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BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions [1].
Bractoppin is a potent and selective agent-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response [1].
AB25583 is a Polθ helicase (Polθ-hel) small molecule inhibitor, with an IC50 value of 6 nM. AB25583 selectively kills BRCA1/2 deficient cells and works in synergy with Olaparib (HY-10162) in cancer cells carrying pathogenic BRCA1/2 mutations. AB25583 can be used for tumor research [1].
Brca1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Brca1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Brca1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Brca1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
BRCA1 Human Pre-designed siRNA Set A contains three designed siRNAs for BRCA1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Anti-BRCA1 Antibody (BR64) is a kind of mouse IgG1 κ chimeric antibody, targeting to human BRCA1. Anti-BRCA1 Antibody (BR64) reacts with BRCA1 (Breast cancer susceptibility gene 1) involved in tumor suppression, transcription, genomic stability, DNA repair and recombination. Anti-BRCA1 Antibody (BR64) can be used for the detections of immunofluorescence, western blot, and immunoprecipitation in cancer, such as breast and ovarian cancer [1].
Human OLA1 mRNA encodes the human Obg like ATPase 1 (OLA1) protein, a member of the GTPase protein family. OLA1 interacts with breast cancer-associated gene 1 (BRCA1) and BRCA1-associated RING domain protein (BARD1), and is involved in centrosome regulation.
PARP1-IN-30 (Compound 3) is a specific and potent PARP1 inhibitor with cytotoxicity. PARP1-IN-30 allows precise inhibition of PARP1 in tumor cells with breast cancer 1 protein (BRCA1) or BRCA2 deficiencies. PARP1-IN-30 is promising for research of cancers [1].
D-G23 is a selective RAD52 inhibitor. D-G23 disrupts RAD52-mediated DNA repair pathways and suppresses the growth of BRCA1- and BRCA2-deficient cancer cells. D-G23 is promising for research of homologous recombination-related cancers, such as hereditary breast cancer and ovarian cancer caused by BRCA1/2 mutations [1].
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 [1].
TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis[1].
Octamethylcyclotetrasiloxane promotes the anchorage-independent growth of MCF-10A and MCF-10F cells. Octamethylcyclotetrasiloxane induces DNA damage, inhibits the expression of DNA-repairing protein BRCA1 under long-term and high-concentration exposure. Octamethylcyclotetrasiloxane exhibits intrinsic estrogenic activity [1].
PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis [1].
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 [1].
PARP1-IN-39 is an inhibitor of PARP1 with an IC50 of 0.22 nM. PARP1-IN-39 has an IC50 of 1.57 nM in human breast cancer cells. PARP1-IN-39 can be studied in breast, ovarian, pancreatic, and prostate cancers associated with DNA repair deficiencies, such as BRCA1/2 mutations [1].
Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. Theophylline-platinum(IV) prodrug-1 enhances DNA
damage, ROS production, mitochondrial dysfunction, apoptosis and S-phase arrest, along with reducing invasion and metastasis in cells. Theophylline-platinum(IV) prodrug-1 exhibits superior antitumor activity in the xenograft SKOV3-BRCA1-KD tumor model. Theophylline-platinum(IV) prodrug-1 can be used for the study of ovarian cancer [1].
Dicycloplatin is a DNA damage inducer. Dicycloplatin induces DNA damage by activating biphosphorylated checkpoint kinase 2 (CHK2), breast cancer 1(BRCA1) and triphosphorylated p53. Dicycloplatin can induce cell cycle arrest, inhibit proliferation and lead to apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. Dicycloplatin can be used in cancer researchr [1].
TNG348 is an orally available allosteric inhibitor of the ubiquitin-specific protease USP1. TNG348 specifically and efficiently inhibits the activity of USP1, inhibiting its deubiquitination of proliferative PCNA and FANCD2, thereby disrupting the DNA repair process. TNG348 has inhibitory activity against breast and ovarian cancers carrying BRCA1/2 mutations and other homologous recombination defects (HRD) [1] .
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research [1].
(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is the orally active inhibitor for PARP1/2 with Ki of 1.2 nM and 0.87 nM. (rac)-Talazoparib inhibits cellular PARylation with an EC50 of 2.51 nM. (rac)-Talazoparib causes the accumulation of DNA damage, inhibits proliferation of BRCA1/2-mutated MX-1 cell and Capan-1 cell with IC50 of 0.3 nM and 5 nM. (rac)-Talazoparib exhibits antitumor efficacy in mouse models [1].
PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations [1].
D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 μM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 μM and 8 μM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin [1] .
A 62176 hydrochloride is a compound that targets DNA topoisomerase II and has the activity of inhibiting purine synthesis in cancer cells. A 62176 hydrochloride interferes with c-MYC mRNA expression by interacting with G-quadruplex. The main mechanism of action of A 62176 hydrochloride is by displacing nucleosomes from the quadruplex of non-template strand rDNA, resulting in rapid redistribution of nucleosomes. The application potential of A 62176 hydrochloride is that it causes DNA damage and relies on BRCA1/2-mediated homologous recombination and DNA-PK-mediated non-homologous end-joining pathways to repair the damage [1].
EXO1-IN-1 (Compound F684) is a potent and selective inhibitor of exonuclease 1(EXO1) (IC50= 15.7 μM). EXO1-IN-1 suppresses DNA end resection, promotes the accumulation of DNA double-strand breaks, and triggers S-phase PARylation, disrupts DNA repair pathways in homologous recombination-deficient (HRD) cancer cells, and selectively kills tumor cells with defects in HR genes like BRCA1/2. EXO1-IN-1 is promising for research of homologous recombination-deficient cancer (such as BRCA-related tumors) [1].
BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer (Pink: ligand for target protein (HY-150948); black: linker (HY-W140827); Blue: E3 ligase ligand (HY-112078)) [1].
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1) [1].
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1) [1].
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1) [1].
Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts [1].
Rucaparib (phosphate) (Standard) is the analytical standard of Rucaparib (phosphate). This product is intended for research and analytical applications. Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (Standard) is the analytical standard of Rucaparib. This product is intended for research and analytical applications. Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research [1] .
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) [1].
Anti-BRCA1 Antibody (BR64) is a kind of mouse IgG1 κ chimeric antibody, targeting to human BRCA1. Anti-BRCA1 Antibody (BR64) reacts with BRCA1 (Breast cancer susceptibility gene 1) involved in tumor suppression, transcription, genomic stability, DNA repair and recombination. Anti-BRCA1 Antibody (BR64) can be used for the detections of immunofluorescence, western blot, and immunoprecipitation in cancer, such as breast and ovarian cancer [1].
BRCC36 is a metalloprotease that selectively cleaves "Lys-63" linked polyubiquitin chains, especially histones H2A and H2AX in the BRCA1-A complex during the DNA damage response. As the catalytic subunit of the BRISC complex, it also targets “Lys-63”-linked ubiquitin in various substrates, affecting mitotic spindle assembly and interferon signaling. BRCC36 Protein, Human (His-SUMO) is the recombinant human-derived BRCC36 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag.
BAP1 protein deubiquitinates histone H2A and HCFC1, mediating deubiquitination of H2AK119ub1. It regulates cell growth by deubiquitinating HCFC1 chains and inhibits BRCA1 and BARD1 activity. BAP1 also protects itself from cytoplasmic sequestration and acts as a tumor suppressor. BAP1 Protein, Human is the recombinant human-derived BAP1 protein, expressed by E. coli , with tag free.
BAP1 protein deubiquitinates histone H2A and HCFC1, mediating deubiquitination of H2AK119ub1. It regulates cell growth by deubiquitinating HCFC1 chains and inhibits BRCA1 and BARD1 activity. BAP1 also protects itself from cytoplasmic sequestration and acts as a tumor suppressor. BAP1 Protein, Human (His) is the recombinant human-derived BAP1 protein, expressed by E. coli , with N-6*His labeled tag.
BRAP protein acts as a negative regulator of MAP kinase activation, inhibits the formation of the Raf/MEK complex, and may inactivate the KSR1 scaffolding protein. As a Ras-responsive E3 ubiquitin ligase, BRAP undergoes autopolyubiquitination upon Ras activation, releasing its inhibitory effect on Raf/MEK complex formation. BRAP Protein, Human is the recombinant human-derived BRAP protein, expressed by E. coli , with tag free.
BRCA1/BRCA2 containing complex, subunit 5; BRCC 5; BRCC5; DNA repair protein RAD51 homolog 1; DNA repair protein rhp51; HRAD51; HsRad51; HsT16930; MRMV2; Rad 51; RAD51; RAD51 homolog; RecA homolog, E. coli; S. cerevisiae; RAD51 homolog A; RAD51 homolog; RAD51 recombinase; RAD51, S. cerevisiae, homolog of; RAD51_HUMAN; RAD51A; RECA; RecA like protein; RecA, E. coli, homolog of; Recombination protein A.
WB
Human, Mouse, Rat, Monkey
Rad51 Antibody (YA5219) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to Rad51.
BRCA 2 antibody; BRCA1/BRCA2 containing complex subunit 2 antibody; BRCA2 antibody; BRCA2, DNA repair associated antibody; BRCA2_HUMAN antibody; BRCC 2 antibody; BRCC2 antibody; Breast and ovarian cancer susceptibility gene early onset antibody; breast and ovarian cancer susceptibility protein 2 antibody; Breast cancer 2 early onset antibody; BRCA 2 antibody; BRCA1/BRCA2 containing complex subunit 2 antibody; BRCA2 antibody; BRCA2, DNA repair associated antibody; BRCA2_HUMAN antibody; BRCC 2 antibody; BRCC2 antibody; Breast and ovarian cancer susceptibility gene early onset antibody; breast and ovarian cancer susceptibility protein 2 antibody; Breast cancer 2 early onset antibody; Breast Cancer 2 tumor suppressor antibody; Breast cancer susceptibility protein BRCA2 antibody; Breast cancer type 2 susceptibility protein antibody; BROVCA2 antibody; FACD antibody; FAD 1 antibody; FAD antibody; FAD1 antibody; FANCB antibody; FANCD 1 antibody; FANCD antibody; FANCD1 antibody; FANCD1 gene antibody; Fanconi anemia complementation group D1 antibody; Fanconi anemia group D1 protein antibody; GLM3 antibody; mutant BRCA2 antibody; OTTHUMP00000018803 antibody; OTTHUMP00000042401 antibody; PNCA2 antibody; XRCC11 antibody;
WB, FC
Human
BRCA2 Antibody (YA6483) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to BRCA2.
Brca1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Brca1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Brca1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Brca1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
BRCA1 Human Pre-designed siRNA Set A contains three designed siRNAs for BRCA1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Human OLA1 mRNA encodes the human Obg like ATPase 1 (OLA1) protein, a member of the GTPase protein family. OLA1 interacts with breast cancer-associated gene 1 (BRCA1) and BRCA1-associated RING domain protein (BARD1), and is involved in centrosome regulation.
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