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Cat. No. | Product Name | Target | Signaling Pathways |
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T1167 |
Cyproterone acetate
Androcur,醋酸环丙氯地孕酮,Cyproterone 17-O-acetate,醋酸环丙孕酮 |
Androgen Receptor | Endocrinology/Hormones |
Cyproterone acetate (Cyproterone 17-O-acetate) 是能够抗雄激素(IC50=7.1 nM) 和孕激素合成的类固醇。它与 progesteron 和糖皮质激素受体有亲和力。 | |||
T6889 |
MI-136
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Apoptosis; Epigenetic Reader Domain; Androgen Receptor | Apoptosis; Chromatin/Epigenetic; Endocrinology/Hormones |
MI136 是 menin-MLL(PPI) 蛋白互作的抑制剂,其 IC50值为31 nM,Kd 值为23.6 nM。它可抑制 DHT 诱导的雄激素受体 (AR) 靶基因的表达,有用于去势抵抗性肿瘤的潜能。 | |||
T60988 |
Androgen receptor antagonist 4
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||
Androgen receptor antagonist 4 (Compound AT2) 表现出抗癌活性。Androgen receptor antagonist 4 有效拮抗 AR 的转录活性,抑制 AR 的下游靶基因,并阻断 DHT 诱导的 AR 核转位。它是雄激素受体 (AR) 的拮抗剂 (IC50 = 0.15 μM)。 | |||
T70956 | JNJ-pan-AR | ||
JNJ-pan-AR, a meylated analogue of JNJ-63576253, is a novel pan-AR antagonist with potent activity against wild-type and clinically relevant AR mutations including F877L. JNJ63576253, also known as TRC253, is a potent and orally active androgen receptor antagonist. TRC253 specifically binds to both wild-type and certain mutant forms of AR, thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot translocate to the nucleus. | |||
T38107 |
JJH260
JJH260 |
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JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA with an IC50 value of 0.57 μM. JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 μM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2. JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysa... | |||
T38316 |
ABC34
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ABC34 is an inactive control probe for JJH260 , the inhibitor of androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). ABC34 demonstrates an IC50 value greater than 25 μM for the inhibition of 9-PAHSA but is more potent in blocking the serine hydrolase ABHD6 and the palmitoyl-protein hydrolase PPT1, which are both off-targets of JJH260. | |||
T71552 | ASC-JM-17 | ||
ASC-JM-17 is an activator of both Nrf1 and Nrf2 proteins. ASC-JM17 acts on Nrf1, Nrf2 and Hsf1 to increase the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. ASC-JM17 ameliorates toxicity of the mutant androgen receptor (AR) responsible for SBMA in cell, fly and mouse models. Knockdown of the Drosophila Nrf1 and Nrf2 ortholog cap ‘n’ collar isoform-C, but not Hsf1, blocks the protective effect of ASC-JM17 on mutant AR-induced eye degeneration in flies. | |||
T35668 |
Neoaureothin
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Neoaureothin is a bacterial metabolite that has been found in Streptomyces. It is an androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs (IC50 = 13 μM) and inhibits DHT-induced expression of prostate-specific antigen in LNCaP cells (IC50 = 1.75 nM). Neoaureothin is cytotoxic to A549, HCT116, and HepG2 cells (IC50s = 34.3, 47, and 37.2 μg/ml, respectively). It also has nematocidal activity against the pine wood nematode B. xylophilus (LC50 = 0.84 μg/ml) and... | |||
T70962 | MHY219 | ||
MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. M... | |||
T35855 |
AAA
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AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 μM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells.In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension... |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN1677 |
Gartanin
1,3,5,8-四羟基-2,4-双(3-甲基-2-丁烯基)-9H-氧杂蒽-9-酮,藤黄苷 |
BCL; Caspase; JNK | Apoptosis; MAPK; Proteases/Proteasome |
Gartanin 是山竹果中的一种天然黄酮,具有抗氧化、抗真菌、抗炎、神经保护和抗肿瘤活性。它能够诱导人脑胶质瘤细胞的细胞周期阻滞和自噬,抑制其迁移。 |
Cat. No. | Product Name | Species | Expression System |
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TMPY-00005 |
FGF-8a Protein, Human, Recombinant
fibroblast growth factor 8 (androgen-induced |
Human | E. coli |
In mammalian embryos, transient Fgf8 expression defines the developing isthmic region, lying between the midbrain and the first rhombomere, but there has been uncertainty about the existence of a distinct isthmic segment in postnatal mammals. Retinoic acid (RA) directly represses Fgf8 through a RARE-mediated mechanism that promotes repressive chromatin, thus providing valuable insight into the mechanism of RA-FGF antagonism during progenitor cell differentiation. Fgf8 encodes a key signaling fac... | |||
TMPY-06986 |
FGF-8b Protein, Human, Recombinant
NEWENTRY,fibroblast growth factor 8 (androgen-i... |
Human | E. coli |
In mammalian embryos, transient Fgf8 expression defines the developing isthmic region, lying between the midbrain and the first rhombomere, but there has been uncertainty about the existence of a distinct isthmic segment in postnatal mammals. Retinoic acid (RA) directly represses Fgf8 through a RARE-mediated mechanism that promotes repressive chromatin, thus providing valuable insight into the mechanism of RA-FGF antagonism during progenitor cell differentiation. Fgf8 encodes a key signaling fac... | |||
TMPY-03259 |
Calreticulin Protein, Human, Recombinant (His)
HEL-S-99n,cC1qR,SSA,CRT,RO,calreticulin |
Human | HEK293 |
Calreticulin is a multifunctional protein. It acts as a main Ca(2+)-binding (storage) protein in the lumen of the endoplasmic reticulum. Calreticulin binds Ca2+ ions (a second messenger in signal transduction), rendering it inactive. The Ca2+ is bound with low affinity, but high capacity, and can be released on a signal. Located in storage compartments associated with the endoplasmic reticulum, calreticulin also binds to misfolded proteins and prevents them from being exported from the endoplasm... | |||
TMPY-03258 |
Calreticulin Protein, Human, Recombinant (hFc)
RO,cC1qR,HEL-S-99n,CRT,calreticulin,SSA |
Human | HEK293 |
Calreticulin is a multifunctional protein. It acts as a main Ca(2+)-binding (storage) protein in the lumen of the endoplasmic reticulum. Calreticulin binds Ca2+ ions (a second messenger in signal transduction), rendering it inactive. The Ca2+ is bound with low affinity, but high capacity, and can be released on a signal. Located in storage compartments associated with the endoplasmic reticulum, calreticulin also binds to misfolded proteins and prevents them from being exported from the endoplasm... | |||
TMPY-06327 |
Calreticulin Protein, Human, Recombinant
HEL-S-99n,calreticulin,cC1qR,CRT,RO,SSA |
Human | HEK293 |
Calreticulin is a multifunctional protein. It acts as a main Ca(2+)-binding (storage) protein in the lumen of the endoplasmic reticulum. Calreticulin binds Ca2+ ions (a second messenger in signal transduction), rendering it inactive. The Ca2+ is bound with low affinity, but high capacity, and can be released on a signal. Located in storage compartments associated with the endoplasmic reticulum, calreticulin also binds to misfolded proteins and prevents them from being exported from the endoplasm... | |||
TMPY-06710 |
PSCA Protein, Mouse, Recombinant (His)
prostate stem cell antigen,2210408B04Rik |
Mouse | HEK293 |
Prostate Stem Cell Antigen (PSCA) is frequently expressed in prostate cancer. Prostate stem cell antigen (PSCA) is a cell-membrane glycoprotein consisting of 123 amino acids. Knockdown of PSCA induced EMT and reduced metastatic potentials of the DU145 cells, suggesting that PSCA played an important role in prostatic carcinogenesis and progression. PSCA gene plays an important role in cell adhesion, proliferation and survival. Increasing studies have focused on the association of PSCA gene rs2294... | |||
TMPY-06655 |
PSCA Protein, Mouse, Recombinant (His & Avi), Biotinylated
prostate stem cell antigen,2210408B04Rik |
Mouse | HEK293 |
Prostate Stem Cell Antigen (PSCA) is frequently expressed in prostate cancer. Prostate stem cell antigen (PSCA) is a cell-membrane glycoprotein consisting of 123 amino acids. Knockdown of PSCA induced EMT and reduced metastatic potentials of the DU145 cells, suggesting that PSCA played an important role in prostatic carcinogenesis and progression. PSCA gene plays an important role in cell adhesion, proliferation and survival. Increasing studies have focused on the association of PSCA gene rs2294... | |||
TMPY-04408 |
CAMKII beta/CAMK2B Protein, Human, Recombinant (His & GST)
calcium/calmodulin-dependent protein kinase II beta,CAM2,CAM... |
Human | Baculovirus-Insect Cells |
Calcium/calmodulin-dependent protein kinase II beta (CAMK2B) is a member of the serine/threonine protein kinase family and to the Ca(2+)/calmodulin-dependent protein kinase subfamily. CaMKII is an important player in prostate cancer cells ability to escape apoptosis under androgen ablation and facilitate the progression of prostate cancer cells to an androgen independent state. As a multifunctional protein kinase, the loss of activity may play a critical role in initiating the changes leading to... | |||
TMPY-04484 |
ACK1 Protein, Human, Recombinant (GST)
ACK-1,ACK1,p21cdc42Hs,ACK,tyrosine kinase, non-receptor, 2 |
Human | Baculovirus-Insect Cells |
ACK1 (also known as ACK, TNK2, or activated Cdc42 kinase) is a structurally unique non-receptor tyrosine kinase that is expressed in diverse cell types. This downstream effector of CDC42 mediates CDC42-dependent cell migration via phosphorylation of BCAR1. The ACK1 protein may be involved in a regulatory mechanism that sustains the GTP-bound active form of Cdc42Hs and which is directly linked to a tyrosine phosphorylation signal transduction pathway. ACK1 integrates signals from plethora of liga... | |||
TMPY-01190 |
INHBB Protein, Human, Recombinant (His)
inhibin beta B,INHBB,Inhibin β B Protein,MGC157939,inhibin β... |
Human | HEK293 |
Activin and inhibin are two closely related protein complexes that have almost directly opposite biological effects. The activin and inhibin protein complexes are both dimeric in structure, and, in each complex, the two monomers are linked to one another by a single disulfide bond. Activin is composed of two ß subunits, ßA ßA (activin A), ßB ßB (activin B), or ßA ßB (activin AB). Inhibin is composed of an alpha and one of two ß subunits, ßA (inhibin A) or ßB (inhibin B). Activins are produced in... | |||
TMPH-02238 |
TMPRSS2 Protein, Human, Recombinant (Avi & His & MBP), Biotinylated
|
Human | E. coli |
Plasma membrane-anchored serine protease that participates in proteolytic cascades of relevance for the normal physiologic function of the prostate. Androgen-induced TMPRSS2 activates several substrates that include pro-hepatocyte growth factor/HGF, the protease activated receptor-2/F2RL1 or matriptase/ST14 leading to extracellular matrix disruption and metastasis of prostate cancer cells. In addition, activates trigeminal neurons and contribute to both spontaneous pain and mechanical allodynia.... | |||
TMPH-02235 |
TMPRSS2 Protein, Human, Recombinant (Cell-Free, His)
|
Human | in vitro E. coli expression system |
Plasma membrane-anchored serine protease that participates in proteolytic cascades of relevance for the normal physiologic function of the prostate. Androgen-induced TMPRSS2 activates several substrates that include pro-hepatocyte growth factor/HGF, the protease activated receptor-2/F2RL1 or matriptase/ST14 leading to extracellular matrix disruption and metastasis of prostate cancer cells. In addition, activates trigeminal neurons and contribute to both spontaneous pain and mechanical allodynia.... | |||
TMPY-01846 |
Activin A Protein, Mouse, Recombinant (His)
inhibin, β A,inhibin, beta A |
Mouse | HEK293 |
Activin and inhibin are two closely related protein complexes that have almost directly opposite biological effects. The activin and inhibin protein complexes are both dimeric in structure, and, in each complex, the two monomers are linked to one another by a single disulfide bond. Activin is composed of two β subunits, βA βA (activin A), βB βB (activin B), or βA βB (activin AB). Inhibin is composed of an alpha and one of two β subunits, βA (inhibin A) or βB (inhibin B). Activins are produced in... | |||
TMPH-02236 |
TMPRSS2 Protein, Human, Recombinant (E. coli, His)
|
Human | E. coli |
Plasma membrane-anchored serine protease that participates in proteolytic cascades of relevance for the normal physiologic function of the prostate. Androgen-induced TMPRSS2 activates several substrates that include pro-hepatocyte growth factor/HGF, the protease activated receptor-2/F2RL1 or matriptase/ST14 leading to extracellular matrix disruption and metastasis of prostate cancer cells. In addition, activates trigeminal neurons and contribute to both spontaneous pain and mechanical allodynia.... | |||
TMPH-02237 |
TMPRSS2 Protein, Human, Recombinant (His & Myc)
|
Human | HEK293 |
Plasma membrane-anchored serine protease that participates in proteolytic cascades of relevance for the normal physiologic function of the prostate. Androgen-induced TMPRSS2 activates several substrates that include pro-hepatocyte growth factor/HGF, the protease activated receptor-2/F2RL1 or matriptase/ST14 leading to extracellular matrix disruption and metastasis of prostate cancer cells. In addition, activates trigeminal neurons and contribute to both spontaneous pain and mechanical allodynia.... |