Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T15641 |
K777
APC-3316 |
P450; Cysteine Protease; CCR | Immunology/Inflammation; Metabolism; Microbiology/Virology; Proteases/Proteasome |
K777 是有效的,具有口服活性的,不可逆的半胱氨酸蛋白酶 (cysteine protease) 抑制剂。K777是有效的 CYP3A4 抑制剂(IC50= 60 nM)。K777也是选择性的 CCR4 拮抗剂,显示出强的趋化性抑制作用。K777 对 Cruzain(克鲁斯锥虫的主要半胱氨酸蛋白酶)和组织蛋白酶 B 和 L 具有不可逆的抑制作用。K777 通过靶向组织蛋白酶介导的细胞进入,显示出广谱的抗病毒作用。K777 抑制 EBOV 和 SARS-CoV 病毒的进入,IC50 值分别为 0.87 nM 和 0.68 nM。 | |||
T39029 |
APC-6860
|
||
APC-6860 is a trypsin-like serine proteases inhibitor with k i values of 0.21, 0.44, 1.5, 16.8, 20, 30 μM for uPA, trypsin, tryptase, tPA, thrombin and factor Xa, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has k i values of 0.1, 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer. | |||
T22189 |
APC 366
|
||
APC 366 是肥大细胞类胰蛋白酶 (tryptase) 的选择性抑制剂,Ki 值为7.1 μM。在羊过敏性哮喘模型中,APC 366 抑制抗原诱导的早期哮喘反应 (EAR)、晚期哮喘反应 (LAR) 和支气管高反应性 (BHR)。 | |||
T30094 |
APC-6336
UNII-4124YUO44Z,CRA-6336,4124YUO44Z |
||
APC-6336 is a bio-active chemical. | |||
T40081 |
APC 366 TFA
|
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APC 366 (TFA) is a potent irreversible inhibitor of mast cell tryptase. It is particularly useful in studies related to allergic diseases. | |||
T38466 | 4-APC hydrobromide | ||
4-APC hydrobromide is a potent and specific aldehyde derivatization agent. It contains an aniline moiety that enables rapid and selective reaction with aliphatic aldehydes, as well as a quaternary ammonium group that enhances sensitivity in mass spectrometry (MS) analysis. By utilizing 4-APC hydrobromide, aldehydes can be detected with exceptional sensitivity and selectivity using MS. | |||
T69182 | APC-3316 hydrochloride | ||
APC-3316 hydrochloride is a vinyl sulfone cysteine protease inhibitor and selective CCR4 antagonist. | |||
T12766 |
RPR121056
APC |
AChR | Neuroscience |
RPR121056 is a Irinotecan metabolite, which is generated by CYP3A4. Irinotecan is an antineoplastic agent that inhibits topoisomerase type I. | |||
T69453 |
APC-0576
|
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APC-0576 is an (S,S)-isomer which inhibits NF-kappaB-dependent gene activation. APC-0576 may prevent pro-inflammatory cytokine-induced chemokine production in human endothelial cells. | |||
T8561 |
Apcin
|
APC | Cell Cycle/Checkpoint |
Apcin 是后期促进复合物/环体 (APC/C(Cdc20)) E3 连接酶活性的有效竞争性抑制剂,可通过与 Cdc20 结合并阻止底物识别竞争性地抑制 APC/C 依赖性泛素化。它占据 WD40 结构域侧面的 D-box 结合口袋,并可以延长有丝分裂。它通过阻断有丝分裂退出并通过共同添加 Ts-Arg-OMe 协同放大而起作用。 | |||
T69183 | APC-3316 tosylate | ||
APC-3316 tosylate is a vinyl sulfone cysteine protease inhibitor and selective CCR4 antagonist. | |||
T70193 |
APC-366 HCl
|
||
APC-366 is a selective inhibitor of the mast cell tryptase that inhibits tryptase-induced histamine release from human tonsil and lung cells. | |||
T22884 |
JW 67
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
JW 67 是典型 Wnt 信号通路的抑制剂,IC50为 1.17 μM。它影响由 β- 连环蛋白/GSK-3β/AXIN/APC/CK1 组成的多蛋白复合物,快速降低活性 β- 连环蛋白,随后下调Wnt 靶基因。它也抑制结直肠癌细胞生长。 | |||
T70192 | NC-2100 | ||
NC-2100 is an aperoxisome proliferator-activated receptor-gamma (PPARgamma) activator. | |||
T12575 |
Unesbulin
PTC596 |
Apoptosis; BMI-1 | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Unesbulin (PTC596) 是一种口服有效和选择性的 B 细胞特异性莫洛尼氏鼠白血病病毒整合位点 1 抑制剂。它在急性髓细胞白血病细胞中可下调 MCL-1 并诱导不依赖 p53 的线粒体凋亡,具有抗白血病作用。 | |||
T1731 |
TAME hydrochloride
NA-P-甲苯磺酰-L-精氨酸甲酯盐酸盐,Tos-Arg-OMe HCl,TOS-ARG-OME hydrochloride |
Amino Acids and Derivatives; APC | Cell Cycle/Checkpoint; Metabolism |
TAME hydrochloride (Tos-Arg-OMe HCl) 是后期促进复合体(APC/C 或 APC)的抑制剂,可与 APC/C 结合并阻止其通过 Cdc20 和 Cdh1 活化,产生有丝分裂阻滞。它是一种 od 氨基酸衍生物。 | |||
T6693 |
TAME
N-[(4-甲基苯基)磺酰基]-L-精氨酸甲酯,Tosylarginine methyl ester,N-4-Tosyl-L-arginine methyl ester |
APC | Cell Cycle/Checkpoint |
TAME (N-4-Tosyl-L-arginine methyl ester) 是后期促进复合体(APC/C 或 APC)的抑制剂,可与 APC/C 结合并阻止其通过 Cdc20 和 Cdh1 活化,产生有丝分裂阻滞。 | |||
T64339 |
Apcin A HCL
|
APC | Cell Cycle/Checkpoint |
Apcin A HCL 是 Apcin 衍生物。 它是一种后期促进复合物 (APC) 抑制剂。它与 Cdc20 强烈相互作用,并抑制 Cdc20 底物的泛素化。它可用于合成 PROTAC CP5V。 | |||
T74235 |
DHAPC
|
||
DHAPC 是一种对氧化非常敏感的磷脂。 | |||
T10345 |
Apcin-A
|
Others | Others |
Apcin-A is an anaphase-promoting complex (APC) inhibitor. It interacts strongly with Cdc20 and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V. | |||
T82888 |
Bibapcitide
|
||
Bibapcitide为含26个氨基酸残基的多肽,表现出抗凝血功能。 | |||
T37586 |
DMHAPC-Chol
|
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DMHAPC-Chol is a cationic cholesterol. Liposomes containing DMHAPC-chol have been used for DNA plasmid delivery in vitro and in vivo in a B16-F10 mouse xenograft model. Liposomes containing DMHAPC-chol are cytotoxic to B16-F10 cells when used at lipid concentrations greater than 20 μM. DMHAPC-Chol, as part of a lipoplex with DOPE , has also been used to deliver DNA into mouse lung via intratracheal injection, resulting in a heterogeneous distribution in the bronchi and bronchioles, and to delive... | |||
T37035 |
HAPC-Chol
|
||
HAPC-Chol is a cationic cholesterol. HAPC-Chol, as part of a lipoplex with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells in a luciferase assay without affecting cell viability. It has also been used to deliver siRNA into mice via intravenous injection, resulting in HAPC-chol accumulation in the lungs. | |||
T71654 |
APcK110
|
||
APcK110 is a novel Kit inhibitor . APcK110 inhibits proliferation of the mastocytosis cell line HMC1.2 and the SCF-responsive cell line OCI/AML3 in a dose-dependent manner . APcK110 is a more potent inhibitor of OCI/AML3 proliferation than the clinically used Kit inhibitors imatinib and dasatinib and at least as potent as cytarabine. APcK110 inhibits the phosphorylation of Kit, Stat3, Stat5, and Akt in a dose-dependent fashion, showing activity of APcK110 on Kit and its downstream signaling path... | |||
T37027 |
MHAPC-Chol
|
||
MHAPC-Chol is a cationic cholesterol. MHAPC-Chol, as part of a lipoplex with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells in a luciferase assay without affecting cell viability. It has also been used to deliver siRNA into mice via intravenous injection, resulting in MHAPC-chol accumulation in the liver. | |||
T24855 |
TASIN-1 Hydrochloride
塔辛-1盐酸盐,TASIN-1 HCl,TASIN 1 HCl,TASIN1 HCl |
APC | Cell Cycle/Checkpoint |
TASIN-1 Hydrochloride (TASIN-1 HCl) 是一种截短型 APC 的选择性抑制剂,通过降低细胞胆固醇水平和通过结肠癌细胞中的 ER 应激/ROS/JNK 信号传导诱导凋亡细胞死亡来选择性杀死表达截短型 APC 的结肠直肠癌细胞。 | |||
T22632 |
TASIN-1
1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine,塔辛-1 |
APC | Cell Cycle/Checkpoint |
TASIN-1 是截短的APC 基因(结肠腺瘤样息肉基因)选择性抑制剂,可以抑制胆固醇生物合成并发挥细胞毒性作用。它是一种预防和干预APC 突变型结直肠癌的潜在治疗策略。 | |||
TP1628L |
Activated Protein C (390-404), human acetate
Activated Protein C (390-404), human acetate(146340-20-7 Free base) |
APC | Cell Cycle/Checkpoint |
Activated Protein C (390-404), human acetate (Activated Protein C ) 抑制 APC 抗凝活性。 | |||
T22646 |
CFM 4
CFM-4,CFM4 |
Apoptosis; APC | Apoptosis; Cell Cycle/Checkpoint |
CFM 4 是一种有效的小分子 CARP-1/APC-2 拮抗剂,阻止 CARP-1 与 APC-2 结合,促使 G2M 细胞周期阻滞,引起细胞凋亡,其 IC50 范围为 10-15 μM。CFM 4 对耐药人类乳腺癌细胞的生长有抑制作用。 | |||
T2052 |
KY02111
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
KY02111 是典型的 WNT 信号抑制剂,能够促进人多潜能干细胞向心肌细胞分化,可用于研究人类心肌细胞再生。 | |||
T8509 |
Danicopan
ACH-4471 |
Complement System | Immunology/Inflammation |
Danicopan (ACH-4471) 是一种可口服的小分子 D 因子选择性抑制剂,对人 D 因子具有高结合亲和力,Kd 值为 0.54 nM。 它可抑制补体替代途径 (APC) 的活性,具有阻断阵发性夜间血红蛋白尿 (PNH) 和非典型溶血性尿毒症综合征 (aHUS) 的补体替代途径的潜力。 | |||
T81876 |
MAIT-203
|
||
MAIT-203为环戊丙氨酸衍生的拟肽,专一抑制APC和Asef (RhoGEF4)的相互作用,不影响APC-Sam68或APC-striatin。该化合物与APC-ARM结合紧密,Ki值为0.015 μM,Kd值为0.036 μM,并有效抑制结直肠癌细胞的迁移与侵袭。 | |||
T28455 |
ProTAME
pro-Tosyl-L-Arginine Methyl Ester |
||
ProTAME is an inhibitor of APC/CFzr and APC/CCdc20. Combinations of proTAME with topoisomerase inhibitors, doxorubicin and etoposide, significantly increase cell death in primary cells and Multiple Myeloma (MM) cell lines, particularly if TOPIIα levels ar | |||
TP1580 |
Activated Protein C (390-404), human TFA
|
||
The peptide region containing residues 390-404 in Activated Protein C (APC) is essential for anticoagulant activity and is available for interaction with antibodies or with other proteins, such as the macromolecular substrates Factors Va or VIIIa. APC reg | |||
T23875 |
CFM-1
CFM 1,CFM1 |
||
CFM-1 is an antagonist of the anaphase-promoting complex (APC)-2. It also is a cell cycle and apoptosis regulatory protein (CARP)-1 interaction antagonist. | |||
TP1628 |
Activated Protein C (390-404), human
|
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Activated Protein C (390-404), human, a peptide derived from the vitamin K-dependent serine protease, effectively suppresses the anticoagulant activity of APC[1]. | |||
TP1196 |
D-Lys(Z)-Pro-Arg-pNA
Chromozym Pca |
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D-Lys(Z)-Pro-Arg-pNA is a luminescent substrate of activated protein C (APC). | |||
TP1995 |
MAIT 203
|
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Inhibits interaction of APC and Asef (RhoGEF4). Inhibits colorectal cancer cell migration and invasion in vitro. | |||
T28247 |
ONO-1714 HCl
ONO-1714,ONO1714,ONO-1714 hydrochloride,ONO 1714 |
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ONO-1714 is a inducible nitric oxide synthase (NOS-2) inhibitor. ONO-1714 reduces hyperoxic lung injury in mice. ONO-1714 attenuates inflammation-related large bowel carcinogenesis in male Apc(Min/+) mice. ONO-1714 also inhibits neuronal NOS and exerts an | |||
T82526 | Drotrecogin alfa (activated) | ||
Drotrecogin alfa activated (DrotAA)为重组人活化蛋白C(APC)。该化合物能够抑制由烟雾引起的大鼠肺微血管通透性上升及促炎细胞因子IL-1β水平增加,具有抗凝血与抗炎作用,并促进纤溶过程。Drotrecogin alfa activated主要用于重症脓毒症的实验研究。 | |||
T27760 | KYA1797 | ||
KYA1797 is an inhibitor of the Wnt/ß-catenin pathway. KYA1797 binds directly to the regulators of G-protein signaling domain of axin, initiats ß-catenin and Ras degradation through enhancement of the ß-catenin destruction complex activating GSK3ß, effecti | |||
T78332 |
Eftilagimod alfa
IMP321,LAG-3Ig |
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Eftilagimod alfa为重组LAG-3Ig融合蛋白,具有MHC II 类分子结合能力。该药物通过介导抗原提呈细胞(APC)的激活进而激活CD8 T细胞,可用于研究转移性黑色素瘤及转移性乳腺癌。 | |||
T38052 | CRA-2059 TFA | ||
CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2]. Tryptase is a trypsin-like serine protease found as a major protein component in human mast cell secretory granules. CRA-2059 has the potential for inflammatory bowel disease research[1]. [1]. Tremaine WJ, et al. Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Aliment Pharmacol Ther. 2002;16... | |||
T38051 | CRA-2059 hydrochloride | ||
CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2]. Tryptase is a trypsin-like serine protease found as a major protein component in human mast cell secretory granules. CRA-2059 hydrochloride has the potential for inflammatory bowel disease research[1]. [1]. Tremaine WJ, et al. Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Ali... | |||
T82517 |
DYSP-C34
|
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DYSP-C34是一种生物相容性强且有效的超声(US)激活多功能分子机器。它提升了亲脂性/亲水性平衡,增强了超声诱导的ROS产生,并改善了细胞渗透能力,进而显著提升了对肿瘤的靶向效果及声动力疗法(SDT)介导的肿瘤缩减能力。此外,DYSP-C34还通过激活APC展示出温和的免疫原性。 |