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.


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RGT-068A

RGT-068A is a potent, selective and oral bioavailable MALT1 inhibitor[1].

  • CAS Number: 2577171-33-4
  • MF: C17H16ClN9O2
  • MW: 413.82
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JNJ-67856633

JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. JNJ-67856633 in some cases lead to tumor stasis[1][2][3].

  • CAS Number: 2230273-76-2
  • MF: C20H11F6N5O2
  • MW: 467.32
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-Val-Arg-Pro-DL-Arg-fluoromethylketone trifluoroacetate salt

Val-Arg-Pro-DL-Arg-Fluoromethylketone is a potent MALT1 inhibitor. Val-Arg-Pro-DL-Arg-Fluoromethylketone inhibits cell proliferation and migration. Val-Arg-Pro-DL-Arg-Fluoromethylketone shows anticancer activity[1].

  • CAS Number: 1926163-57-6
  • MF: C31H49FN10O6
  • MW: 676.78
  • Catalog: MALT1
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MI 2

MI 2 (MALT1 inhibitor) is an irreversible MALT1 protease inhibitor with an IC50 of 5.84 μM.

  • CAS Number: 1047953-91-2
  • MF: C19H17Cl3N4O3
  • MW: 455.72200
  • Catalog: MALT1
  • Density: 1.44±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mepazine hydrochloride

Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride affects viability of ABC-DLBCL cells by enhancing apoptosis[1].

  • CAS Number: 2975-36-2
  • MF: C19H23ClN2S
  • MW: 346.91700
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: 444.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 222.6ºC

MALT1-IN-7

MALT1-IN-7 (compound 142b) is a potent MALT1 protease inhibitor. MALT1-IN-7 has the potential for cancer research[1].

  • CAS Number: 2178993-11-6
  • MF: C19H17F3N8O2S
  • MW: 478.45
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(R)-MALT1-IN-7

(R)-MALT1-IN-7 (compound 142a) is a potent MALT1 protease inhibitor. (R)-MALT1-IN-7 has the potential for cancer research[1].

  • CAS Number: 2178993-10-5
  • MF: C19H17F3N8O2S
  • MW: 478.45
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-VRPR-FMK(Z-Val-Arg-Pro-DL-Arg-FMK

Z-VRPR-FMK is an irreversible MALT1 protein inhibitor. Z-VRPR-FMK inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression[1].

  • CAS Number: 1381885-28-4
  • MF: C84H140N14O18S
  • MW: 1666.158
  • Catalog: MALT1
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 1659.8±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 957.6±34.3 °C

(R)-MALT1-IN-3

(R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM. (R)-MALT1-IN-3 has IC50 of 60 nM, 40 nM for human IL6/IL10 in OCI-LY3 cells, respectively[1].

  • CAS Number: 2504229-61-0
  • MF: C21H19F3N8O2
  • MW: 472.42
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MALT1-IN-3

MALT1-IN-3 (compound 122) is a potent MALT1 protease inhibitor, with an IC50 of 0.06 μM. MALT1-IN-3 has IC50 of 0.14 and 0.13 μM for human IL6/IL10 in OCI-LY3 cells, respectively[1].

  • CAS Number: 2504229-63-2
  • MF: C21H19F3N8O2
  • MW: 472.42
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MALT1-IN-9

MALT1-IN-9 is a potent MALT1 protease inhibitor with a IC50 of <500 nM in Raji MALT1-GloSensor cells. MALT1-IN-9 has anticancer effects (WO2021000855A1; Compound 5)[1].

  • CAS Number: 2577170-77-3
  • MF: C16H12ClF3N6O
  • MW: 396.75
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MLT-748

MLT-748 is an allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM. MLT-748 also reversibly binds to human mutant MALT1(329-728)-W580S (Kd, 13 nM) with affinity similar to that of the wild type MALT1(329-728) (Kd, 42 nM)[1].

  • CAS Number: 1832578-30-9
  • MF: C19H19Cl2N9O3
  • MW: 492.32
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(S)-MALT1-IN-5

(S)-MALT1-IN-5 is a potent inhibitor of MALT1 protease. (S)-MALT1-IN-5 inhibits the activity of MALT1 is expected to be able to correct the enhancement of MALT1 activity due to abnormality of T cell receptor signal or B cell receptor signal, and cancer or inflammatory disease caused by MALT1 activity is expected. (S)-MALT1-IN-5 has the potential for the research of MALT1-related diseases (extracted from patent WO2020111087A1, compound 1)[1].

  • CAS Number: 2434602-25-0
  • MF: C17H17ClF2N6O3
  • MW: 426.81
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MALT1-IN-6

MALT1-IN-6 is a potent MALT1 protease inhibitor with a Ki of 9 nM. MALT1-IN-6 has anticancer effects (WO2018226150A1; Compound 4)[1].

  • CAS Number: 2254669-07-1
  • MF: C18H12Cl2F3N9O
  • MW: 498.25
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(R)-MLT-985

(R)-MLT-985 (compound 11) is a potent MALT1 protease inhibitor with an IC50 of 3 nM. (R)-MLT-985 has an IC50 of 20 nM for MALT1-dependent IL-2 production in Jurkat cells. (R)-MLT-985 suppresses growth and aberrant CARD11/BCL10/MALT1 complex signaling in ABC-DLBCL cells[1].

  • CAS Number: 1832577-07-7
  • MF: C17H15Cl2N9O2
  • MW: 448.27
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MLT-985

MLT-985 is a highly selective allosteric MALT1 inhibitor with an IC50 value of 3 nM.

  • CAS Number: 1832576-25-6
  • MF: C17H15Cl2N9O2
  • MW: 448.27
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MLT-747

MLT-748 is a allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM. MLT-748 also reversibly binds to human mutant MALT1(329-728)-W580S (Kd, 13 nM) with affinity similar to that of the wild type MALT1(329-728) (Kd, 42 nM)[1].

  • CAS Number: 2097853-86-4
  • MF: C20H21Cl2N7O3
  • MW: 478.33
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MALT1-IN-5

MALT1-IN-5 (compound 1) is a potent MALT1 protease inhibitor. MALT1-IN-5 can be used for cancer research[1].

  • CAS Number: 2434602-73-8
  • MF: C17H17ClF2N6O3
  • MW: 426.81
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MALT1-IN-8

MALT1-IN-8 is a potent MALT1 protease inhibitor with a IC50 of 2 nM. MALT1-IN-8 inhibits the growth of OCI-LY3 lymphoma cells with an IC50 of 1.16 μM. MALT1-IN-8 has anticancer effects (WO2018165385A1; Compound 8)[1].

  • CAS Number: 2244109-29-1
  • MF: C20H15Cl2N7O
  • MW: 440.29
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MALT1-IN-11

MALT1-IN-11 (Example 151 in reference Patent) is a MALT1 protease inhibitor (IC50 < 10 nM). MALT1-IN-11 inhibits IL10 secretion with an IC50 of 10-100 nM. MALT1-IN-11 can be used for the research of cancer, autoimmune and inflammatory disorders[1].

  • CAS Number: 2812352-99-9
  • MF: C20H16F4N8O
  • MW: 460.39
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mepazine

Mepazine (Pecazine) is a potent and selective MALT1 inhibitor. Mepazine inhibits GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 and 0.42 μM, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis[1].

  • CAS Number: 60-89-9
  • MF: C19H22N2S
  • MW: 310.45600
  • Catalog: Apoptosis
  • Density: 1.159 g/cm3
  • Boiling Point: 444.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 222.6ºC