32
5
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1803 |
GNF-5
GNF 5 |
SARS-CoV; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Microbiology/Virology; Tyrosine Kinase/Adaptors |
GNF-5是 Bcr-Abl 的特异性非 ATP 竞争性抑制剂,IC50为0.22uM。它是 GNF-2 的类似物,具有改进的药代动力学特性。 | |||
T64338 |
AKI603
AKI 603,AKI-603 |
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
AKI603 是一种极光激酶 A 抑制剂,IC50值为 12.3 nM。它对白血病细胞具有很强的抗增殖活性,可用于克服白血病中 BCR-ABL-T315I 耐药性突变。 | |||
T3196 |
GNF-7
GNF7 |
Bcr-Abl; ACK; AChR | Angiogenesis; Cytoskeletal Signaling; Neuroscience; Tyrosine Kinase/Adaptors |
GNF-7 是一种多重激酶抑制剂。它对ACK1和GCK 具有抑制活性,IC50分别为 25 nM 和 8 nM。它是一种 Bcr-Abl 的抑制剂,对 Bcr-AblWT 和 Bcr-AblT315I 作用的IC50值分别为 133 nM 和 61 nM。它可用于研究血液恶性肿瘤。 | |||
T1448 |
Dasatinib
BMS-354825,达沙替尼 |
Apoptosis; Bcr-Abl; Src; c-Kit; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Dasatinib (BMS-354825) 是一种酪氨酸激酶抑制剂,抑制 Src 和 Bcr-Abl (Ki=16/30 pM),具有口服活性和 ATP 竞争性。Dasatinib 具有抗肿瘤活性,用于治疗白血病和淋巴瘤等。 | |||
T22553 |
Adaphostin
1-Adamantyl 4-((2,5-Dihydroxybenzyl)Amino)Benzoate,NSC 680410 |
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Adaphostin (NSC-680410) 是 AG957 金刚烷酯,是一种 p210bcr/abl 抑制剂,可诱导 T 淋巴细胞白血病细胞系凋亡。它增加了 CLL B 细胞内活性氧的水平,对慢性和急性髓系白血病细胞具有显著的选择性活性。 | |||
T16545 |
Pivanex
Pivalyloxymethyl butyrate,AN-9 |
Apoptosis; HDAC; Bcr-Abl | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; Tyrosine Kinase/Adaptors |
Pivanex (Pivalyloxymethyl butyrate) 是丁酸的一种衍生物,是具有口服活性的 HDAC 抑制剂。Pivanex 通过下调 bcr-abl 蛋白增强凋亡。Pivanex 显示出抗转移和抗血管生成的活性。 | |||
T1448L |
Dasatinib monohydrate
达沙替尼,BMS-354825 Monohydrate |
Apoptosis; Bcr-Abl; Src; c-Kit; Ephrin Receptor; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Dasatinib monohydrate (BMS-354825 Monohydrate) 是一种具有口服活性的,ATP 竞争性的双重Src/Bcr-Abl 抑制剂,有抗肿瘤活性,还诱导凋亡和自噬。它抑制Src 和Bcr-Abl 的IC50分别为 0.5 nM 和 <1.0 nM,Ki 值分别为 16 pM 和 30 pM。 | |||
T36493 |
CMLD-2
|
Apoptosis; HuR | Apoptosis; Chromatin/Epigenetic |
CMLD-2是一种 HuR-ARE 相互作用的抑制剂(Ki:350 nM),能竞争性地结合 HuR 蛋白并破坏其与富含腺嘌呤元素(ARE)的 mRNA 目标的相互作用。CMLD-2诱导细胞凋亡并通过 MAD2下调表现出抗肿瘤作用。CMLD-2 (1-75 μM ; 24-72 h) 对甲状腺癌细胞的活力具有抑制作用.CMLD-2 (20-30 μM ; 24-48 h) 激活 Caspases 并诱导H1299和A549细胞凋亡.CMLD-2 (30 μM ; 24-48 h) 诱导H1299和A549细胞的G1细胞周期停止和线粒体扰动。 CMLD-2(30μM;24-48小时)减少H1299细胞中HuR 和HuR 调节的mRNAs 和蛋白质的表达.CMLD-2(35μM;72小时)降低SW1736、8505C、BCPAP 和K1细胞的定向迁移能力。CMLD-2诱导SW1736、8505C、BCPAP 和K1细胞中的MAD2 mRNA 水平强烈下降。 | |||
T10848 | CMLD012073 | Others | Others |
CMLD012073 is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. It inhibits NIH/3T3 cells (IC50: 10 nM). CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A). | |||
T10847 |
CMLD012072
|
Others | Others |
CMLD012072 is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor with potent anti-neoplastic activity. It can induce RNA clamping of eIF4A1 and eIF4A2. | |||
T10846 |
CMLD010509
SDS-1-021 |
Others | Others |
CMLD010509 (SDS-1-021) is a highly selective inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MDM2, CCND1, MYC, MAF, and MCL-1. | |||
T10849 |
CMLD012612
|
Others | Others |
CMLD012612 is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. It inhibits cell translation and is cytotoxic to NIH/3T3 cells (IC50: 2 nM). | |||
T26625 |
AN-019
NRC-AN-019,NRC-019 |
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
AN-019 (NRC-019) 是一种 Bcr-Abl 激酶抑制剂, 具有抗肿瘤活性,可用于研究慢性粒细胞白血病(CML)和乳腺癌。 | |||
T72958 |
BCR-ABL-IN-7
|
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
BCR-ABL-IN-7 是一种 WT 和 T315I 突变体 ABL 激酶抑制剂。BCR-ABL-IN-7 有效抑制 WT 和 T315I 突变体 ABL 激酶的活性。BCR-ABL-IN-7 可以用于慢性髓系白血病 (CML) 的研究。 | |||
T34656 |
SKLB 1028
Ruserontinib |
EGFR; FLT; Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
SKLB 1028 (Ruserontinib) 是口服活性的、新型的EGFR、FLT3和Abl 多激酶抑制剂。SKLB 1028 在FLT3驱动的AML 模型中显示出优异的活性,在含有Abl 突变体的CML 模型中显示了相当大的效力 | |||
T2328 |
Radotinib
IY-5511,Supect,雷度替尼 |
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Radotinib (IY-5511) 有时被称为 IY5511,是一种用于治疗不同类型 Y 的药物,最显着的是费城染色体阳性 (Ph+) 慢性粒细胞白血病 (CML) 对其他酪氨酸激酶 Bcr-Abl 的耐药性或不耐受性抑制剂 | |||
T8882 |
Vodobatinib
K-0706 |
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Vodobatinib (K-0706) 是第三代具有口服活性的Bcr-Abl1酪氨酸激酶抑制剂,IC50=7 nM,对大多数 BCR-ABL1 点突变体具有活性,但对 BCR-ABL1T315I 无活性。它可用于研究慢性粒细胞白血病 (CML)。 | |||
T10799 |
CHMFL-ABL-039
|
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
CHMFL-ABL-039 是一种具有高效选择性的 Ⅱ 型野生型 ABL 激酶和耐药 V299L 突变型 BCR-ABL 激酶的抑制剂,IC50 分别为 7.9 nM、27.9 nM。CHMFL-ABL-039 可用于慢性粒细胞白血病 (CML) 的研究。 | |||
T10897 |
CT-721
|
Others | Others |
CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM against wild-type Bcr-Abl kinase and has anti-chronic myeloid leukemia (CML) activity. | |||
T77969 |
SIAIS100 TFA
|
Bcr-Abl | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
SIAIS100 TFA是一款高效的BCR-ABL PROTAC降解剂,其DC50值为2.7 nM,主要应用于慢性粒细胞白血病(CML)的研究。 | |||
T62496 | IST5-002 | ||
IST5-002 是一种 Stat5a/b 的有效抑制剂,能够选择性地抑制 Stat5a/b 的转录活性,对 Stat5a 和 Stat5b 的 IC50 值分别为 1.5 μM 和 3.5 μM。IST5-002 能够诱导前列腺癌细胞和慢性粒细胞白血病 (CML) 细胞凋亡 (apoptotic) 及死亡。IST5-002 能够用于研究前列腺癌和慢性粒细胞白血病 (CML)。 | |||
T10567 | BMS-214662 | Raf | MAPK |
BMS-214662是一种有效的、有选择性的 farnesyl transferase 抑制剂,可诱导原始CD34+慢性髓性白血病(CML)干细胞/祖细胞的线粒体凋亡,具有选择性靶向CML 干细胞/祖细胞的能力,具有抗肿瘤活性。 | |||
T78608 | Anticancer agent 164 | Apoptosis | Apoptosis |
CML-IN-1(compound 7)是一种高效抗癌药物,针对人类慢性粒细胞白血病(CML)细胞系K562,能有效诱导凋亡(apoptosis)。该化合物主要通过显著抑制PI3K/Akt信号通路的蛋白磷酸化来发挥作用,同时CML-IN-1(compound 4)也能通过抑制结直肠癌的MEK/ERK信号通路来阻止细胞增殖。 | |||
T71581 |
SGX393
|
||
SGX393 is an inhibitor of the CML mutant Bcr-AblT315I, thereby preempting in vitro resistance when combined with nilotinib or dasatinib. | |||
T75012 | SIAIS100 | ||
SIAIS100 是一种有效的BCR-ABLPROTAC 降解剂,DC50为 2.7 nM。SIAIS100 可用于研究慢性粒细胞白血病 (CML)。 | |||
T22067 |
CHMFL-ABL-053
|
||
CHMFL-ABL-053 (Compound 18a) 是一种有效的、选择性的、具有口服活性的 BCR-ABL、SRC 和 p38激酶抑制剂,IC50值分别为 70、90 和 62 nM。CHMFL-ABL-053 是一种潜在有效的慢性粒细胞白血病 (CML) 候选药物 [1]。 | |||
T22859 | Imatinib hydrochloride | Others | Others |
Imatinib is a multi-target inhibitor of v-Abl, c-Kit, and PDGFR (IC50: 0.6 μM, 0.1 μM, and 0.1 μM, respectively). Imatinib is used to treat chronic myelogenous leukemia (CML), gastrointestinal stromal tumors (GISTs), and a number of other malignancies. | |||
T71313 |
BVB-808
|
||
BVB-808 is a selective Jak2 type 1 inhibitor. Janus kinases are critical components of signaling pathways that regulate hematopoiesis. Mutations of the non-receptor tyrosine kinase JAK2 are found in many BCR-ABL-negative myeloproliferative neoplasms. Preclinical results support that JAK2 inhibitors could show efficacy in treating chronic myeloproliferative neoplasms. JAK2 has also been postulated to play a role in BCR-ABL signal transduction. Therefore, inhibitors of JAK2 kinases are turning int... | |||
T40594 |
iHCK-37
iHCK-37,ASN05260065 |
||
iHCK-37 (ASN05260065) is a high-potency, selective inhibitor of Hck with a Ki value of 0.22 μM. It effectively inhibits HIV-1 viral replication, exhibiting an EC50 value of 12.9 μM. Primarily employed in chronic myeloid leukemia (CML) research, iHCK-37 demonstrates promising potential for studying and understanding this disease. | |||
T68581 |
AP23464
|
||
AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba/F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the lo... | |||
T74644 |
DB0614
|
||
DB1113 (Example 24) 是一种靶向蛋白激酶降解的双功能化合物。DB1113 可降解ABL1,ABL2,BLK,CDK11B,CDK4,CSK,EPHA3,FER,GAK,LIMK1,MAP3K20,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK3,NLK,PDIK1L,PTK2B,RIPK1,RPS6KA1,RPS6KA3,SIK2,SIK3,STK35,TNK2 和ULK1。DB1113 可用于研究异常激酶活性介导的疾病或紊乱。 | |||
T71227 | LGB-321 HCl | ||
LGB-321 is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor). LGB321 is unique relative to previously described PIM inhibitors, in that it is active in PIM2 dependent cell lines. , a kinase that has proven difficult to inhibit in the cellular context. Consistent with its activity on all three PIM kinases, LGB321 inhibits proliferation of a number of cell lines derived from diverse hematological malignancies, including MM, AML, CML and B-Cel... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3398 |
Icaritin
Anhydroicaritin,去水淫羊藿黄素,Cycloicaritin |
Apoptosis; JAK; STAT; Autophagy | Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
Icaritin (Anhydroicaritin) 是Epimedium Genusis 的异戊二烯类黄酮衍生物,有效抑制 K562 细胞和原代 CML 细胞的增殖。它可以调节MAPK/ERK/JNK 和JAK2/STAT3/AKT 信号传导,并具有增强成骨的作用。 | |||
TN3972 |
Epimedokoreanin B
|
Apoptosis; Others; Antibacterial | Apoptosis; Microbiology/Virology; Others |
Epimedokoreanin B (EKB) 是一种从韩国淫羊藿中分离出的异戊烯化类黄酮,在人非小细胞肺癌(NSCLC)A549和NCI-H292细胞中展现出抗癌活性。Epimedokoreanin B 还具有抗炎和抗菌活性,可有清除 DPPH 自由基的活性,能以剂量依赖的方式抑制 MCF-7 和 HepG2 的增殖。Epimedokoreanin B 能显著抑制 N (δ) -(羧甲基)赖氨酸(CML)和 N (Ï) -(羧甲基)精氨酸(CMA)的形成,可通过抑制高级糖化终产物(AGEs)预防糖尿病的临床并发症。 | |||
T3S1553 |
trans-Cinnamaldehyde
Cinnamaldehyde,Cinnamic aldehyde,桂皮醛,反式肉桂醛,Cinnamal,Phenylacrolein |
COX; Endogenous Metabolite | Immunology/Inflammation; Metabolism; Neuroscience |
trans-Cinnamaldehyde (Phenylacrolein) 是一种能够用于合成反式肉桂醛-β-环糊精复合物,一种能够食用的抗菌涂层,能够延长鲜切水果的保质期。它是一种能够通过烷基异氰化物与乙炔二羧酸二烷基酯的反应来合成高度多官能的呋喃环。 | |||
T6S1315 |
Oroxylin A
千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether |
Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy | Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology |
Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮,具有较强的抗癌作用。 | |||
TN2646 |
16-Hydroxycleroda-3,13-dien-15,16-olide
|
Autophagy | Autophagy |
16-Hydroxycleroda-3,13-dien-15,16-olide, and prodigiosin are presented as candidates for autophagy inducers that can trigger cell death in a supplement or alternative medicine for cancer therapy. 16-Hydroxycleroda-3,13-dien-15,16-olide regulates the expre |