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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].
TNG348 is an orally active ubiquitin-specific protease USP1 inhibitor that can be used in research on cancers with BRCA1/2 mutations or HRD+ (Homologous Recombination Deficiency positive) status [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].
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. The recommend isotype control of Anti-BRCA1 Antibody (BR64): Mouse IgG1 kappa, Isotype Control (HY-P99977).
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].
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].
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].
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].
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].
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] .
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].
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].
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-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].
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].
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) 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) 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] .
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] .
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].
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. The recommend isotype control of Anti-BRCA1 Antibody (BR64): Mouse IgG1 kappa, Isotype Control (HY-P99977).
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. The total length of BRCC36 Protein, Human (His-SUMO) is 315 a.a., with molecular weight of ~51.9 kDa.
BRCA1 Protein, Human is the recombinant human-derived BRCA1, expressed by E. coli , with tag Free labeled tag. The total length of BRCA1 Protein, Human is 214 a.a.,
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. The total length of BAP1 Protein, Human is 728 a.a., .
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. The total length of BAP1 Protein, Human (His) is 728 a.a., .
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. The total length of BRAP Protein, Human is 591 a.a., .
BRCA1 Antibody (YA819) is a non-conjugated and Mouse origined monoclonal antibody about 208 kDa, targeting to BRCA1. It can be used for IHC-P assays with tag free, in the background of Human, Mouse.
BRCA1; RNF53; Breast cancer type 1 susceptibility protein; RING finger protein 53
WB, IHC-F, IHC-P, ICC/IF, ELISA
Human, Rat
BRCA1 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 208 kDa, targeting to BRCA1. It can be used for WB,IHC-F,IHC-P,ICC/IF,ELISA assays with tag free, in the background of Human, Rat.
BRCA1-associated ATM activator 1; BRCA1-associated protein required for ATM activation protein 1
WB, ICC/IF, IP
Human
BRAT1 Antibody (YA2294) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2294), targeting BRAT1, with a predicted molecular weight of 88 kDa (observed band size: 88 kDa). BRAT1 Antibody (YA2294) can be used for WB, ICC/IF, IP experiment in human background.
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.
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