10
1
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2399 |
Bortezomib
Radiciol,NSC 681239,硼替佐米,MG 341,DPBA,Brotezamide,LDP 341 |
Apoptosis; NF-κB; Proteasome; Autophagy | Apoptosis; Autophagy; NF-κB; Proteases/Proteasome; Ubiquitination |
Bortezomib (LDP 341) 是一种 20S 蛋白酶体抑制剂 (Ki=0.6 nM),具有可逆性和选择性。Bortezomib 具有抗肿瘤活性,可以抑制 NF-κB,可破坏细胞周期、诱导细胞凋亡。 | |||
T10061 |
(1S,2S)-Bortezomib
Bortezomib,硼替佐米(1S,2S) |
Proteasome | Proteases/Proteasome; Ubiquitination |
(1S,2S)-Bortezomib (Bortezomib) 是 Bortezomib 的对映异构体。 Bortezomib 是一种可逆的选择性蛋白酶体抑制剂,对 20S 蛋白酶体的 Ki 为 0.6 nM。 | |||
T7854 |
Bortezomib-pinanediol
|
Proteasome | Proteases/Proteasome; Ubiquitination |
Bortezomib-pinanediol 是一种蛋白酶体抑制剂。是硼替佐米的前药。 | |||
T3971 |
CASIN
Pirl1-related Compound 2 |
CDK; STAT; Ras | Cell Cycle/Checkpoint; GPCR/G Protein; JAK/STAT signaling; MAPK; Stem Cells |
CASIN (Pirl1-related Compound 2) 是选择性GTPase Cdc42抑制剂,IC50值是 2 uM。 | |||
T24130 |
HCI-2184
HCI2184,HCI 2184 |
||
HCI-2184 is an inhibitor of AXL kinase and Nek2 that acts by successfully mitigating drug resistance in bortezomib-resistant multiple myeloma. | |||
T69983 |
Ixazomib citrate EtOH
|
||
Ixazomib citrate, also known as MLN9708, is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. MLN9708, after hydrolyzing to pharmacologically active MLN2238 (ixazomib), is a next-generation proteasome inhibitor with demonstrated preclinical and clinical antimyeloma activity. MLN9708, compared with bortezomib, has improved pharmacokinetics, pharmacodynamics, and antitumor activity in preclinic... | |||
T37581 | SCIO 469 hydrochloride | ||
Selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38α in vitro). Displays approximately 10-fold selectivity for p38α over p38β and 2000-fold selectivity for p38α over 20 other kinases. Reduces p38α phosphorylation in multiple myeloma cells in vitro and in vivo; activity results in decreased tumor burden and angiogenesis in murine models of multiple myeloma. Also enhances bortezomib-induced cytotoxicity against multiple myeloma cells. Hideshima et al (2004) p38 MAPK inhibition enhances P... | |||
T37068 |
NR-160
|
||
NR-160 is an inhibitor of histone deacetylase 6 (HDAC6; IC50= 0.03 μM).1It is selective for HDAC6 over HDAC1, -2, -3, -4, and -8 (IC50s = 5.18, 2.26, 8.48, 55.4, and 14.7 μM, respectively). NR-160 is cytotoxic against a panel of seven cancer cell lines (IC50s = 22.5-51.8 μM). It enhances cytotoxicity induced by bortezomib in HL-60 cells, as well as cytotoxicity induced by epirubicin or daunorubicin in CCRF-HSB-2 T cell acute lymphoblastic leukemia cells. | |||
T69288 |
CEP-7055
|
||
CEP-18770 is an orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cel... | |||
T68306 |
INCB16562
|
||
INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced phosphorylation of STAT3. INCB16562 abrogated the protective effects of recombinant cytokines or bone marrow stromal cells and sensitized myeloma cells to cell death by exposure to dexamethasone, melphalan, or bortezomib. Oral administration of INCB16562 antagonized the growth of ... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TCS2170 |
2,5-Dihydroxyacetophenone
Quinacetophenone,2-Acetylhydroquinone,2-5-dihydroxyacetophenone,2 ',5'-二羟基苯乙酮,Acetylhydroquinone,2,5-二羟基苯乙酮,DHAP |
ERK; NF-κB; Tyrosinase | MAPK; NF-κB; Proteases/Proteasome |
2,5-Dihydroxyacetophenone (Quinacetophenone) 是从熟地黄中分离出的一种天然产物,通过阻断 ERK1/2和 NF-κB 信号通路,抑制活化巨噬细胞中炎症介质的产生。 |