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Cat. No. | Product Name | ||
---|---|---|---|
L3500 | 组蛋白修饰化合物库 | 469 compounds | |
469 个组蛋白修饰相关的小分子化合物的特有集合,用于高通量、高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T39710 |
ARV-471
Vepdegestrant |
Estrogen Receptor/ERR; PROTACs | Endocrinology/Hormones; PROTAC |
ARV-471 (Vepdegestrant) 是一种高效的,口服有效的基于 Cereblon 配体的雌激素受体降解剂 PROTAC 。ARV-471 常用于研究乳腺癌。 | |||
T3110 |
PRT4165
NSC600157,PRT 4165 |
BMI-1; Others; E1/E2/E3 Enzyme | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others; Ubiquitination |
PRT4165 (NSC600157) 是有效的 PRC1介导 H2A 泛素化的抑制剂。 | |||
T11879 |
LS-102
LS102 |
Ligand for E3 Ligase | PROTAC |
LS-102 是一种选择性的 E3 连接酶 synoviolin (Syvn1) 抑制剂,是 黄芪甲苷IV衍生物,通过抑制线粒体裂变来缓解心肌缺血再灌注损伤。LS-102 抑制 Syvn1 自泛素化,可改善阿霉咪唑诱导的心率减慢,有研究心血管疾病。 | |||
T25465 |
GS143
GS-143,GS 143 |
IκB/IKK; E1/E2/E3 Enzyme; NF-κB | NF-κB; Ubiquitination |
GS-143 是选择性的IκBα泛素化抑制剂,抑制 SCFβTrCP1介导的IκBα泛素化作用,IC50=5.2 μM。GS143 抑制NF-κB 的活化和靶基因的转录,并且不抑制蛋白酶体的特性,并具有抗哮喘作用。 | |||
T69642 |
FT385
|
Others | Others |
FT385 is a novel USP30 inhibitor, recapitulating genetic loss of USP30 and setting the trigger for PINK1-PARKIN amplification of mitochondrial ubiquitylation. | |||
T61512 |
FT3967385
|
Others | Others |
FT3967385 is a newly developed compound that functions as a USP30 inhibitor, emulating the genetic deficiency of USP30. This inhibition serves as a catalyst for the amplification of mitochondrial ubiquitylation through the PINK1-PARKIN pathway. | |||
T75133 |
NRX-0492
|
Others | Others |
NRX-0492 是一种口服有效的 BTK 降解剂。NRX-0492 催化 BTK 泛素化和蛋白酶体降解 (DC50≤0.2 nM,DC90≤0.5 nM)。NRX-0492 抑制 B 细胞受体 (BCR) 介导的信号、转录程序和趋化因子分泌。NRX-0492 能够把非共价 BTK 结合域连接到 Cereblon。Cereblon 是 E3泛素连接酶复合物的一种衔接蛋白。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-00611 |
UBE2B Protein, Mouse, Recombinant
mHR6B,ubiquitin-conjugating enzyme E2B,Rad6b,HR6B,E2-14k,261... |
Mouse | E. coli |
The ubiquitin-conjugating enzyme E2B (Ube2b) is a critical target gene of androgen receptor (AR), mediating the function of AR in spermatogenesis by promoting H2A ubiquitylation. Moreover, UBE2B plays an important role in muscle protein homeostasis during catabolic conditions. | |||
TMPJ-01386 |
STUB1 Protein, Human, Recombinant
Carboxy Terminus of Hsp70-Interacting Protein,STIP1 Homology... |
Human | E. coli |
E3 Ubiquitin-Protein Ligase CHIP is a cytoplasmic protein. CHIP is highly expressed in skeletal muscle, heart, pancreas, brain and placenta. CHIP interacts with the molecular chaperones Hsc70-Hsp70 and Hsp90 through its TPR domain; lead to in client substrate ubiquitylation and degradation by the proteasome. CHIP targets misfolded chaperone substrates towards proteasomal degradation. CHIP mediates transfer of non-canonical short ubiquitin chains to HSPA8 that have no effect on HSPA8 degradation.... | |||
TMPY-02496 |
Rad6/UBE2A Protein, Human, Recombinant (His)
UBC2,HHR6A,MRXS30,MRXSN,RAD6A,ubiquitin-conjugating enzyme E... |
Human | E. coli |
Ubiquitin-conjugating enzyme E2 A (also known as HHR6A or UBE2A), encoded by human DNA repair genes HHR6A, belongs to the ubiquitin-conjugating enzymes (E2 enzymes) family and is likely to be involved in postreplication repair and induced mutagenesis. UBE2A is described as a CDK2 substrate. It is the human homologue of the product of the Saccharomyces cerevisiae RAD6 / UBC2 gene, a member of the family of ubiquitin-conjugating enzymes. In vivo, HHR6A phosphorylation peaks during the G2/M phase o... | |||
TMPY-02522 |
OTUB2 Protein, Human, Recombinant (His)
OTU deubiquitinase, ubiquitin aldehyde binding 2,OTU2,OTB2,C... |
Human | E. coli |
Otubain 2 (OTUB2) is a member of DUBs that belong to the ovarian tumour (OTU) superfamily of proteins which consists of a five-stranded β-sheet sandwiched in between a small helical amino-terminal region consisting of α1 and α2, and a large helical region comprised of α3-α10. Like other DUBs, otubain 2 (OTUB2) cleaves proteins precisely at the ubiquitin-protein bond so that ubiquitylation process can be reversed and regulated. Otubain 2 (OTUB2)'s active-site cleft is sterically occluded by a nov... | |||
TMPY-04813 |
ACAT2 Protein, Rat, Recombinant (His)
acetyl-CoA acetyltransferase 2 |
Rat | E. coli |
Acyl-coenzyme A: cholesterol acyltransferase (ACAT) is an intracellular enzyme that produces cholesteryl esters in various tissues. In mammals, two ACAT genes (ACAT1 and ACAT2) have been identified. Together, these two enzymes are involved in storing cholesteryl esters as lipid droplets, in macrophage foam-cell formation, in absorbing dietary cholesterol, and in supplying cholesteryl esters as part of the core lipid for lipoprotein synthesis and assembly. The key difference in tissue distributio... | |||
TMPY-02510 |
HIST2H2BE Protein, Human, Recombinant
MGC129734,H2BGL105,H2B.1,histone cluster 2, H2be,H2B,H2BFQ,G... |
Human | E. coli |
Histones are a complex family of highly conserved basic proteins responsible for packaging chromosomal DNA into nucleosomes. Histone proteins exhibit two levels of diversity: 1. evolutionary diversity between species and 2. subtype diversity in a class(H1, H2A, H2B, H3 or H4) within a species. It has become more and more evident that histone modifications are key players in the regulation of chromatin states and dynamics as well as in gene expression. Therefore, histone modifications and the enz... |