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Chemical Structure| 1258-84-0 Chemical Structure| 1258-84-0

Structure of Pristimerin
CAS No.: 1258-84-0

Chemical Structure| 1258-84-0

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Pristimerin is a highly efficient reversible inhibitor of monoglyceride lipase (MGL) with an IC50 of 93 nM.

Synonyms: Celastrol methyl ester; NSC 99281; UNII-28ZK7PR57S

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of Pristimerin

CAS No. :1258-84-0
Formula : C30H40O4
M.W : 464.64
SMILES Code : C[C@@]12[C@](C)([C@]3([C@@](C)(CC1)CC[C@](C(OC)=O)(C)C3)[H])CC[C@]4(C)C2=CC=C5C4=CC(=O)C(O)=C5C
Synonyms :
Celastrol methyl ester; NSC 99281; UNII-28ZK7PR57S
English Name :Methyl (2R,4aS,6aS,12bR,14aS,14bR)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxylate
MDL No. :MFCD01711331

Safety of Pristimerin

Related Pathways of Pristimerin

pyroptosis

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HTR-8/SVneo cells 0.25-4 µM 24 hours Inhibited trophoblast cell proliferation Drug Des Devel Ther. 2020 Nov 2;14:4659-4670
KBM5-T315I cells 135 nM (IC50) 72 hours Inhibited growth and induced apoptosis Mol Cancer. 2010 May 19;9:112
HTR-8/SVneo cells 0.5 µM 24 hours Induced trophoblast cell apoptosis Drug Des Devel Ther. 2020 Nov 2;14:4659-4670
HTR-8/SVneo cells 0.5 µM 24 hours Inhibited trophoblast cell migration Drug Des Devel Ther. 2020 Nov 2;14:4659-4670
KBM5 cells 199 nM (IC50) 72 hours Inhibited growth and induced apoptosis Mol Cancer. 2010 May 19;9:112
Panc-1 cells 0.625 to 5 µM 72 hours Inhibited cell proliferation and induced apoptosis Int J Oncol. 2014 May;44(5):1707-15.
Bone marrow-derived macrophages (BMMs) 75 nM 1, 3, 5 days To determine the stage at which Pristimerin inhibits osteoclast formation, results showed that Pristimerin inhibited osteoclast formation at the early stage (1-3 days). Front Pharmacol. 2021 Jan 15;11:621110
Bone marrow-derived macrophages (BMMs) 100 nM 1, 3, 5 days To evaluate the effect of Pri on osteoclast-related gene expression, results showed Pri significantly downregulated the expression of TRAP, CTSK, c-Fos, NFATc1, DC-STAMP, and V-ATPase d2 Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
Bone marrow-derived macrophages (BMMs) 0, 25, 50, 100 nM 10 days To evaluate the effect of Pri on bone resorption function, results showed Pri significantly reduced the bone resorption ability of osteoclasts Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
Rat Brain Astrocytes (RBA-1) 0.1, 0.3, 0.5 µM 12 and 24 hours Pristimerin inhibited LPS-induced MMP-9 expression and cell migration through attenuating NOX/ROS-dependent NF-κB activation. J Inflamm Res. 2020 Jul 20;13:325-341
MDA-MB-231 cells 0.1, 0.2, 0.5, 1 mM 14 days Pristimerin significantly inhibited the colony formation ability of MDA-MB-231 cells. Biomed J. 2021 Dec;44(6 Suppl 1):S84-S92
BV2 cells 10 µM 15 minutes To evaluate the inhibitory effect of Pristimerin on 2-AG hydrolysis. Results showed that 10 μM Pristimerin inhibited [3H]-2-OG hydrolysis by 25%. Br J Pharmacol. 2012 Dec;167(8):1596-608
Mouse chondrocytes 50 nM, 100 nM, 200 nM 24 and 48 hours To assess the effect of Pristimerin on chondrocyte viability, results showed no apparent effect on cell viability at concentrations below 400 nmol Drug Des Devel Ther. 2024 Nov 27;18:5445-5459
Human brain vascular pericytes (HBVPs) 125, 250, 500 nM 24 hours To evaluate the inhibitory effect of Pristimerin on Shh-induced pericyte adhesion and migration Cell Death Dis. 2020 Apr 14;11(4):232
NCI-H446 cells 0.25 µM 24 hours Inhibited cell proliferation, induced G0/G1 arrest and cell apoptosis Int J Mol Med. 2019 Mar;43(3):1382-1394
A549 cells 0.25 µM 24 hours Inhibited cell proliferation, induced G0/G1 arrest and cell apoptosis Int J Mol Med. 2019 Mar;43(3):1382-1394
D-407 cells 30 µM 24 hours D-407 cells showed higher resistance to the cytotoxic effect of Pristimerin, displaying only 20% cytotoxicity upon treatment with 30 µM Pristimerin. J Cell Mol Med. 2020 Jun;24(11):6208-6219
RGC-5 cells 30 µM 24 hours RGC-5 cells showed higher resistance to the cytotoxic effect of Pristimerin, displaying only 20% cytotoxicity upon treatment with 30 µM Pristimerin. J Cell Mol Med. 2020 Jun;24(11):6208-6219
UM-1 cells 1-30 µM 24 hours Pristimerin inhibited UM-1 cell viability in a dose-dependent manner, reaching 80% cell death at 30 µM. Moreover, Pristimerin inhibited the migration and invasion of UM-1 cells, caused a rapid increase of ROS, decreased mitochondrial membrane potential, induced the accumulation of cells in G0/G1 phase, ending with apoptotic cell death. J Cell Mol Med. 2020 Jun;24(11):6208-6219
Human uveal melanoma cells (UM cells) 1 µM 24 hours To assess the effect of PRI on UM cell cycle distribution, results showed that PRI induced G1 phase accumulation and reduced G2 phase accumulation. J Cell Mol Med. 2019 Nov;23(11):7545-7553
Human uveal melanoma cells (UM cells) 0-10 µM 24 hours To evaluate the inhibitory effect of PRI on UM cell proliferation, results showed that PRI inhibited cell proliferation in a dose-dependent manner. J Cell Mol Med. 2019 Nov;23(11):7545-7553
MDA-MB-231 cells 0.1, 0.2, 0.3 mM 24 hours Pristimerin significantly reduced the numbers of invasion and adhesion of MDA-MB-231 cells, and its inhibitory effects were dose-dependent. Biomed J. 2021 Dec;44(6 Suppl 1):S84-S92
Lymph node cells (LNC) 0.1/0.3 µM 24 hours To test the effect of Pristimerin on transcription factors STAT3 and ROR-γt. Results showed Pristimerin reduced the expression of ROR-γt and pSTAT3. Oncol Rep. 2015 Jul;34(1):518-24
GL261 cells 0, 0.25, 0.5, 1, 2 µM 24 hours To evaluate the effect of Pristimerin on GL261 cell viability. Results showed that Pristimerin at 0.25 μM severely inhibited GL261 cell viability. Biosci Rep. 2019 May 14;39(5):BSR20182389
U373 cells 0, 0.25, 0.5, 1, 2 µM 24 hours To evaluate the effect of Pristimerin on U373 cell viability. Results showed that Pristimerin at 0-1 μM did not significantly affect U373 cell viability, but at 2 μM, it remarkably inhibited cell proliferation. Biosci Rep. 2019 May 14;39(5):BSR20182389
Mouse chondrocytes 50 nM, 100 nM, 200 nM 24 hours To assess the effect of Pristimerin on ECM degradation, results showed Pristimerin could concentration-dependently reverse IL-1β-induced ECM degradation Drug Des Devel Ther. 2024 Nov 27;18:5445-5459
Mouse chondrocytes 50 nM, 100 nM, 200 nM 24 hours To assess the effect of Pristimerin on IL-1β-induced inflammatory factor expression, results showed Pristimerin could partially reverse the upregulation of inflammatory factors induced by IL-1β Drug Des Devel Ther. 2024 Nov 27;18:5445-5459
Lymph node cells (LNC) 0.1/0.3 µM 24 hours To test the effect of Pristimerin on transcription factors STAT3 and ROR-γt. Results showed Pristimerin reduced the expression of ROR-γt and pSTAT3. Clin Immunol. 2014 Dec;155(2):220-30
Human umbilical vascular endothelial cells (HUVECs) 0.5 µM, 1 µM, 2 µM 24 hours (proliferation assay), 8 hours (migration assay), 6 hours (tube formation assay) Pristimerin inhibited VEGF-induced HUVECs proliferation, migration, and tube formation in a concentration-dependent manner. 0.5 μM significantly inhibited proliferation, 1 μM significantly inhibited migration, and 0.5 μM significantly inhibited tube formation. Molecules. 2012 Jun 5;17(6):6854-68
Bone marrow-derived macrophages (BMMs) 0, 10, 25, 50, 75 nM 3 days To evaluate the effect of Pristimerin on osteoclast function, results showed that Pristimerin significantly inhibited bone resorption and actin ring formation. Front Pharmacol. 2021 Jan 15;11:621110
Bone-marrow dendritic cells (BMDCs) 0.1-0.4 µM 30 min Inhibited caspase-1 activation and IL-1β secretion Acta Pharmacol Sin. 2021 Jun;42(6):975-986
Mouse peritoneal macrophages 0.1-0.4 µM 30 min Inhibited caspase-1 activation and IL-1β secretion Acta Pharmacol Sin. 2021 Jun;42(6):975-986
Bone-marrow-derived macrophages (BMDMs) 0.1-0.4 µM 30 min Inhibited caspase-1 activation and IL-1β maturation Acta Pharmacol Sin. 2021 Jun;42(6):975-986
Bacillus subtilis 10 µg/mL 30 minutes Evaluation of the antimicrobial activity of Pristimerin against B. subtilis, showing weaker inhibitory effects on DNA and RNA synthesis. Foods. 2021 Mar 11;10(3):591
Human uveal melanoma cells (UM cells) 0.1-3 µM 40 minutes To evaluate the effect of PRI on IGF-1-induced IGF-1R and its downstream signaling pathways, results showed that PRI inhibited the phosphorylation of IGF-1R and its downstream pathways in a dose-dependent manner. J Cell Mol Med. 2019 Nov;23(11):7545-7553
Human microvascular endothelial cell line (HMEC-1) 125, 250, 500 nM 48 hours To evaluate the inhibitory effect of Pristimerin on Shh-induced endothelial cell proliferation Cell Death Dis. 2020 Apr 14;11(4):232
Human umbilical vein endothelial cells (HUVEC) 125, 250, 500 nM 48 hours To evaluate the inhibitory effect of Pristimerin on Shh-induced endothelial cell proliferation Cell Death Dis. 2020 Apr 14;11(4):232
A549 cells 1.91 µM (IC50) 48 hours Evaluate the synergistic inhibitory effects of Pristimerin and paclitaxel on the viability of A549 cells, results showed that Pristimerin significantly enhanced the chemosensitivity of paclitaxel Nano Converg. 2022 Nov 24;9(1):52
MDA-MB-231 cells 0.1, 0.2, 0.5, 1 mM 48 hours Pristimerin significantly inhibited cell proliferation, and its inhibitory effect was dose-dependent. Biomed J. 2021 Dec;44(6 Suppl 1):S84-S92
Bone marrow-derived macrophages (BMMs) 0, 25, 50, 100 nM 48 or 96 hours To evaluate the effect of Pri on BMMs cell viability, results showed no significant effect on cell viability at concentrations below 100 nM Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
Bone marrow-derived macrophages (BMMs) 0, 25, 50, 100 nM 5 days To evaluate the effect of Pri on F-actin ring formation, results showed Pri reduced the size and number of F-actin rings in a dose-dependent manner Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
U937 cells 10 µM 5 minutes To assess the effect of Pristimerin on 2-AG uptake and degradation. Results showed that 10 μM Pristimerin increased intracellular [3H]-2-AG accumulation by 125% and inhibited [3H]-glycerol formation by 25%. Br J Pharmacol. 2012 Dec;167(8):1596-608
Bone marrow macrophages (BMMs) 0.3125, 0.625, 1.25 µM 6 days To evaluate the inhibitory effect of PRI on RANKL-induced osteoclastogenesis. Results showed that PRI dose-dependently inhibited the formation of TRAP-positive multinucleated osteoclasts, with 1.25 μM PRI treatment group predominantly showing TRAP-positive mononuclear cells. Drug Des Devel Ther. 2021 Jan 7;15:61-74
U373 cells 4-16 µM 6 hours To evaluate the effect of Pristimerin on U373 cell apoptosis. Results showed that Pristimerin at 4-16 μM significantly induced cell apoptosis. Biosci Rep. 2019 May 14;39(5):BSR20182389
32D-Bcr-Abl-T315I cells 387 nM (IC50) 72 hours Inhibited growth and induced apoptosis Mol Cancer. 2010 May 19;9:112
32D-Bcr-Abl cells 242 nM (IC50) 72 hours Inhibited growth and induced apoptosis Mol Cancer. 2010 May 19;9:112
K562 cells 450 nM (IC50) 72 hours Inhibited growth and induced apoptosis Mol Cancer. 2010 May 19;9:112
Bone marrow-derived macrophages (BMMs) 0, 5, 10, 25, 50, 75 nM 6-7 days To evaluate the effect of Pristimerin on osteoclast formation, results showed that Pristimerin significantly inhibited RANKL-induced osteoclast differentiation. Front Pharmacol. 2021 Jan 15;11:621110
Bone marrow-derived macrophages (BMMs) 0, 25, 50, 100 nM 7 days To evaluate the effect of Pri on RANKL-induced osteoclast differentiation, results showed Pri reduced the number and size of TRAP-positive multinucleated osteoclasts in a dose-dependent manner Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
MiaPaCa-2 cells 0.625 to 5 µM 72 hours Inhibited cell proliferation and induced apoptosis Int J Oncol. 2014 May;44(5):1707-15.
Bone marrow-derived macrophages (BMMs) 100 nM Different time stages (D0-D2, D2-D4, D4-D6, D0-D6) To evaluate the effect of Pri on osteoclast differentiation at different time stages, results showed Pri significantly inhibited osteoclastogenesis at the mid-stage (D2-D4) Drug Des Devel Ther. 2020 Oct 9;14:4189-4203

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice NCI-H1299 xenograft model Intraperitoneal injection 0.2, 0.4 mg/kg Every two days for a total of 16 days To evaluate the inhibitory effect of Pristimerin on tumor growth and angiogenesis Cell Death Dis. 2020 Apr 14;11(4):232
Male Swiss albino mice Autoimmune hepatitis model Intravenous injection 0.4 and 0.8 mg/kg 5 consecutive days To evaluate the ability of Pris to protect against autoimmune hepatitis (AIH). Results showed that Pris pretreatment significantly ameliorated Con A-induced hepatic damage, reduced serum indices of hepatic damage (ALT, AST, ALP, and LDH), improved liver histopathology, decreased neutrophil infiltration and CD4+T-cell infiltration in hepatic tissue, enhanced antioxidant capacity, inhibited NF-κB activation and inflammatory cytokine release, and reduced hepatocyte apoptosis. Front Pharmacol. 2018 Mar 28;9:292
Nude mice MDA-MB-231 xenograft model Intraperitoneal injection 0.5 mg/kg Daily for 14 days Pristimerin significantly suppressed tumor volume and weight, increased expression of cleaved caspase-3, LC-3 II, and phosphorylation-JNK Cell Death Discov. 2019 Aug 5;5:125
BALB/c mice Subcutaneous xenograft tumor model Intraperitoneal injection 1 mg/kg Every other day for a total of 7 times To investigate the effect of pristimerin on TNBC growth in vivo, results showed that pristimerin effectively hindered the growth of TNBC, with no significant toxic side effects observed. Adv Sci (Weinh). 2025 Mar;12(10):e2413174
C57BL/6 mice Ovariectomized (OVX) osteoporosis model Intraperitoneal injection 1 mg/kg 5 days per week for 8 weeks To evaluate the protective effect of Pristimerin on osteoporosis, results showed that Pristimerin significantly ameliorated ovariectomy-induced bone loss and reduced serum inflammatory factor levels. Front Pharmacol. 2021 Jan 15;11:621110
BALB/C nude mice MDA-MB-231 xenograft model Oral gavage 1 mg/kg Every 2 days for 6 weeks Pristimerin significantly inhibited tumor growth and reversed EMT by downregulating integrin b3 expression. Biomed J. 2021 Dec;44(6 Suppl 1):S84-S92
Lewis rats Adjuvant arthritis (AA) Intraperitoneal injection 1 mg/kg Once daily for 5 days To evaluate the therapeutic effect of Pristimerin on arthritis. Results showed Pristimerin significantly reduced arthritis inflammation and joint damage, decreased pro-inflammatory cytokines (IL-6, IL-17, IL-18, IL-23) expression, and increased immunomodulatory cytokine IL-10 and IFN-γ expression. Oncol Rep. 2015 Jul;34(1):518-24
Lewis rats Adjuvant arthritis (AA) Intraperitoneal injection 1 mg/kg Once daily for 5 days To evaluate the therapeutic effect of Pristimerin on arthritis. Results showed Pristimerin significantly reduced arthritis inflammation and joint damage, decreased pro-inflammatory cytokines (IL-6, IL-17, IL-18, IL-23) expression, and increased immunomodulatory cytokine IL-10 and IFN-γ expression. Clin Immunol. 2014 Dec;155(2):220-30
Nude mice KBM5-T315I xenograft model Intratumoral injection 1.0 mg/kg Daily for 14 days Inhibited tumor growth Mol Cancer. 2010 May 19;9:112
C57BL/6 mice Ovariectomy (OVX) model Intragastric administration 10 mg/kg Every 2 days for 2 months To evaluate the protective effect of Pri on OVX-induced bone loss, results showed Pri significantly prevented OVX-induced reduction in bone mass and trabecular structure damage Drug Des Devel Ther. 2020 Oct 9;14:4189-4203
Mice Destabilization of the medial meniscus (DMM) model Intra-articular injection 200 nmol Once a week for four consecutive weeks To assess the effect of Pristimerin on OA progression in vivo, results showed Pristimerin could reduce cartilage degradation and slow OA progression Drug Des Devel Ther. 2024 Nov 27;18:5445-5459
BALB/c nude mice Human breast cancer xenograft model Subcutaneous injection 3 mg/kg Every other day for 16 days Pristimerin significantly reduced both tumor volume and tumor weight, and decreased angiogenesis in a xenograft mouse tumor model in vivo. The mean number of blood vessels in the treated group was significantly lower than in the control group. Molecules. 2012 Jun 5;17(6):6854-68
C57BL/6 mice Ovariectomy (OVX)-induced osteoporosis model Intraperitoneal injection 5 mg/kg Once every two days for 6 weeks To evaluate the protective effect of PRI against OVX-mediated bone loss. Results showed that PRI treatment significantly improved bone parameters such as bone volume (BV/TV), trabecular number (Tb.N), bone mineral density (BMD), and reduced the number of TRAP-positive osteoclasts. Drug Des Devel Ther. 2021 Jan 7;15:61-74
C57BL/6J mice LPS-induced systemic inflammation model Intraperitoneal injection 500 μg/kg Single injection Significantly reduced serum IL-1β and IL-18 levels Acta Pharmacol Sin. 2021 Jun;42(6):975-986
C57BL/6 mice Pregnancy model Intraperitoneal injection 5μg/30g Single dose, until day 13.5 Induced fetal resorption and placental hemorrhage Drug Des Devel Ther. 2020 Nov 2;14:4659-4670

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.52mL

4.30mL

2.15mL

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