Rohitukine 

Rohitukine is an orally active CDK9/T1 inhibitor with an IC₅₀ of 0.3 μM. Rohitukine blocks ATP binding sites of CDK2/A and CDK9/T1, suppresses PPARγ, AKT, mTOR, C/EBPα, SREBP-2, and NF-κB signaling, and increases hepatic LXRα expression. Rohitukine induces S-phase cell cycle arrest, ROS generation, apoptosis, and exhibits anti-inflammatory activity. Rohitukine can be used for the research of leukemia, pancreatic cancer, prostate cancer, breast cancer, CNS cancer, ovarian cancer, lung cancer, dyslipidemia, inflammatory diseases, inflammatory bowel disease, and arthritis^[1][2][3][4].

Rohitukine (48 h) exhibits selective cytotoxicity against cancer cells, with the highest potency against HL-60 leukemia (GI₅₀ = 10 μM) and Molt-4 leukemia (GI₅₀ = 12 μM), and minimal cytotoxicity against normal fR2 and HEK-293 cell lines (GI₅₀ > 50 μM)^[1].
Rohitukine (1-10 μM) induces S-phase cell cycle arrest in HL-60 leukemia cells in a concentration-dependent manner^[1].
Rohitukine potently inhibits Cdk9/cyclin T1 (IC₅₀ = 0.3 μM) and weakly inhibits Cdk2/A (IC₅₀ = 7.3 μM) in cell-free biochemical assays^[1].
Rohitukine (50 μM) strongly inhibits Dyrk1A, AMPK, and VEGFR kinases in a cell-free profiling assay^[1].
Rohitukine (5-20 μM; 2-8 days) inhibits lipid accumulation in 3T3-L1 and C3H10T1/2 adipocytes in a concentration- and time-dependent manner^[2].
Rohitukine (20 μM; 48 h-6 days) downregulates pro-adipogenic gene expression (LPL, aP2, SREBP-1c, FAS, PPARγ) and upregulates anti-adipogenic gene expression (Wnt3a, GATA2) in 3T3-L1 adipocytes when treated with 20 μM for 6 days^[2].
Rohitukine (20 μM; 15 min-6 days) downregulates late-phase adipogenic protein expression (PPARγ, C/EBPα, aP2, FAS, GLUT4) and inhibits early AKT/mTOR/4EBP signaling in 3T3-L1 adipocytes^[2].
Rohitukine (1-20 μM; 24 h) arrests 3T3-L1 preadipocytes in S phase during mitotic clonal expansion in a concentration-dependent manner^[2].
Rohitukine (20 μM; 16-24 h) downregulates cell cycle progression proteins (cyclin-D, CDK6, CDK4, cyclin-E, CDK2, C/EBPβ) and stabilizes the CDK inhibitor P27 in 3T3-L1 preadipocytes^[2].
Rohitukine (20 μM; 48 h) significantly inhibits 3T3-L1 preadipocyte proliferation during mitotic clonal expansion^[2].
Rohitukine (3-100 μM; 24 h) exhibits no cytotoxicity toward J774A.1 macrophage cells, with a cytotoxic IC₅₀ >50 μM^[3].
Rohitukine (3-30 μM; 1 h pretreatment, followed by 18 h incubation) dose-dependently inhibits LPS (HY-D1056)-induced nitric oxide production in J774A.1 macrophage cells^[3].
Rohitukine (3-30 μM; 18 h) inhibits LPS-induced reactive oxygen species production in J774A.1 macrophage cells^[3].
Rohitukine (3-30 μM; 1 h pretreatment, followed by 18 h incubation) inhibits LPS-induced production of IL-1β, TNF-α, IL-6, and PGE₂ in J774A.1 macrophage cells^[3].
Rohitukine (3-30 μM; 1 h pretreatment, followed by 18 h incubation) dose-dependently inhibits LPS-induced NF-κB transcriptional activity in J774A.1 macrophage cells^[3].
Rohitukine (10-30 μM; 1 h pretreatment, followed by incubation) inhibits LPS-induced nuclear translocation of NF-κB in J774A.1 macrophage cells at concentrations of 10 and 30 μM^[3].
Rohitukine (10-30 μM; 1 h pretreatment, followed by 2 h incubation) suppresses LPS-induced iNOS and COX-2 protein expression in J774A.1 macrophage cells^[3].
Rohitukine (10-30 μM; 1 h pretreatment, followed by 30 min incubation) inhibits LPS-induced activation of the NF-κB pathway by reducing IκB-α phosphorylation and preserving cytosolic NF-κB p65, and inhibits LPS-induced activation of the MAPK pathway by reducing ERK and JNK phosphorylation in J774A.1 macrophage cells^[3].
Rohitukine (3-30 μM; 48 h) is non-toxic to primary murine peritoneal macrophages up to 50 μM, and dose-dependently inhibits LPS-induced NO production and release of IL-1β, IL-6, and TNF-α^[3].
Rohitukine (0.25-1.0 mM) dose-dependently inhibits growth of five-week-old wild-type Arabidopsis thaliana (Col-0) plants^[4].
Rohitukine (0.25-1.0 mM) dose-dependently induces ROS accumulation and increases antioxidant enzyme activity in five-week-old wild-type Arabidopsis thaliana (Col-0) plants^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rohitukine (50 mg/kg; p.o.; once daily; 7 days) significantly ameliorates high-fat diet-induced dyslipidemia in Syrian golden hamsters, reduces hepatic and gonadal lipid accumulation, and modulates key lipid-regulating genes and proteins^[2].
Rohitukine (12.5-50 mg/kg; p.o.; daily; 5 days) dose-dependently inhibits LPS-induced pro-inflammatory cytokine production in mice^[3].
Rohitukine (12.5-50 mg/kg; p.o.; single dose) dose-dependently reduces Acetic Acid (HY-Y0319)-induced vascular permeability in mice^[3].
Rohitukine (12.5-50 mg/kg; p.o.; single dose) dose-dependently inhibits Carrageenan (HY-125474)-induced paw oedema in rats^[3].
Rohitukine (12.5-50 mg/kg; p.o.; single dose) inhibits Carrageenan-induced pleurisy in mice^[3].
Rohitukine (12.5-50 mg/kg; p.o.; daily; 14 days) dose-dependently reduces Freund's complete adjuvant-induced arthritis in rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

305.33

C₁₆H₁₉NO₅

71294-60-5

O=C1C=C(OC2=C1C(O)=CC(O)=C2[C@@H]3[C@@H](CN(CC3)C)O)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kumar V, et al. A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3457-63.  [Content Brief]

  [2]. Varshney S, et al. Rohitukine inhibits in vitro adipogenesis arresting mitotic clonal expansion and improves dyslipidemia in vivo. J Lipid Res. 2014 Jun;55(6):1019-32.  [Content Brief]

  [3]. Singh A, et al. Rohitukine inhibits NF-κB activation induced by LPS and other inflammatory agents. Int Immunopharmacol. 2019 Apr;69:34-49.  [Content Brief]

  [4]. Ahmed S, et al. Exogenously Applied Rohitukine Inhibits Photosynthetic Processes, Growth and Induces Antioxidant Defense System in Arabidopsis thaliana. Antioxidants (Basel). 2022 Aug 3;11(8):1512.  [Content Brief]

  [5]. Kumara PM, et al. Rohitukine, a chromone alkaloid and a precursor of flavopiridol, is produced by endophytic fungi isolated from Dysoxylum binectariferum Hook.f and Amoora rohituka (Roxb).Wight & Arn. Phytomedicine. 2014 Mar 15;21(4):541-6.  [Content Brief]

  [6]. Houghton PJ, et al. Further Chromone Alkaloids from Schumanniophyton magnificum. Planta Med. 1987 Jun;53(3):262-4.  [Content Brief]