MALT1(黏膜相关淋巴瘤转运蛋白1)
MALT1 is a paracaspase, which is related to the caspase (cysteine-aspartic proteases) family of proteases but cleaves after Arg residues instead of Asp. MALT1 cleavage activity is linked to the pathogenesis of activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL), a chemoresistant form of DLBCL. MALT1 is a unique paracaspase protein that transduces aberrant oncogenic signaling in ABC-DLBCL. MALT1 represents a potentially important therapeutic target for ABC-DLBCL and MALT lymphoma. MALT1 small molecule inhibitors might be useful chemical tools for studying MALT1 biology and treating MALT1-addicted tumors.
Products for MALT1
- Cat.No. 产品名称 Information
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GC68218
Mepazine
甲哌啶嗪; Pecazine
Mepazine (Pecazine) 是一种有效的选择性 MALT1 蛋白酶抑制剂。Mepazine 抑制全长 GSTMALT1 和 GSTMALT1 325-760 段的 IC50 分别为 0.83 和 0.42 μM。Mepazine 通过增强细胞凋亡 (Apoptosis) 来影响 ABC-DLBCL 细胞的生存能力。 - GC67992 MLT-747 MLT-747 是一种有效、选择性的 MALT1 的别构抑制剂,与 MALT1 的别构 Trp580 口袋结合,IC50 值为 14 nM。
- GC65505 MLT-985 MLT-985 是一种高度选择性的 MALT1 变构抑制剂,IC50 值为 3 nM。
- GC65301 MLT-748 MLT-748 is a potent, selective and allosteric inhibitor of MALT1 with IC50 of 5 nM, binding at the interface between the caspase and immunoglobulin (Ig3) domains by displacing Trp580 and locking the catalytic site in an inactive state.
- GC62611 MLT-231 MLT-231 是一种高效、高选择性的变构 MALT1 抑制剂,IC50 为 9 nM。MLT-231 特异性地阻止内源性 BCL10 断裂,IC50 为 160 nM。MLT-23 在 ABC-DLBCL 型异种移植模型中具有抗肿瘤活性。
- GC62464 MLT-943 MLT-943 是一种有效的、选择性的、口服活性的 MALT1 protease 抑制剂。MLT-943 可抑制 PBMC 或全血中 IL-2 的分泌,PBMC 中抑制的 IC50 值为 0.07~0.09 μM,全血中抑制的 IC50 值为 0.6~0.8 μM)。MLT-943具有抗炎活性,可用于 FcgR 介导的炎症研究。
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GC62115
JNJ-67856633
JNJ-67856633
JNJ-67856633 (JNJ-6633) is a potent, selective, allosteric inhibitor of MALT1 protease. -
GC61041
Mepazine hydrochloride
哌卡嗪盐酸盐,Pecazine hydrochloride
Mepazinehydrochloride(Pecazinehydrochloride)是一种有效的选择性MALT1蛋白酶抑制剂。Mepazinehydrochloride抑制全长GSTMALT1和GSTMALT1325-760段的IC50分别为0.83和0.42μM。Mepazinehydrochloride通过增强细胞凋亡(apoptosis)来影响ABC-DLBCL细胞的生存能力。 -
GC36534
MALT1 inhibitor MI-2
2-氯-N-[4-[5-(3,4-二氯苯基)-3-(2-甲氧基乙氧基)-1H-1,2,4-三唑-1-基]苯基]乙酰胺
A MALT1 inhibitor -
GC45192
Z-VRPR-FMK (trifluoroacetate salt)
Z-Val-Arg-Pro-DL-Arg-FMK
An irreversible inhibitor of MALT1