Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T13627 |
CP-10
|
CDK | Cell Cycle/Checkpoint |
CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpressed CDK6. | |||
T4014 |
CP-724714
CP724714,CP 724714 |
Apoptosis; EGFR | Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
CP-724714 (CP724714) 是一种高效、选择性口服活性的 ErbB2 (HER2)酪氨酸激酶抑制剂,IC50为 10 nM。它能抑制完整细胞中 ErbB2 受体的自磷酸化,具有抗肿瘤活性。它对 EGFR 激酶有明显的选择性,IC50值为6400 nM。 | |||
T6091 |
CP-673451
|
VEGFR; PDGFR; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
CP673451 是选择性的血小板源生长因子受体 (PDGFR) 抑制剂,能够抑制 PDGFRα (IC50:10 nM) 和 PDGFRβ (IC50:1 nM) 的活性。 | |||
T6455 |
CP-91149
|
Phosphorylase | Metabolism |
CP91149 是GP (糖原磷酸化酶)的抑制剂,能够促进糖原的重新合成,但不会造成糖原的过度积累。它对2型糖尿病具有潜在的研究价值。 | |||
T8425 |
Linoleoyl Ethanolamide
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
Linoleoyl ethanolamide 是脂肪酸乙醇酰胺。它可弱结合 CB1 和 CB2 受体,并分别抑制[3H]CP-55,940的结合,Ki 分别为 10 和 25μM。它在引起小鼠过氧化氢酶方面的效力是 anandamide 的4倍,且对睡眠时间无延长效果。 | |||
T18515 |
Palbociclib-propargyl
PROTAC CDK6 ligand 1 |
Others | Others |
Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1]. | |||
T17904 |
Pomalidomide-PEG1-C2-N3
E3 ligase Ligand-Linker Conjugates 50,Cereblon Ligand-Linker Conjugates 13 |
Others | Others |
Pomalidomide-PEG1-C2-N3 is a compound that has been synthesized as a conjugate of an E3 ligase ligand-linker. This compound incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, which are commonly used in PROTAC technology. Utilizing Pomalidomide-PEG1-C2-N3, it is possible to design a selective CDK6 PROTAC degrader known as CP-10. CP-10 effectively induces the degradation of CDK6, displaying a DC50 value of 2.1 nM[1]. | |||
T70049 |
Ro 04-5595 free base
|
||
Ro 04-5595 is a selective antagonist of NMDA receptors NR2B subunits. Ro 04-5595 had an EC 50 of 186 ± 32 nmol/L. Ro 04-5595 was predicted to bind the EVT-101 binding site, not the ifenprodil-binding site. Specific binding, defined with a new NR2B-specific antagonist Ro 04-5595 at 10 microM was fully inhibited by several compounds with the following rank order of affinities--Ro 25-6981 > CP-101,606 > Ro 04-5595 = ifenprodil >> eliprodil > haloperidol > spermine > spermidine > MgCl2 > CaCl2--and... |