98
9
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。 | |||
T16670 |
PS210
|
PDK | PI3K/Akt/mTOR signaling |
PS210 是针对 PDK1的 PIF 结合口袋的、选择性的、有效的 PDK1激活剂,对其他蛋白激酶无活性。在细胞中,它的前药 PS423 可作为 PDK1的底物选择性抑制剂,抑制 S6K 的磷酸化和活化。 | |||
T9627 |
PHD-1-IN-1
|
HIF/HIF Prolyl-Hydroxylase | Chromatin/Epigenetic; Metabolism |
PHD-1-IN-1 是口服有效的缺氧诱导因子脯氨酰羟化酶结构域 1抑制剂,IC50为 0.034 μM。它与活性位 Fe2+具有独特的单齿结合相互作用,并诱导形成一个 “Arg367-out” 口袋。 | |||
T2301 |
SB 202190
FHPI,SB202190 |
Apoptosis; p38 MAPK; Autophagy | Apoptosis; Autophagy; MAPK |
SB 202190 (FHPI) 是一种 p38 MAPK 抑制剂,可以抑制 p38α 和 p38β2 (IC50=50/100 nM),具有选择性和细胞渗透性。SB 202190 具有抗肿瘤活性,还可以诱导人胚胎干细胞向心肌细胞分化。 | |||
T8719 |
SC99
|
Apoptosis; JAK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
SC99 是一种口服有效选择性STAT3抑制剂,靶向 JAK2-STAT3 途径,抑制血小板活化和聚集,有抗骨髓瘤和抗血栓活性。它结合在 JAK2 的 ATP 结合袋中,抑制 JAK2 和 STAT3 的磷酸化。 | |||
T9079 |
Apostatin-1
Apt-1 |
Others | Others |
Apostatin-1 (Apt-1) 是一种新型 TRADD 抑制剂。 Apostatin-1 可以与 TRADD 的 N 末端 TRAF2 结合域上的口袋结合。 | |||
T10533 |
BI-2852
|
Ras | GPCR/G Protein; MAPK |
BI-2852 是具有纳摩尔亲和力的开关 I/II 口袋(SI/II-口袋)的 KRAS 抑制剂,可抑制 KRAS 突变细胞的下游信号传导和抗增殖作用。 | |||
T23969 |
DCAI
|
Others | Others |
DCAI 是一种核苷酸交换和核苷酸释放的抑制剂,通过与 Ras-SOS 界面附近的口袋结合而起作用。 | |||
T8700 |
TKIM
|
Potassium Channel | Membrane transporter/Ion channel |
TKIM 是一种 TWIK 相关的钾通道 1 (TREK-1) 抑制剂,与 TREK-1 的中间 (IM) 状态的口袋结合。 | |||
T15579 |
INDY
1-(3-ethyl-5-hydroxy-1,3-benzothiazol-2-ylidene)propan-2-one |
DYRK | Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors |
INDY 是 Dyrk1A 和 Dyrk1B 的 ATP 竞争性抑制剂,IC50 分别为 0.24 μM 和 0.23 μM,对 Dyrk1A ATP 口袋的 Ki 为 0.18 μM。 | |||
T1980 |
HA14-1
|
BCL | Apoptosis |
HA14-1 是一种 Bcl-2/Bcl-xL 拮抗剂,与 Bcl-2 上的特定口袋结合,IC50约为 9 μM。 | |||
T17205 |
UNC2541
|
Others; FLT; TAM Receptor | Angiogenesis; Others; Tyrosine Kinase/Adaptors |
UNC2541 是 Mer 酪氨酸激酶特异性抑制剂,与 MerTK ATP 结合口袋结合的IC50值为 4.4 nM,对其选择性远高于 Axl,Tyro3 和 Flt3。它能够抑制磷酸化的 MerTK (pMerTK;EC50,510 nM)。 | |||
T8659 |
K-Ras-PDEδ-IN-1
|
PDE | Metabolism |
K-Ras-PDEδ-IN-1 是新型的 K-Ras-PDEδ 抑制剂,它能够以低纳摩尔Kd8 nM 与 PDEδ 的法尼基结合袋竞争性结合。 | |||
T9095 |
Necrostatin-34
2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4 |
RIP kinase | Apoptosis; NF-κB |
Necrostatin-34 (2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4) 是一种 RIPK1 激酶抑制剂,通过在激酶结构域中占据一个独特的结合口袋,将 RIPK1 激酶稳定在非活性构象中。 | |||
T3163 |
PS 48
|
PDK | PI3K/Akt/mTOR signaling |
PS 48 已被证明是一种 PKB 激酶 (PDK1) 激活剂 (Kd: 10.3 μM)。该化合物选择性地与 PKB 激酶 (PDK1) 的 PIF 结合口袋结合。 | |||
T27133 |
DCLX069
DCLX 069,DCLX-069 |
Histone Methyltransferase | Chromatin/Epigenetic |
DCLX069 是一种选择性蛋白精氨酸甲基转移酶 1 抑制剂,IC50值为 17.9 µM,对 PRMT4 和 PRMT6 的活性较低。它可有效阻断乳腺癌、肝癌和急性髓性白血病细胞系中的细胞增殖。 | |||
T14978 |
CL-82198
|
MMP | Proteases/Proteasome |
CL-82198 是 MMP-13选择性抑制剂。它能够与 MMP-13 的整个 S1' 口袋结合,这是其对 MMP-13 选择性和对其他 MMP 缺乏抑制活性的基础。它可用于研究骨关节炎。 | |||
T35694 |
OD36
OD 36,OD 36 hydrochloride,OD-36 |
ALK; RIP kinase | Angiogenesis; Apoptosis; NF-κB; Tyrosine Kinase/Adaptors |
OD36 是一种选择性强效 RIPK2 抑制剂,IC50 为 5.3 nM。OD36 可抑制 ALK2 信号传导和成骨分化(KD:37 nM),并能与 ALK2 激酶 ATP 袋有效结合。 | |||
T10585 |
Bozitinib
CBT-101,PLB-1001 |
c-Met/HGFR | Tyrosine Kinase/Adaptors |
Bozitinib (PLB-1001) 是一种可透过血脑屏障的、高效的、选择性的的、 ATP 竞争性的小分子 c-MET 激酶抑制剂,能够与酪氨酸激酶超家族的常规 ATP 结合口袋结合。 | |||
T67753 |
Trifluoromethyl-tubercidin
|
Influenza Virus | Microbiology/Virology |
Trifluoromethyl-tubercidin (TFMT)可抑制宿主Mtr1并抑制病毒复制。TFMT 通过其S-adenosyl-l-methionine 结合袋相互作用抑制Mtr1,限制流感病毒复制。TFMT 能有效抑制病毒在小鼠体内的复制,毒性很小。 | |||
T9103 |
BVDV-IN-1
|
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
BVDV-IN-1 是一种牛病毒性腹泻病毒 (BVDV) 的非核苷抑制剂 (NNI),EC50 为 1.8 μM。它直接与 BVDV RdRp 的疏水口袋结合,对耐 NNI 氨基硫脲 (TSC) 的 BVDV 具有抗病毒活性。 | |||
T12609 |
R-10015
|
LIM Kinase; Reverse Transcriptase | Cell Cycle/Checkpoint; Microbiology/Virology |
R-10015 是一种高效选择性 LIMK 抑制剂,通过结合 ATP 结合口袋阻断 LIMK,抑制人 LIMK1 的 IC50值为 38 nM。它还发挥广谱抗病毒作用,可用于 HIV 感染研究。 | |||
T11807 |
L002
|
Others; Histone Acetyltransferase; STAT | Chromatin/Epigenetic; JAK/STAT signaling; Others; Stem Cells |
L002 是一种细胞可渗透的,可逆特定性乙酰转移酶 p300(KAT3B)抑制剂,IC50为 1.98 μM。 它结合乙酰辅酶 A 口袋并竞争性抑制 FATp300 催化结构域,阻断组蛋白乙酰化和 p53 乙酰化,且抑制 STAT3 激活,有用于高血压引起的心脏肥大和纤维化的研究潜力。 | |||
T8931L |
ICCB-19 hydrochloride
ICCB-19 HCl(750621-52-4 free base) |
Apoptosis; Others; Autophagy; RIP kinase | Apoptosis; Autophagy; NF-κB; Others |
ICCB-19 hydrochloride (ICCB-19 HCl) 是RIPK1激酶活性的间接抑制剂。它是一种 TRADD 抑制剂,可与 TRADD 的 N 端结构域结合,破坏其与 TRADD-C 和 TRAF2 的结合,诱导自噬和长寿命蛋白质的降解。 | |||
T29111 |
VPC-13566
|
Androgen Receptor | Endocrinology/Hormones |
VPC-13566 是一种 BF3 特异性小分子,可有效抑制雄激素受体转录活性并从 BF3 口袋中置换出 BAG1L 肽。 VPC-13566 抑制各种前列腺癌细胞系的生长,并减少小鼠中 AR 依赖性前列腺癌异种移植肿瘤的生长。 | |||
T8873 |
Bractoppin
|
Others; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others |
Bractoppin 是一种BRCA1 (t)BRCT domain 识别磷酸肽的选择性抑制剂,IC50为 74 nM。它优先抑制 BRCA1 -tBRCT 依赖的 DNA 损伤。它减少 BRCA1 对 DNA 断裂片段的招募,进而抑制损伤诱导的 G2 期阻滞和重组酶 RAD51 的组装。 | |||
T14322 |
ARP-100
MMP-2 Inhibitor III |
MMP | Proteases/Proteasome |
ARP-100 (MMP-2 Inhibitor III) 是选择性基质金属蛋白酶MMP-2抑制剂 (IC50=12 nM)。它对 MMP-1 (>50 μM),MMP-3 (4.5 μM),MMP-7 (>50 μM) 和MMP-9 (0.2 μM) 的抑制活性较小。它与 MMP-2 的 S1'口袋相互作用,并在体外对基质胶的侵袭模型中显示抗侵袭特性。 | |||
T72055 |
FM04
|
P-gp | Membrane transporter/Ion channel; Neuroscience |
FM04 是一种具有口服活性和高效性的 P-糖蛋白 (P-gp) 抑制剂 ,EC50 值为 83 nM。FM04 可以与人P-gp核苷酸结合域2(NBD2)中的Q1193和I1115相互作用。从而破坏 R262-Q1081-Q1118 相互作用口袋并解偶联 ICL2-NBD2 相互作用,从而抑制 P-gp。FM04 可用于癌症和肿瘤的治疗。 | |||
T3157 |
COH29
RNR Inhibitor COH29 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
COH29 (RNR Inhibitor COH29) 是一种口服可用的芳香族取代噻唑,是人类核糖核苷酸还原酶 (RNR) 的抑制剂,具有潜在的抗肿瘤活性。它抑制核糖核苷酸还原酶的IC50为 16 μM。 | |||
T24676 |
PS423
PS210AM,PS 210 AM,PS 423,PS210-AM,PS-423 |
Others | Others |
PS423 is a substrate-selective protein kinase PDK1 inhibitor that acts by binding to the PIF-pocket allosteric docking site. | |||
T39440 |
CXCL12 ligand 1
|
Others | Others |
CXCL12 ligand 1 is the first ligand of the sY12-binding pocket on chemokine CXCL12 . | |||
T23656 |
VUF11211
VUF-11211,VUF 11211 |
Others | Others |
VUF11211 is an effective antagonist of CXCR3 that acts by extending from the minor pocket into the major pocket of the transmembrane domains. | |||
T71939 |
PS77
|
Others | Others |
PS77 is a Pkh inhibitor directed to the PIF-pocket with increased selectivity for C. albicans Pkh2. | |||
T24099 |
GP29
GP-29,GP 29 |
Others | Others |
GP29 is a Type II kinase inhibitor of the IRE1α endoribonuclease that acts by targeting the ATP-binding pocket of IRE1α. | |||
T10446 |
BA-53038B
|
Others | Others |
BA-53038B is an HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly in a distinct manner (EC50: 3.32 μM). | |||
T23901 |
CM026
CM 026,CM-026 |
Others | Others |
CM026 is a selective aldehyde dehydrogenase 1A1 inhibitor that acts by binding within the aldehyde binding pocket of ALDH1A1 in an uncompetitive partial mode of inhibition. | |||
T24740 |
RS-104966
|
Others | Others |
RS-104966 is an inhibitor of collagenase that acts by inducing the conformational change in the side-chains of the S1 pocket of MMP-1. | |||
T24543 |
NP603
NP 603,NP-603 |
Others | Others |
NP603 is a cell-permeable inhibitor of FGFR1, PDGFRβ, and VEGFR2 that binds to the ATP pocket. It also is a very weak EGFR inhibitor. | |||
T68466 |
BI-207524
|
Others | Others |
BI-207524 is a novel NS5B Thumb Pocket 1 Inhibitor with Improved Potency for the Potential Treatment of Chronic Hepatitis C Virus Infection. | |||
T24806 |
SMBA2
SMBA-2,NSC4436,NSC 4436,NSC-4436,SMBA 2 |
Others | Others |
SMBA2 is a Bax activator. It acts by specifically targeting the binding pocket at S184. | |||
T41113 |
3BrB-PP1
3BrB-PP1 |
Others | Others |
3BrB-PP1 is an ATP-competitive analog that exhibits specific inhibitory activity towards protein kinase. It is effective in inhibiting protein kinase with mutations in the ATP-binding pocket, specifically the mutation of Thr97 within Sty1's ATP-binding pocket. | |||
T39955 |
JNJ-67569762
|
Others | Others |
JNJ-67569762 is a selective BACE1 inhibitor targeting the S3 pocket ( IC 50 = 2.7 nM). | |||
T30089 |
AP-22161
AP22161,G7VE62573J,UNII-G7VE62573J,SCHEMBL7243003,AP 22161 |
Others | Others |
AP-22161 selectively binds the Src SH2 domain by targeting highly conserved phosphotyrosine binding to cysteine residues in the pocket. AP-22161 selectively inhibits Src SH2 binding and can be used to inhibit osteoclast absorption. | |||
T28389 |
PF-6422899
PF6422899,PF 6422899 |
Others | Others |
PF-6422899 irreversibly inhibits EGFR kinase activity by binding covalently to active-site cysteine residues in the ATP binding pocket of EGFR. | |||
T24098 |
GP17
GP-17,GP 17 |
Others | Others |
GP17 is a type II kinase inhibitor of the IRE1α endoribonuclease that acts by targeting the ATP-binding pocket of IRE1α. | |||
T16119 |
MLT-747
|
Others | Others |
MLT-747 is an effective and allosteric inhibitor of MALT1. It binds MALT1 in the allosteric Trp580 pocket (IC50: 14 nM). | |||
T26343 |
YK5
YK 5,YK-5 |
Others | Others |
YK5 is an allosteric inhibitor pocket of Hsp70 and represents a previously unknown chemical tool to investigate cellular mechanisms associated with Hsp70. | |||
T10374 |
ARS-1323-alkyne
|
Ras | GPCR/G Protein; MAPK |
ARS-1323-alkyne 是switch-II pocket (S-IIP)抑制剂,能够特异性报告活体细胞中 KRASG12C 核苷酸的状态。 | |||
T32500 |
L6Y
TTR stabilizer L6 |
Others | Others |
L6Y is a transthyretin (TTR) stabilizer which binds to the T4 binding pocket of TTR and prevents the dissociation of TTR to monomer. | |||
T71843 |
HPA-12
|
Others | Others |
HPA-12 is a novel potent inhibitor of cert, binding to the ceramide-binding pocket in the cert start domain |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-02028 |
RON/CD136 Protein, Human, Recombinant (His)
CD136,macrophage stimulating 1 receptor,CDw136,PTK8,RON |
Human | HEK293 Cells |
The tyrosine kinase receptor, macrophage-stimulating 1 receptor (MST1R), a c-met-related tyrosine kinase, also known as the Ron receptor or CD136, controls cell survival and motility programs related to invasive growth. As the tyrosine kinase receptor is comprised of an extracellular domain, MST1R protein contains the ligand-binding pocket and an intracellular region where the kinase domain is located. MST1R signaling may be involved in the regulation of macrophage and T-lymphocyte activation in... | |||
TMPK-00982 |
NTS1 Protein, Cynomolgus, Recombinant (His)
NTR1,NT,NTRR,NTRH,NTS1,NTSR1,NT/N,NTS,NMN-125,NN,NTR |
Cynomolgus | HEK293 Cells |
Crystal structures of neurotensin receptor subtype 1 (NTS1) allowed us to visualize the binding mode of the endogenous peptide hormone neurotensin and its pharmacologically active C-terminal fragment NT(8-13) within the orthosteric binding pocket of NTS1. NTS1 Protein, Cynomolgus, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 18.84 kDa and the accession number is Q2PG57. | |||
TMPH-03158 |
PAD Protein, Porphyromonas gingivalis, Recombinant (His)
Peptidylarginine deiminase |
Porphyromonas gingivalis | E. coli |
Deiminates the guanidino group of C-terminal arginine residues on a variety of peptides, including the vasoregulatory peptide-hormone bradykinin, to yield ammonia and a citrulline residue. May promote the growth of the pathogen in the periodontal pocket by producing ammonia, ammonia having a protective effect during acidic cleaning cycles in the mouth. PAD Protein, Porphyromonas gingivalis, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weig... | |||
TMPK-01162 |
NTS1 Protein, Mouse, Recombinant (hFc)
NTS1,NTRH,NN,NT,NTR1,NMN-125,NT/N,NTSR1,NTR,NTRR |
Mouse | HEK293 Cells |
Crystal structures of neurotensin receptor subtype 1 (NTS1) allowed us to visualize the binding mode of the endogenous peptide hormone neurotensin and its pharmacologically active C-terminal fragment NT(8-13) within the orthosteric binding pocket of NTS1. NTS1 Protein, Mouse, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The predicted molecular weight is 42.9 kDa and the accession number is Q9D3P9. | |||
TMPK-00545 |
HPX Protein, Cynomolgus, Recombinant (His)
Hemopexin,Hpx,Hpxn |
Cynomolgus | HEK293 Cells |
Hemopexin (HPX) serves as scavenger and transporter of toxic plasma heme to the liver. HPX is formed by two four-bladed beta-propeller domains, resembling two thick disks that lock together at a 90 degrees angle. The heme is bound between the two beta-propeller domains in a pocket formed by the interdomain linker peptide.HPX, acting not only as a heme carrier but also displaying transient heme-based ligand binding and (pseudo-)enzymatic properties, could be considered a 'chronosteric' heme-prote... | |||
TMPY-02390 |
SSPA Protein, E. coli, Recombinant (His)
ssp,pog |
E. coli | E. coli |
Stringent starvation protein A (ssPA), a member of the GST superfamily, is an RNA polymerase-associated transcriptional activator for the lytic development of phage P1 and is essential for stationary phase-induced acid tolerance of E. coli. It indicates that the flexible regions are not critical for SspA function, whereas the surface pocket is important for both transcriptional activation of the phage P1 late promoter and acid resistance of E. coli. SspA is known to be implicated in survival dur... | |||
TMPY-05438 |
CAN F 4 Protein, Canine, Recombinant (His)
|
Canine | HEK293 Cells |
Dog dander is an important cause of respiratory allergy but its content of allergenic components is still incompletely known. The size and the amino acid composition of the ligand-binding pocket indicate that Can f 4 is capable of binding only relatively small hydrophobic molecules which are different from those that Can f 2 is able to bind. The crystal structure of Can f 4 contained both monomeric and dimeric forms of the allergen, suggesting that Can f 4 is able to form transient (weak) dimers... | |||
TMPY-02461 |
AKR1A1 Protein, Human, Recombinant (His)
DD3,ALDR1,HEL-S-6,aldo-keto reductase family 1, member A1 (a... |
Human | E. coli |
Aldehyde reductase (AKR1A1) is a member of the aldo-keto reductase superfamily, which consists of more than 40 known enzymes and proteins that includes variety of monomeric NADPH-dependent oxidoreductases, such as aldehyde reductase. Aldehyde reductase has wide substrate specificities for carbonyl compounds. These enzymes are implicated in the development of diabetic complications by catalyzing the reduction of glucose to sorbitol. Aldehyde reductase possess a structure with a beta-alpha-beta fo... | |||
TMPY-01679 |
LCN1 Protein, Human, Recombinant (His)
TLC,MGC71975,TP,VEGP,Lipocalin 1,PMFA |
Human | HEK293 Cells |
Lipocalin-1, also known as Von Ebner gland protein, VEG protein, Tear Prealbumin, VEGP, Tear lipocalin, and LCN1 is a secreted protein that belongs to the calycin superfamily and Lipocalin family. Human Lipocalin-1 / VEGP was originally described as a major protein of human tear fluid, which was thought to be tear specific. Lipocalin-1 / VEGP is identical to lingual von Ebner's gland protein and is also produced in the prostate, nasal mucosa, and tracheal mucosa. Homologous proteins have been fo... |