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MDA-MB-436 cell

" in MedChemExpress (MCE) Product Catalog:

33

Inhibitors & Agonists

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Inhibitory Antibodies

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-136057
    iFSP1
    Maximum Cited Publications
    29 Publications Verification

    		 Ferroptosis Ligands for Target Protein for PROTAC Cancer
    iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A) .
    iFSP1
  • HY-139156
    SK-575
    5 Publications Verification

    		 PROTACs PARP Cancer
    SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations .
    SK-575
  • HY-174143
    EXO1-IN-1

    		Apoptosis Cancer
    EXO1-IN-1 is a human exonuclease 1 (EXO1) inhibitor (IC50 = 15.7 μM). EXO1-IN-1 inhibits DNA end resection, promotes the accumulation of DNA double-strand breaks, and triggers S-phase polyamylation. EXO1-IN-1 induces apoptosis (Apoptosis) in BRCA1-deficient breast cancer cells. EXO1-IN-1 suppresses the growth of BRCA1-deficient breast cancer xenografts. EXO1-IN-1 can be used in research related to BRCA1-deficient breast cancer .
    EXO1-IN-1
  • HY-139289
    ART812
    3 Publications Verification

    		 DNA/RNA Synthesis Cancer
    ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 has an IC50 value of 240 nM for cell based microhomology-mediated end joining (MMEJ) .
    ART812
  • HY-168162
    ZLC491

    		PROTACs CDK Cancer
    ZLC491 is an orally active PROTAC degrader that selectively targets CDK12/CDK13 and exhibits certain oral bioavailability. ZLC491 induces cereblon- and proteasome-dependent selective degradation of CDK12 and CDK13. ZLC491 inhibits the transcription and expression of long genes, and mainly acts on a subset of DNA damage response genes. ZLC491 inhibits the proliferation of various triple-negative breast cancer cells. ZLC491 can be used in research related to triple-negative breast cancer .
    ZLC491
  • HY-132305
    VEGFR-3-IN-1
    2 Publications Verification

    		 VEGFR Cancer
    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 .
    VEGFR-3-IN-1
  • HY-P99345
    Dostarlimab

    TSR-042; ANB-011; WBP-285

    		 PD-1/PD-L1 Cancer
    Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
    Dostarlimab
  • HY-155351
    PARP7-IN-15

    		PARP Cytochrome P450 Cancer
    PARP7-IN-15 is an orally active and selective PARP7 inhibitor with an IC50 of 0.56 nM. PARP7-IN-15 inhibits the enzymatic activity of PARP7 and induces anti-tumor activity against lung cancer in vivo. PARP7-IN-15 can be used for the research of lung cancer .
    PARP7-IN-15
  • HY-161302
    Polθ/PARP-IN-1

    		Apoptosis DNA/RNA Synthesis PARP Cancer
    Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity .
    Polθ/PARP-IN-1
  • HY-176495
    SG3683

    		DNA Alkylator/Crosslinker DNA/RNA Synthesis Cancer
    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 .
    SG3683
  • HY-D1726
    8RK59

    		Deubiquitinase Cancer
    8RK59, a Bodipy probe, is a potent UCHL1 (ubiquitin C-terminal hydrolase L1) inhibitor, with an IC50 close to 1 μM. 8RK59 could penetrate and label living cells. BodipyFL-alkyne is coupled to the azide of 8RK64 (HY-148254) using copper(I)-mediated click chemistry, resulting in compound 8RK59 .
    8RK59
  • HY-164306
    PROTAC PARP1 degrader-2

    		PROTACs PARP Cancer
    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))
    PROTAC PARP1 degrader-2
  • HY-147101
    SK-575-NEG

    		PARP Cancer
    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 .
    SK-575-NEG
  • HY-156525
    USP1-IN-6

    		Deubiquitinase Cancer
    USP1-IN-6 (compound 11) is a USP1 inhibitor (IC50<50 nM). USP1-IN-5 also inhibits MDA-MB-436 cells with IC50 <50 nM .
    USP1-IN-6
  • HY-156524
    USP1-IN-5

    		Deubiquitinase Cancer
    USP1-IN-5 (compound 10) is a USP1 inhibitor (IC50<50 nM). USP1-IN-5 also inhibits MDA-MB-436 cells with IC50 <50 nM .
    USP1-IN-5
  • HY-174442
    PARP1-IN-40

    		PARP Cancer
    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 .
    PARP1-IN-40
  • HY-162633
    USP1-IN-9

    		Deubiquitinase 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 .
    USP1-IN-9
  • HY-170921
    USP1-IN-11

    		Deubiquitinase Cancer
    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 .
    USP1-IN-11
  • HY-155766
    PARP1-IN-14

    		PARP Apoptosis 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 .
    PARP1-IN-14
  • HY-161868
    DLC-50

    		PARP HDAC Apoptosis Cancer
    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 .
    DLC-50
  • HY-146616
    GLS1 Inhibitor-3

    		Glutaminase Cancer
    GLS1 Inhibitor-3 (compound C147) is a potent GLS1 inhibitor with an IC50 of 27.98 nM. GLS1 Inhibitor-3 shows antiproliferative activity .
    GLS1 Inhibitor-3
  • HY-158680
    PARP1-IN-21

    		PARP Cancer
    PARP1-IN-21 (example 16) is a potent inhibitor of PARP1, with the IC50 of ＜ 10 nM .
    PARP1-IN-21
  • HY-183363
    USP1-IN-17

    		Deubiquitinase Cancer
    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 .
    USP1-IN-17
  • HY-179413
    Polθ-IN-9

    		DNA/RNA Synthesis Cancer
    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 .
    Polθ-IN-9
  • HY-169170
    PARP1/BRD4-IN-3

    		Apoptosis DNA/RNA Synthesis Epigenetic Reader Domain PARP Cancer
    PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy .
    PARP1/BRD4-IN-3
  • HY-168851
    PARP1-IN-35

    		PARP Cancer
    PARP1-IN-35 (compound T26) is a selective, orally active, cross -the blood-brain barrierPARP1 inhibitor with IC50 values of 0.2, 122 nM for PARP1, PARP2, respectively. PARP1-IN-35 shows antiproliferative activity and anticancer activity. PARP1-IN-35 has the potential for the research of breast cancer .
    PARP1-IN-35
  • HY-149003
    PARP1-IN-10

    		PARP Apoptosis Cancer
    PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC50 value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) .
    PARP1-IN-10
  • HY-181664
    YCH3971

    		PARP Apoptosis Caspase Cancer
    YCH3971 is a PARP1 inhibitor with a PARP1 IC50 of 7.52 nM and a PARP1 EC50 of 67.75 nM. YCH3971 inhibits the proliferation of BRCA-deficient tumor cells. YCH3971 induces DNA damage, G2/M phase arrest, and caspase-mediated Apoptosis in triple-negative breast cancer cells. YCH3971 can be used for the research of BRCA-deficient tumors .
    YCH3971
  • HY-183013
    PROTAC PARP2 degrader-1

    		PROTACs PARP Apoptosis Cancer
    PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer .
    PROTAC PARP2 degrader-1
  • HY-183748
    XL-20

    		DNA/RNA Synthesis PD-1/PD-L1 IKK STAT STING Cancer
    XL-20 is an orally active DNA polymerase θ (Polθ) ATPase inhibitor with an IC50 of 4.3 nM against human targets. XL-20 activates the cGAS-STING pathway. XL-20 upregulates the expression of PD-L1 in HR-deficient cancer cells. XL-20 acts synergistically with PARP inhibition in HR-deficient cancer cells and in vivo xenograft models. XL-20 can be used in studies related to HR-deficient cancers .
    XL-20
  • HY-181611
    Polθ-IN-10

    		DNA/RNA Synthesis Apoptosis Cytochrome P450 Cancer
    Polθ-IN-10 is an orally active Polθ-pol inhibitor (with a human IC50 of 1.3 nM) that exhibits oral bioavailability in mice and rats. Polθ-IN-10 binds to the allosteric site of Polθ-pol, disrupts the microhomology-mediated end-joining DNA repair pathway, and inhibits CYP2C9 (IC50=1.63 μM). Polθ-IN-10 selectively inhibits the proliferation of HR-deficient cancer cells and induces apoptosis. Polθ-IN-10 is applicable to the research of HR-deficient cancers .
    Polθ-IN-10
  • HY-183581
    USP1-IN-18

    		Deubiquitinase DNA/RNA Synthesis Cancer
    USP1-IN-18 is an orally active USP1 inhibitor with a human IC50 of 17.0 nM. USP1-IN-18 inhibits USP1-UAF1 deubiquitinase activity and drives ubiquitinated PCNA accumulation. USP1-IN-18 induces DNA damage, replication stress, and G2-M phase cell cycle arrest. USP1-IN-18 can be used for the research of triple-negative breast cancer .
    USP1-IN-18
  • HY-171171
    NERx 329

    		DNA/RNA Synthesis Cancer
    NERx 329 is a replication protein A (RPA) inhibitor with an IC50 of 4.9 μM. NERx 329 blocks the interaction between RPA and single-stranded DNA, and induces functional RPA depletion, loss of single-stranded DNA gap protection, chromosome fragmentation and cell death. NERx 329 inhibits the DNA damage response signaling pathway, exhibits broad single-agent anticancer activity, and enhances the activity of DNA-damaging agents. NERx 329 can be used in research related to brca1-deficient breast cancer, non-small cell lung cancer, and brca1-deficient ovarian cancer .
    NERx 329

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