主页 /
JAK / Stat

JAK / Stat

Quick View
Gusacitinib

Catalog No. A19883
Quick View

添加到收藏
SYK/JAK inhibitor

Gusacitinib (ASN-002) is a potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. 了解更多

Bulk Inquiry
Quick View
AT9283

Catalog No. A10095
Quick View

添加到收藏
Aurora/JAK 抑制剂

AT9283抑制极光激酶A和B，并靶向与骨髓细胞增殖相关的其他酪氨酸和丝氨酸/苏氨酸激酶。了解更多

Product Citations (1)

Bulk Inquiry Free Sample
- Tomoya Takeda, .et al. AT9283 exhibits antiproliferative effect on tyrosine kinase inhibitor-sensitive and -resistant chronic myeloid leukemia cells by inhibition of Aurora A and Aurora B, Oncol Rep, 2020, August 18
Quick View
AG-490

Catalog No. A10047
Quick View

添加到收藏
EGFR 抑制剂

AG 490是EGF受体酪氨酸激酶的选择性抑制剂 (EGFR和ErbB2的IC50值分别为2和13.5μM)。也抑制对Lck，Lyn，Btk，Syk和Src无活性的JAK2。了解更多

Product Citations (1)

Bulk Inquiry Free Sample
- Matozaki M, .et al. Involvement of Stat3 phosphorylation in mild heat shock-induced thermotolerance, Exp Cell Res, 2019, Feb 15. pii: S0014-4827(18)31030-9 PMID: 30776355
Quick View
Cyt387 (Momelotinib)

Catalog No. A10263
Quick View

添加到收藏
JAK 抑制剂

Cyt387 (Momelotinib)是Janus激酶JAK1和JAK2的抑制剂，可作为ATP竞争者，IC50值分别为11和18 nM。了解更多

Product Citations (1)

Bulk Inquiry Free Sample
- Alex Bainbridge, .et al. IKBKE activity enhances AR levels in advanced prostate cancer via modulation of the Hippo pathway, Nucleic Acids Research, 2020, April
Quick View
Pacritinib (SB1518)

Catalog No. A12694
Quick View

添加到收藏
JAK2/FLT3 抑制剂

Pacritinib (SB1518)是Janus激酶2（JAK2）和JAK2突变体JAK2V617F的口服生物利用抑制剂，无细胞试验中IC50分别为23和22 nM，具有潜在的抗肿瘤活性。Pacritinib与JAK2竞争ATP结合，这可能导致抑制JAK2活化，抑制JAK-STAT信号传导途径以及半胱天冬酶依赖性凋亡。了解更多

Product Citations (1)

Bulk Inquiry Free Sample
- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
Quick View
INCB39110 (Itacitinib)

Catalog No. A14390
Quick View

添加到收藏
JAK1 抑制剂

INCB39110 (Itacitinib)是一种有效的JAK1酪氨酸激酶抑制剂，目前正在II期试验中，用于治疗类风湿关节炎，骨髓纤维化，类风湿关节炎和斑块状牛皮癣。了解更多

Product Citations (1)

Bulk Inquiry
- Czech J, .et al. JAK2V617F but not CALR mutations confer increased molecular responses to interferon-α via JAK1/STAT1 activation, Leukemia, 2018, Nov 23 PMID: 30470838
Quick View
GLPG0634

Catalog No. A13162
Quick View

添加到收藏
JAK1 抑制剂

GLPG0634是一种口服的JAK1(Janus激酶1)选择性抑制剂，对 JAK1/JAK2/JAK3的IC50值为50-200 nM。用于治疗类风湿性关节炎和潜在的其他炎性疾病。了解更多

Product Citations (1)

Bulk Inquiry Free Sample
- Keisuke Nishimura, .et al. Tofacitinib facilitates the expansion of myeloid-derived suppressor cells and ameliorates arthritis in SKG mice., Arthritis Rheumatol., 2015, Apr;67(4):893-902 PMID: 25545152
Quick View
CP-690550 (Tofacitinib citrate)

Catalog No. A10241
Quick View

添加到收藏
JAK3 抑制剂

CP-690550 (Tofacitinib citrate)是口服的高选择性Janus激酶（JAK）酶抑制剂。了解更多

Product Citations (1)

Bulk Inquiry Free Sample
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
Quick View
PF-03394197 (oclacitinib)

Catalog No. A13082
Quick View

添加到收藏
JAK1 抑制剂

PF-03394197 (oclacitinib)是有效的JAK1抑制剂。了解更多

Product Citations (3)

Bulk Inquiry
- Banovic F, .et al. Immunomodulatory in vitro effects of oclacitinib on canine T-cell proliferation and cytokine production, Vet Dermatol, 2018, Nov 12 PMID: 30417482
- Nicholas B, .et al. Susceptibility to influenza virus infection of bronchial biopsies in asthma, J Allergy Clin Immunol, 2017, Jul;140(1):309-312.e4 PMID: 28259448
- Fukuyama T, .et al. Topically Administered Janus-Kinase Inhibitors Tofacitinib and Oclacitinib Display Impressive Antipruritic and Anti-Inflammatory Responses in a Model of Allergic Dermatitis., J Pharmacol Exp Ther., 2015, Sep;354(3):394-405 PMID: 26159873
Quick View
INCB018424 (Ruxolitinib)

Catalog No. A11041
Quick View

添加到收藏
JAK1/2 抑制剂

INCB018424 (Ruxolitinib)是有效和选择性的Janus相关激酶JAK1/2抑制剂，对JAK1，JAK2和JAK3的IC50分别为2.7、4.5和332 nM。了解更多

Product Citations (6)

Bulk Inquiry Free Sample
- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Rasmus Siersbek, .et al. IL6/STAT3 Signaling Hijacks Estrogen Receptor α Enhancers to Drive Breast Cancer Metastasis, Cancer cell, 2020, Jul 6;S1535-6108(20)30311-1 PMID: 32679107
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Kagoya Y, .et al. JAK2V617F+ myeloproliferative neoplasm clones evoke paracrine DNA damage to adjacent normal cells through secretion of lipocalin-2., Blood., 2014, Nov 6;124(19):2996-3006 PMID: 25217696