNF-α, IL-1β, IL-6, PGE2 and COX-2 .
EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
PARP1 PROTAC 180055 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787)) .
EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer .
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
BER-IN-1 is a base excision repair (BER) inhibtor, targeting DNA abasic sites. BER-IN-1 cleaves abasic sites via β- and β,δ-elimination mechanisms, disrupts the base excision repair (BER) pathway and leads to DNA double-strand breaks (DSBs). BER-IN-1 can enhance the effectiveness of the PARP inhibitor Olaparib (HY-10162) in homologous recombination (HR)-proficient cancer cells (MDA-MB-231, HeLa, and SKOV3). BER-IN-1 induces an S-phase arrest and apoptosis companied with Olaparib (HY-10162). BER-IN-1 can be used for the research of cancer, such as breast, cervical and ovarian cancer .
SJ44236 is the PROTAC degrader for BET that degrades BRD2 (DC50 = 0.127 nM), BRD3 and BRD4. SJ44236 exhibits cytotoxicity in cell MV4-11 and HD-MB03 with IC50s of 0.12 nM and 0.92 nM. SJ44236 downregulates the expression of c-Myc, upregulates the expression of p53. SJ44236 exhibits a good orally bioavailability of 45% in mice . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W012935); Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 54 (HY-W890189))
MKK7-JNK activator 1 (Compound 10) is a MKK7-JNK pathway activator. MKK7-JNK activator 1 effectively inhibits the proliferation and migration of MDA-MB-468 cells, induces G2/M phase arrest and caspase -dependent apoptosis (independent of ROS production). MKK7-JNK activator 1 significantly increases the levels of p-MKK7 and p-JNK, but does not affect p-ERK or p-p38. MKK7-JNK activator 1 can be used for the study of triple-negative breast cancer (TNBC) .
USP1-IN-17 is an orally active USP1/UAF1 complex inhibitor. USP1-IN-17 exhibits potent anti-proliferative activity against BRCA1-mutant human breast cancer MDA-MB-436 cells, with an IC50 value of 8.1 nM. USP1-IN-17 binds to USP1 to stabilize the enzyme conformation, impairs deubiquitination function, elevates the monoubiquitination level of PCNA, inhibits cancer cell proliferation, and induces DNA damage accumulation. USP1-IN-17 can be used for the research of BRCA1-mutated cancers .
anti-TNBC agent-9 (Compound 3as) is an anti-cancer agent for triple-negative breast cancer (TNBC). anti-TNBC agent-9 exhibits significant inhibitory activity against MDA-MB-453 cells with an IC50 value of 8.5 μM. anti-TNBC agent-9 inhibits tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. anti-TNBC agent-9 induces apoptosis by increasing the expression of the pro-apoptotic protein BAX and decreasing the expression of the anti-apoptotic protein BCL-2, thereby inhibiting tumor cell proliferation .
Tubulin-IN-55 is a tubulin inhibitor. Tubulin-IN-55 disrupts the PI3K/Akt signaling pathway in cancer cells. Tubulin-IN-55 exerts broad-spectrum anti-proliferative activity against multiple tumor cells (HeLa, HCT116, 4T1, A549, H1299, MDA-MB231). Tubulin-IN-55 induces G2/M phase arrest and apoptosis, and inhibits tumor cell migration/invasion in cancer cells. Tubulin-IN-55 demonstrates potent antitumor efficacy in orthotopic autologous transplantation mice. Tubulin-IN-55 can be used for the study of cancer .
EGFR/CA-IX-IN-1 (Compound 14) is a dual inhibitor against epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX) with IC50 values of 5.92 nM and 63 nM, respectively. EGFR/CA-IX-IN-1 shows strong cytotoxicity against breast cancer cells (MDA-MB-231, MCF-7) with IC50 values of 5.78 μM and 8.05 μM, respectively. EGFR/CA-IX-IN-1 inhibits the catalytic activity of CA-IX, up-regulates BAX/Bcl-2, activates caspases, and arrests the cell cycle at the G1 phase. EGFR/CA-IX-IN-1 is promising for research of breast cancer .
Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity .
USP1-IN-11 (compound 38-P2) is a selective, reversible, and noncompetitive USP1 (Ubiquitin-specific protease 1) inhibitor. USP1-IN-11 activates the DDR (DNA damage repair) pathway, induces cell cycle arrest and cell Apoptosis, and inhibits cell survival. USP1-IN-11 enhances the sensitivity of Olaparib (HY-10162)-resistant cells to Olaparib (HY-10162) and shows a synergetic effect with Andrographolide (HY-N0191) in BRCA-proficient cancer cells. USP1-IN-11 displays significant, dose-dependent antitumor efficacy in the MDA-MB-436 xenograft model .
SB-T-101141 is a novel taxane. SB-T-101141 effectively induces a noncanonical ferroptosis to overcome Paclitaxel (HY-B0015) resistance of breast cancer. SB-T-101141 facilitates the production of iron and ferrous ions and ROS. SB-T-101141 stably binds to KHSRP to inhibit the iron-dependent expression of CISD1 related to iron homeostasis. SB-T-101141 synergistically enhances the iron-dependent activation of JNK and PERK pathways via KHSRP. SB-T-101141 suppresses breast tumor growth in MCF-7(PR)/MDA-MB-231(PR) or KHSRP knock-down MCF-7 xenograft mice model .
DW-229 is a PROTAC degrader derived from Deferiprone (HY-B0568), targeting Fe(II)/α‑ketoglutarate‑dependent histone lysine demethylases (KDMs). DW-229 degrades KDM2A, KDM3A, KDM5B, KDM4A‑C, KDM5C, KDM6B in breast cancer cells. DW-229 shows IC50 < 0.5 μM against MCF‑7 cells and IC50 of 8.87 μM against MDA‑MB‑231 cells, with high cancer cell selectivity. DW-229 can be used for the research of breast cancer, liver cancer, prostate cancer, lung cancer .
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.
SKF-83566-PEG1-pomalidomide is an anti-tumor agent and is formed by the covalent connection of SKF-83566 (HY-103430A) (dopamine D1 receptor antagonist) and Pomalidomide (HY-10984) (immunomodulatory agent). SKF-83566-PEG1-pomalidomide can inhibit cancer cells invasion, migration and colony formation. SKF-83566-PEG1-pomalidomide can inhibit tumor growth and angiogenesis in MDA-MB-231 cell chicken embryo chorioallantoic membrane (CAM) xenograft model. SKF-83566-PEG1-pomalidomide can be used for research of breast cancer .
Anticancer agent 264 (Compound 5w) is an anticancer agent that exhibits significant antiproliferative activity across tumor cell lines, with an IC50 range of 7.5-33.67 μM.
Anticancer agent 264 significantly induces G2/M phase arrest in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines.
Anticancer agent 264 reduces the expression of key cell cycle proteins, including CDK1, CDK2, and Cyclin B1, in a dose-dependent manner, and shows strong binding affinity with inhibitor of differentiation (ID) proteins and DNA-binding proteins.
Anticancer agent 264 can be used for research in the field of cancer-related diseases .
Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) (Compound 4C) is a metal palladium (II) complex. Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) exhibits potent anti-proliferative activity against cells such as MDA-MB-231 and HCT116, significantly inducing apoptosis. Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) does not directly damage DNA or cause significant cell cycle arrest. Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) can be used in studies on Cisplatin (HY-17394) resistance .
H8-A5 is a novel human histone deacetylase 8 (HDAC8) inhibitor. A highly specific ZBG-based pharmacophore model was developed by incorporating a custom zinc-binding group (ZBG) feature. Pharmacophore-based virtual screening identified three novel HDAC8 inhibitors with low micromolar IC50 values (1.8-1.9 μM). Further studies showed that H8-A5 was more selective for HDAC8 than HDAC1/4 and exhibited antiproliferative activity in MDA-MB-231 cancer cells. Molecular docking and molecular dynamics studies showed that H8-A5 could bind to HDAC8, providing a good starting point for the development of HDAC8 inhibitors for cancer treatment.
PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC50s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC .
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
Carbonic anhydrase-IN-35 is a selective carbonic anhydrase (CA) inhibitor. Carbonic anhydrase-IN-35 potently inhibits tumor-associated hCA IX (Ki = 0.6 nM) and hCA XII (Ki = 2.2 nM). Carbonic anhydrase-IN-35 induces apoptosis in MCF-7 cells by elevating Bax, reducing Bcl-2, and downregulating CDK4/6. Carbonic anhydrase-IN-35 exhibits potent cytotoxicity against MCF-7 (IC50 = 0.3975 μM normoxic/0.6575 μM hypoxic), MCF-7-ADR (IC50> = 0.3975 μM normoxic/4.488 μM hypoxic), MDA-MB-231, and 4T1 breast cancer cells. Carbonic anhydrase-IN-35 can be used for the study of breast cancer .
USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
Anticancer agent 139 (Compound 6h) has potent anticancer activity. Anticancer agent 139 displayed a π–cationic interaction with the residue Lys352 of Tublin. Anticancer agent 139 has good anticancer activity against SNB-19, OVCAR-8, and NCI-H40 with PGIs of 86.61, 85.26, and 75.99, respectively. Anticancer agent 139 also has moderate anticancer activity against HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 with PGIs of 67.55, 65.46, 59.09, 59.02, 57.88, 56.88, 56.53, 56.4, and 51.88 respectively .
dTAG-47 is a FKBP12F36V PROTAC degrader. dTAG-47 efficiently degrades FKBP12F36V-MELK(sg3R) in MELK ⁻/⁻ MDA-MB-468-FKBP12F36V-MELK(sg3R) cells. dTAG-47 can be used for the research of basal-like breast cancers (BBC). (Pink: FKBP12F36V ligand (HY-114420), Blue: CRBN Ligand (HY-W087383), Black: Linker (HY-42773), E3 ligase ligand-linker conjugate (HY-175952)) .
GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells. GP262 induces degradation of p110α and p110γ with a DC50 of 227.4 and 42.23 nM. GP262 efficient modulates the PI3K/AKT/mTOR pathway, achieving degradation through the ubiquitin-proteasome system (UPS). GP262 also exhibits robust antiproliferative activity and induces apoptosis in vitro. GP262 exhibits tumor growth suppression capability and biosafety profile. GP262 can be used for leukemia and triple-negative breast cancer (TNBC) .
Meso-tetraphenylchlorin (TPCS2a) is a photosensitizer with poor water solubility, which limits its use in the blood circulation. However, TPCS2a@NPs nanoparticles can be prepared based on polylactic-co-polyethylene glycol acid (PLGA) polymer core loaded with TPCS2. Such nanoparticles can be coated with mesenchymal stem cell-derived plasma membranes (mMSCs) to form mMSC-TPCS2a@NPs, which prolongs blood circulation time and improves tumor targeting ability. Compared with uncoated TPCS2a@NPs, mMSC-TPCS2a@NPs can reduce macrophage uptake by 54% to 70% under different conditions. Both nanoparticle forms are effectively accumulated in MCF7 and MDA-MB-231 breast cancer cells, while uptake in normal breast epithelial cells MCF10A is significantly lower .
STAT3-IN-52 (Compound 9) is a selective and orally active signal transducer and activator of transcription 3 (STAT3) inhibitor. STAT3-IN-52 binds to the pY705 site of STAT3 (Ki = 440 nM), blocking the phosphorylation and dimerization of STAT3. STAT3-IN-52 shows strong cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 = 0.7 μM), medulloblastoma UW426, pancreatic cancer BKPC3 cells. STAT3-IN-52 can induce cell apoptosis, inhibit the STAT3 nuclear transport and DNA binding activity and downregulate the expression of the STAT3 target gene MMP9. STAT3-IN-52
can be used for research related to STAT3 abnormal activation in cancer .
Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with anIC50 = 10.9 μM. Tubulin polymerization-IN-84 shows antiproliferative activity against Jurkat, B16-F10, HCT116, and MDA-MB-231 cells (IC50= 60 nM, 380 nM, 138 nM, and 1.054 μM). Tubulin polymerization-IN-84 induces G2/M-phase arrest and apoptosis in B16-F10 cells. Tubulin polymerization-IN-84 suppresses tumor growth in a B16-F10 melanoma model and potentiates anti-tumor immunity in combination with a PD-L1 mAb for the research of T-cell acute lymphoblastic leukemia, melanoma, colon cancer, and breast cancer.
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis .
Axl-IN-21 is an orally active and selective AXL inhibitor (Kd = 2.7 nM, IC50 = 4.0 nM). Axl-IN-21 displays kinase selectivity and retains strong activity against cancer-related mul-kinases (Mer with Kd = 1.4 nM, DDR1 with IC50 = 22.2 nM, HIPK4 with Kd = 11.0 nM and LOK with Kd =10 nM). Axl-IN-21 overcomes tumor microenvironment-driven resistance by blocking CAF-derived GAS6-induced AXL/STAT3/ABCG1 signaling, restoring chemosensitivity and inhibiting drug efflux in gastric cancer (GC). Axl-IN-21 suppresses TGF-β1-induced epithelial-mesenchymal transition (EMT), migration, and invasion in MDA-MB-231 cells. Axl-IN-21 exhibits no significant cytotoxicity in non-cancerous cells. Axl-IN-21 can be research for triple negative breast cancer and gastric cancer [1] [2] .
Anticancer agent 255 is a monocarbonylated curcumin-1,2,3-oxazole conjugate with significant anticancer activity. The IC50 values of Anticancer agent 255 in prostate cancer cells PC-3 and DU-145 are 8.8μM and 9.5μM respectively. The IC50 values of Anticancer agent 255 against breast cancer cells MCF-7, MDA-MB-231 and 4T1 are 6μM, 10μM and 6.4μM, showing good anti-cancer activity Effect. Anticancer agent 255 can induce mitochondria-mediated apoptosis in cancer cells and prevent cell cycle progression. Anticancer agent 255 down-regulated the cell proliferation marker PCNA and inhibited the activation of cell survival proteins. Anticancer agent 255 up-regulated the pro-apoptotic protein Bax and down-regulated the anti-apoptotic protein Bcl-2 .
CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC50 s of 0.17 μM, 1.73 μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer .
FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) .
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells .
GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)) .
Anti-Mouse PD-L1/B7-H1 Antibody (10F.2H11) is rat-derived IgG2b κ type antibody inhibitor, targeting to PD-L1/B7-H1. Anti-Mouse PD-L1/B7-H1 Antibody (10F.2H11) can block PD-L1/ B7-1 interactions and does not block PD-L1/PD-1 interactions. Anti-Mouse PD-L1/B7-H1 Antibody (10F.2H11) can be used for the researches of cancer, infection, immunology and metabolic disease, such as MB49 tumor, heart graft and diabetes .
Mordant Blue 13 is a synthetic dye used in the textile industry. It belongs to a class of metal complex dyes that are able to form strong bonds with fabrics and other materials. Mordant Blue 13 is commonly used for dyeing cotton, wool and silk fibres, it produces a fast blue color. It can be applied to textiles by a variety of methods including impregnation, padding and printing.
MB 488 NHS ester is a fluroescent agent with a terminal NHS ester group. MB 488 NHS ester is a green fluorescent, very hydrophilic dye molecule that has a maximal absorption of 501 nm and emission at 524 nm. The NHS ester can be applied to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.
MB 660R NHS Ester is a fluroescent agent with a terminal NHS ester group.MB 660R NHS Ester is a far-red fluorescent dye that has a maximal absorption of 665 nm and emission at 690 nm. The NHS ester can be applied to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.
MB-m-borate is a double-locked near-infrared fluorescence-activated probe (Ex/Em ≈ 647 nm/684 nm). MB-m-borate undergoes cascade activation by hydrogen peroxide and tyrosinase to release the fluorophore methylene blue, thereby generating a fluorescence activation response. MB-m-borate enables precise detection of melanoma in melanoma cells and mouse models. MB-m-borate can be used for melanoma research .
Tetrabutylammonium hydrosulfate is a quaternary ammonium salt that is commonly used as a phase transfer catalyst, acid catalyst and reagent in various chemical reactions, especially in organic synthesis. Tetrabutylammonium hydrosulfate has unique chemical properties that allow it to facilitate the transfer of ions or molecules from one phase to another, making it an important ingredient in a variety of industrial processes.
Myoglobin is a small molecular pigment protein formed by binding globin to Heme, which can be reversibly bound to oxygen to form MbO2, MbO2 is called oxymyoglobin, and Mb is called deoxymyoglobin. Myoglobin has the role of transporting and storing oxygen in muscle cells .
LyP-2 is a peptide that homes to tumor lymphatics. LyP2 homes to lymphatics of C8161 melanomas and cervical carcinomas and K14-HPV16 skin, but not to MDA-MB435 tumors, showing heterogeneity in the molecular markers of tumor cells and lymphatics .
PhAc-ALGP-Dox, a peptide-drug conjugate, is a novel anticancer prodrug, with IC50 values ranged from 311 nM to 34.25 μM for TNBC (E0771), normal murine epithelium (HC-11), human TNBC (MDA-MB-231 and MDA-MB-468), human CrC (LS 174T), normal human epithelium (HME-1) cells .
Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
Breast cancer targeting peptide 18–4 is a KRT1 receptor-targeting peptide, with a Kd of 0.98 μM. The amino acid sequence of Breast cancer targeting peptide 18–4 is WxEAAYQrFL, and it is an analogue of P160 peptide (HY-P10789). When covalently conjugated with the anticancer peptide MccJ25, Breast cancer targeting peptide 18–4 significantly increases the cellular uptake of MccJ25 in breast cancer cells and enhances its anticancer activity. The covalent conjugate exhibits IC50 values of 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR cells, respectively .
Pantinin-3 is an antimicrobial peptide with antitumor activity found in the venom of the emperor scorpion (Pandinus imperator). Pantinin-3 shows selective toxicity against breast cancer cells (MDA-MB-231) and prostate cancer cells (DU-145). Pantinin-3 can induce apoptosis in tumor cells. Pantinin-3 can be used in cancer research .
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
Bacilotetrin C analogue is cytotoxic to triple-negative breast cancer cell line MDA-MB-231 with an IC50 of 0.48 μM. Bacilotetrin C analogue can induce tumor cell autophagy and has anti-tumor activity .
Anti-Mouse CD20 Antibody (MB20-11) is a kind of mouse IgG2c antibody inhibitor, targeting to CD20. Anti-Mouse CD20 Antibody (MB20-11) can deplete mature B cells in lymphoid tissues. Anti-Mouse CD20 Antibody (MB20-11) can be used for the researches of cancer, immunology and metabolic Disease, such as lymphoma and diabetes .
MB-66 (MAPP-66) is a fully human IgG1 antibody that targets HSV and HIV. MB-66 is a monoclonal antibody film for vaginal application. The isotype control for MB-66 can refer to Human IgG1 kappa, Isotype Control (HY-P99001) .
SBT-100 (His Tag) is a human monoclonal antibody (mAb) targeting STAT3. SBT-100 (His Tag) inhibits IL-6-mediated P-STAT3 nuclear translocation in HEp-2 and PANC-1 cells. SBT-100 (His Tag) has tumor growth inhibitory effects on MDA-MB-231 .
MB-314 is a human IgG1 monoclonal antibody (mAb) targeting Lewis Y. MB-314 induces enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. MB-314 increases the release of IFN-γ, TNF-α, MCP-1, and IL-6. MB-314 can be used in cancer research .
MB-311 is a humanized antibody expressed in CHO cells, targeting Lewis Y. MB-311 has a huIgG1 heavy chain and a huλ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for MB-311 can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
Anti-Mouse CD45RB Antibody (MB23G2) is a rat-derived IgG2a κ type antibody inhibitor, targeting to mouse CD45RB. Anti-Mouse CD45RB Antibody (MB23G2) blocks CD45RB and induces transplantation tolerance. Anti-Mouse CD45RB Antibody (MB23G2) can be used for the researches of infection, immunology and metabolic disease, such as diabetes and Mem71 (H3N1) virus-infection .
IBI-397 is a human monoclonal antibody (mAb) targeting SIRPα/CD172a . IBI-397 promotes human monocyte-derived dendritic cell-mediated T cell proliferation and increases the expression of CD86 and HLA-DR. IBI-397 has antitumor activity in the mouse MDA-MB-231 tumor model. IBI-397 can be used in Myeloma research .
MAb604.107 is a human monoclonal antibody (mAb) targeting NOTCH1. MAb604.107 inhibits the proliferation and CD34/CD44 expression of primary T-ALL cells. MAb604.107 has anti-tumor activity in four tumor xenograft mouse models: MDA-MB-231, HCC-1806, BT-474, and HCT-116. MAb604.107 can be used in T acute lymphoblastic leukemia research .
Anti-Mouse PD-L1/B7-H1 Antibody (10F.2H11) is rat-derived IgG2b κ type antibody inhibitor, targeting to PD-L1/B7-H1. Anti-Mouse PD-L1/B7-H1 Antibody (10F.2H11) can block PD-L1/ B7-1 interactions and does not block PD-L1/PD-1 interactions. Anti-Mouse PD-L1/B7-H1 Antibody (10F.2H11) can be used for the researches of cancer, infection, immunology and metabolic disease, such as MB49 tumor, heart graft and diabetes .
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties.? Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways .
10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC50 value of 10.47 μM against DPPH radical, an IC50 value of 1.68 μM against superoxide radical and an IC50 value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol can be used in research on various common cancers such as ovarian cancer and colon cancer, as well as colitis and neurodegenerative diseases .
Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT2C receptor with an EC50 of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB) .
Notoginsenoside Fe (Notoginseng triterpenes; Ginsenoside Mb) is a saponin with anti-obesity and anti-neuroblastoma activities. Notoginsenoside Fe can be isolated from leaves of Panax notoginseng. Notoginsenoside Fe specifically activates paraventricular nucleus neurons in the hypothalamus, effectively reducing body weight, improving fasting blood glucose and protecting liver function by decreasing food intake, increasing resting metabolic rate and enhancing energy expenditure. Notoginsenoside Fe also inhibits the c-Src signaling pathway, blocks the proliferation and viability of human neuroblastoma cells, while improving mitochondrial dysfunction and alleviating apoptosis. Notoginsenoside Fe can be used in studies related to diet-induced obesity and neuroblastoma .
Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively .
Astragaloside IV (Standard) is the analytical standard of Astragaloside IV. This product is intended for research and analytical applications. Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
Anhydrosecoisolariciresinol is from the flower of Wedelia biflora, has anti-tumor activities .
Anhydrosecoisolariciresinol decreases the growth of human breast cancer MCF-7 and MDA-MB-231 cell lines .
Pinostrobin chalcone is found to be potent natural cytotoxic compounds against MDA-MB-231 and HT-29 colon cancer cell lines(IC50 = 20.42±2.23 and 22.51±0.42 μg/mL) .
Catechol O-methyltransferase, porcine liver (COMT), the magnesium-dependent transfer of methyl groups from S-adenosyl methionine to a hydroxyl group on dopamine, converting it to 3-methoxytyramine. Catechol O-methyltransferase has two forms in tissues, a soluble form (S-COMT) and a membrane-bound form (MB-COMT). Catechol O-methyltransferase is to regulate epinephrine, norepinephrine, and dopamine levels in the brain .
N1-Phenylsuberamide is an organic amide compound, and its structure can be regarded as a simplified analogue of Vorinostat (HY-10221). N1-Phenylsuberamide exhibits moderate anti-proliferative activity against MDA-MB-231 and MCF-7 cells. N1-Phenylsuberamide does not show significant HDAC inhibitory activity and can only weakly induce the expression of the p21 gene. N1-Phenylsuberamide has extremely low relative binding affinity of estrogen receptor. N1-Phenylsuberamide can be used as a control compound .
Carlina oxide is an AChE inhibitor and antioxidant that kills Culex pipiens larvae (LC50=1.39 μg/mL). Carlina oxide is cytotoxic to vertebrate cells, human dermis, HCT116 and MDA-MB231 cell lines .
Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes .
10-Gingerol (Standard) is the analytical standard of 10-Gingerol (HY-N0448). This product is intended for research and analytical applications. 10-Gingerol is an AMPK agonist, which is found in the ginger oleoresin from fresh rhizome with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol suppresses neointimal hyperplasia and inhibits vascular smooth muscle cell proliferation. 10-Gingerol exhibits substantial scavenging activities with an IC50 value of 10.47 μM against DPPH radical, an IC50 value of 1.68 μM against superoxide radical and an IC50 value of 1.35 μM against hydroxyl radical. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM. 10-Gingerol suppresses the proliferation, migration, invasion, and induced apoptosis through targeting the PI3K/Akt signaling pathway in MDA-MB-231/IR cells. 10-Gingerol is promising for research of ulcerative colitis .
Sinopodophylline B (compound 2) is a flavonoid glycoside compound that is cytotoxic to breast cancer cells. For example, the IC50 of Sinopodophylline B is 1.5 μM (T47D) and 44.2 μM (MDA-MB-231), respectively .
2-Epitripdiolide is a diterpenoid compound derived from Tripterygium hypoglaucum with significant antitumor activity. Its IC50 values against A549, KB, KBvin, and MDA-MB-231 cells are 1.34, 0.4, 4.4, and 1.2 nM, respectively .
Sempervirine is an indole alkaloid isolated from Gelsemium sempervirens with anti-tumor activities. Sempervirine is against sempervirine-sensitive tumor cells with EC50 values of 2.7 μM, 1.77 μM, and 1.96 μM for Raji, MDA-MB-231 and HeLa cells, respectively .
Anthragallol 1,2-dimethyl ether (compound 11) can be isolated from O. umbellata. Anthragallol 1,2-dimethyl ether has cytotoxicity, with IC50 values of 5.9 and 8.8 μg/ml against A549 cells and MDA-MB-231 cells, respectively .
(−)-Voacangarine is an indole alkaloid, which exhibits cytotoxic effects against cancer cells HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 of 5~20 mg/mL. (−)-Voacangarine inhibits the cultivation of Saccharomyces cerevisiae wildtype and repair-deficient mutants .
Pinostrobin chalcone (Standard) is the analytical standard of Pinostrobin chalcone. This product is intended for research and analytical applications. Pinostrobin chalcone is found to be potent natural cytotoxic compounds against MDA-MB-231 and HT-29 colon cancer cell lines(IC50 = 20.42±2.23 and 22.51±0.42 μg/mL) .
Asperphenamate (Standard) is the analytical standard of Asperphenamate. This product is intended for research and analytical applications. Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively[1][2].
Vitexin B-1 is an inhibitor of Bcl-2 and the agonist of Caspase. Vitexin B-1 has cytotoxic effect and induces apoptosis in MCF-7, ZR-75-1, MDA-MB-231, and COC1 cells with IC50s of 3.2, 2.1, 1.8 and 0.39 μM, respectively .
N,O-Diacetyltyramine is a compound with antibacterial activity and cytotoxicity that can be isolated from the actinomycete Pseudonocardia endophytica VUK-10. N,O-Diacetyltyramine has antibacterial activity against Gram-positive and Gram-negative bacteria and fungi. N,O-Diacetyltyramine is cytotoxic to MDA-MB-231, HeLa, MCF-7 and OAW-42 cells .
Sophoraflavanone G (Standard) is the analytical standard of Sophoraflavanone G. This product is intended for research and analytical applications. Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties. Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways .
Ilexsaponin A (Standard) is the analytical standard of Ilexsaponin A. This product is intended for research and analytical applications. Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes .
1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone is a xanthone that can be isolated from Garcinia xanthochymus. 1,4,5,6-Tetrahydroxy-7,8-diprenylxanthone shows moderate cytotoxicities against MDA-MB-435S and A549 cell lines with IC50s of 1.3 and 3.86 μg/ml, respectively .
Coccinine ((-)-Coccinine) is a weak inhibitor of SERT (IC50: 196.3 μM; Ki: 106.8 μM) and P-gp (IC50: 0.96 mM). Coccinine exhibits significant anti-tumor activity against various cancer cell lines, such as breast cancer (MCF7, Hs578T, MDA-MB-231), colon cancer (HCT-15), and lung cancer (A549). Coccinine can be used in the research of tumors and neurological diseases .
Saikosaponin B1 (Standard) is the analytical standard of Saikosaponin B1. This product is intended for research and analytical applications. Saikosaponin B1 is a bioactive constituent of Radix Bupleuri. Saikosaponin B1 is an agonist of the 5-HT2C receptor with an EC50 of 147.41 μM. Saikosaponin B1 inhibits the Hedgehog (Hh) signaling pathway by targeting the transmembrane protein SMO. Sailosaponin B1 can reduce liver fibrosis. Saikosaponin B1 has anti-cancer activities thus can be studies in research for cancers such as Medulloblastoma (MB) .
Patrinoside aglucone (Compound 8) is an iridoid glucoside that can be isolated from the Valeriana tuberosa. Patrinoside aglucone has potent anticancer activity with G2/M phase tumor cell cycle arrest and apoptosis induction. Patrinoside aglucone also significantly inhibits the proliferation of cancer stem cells (such as MDA-MB-231 and U-251MG cells). Patrinoside aglucone has great anti-inflammatory activity by inhibiting NO release (IC50: 43.44 μM) and significantly reduces the level of TNF-α, IL-1β, IL-6, PGE2 and COX-2 .
Anticancer agent 180 (compound 4) is a secondary metabolite present in fungal strains and extracted through physical interaction with Streptomyces sp. Anticancer agent 180 has potential anti-tumor activity and can inhibit the migration of MDA-MB-231 breast cancer cells .
Crispene E is a STAT3 inhibitor with an IC50 of 10.27 μM against STAT3 dimerization. Crispene E exerts specific cytotoxicity against STAT3-dependent MDA-MB-231 breast cancer cells. Crispene E is applicable to research related to breast cancer .
Myoglobin Protein, a crucial member of the globin family, acts as a reserve oxygen supply, facilitating efficient oxygen transport within muscles.Myoglobin Protein, Mouse (P.pastoris, His) is the recombinant mouse-derived Myoglobin protein, expressed by P.pastoris , with C-Myc, N-6*His labeled tag.
Myoglobin Protein, a globin family member, reserves oxygen and facilitates its movement in muscles. Myoglobin Protein, Human (His) is the recombinant human-derived Myoglobin protein, expressed by E. coli , with C-6*His labeled tag.
The CD79A protein is critical for initiating the B cell antigen receptor complex (BCR) signaling cascade upon antigen binding. It promotes internalization, transport to late endosomes, and antigen presentation of BCR complexes. CD79A Protein, Human (HEK293, His) is the recombinant human-derived CD79A protein, expressed by HEK293 , with C-6*His labeled tag.
CD79A cooperates with CD79B to initiate the B cell antigen receptor complex (BCR) signaling cascade upon antigen binding. This results in complex internalization, transport and antigen presentation. CD79A Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived CD79A protein, expressed by HEK293 , with C-hFc labeled tag.
CD79A cooperates with CD79B to initiate the B cell antigen receptor complex (BCR) signaling cascade upon antigen binding. This results in complex internalization, transport and antigen presentation. CD79 Protein, Mouse (HEK293, His) is a recombinant protein dimer complex containing mouse-derived CD79 protein, expressed by HEK293 , with C-His labeled tag. CD79 Protein, Mouse (HEK293, His), has molecular weight of 23-43 kDa, respectively.
The CD79A protein is critical for initiating the B cell antigen receptor complex (BCR) signaling cascade upon antigen binding. It promotes internalization, transport to late endosomes, and antigen presentation of BCR complexes. CD79 Protein, Human (HEK293, His) is the recombinant human-derived CD79, expressed by HEK293, with C-6*His labeled tag.
The CD79A protein is critical for initiating the B cell antigen receptor complex (BCR) signaling cascade upon antigen binding. It promotes internalization, transport to late endosomes, and antigen presentation of BCR complexes. CD79 Protein, Human (HEK293, Flag-His) is a recombinant protein dimer complex containing human-derived CD79 protein, expressed by HEK293 , with C-His, C-Flag labeled tag. CD79 Protein, Human (HEK293, Flag-His), has molecular weight of ~37.5 kDa.
cGAS is a cytosolic DNA sensor. cGAS binds double-stranded DNA (dsDNA) and catalyzes the generation of cyclic guanosine-adenylate (cGAMP), which in turn activates the STING protein. cGAS induces the production of type I interferon (IFN-I) and pro-inflammatory cytokines. cGAS Protein, Human (His) is a recombinant cGAS protein expressed in E. coli with a C-6*His tag.
The cGAS protein is a nucleotidyl transferase that crucially mediates innate immunity by catalyzing the formation of 2',3'-cGAMP from ATP and GTP upon binding to double-stranded DNA (dsDNA). As a DNA sensor, cGAS detects exogenous and endogenous DNA, triggering STING1 activation and type I interferon production. cGAS Protein, Human (His-SUMO) is the recombinant human-derived cGAS protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag.
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
USP1-IN-8 (Compound 16) is an inhibitor for ubiquitin specific peptidase 1 (USP1) and its cofactor UAF1, with IC50 ≤50 nM. USP1-IN-8 inhibits proliferation of MDA-MB-436 with IC50 ≤50 nM .
Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
SG3683 is a DNA-targeted cytotoxic agent belonging to pyrrolobenzodiazepine (PBD) dimers. SG3683 exerts antitumor activity with an IC50 value of 0.74 nM in MDA-MB-436 cells. SG3683 is promising for research of cancers, such as breast cancer .
ERα antagonist 2 (Compound 5b) is an ER-α antagonist with an IC50 value of 1729 nM. ERα antagonist 2 exhibits significant inhibitory activity against breast cancer cell lines, and is still effective against ER-negative cells (MDA-MB-231), suggesting the existence of ER-independent pathways. ERα antagonist 2 can be used for the study of breast cancer .
hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC50 of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC50 of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .
anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
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 .
SYL3C aptamer sodium is a DNA aptamer that targets epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets a variety of human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd values of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III are 38 nM and 67 nM, respectively. SYL3C aptamer sodium possesses stability, high binding affinity and selectivity, and can be used for targeted cancer cell imaging and circulating tumor cell detection .
CD63-1 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 38.71 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
MB Human Pre-designed siRNA Set A contains three designed siRNAs for MB gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Mb Mouse Pre-designed siRNA Set A contains three designed siRNAs for Mb gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
MB21D2 Human Pre-designed siRNA Set A contains three designed siRNAs for MB21D2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
CD63-2 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 78.43 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
Mb Rat Pre-designed siRNA Set A contains three designed siRNAs for Mb gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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