1. JAK/STAT Signaling
    Stem Cell/Wnt
    Epigenetics
    Apoptosis
  2. STAT
    JAK
    Apoptosis
  3. SC99

SC99 

Cat. No.: HY-124858 Purity: 99.07%
Handling Instructions

SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities.

For research use only. We do not sell to patients.

SC99 Chemical Structure

SC99 Chemical Structure

CAS No. : 882290-02-0

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10 mM * 1 mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 400 In-stock
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50 mg USD 1150 In-stock
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100 mg USD 1750 In-stock
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Description

SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities[1][2][3].

IC50 & Target[1][2][3]

STAT3

 

JAK2

 

In Vitro

SC99 (10 or 30 μM; for 72 hours) induces MM cell death[1].
SC99 (10 μM; 24 hours) decreases the p-STAT3 level but has no effects on total STAT3 expression. SC99 (2.5, 5, 10, 20 μM; for 60 mins) inhibits JAK2 phosphorylation in a concentration-dependent manner but does not inhibit the phosphorylation levels of AKT, ERK, mTOR or c-Src at a concentration up to 20 μM[1].
SC99 (1.25, 2.5, 5 μM; pre-treated for 10 min) inhibits collagen (2 μg/mL) and thrombin (0.02 U/mL) induced phosphorylation of STAT3 in a concentration-dependent manner[2].
SC99 (pre-treated for 2 hours) inhibits IL-6 (50 ng/ml; for 20 min) induced STAT3 nuclear translocation in OPM2 cells[3].

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

Apoptosis Analysis[1]

Cell Line: Six multiple myeloma (MM) cell lines (LP1, JJN3, RPMI-8226, U266, OPM2 and OCI-MY5)
Concentration: 10 or 30 μM
Incubation Time: For 72 hours
Result: Induced MM cell death.

Apoptosis Analysis[1]

Cell Line: MM cell lines[1]
Concentration: 10 μM
Incubation Time: 24 hours
Result: Decreased the p-STAT3 level but had no effects on total STAT3 expression in all cell lines examined.
In Vivo

SC99 (30 mg/kg; orally; daily; for continuous 14 or 28 days) delays myeloma tumor growth in xenograft mice models[1].
SC99 (5, 10, 15 mM, 15 μL; ICV) produces an effective inhibitory effect on the phosphorylation of JAK2 and STAT3 in middle cerebral artery occlusion and reperfusion (MCAO/R) model (adult male SD rats; 250-300 g). SC99 ameliorates neuronal apoptosis and degeneration, neurobehavioral deficits, inflammatory response and brain edema[3].

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

Animal Model: Nude mice with Human MM cells OPM2 or JJN3[1]
Dosage: 30 mg/kg
Administration: Orally; daily; for continuous 14 or 28 days
Result: Delayed myeloma tumor growth in xenograft mice models and suppressed tumor growth more than 40% in 14 days in the OPM2 model.
Molecular Weight

336.15

Formula

C₁₅H₈Cl₂FN₃O

CAS No.

882290-02-0

SMILES

N#C/C(C(C1=CC=C(Cl)C=C1)=O)=N\NC2=CC=C(F)C(Cl)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (247.90 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9749 mL 14.8743 mL 29.7486 mL
5 mM 0.5950 mL 2.9749 mL 5.9497 mL
10 mM 0.2975 mL 1.4874 mL 2.9749 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (6.19 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (6.19 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

SC99SC 99SC-99STATJAKApoptosisJanus kinaseorallyATP-bindingpocketphosphorylationplateletactivationaggregationanti-myelomaanti-thromboticAKTERKmTORc-SrcOPM2multiplemyelomaInhibitorinhibitorinhibit

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